U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C22H17F2N5OS
Molecular Weight 437.465
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of Isavuconazole

SMILES

C[C@@H](C1=NC(=CS1)C2=CC=C(C=C2)C#N)[C@](O)(CN3C=NC=N3)C4=CC(F)=CC=C4F

InChI

InChIKey=DDFOUSQFMYRUQK-RCDICMHDSA-N
InChI=1S/C22H17F2N5OS/c1-14(21-28-20(10-31-21)16-4-2-15(9-25)3-5-16)22(30,11-29-13-26-12-27-29)18-8-17(23)6-7-19(18)24/h2-8,10,12-14,30H,11H2,1H3/t14-,22+/m0/s1

HIDE SMILES / InChI
Molecular Formula C22H17F2N5OS
Molecular Weight 437.465
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/24187505

Isavuconazole is an active form of isavuconazonium, a prodrug which is marketed under the name Cresemba. Isavuconazole inhibits lanosterol 14-alpha demethylase (or CYP51A1) and leads to the accumulation of ergosterol toxic precursors in the fungal cytoplasm. Isavuconazole is indicated for the treatment of invasive aspergillosis and invasive mucormycosis.

CNS Activity

CNS Penetrant
2588
Curator's Comment: Oral administration of 25 mg/kg isavuconazonium sulfate to rats resulted in isavuconazole brain at levels about twice those detected in the plasma.

Originator

Hoffman-La Roche
135
Curator's Comment: # Hoffmann-La Roche

Approval Year

2015
472
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8504
Inhibitor
8504
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
Approved
8583
CRESEMBA

Approved Use

Cresemba is an azole antifungal indicated for use in the treatment of invasive aspergillosis and invasive mucormycosis.

Launch Date

2015
Curative
Approved
8583
CRESEMBA

Approved Use

Cresemba is an azole antifungal indicated for use in the treatment of invasive aspergillosis and invasive mucormycosis.

Launch Date

2015
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
7499 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/207500s005,207501s004lbl.pdf
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
20028 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/207500s005,207501s004lbl.pdf
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
121402 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/207500s005,207501s004lbl.pdf
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
352805 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/207500s005,207501s004lbl.pdf
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
130 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/207500s005,207501s004lbl.pdf
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/207500s005,207501s004lbl.pdf
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Diarrhea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (0.2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Vomiting...
AEs leading to
discontinuation/dose reduction:
Vomiting (0.4%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Blood creatinine increased...
AEs leading to
discontinuation/dose reduction:
Blood creatinine increased (0.6%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Headache...
AEs leading to
discontinuation/dose reduction:
Headache (0.2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
40 mg 1 times / day multiple, oral
Studied dose
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Diarrhea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (16.7%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
40 mg 1 times / day multiple, oral
Studied dose
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Headache...
AEs leading to
discontinuation/dose reduction:
Headache (16.7%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Diarrhea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (2.6%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Nausea...
AEs leading to
discontinuation/dose reduction:
Nausea (5.1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Vomiting...
AEs leading to
discontinuation/dose reduction:
Vomiting (2.6%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Disturbance in attention...
AEs leading to
discontinuation/dose reduction:
Disturbance in attention (5.1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Dizziness...
AEs leading to
discontinuation/dose reduction:
Dizziness (5.1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Headache...
AEs leading to
discontinuation/dose reduction:
Headache (7.7%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Anxiety...
AEs leading to
discontinuation/dose reduction:
Anxiety (7.7%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Hot flush...
AEs leading to
discontinuation/dose reduction:
Hot flush (7.7%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
100 mg 1 times / day multiple, oral
Studied dose
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/25561337/
unhealthy, mean age 39.1 years
Health Status: unhealthy
Age Group: mean age 39.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25561337/
Disc. AE: Atrioventricular block...
AEs leading to
discontinuation/dose reduction:
Atrioventricular block (grade 2, 2.4%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25561337/
533.3 mg 3 times / day multiple, oral
Highest studied dose
Dose: 533.3 mg, 3 times / day
Route: oral
Route: multiple
Dose: 533.3 mg, 3 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/25624327/
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/25624327/
Other AEs: Rash...
Other AEs:
Rash (8.3%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/25624327/
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
Disc. AE: Dizziness, Hypersensitivity...
Other AEs: Headache, Headache...
AEs leading to
discontinuation/dose reduction:
Dizziness (8.3%)
Hypersensitivity (8.3%)
Nausea (8.3%)
Other AEs:
Headache (grade 1, 8.3%)
Headache (grade 2, 8.3%)
Rash (grade 1, 8.3%)
Rash (grade 2, 8.3%)
Cough (grade 1, 16.7%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Pancytopenia, Cardiac arrest...
AEs leading to
discontinuation/dose reduction:
Pancytopenia (0.4%)
Cardiac arrest (0.4%)
Cardio-respiratory arrest (0.4%)
Congestive cardiomyopathy (0.4%)
Supraventricular tachycardia (0.4%)
Optic neuropathy (0.4%)
Dysphagia (0.4%)
Small intestinal obstruction (0.4%)
Vomiting (0.4%)
Chills (0.4%)
Hepatitis acute (0.4%)
Aspergillosis (0.4%)
Bronchopneumonia (0.4%)
Bronchopulmonary aspergillosis (0.4%)
Endocarditis (0.4%)
Fungal infection (0.8%)
Infection (0.4%)
Pneumonia (0.4%)
Sepsis (0.4%)
Septic shock (0.8%)
Blood bilirubin increased (0.8%)
Blood sodium decreased (0.4%)
Transaminases increased (0.4%)
Myositis (0.4%)
Convulsion (0.8%)
Encephalopathy (0.4%)
Epilepsy (0.8%)
Confusional state (0.8%)
Renal failure (0.8%)
Renal failure acute (0.4%)
Acute respiratory failure (0.4%)
Dyspnoea (0.8%)
Respiratory distress (0.4%)
Respiratory failure (0.8%)
Dermatitis (0.4%)
Dermatitis allergic (0.4%)
Hypotension (0.4%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disc. AE: Acute respiratory failure, Chills...
AEs leading to
discontinuation/dose reduction:
Acute respiratory failure (0.4%)
Chills (0.4%)
Convulsion (0.8%)
Dyspnoea (0.8%)
Epilepsy (0.4%)
Hypotension (0.4%)
Respiratory failure (0.8%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
AEs

AEs

AESignificanceDosePopulation
Diarrhea 0.2%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Vomiting 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Blood creatinine increased 0.6%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Headache 0.2%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Diarrhea 16.7%
Disc. AE
40 mg 1 times / day multiple, oral
Studied dose
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Headache 16.7%
Disc. AE
40 mg 1 times / day multiple, oral
Studied dose
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Diarrhea 2.6%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Nausea 5.1%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Vomiting 2.6%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Disturbance in attention 5.1%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Dizziness 5.1%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Headache 7.7%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Anxiety 7.7%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Hot flush 7.7%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
healthy, adult
Health Status: healthy
Age Group: adult
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Atrioventricular block grade 2, 2.4%
Disc. AE
100 mg 1 times / day multiple, oral
Studied dose
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/25561337/
unhealthy, mean age 39.1 years
Health Status: unhealthy
Age Group: mean age 39.1 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25561337/
Rash 8.3%
533.3 mg 3 times / day multiple, oral
Highest studied dose
Dose: 533.3 mg, 3 times / day
Route: oral
Route: multiple
Dose: 533.3 mg, 3 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/25624327/
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
https://pubmed.ncbi.nlm.nih.gov/25624327/
Dizziness 8.3%
Disc. AE
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
Hypersensitivity 8.3%
Disc. AE
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
Nausea 8.3%
Disc. AE
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
Cough grade 1, 16.7%
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
Headache grade 1, 8.3%
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
Rash grade 1, 8.3%
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
Headache grade 2, 8.3%
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
Rash grade 2, 8.3%
400 mg 1 times / day multiple, oral
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
unhealthy, mean age 48.4 years
Health Status: unhealthy
Age Group: mean age 48.4 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/25624327/
Acute respiratory failure 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Aspergillosis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Blood sodium decreased 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Bronchopneumonia 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Bronchopulmonary aspergillosis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Cardiac arrest 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Cardio-respiratory arrest 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Chills 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Congestive cardiomyopathy 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Dermatitis allergic 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Dermatitis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Dysphagia 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Encephalopathy 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Endocarditis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Hepatitis acute 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Hypotension 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Infection 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Myositis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Optic neuropathy 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Pancytopenia 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Pneumonia 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Renal failure acute 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Respiratory distress 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Sepsis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Small intestinal obstruction 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Supraventricular tachycardia 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Transaminases increased 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Vomiting 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Blood bilirubin increased 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Confusional state 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Convulsion 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Dyspnoea 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Epilepsy 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Fungal infection 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Renal failure 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Respiratory failure 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Septic shock 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Acute respiratory failure 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Chills 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Epilepsy 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Hypotension 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Convulsion 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Dyspnoea 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Respiratory failure 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
unhealthy, mean age 51.1 years
Health Status: unhealthy
Age Group: mean age 51.1 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000MedR.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
2252

substrate
1946
inhibitor
2438

inducer
440
inhibitor
2507
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2C8
1057

CYP2C19
2057

P-gp
1741

BCRP
910

OCT2
779

OATP1B1
1079

OCT1
620

MATE1
415

Cav1.2
58

Nav1.5
116
CYP3A
220

CYP3A5
446

P-gp
2052

BCRP
697

OATP1B1
503

OATP1B3
435
CYP3A4/5
133

CYP2B6
669

CYP2C8
198
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
OATP1B1
1095
 yes [IC50 11.2 uM]
P-gp
1932
 yes [IC50 25.7 uM]
MATE1
416
 yes [IC50 6.31 uM]
BCRP
985
 yes [IC50 92 uM]
OCT2
782
 yes [Ki 0.59 uM]
CYP3A4
2633
 yes [Ki 0.622 uM]
OCT1
656
 yes [Ki 1.74 uM]
CYP2C8
1117
 yes [Ki 2.86 uM]
CYP2C9
2497
 yes [Ki 4.78 uM]
CYP2D6
2546
 yes [Ki 4.82 uM]
CYP2C19
2141
 yes [Ki 5.4 uM]
CYP2B6
1160
 yes
CYP2C8
1117
 yes
CYP2C9
2497
 yes
CYP3A4/5
357
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BCRP
697
 no
OATP1B1
503
 no
OATP1B3
435
 no
P-gp
2052
 no
CYP3A
220
 yes
CYP3A5
446
 yes
CYP3A4
1946
 yes
yes (co-administration study)
Comment: Upon coadministration, ketoconazole increased the isavuconazole Cmax by 9% and isavuconazole AUC by 422% after multiple dose administration of ketoconazole (200 mg twice daily) for 24 days and a single dose of isavuconazonium equivalent to 200 mg of isavuconazole.
Page: 19.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
Cav1.2
63
Nav1.5
119
hERG
2263
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:85979
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:85979
MolPort
MolPort-039-139-689
https://www.molport.com/shop/molecule-link/MolPort-039-139-689
ZINC
ZINC000001485935
http://zinc15.docking.org/substances/ZINC000001485935
PubMed

PubMed

TitleDatePubMed
Isavuconazole: A New Broad-Spectrum Triazole Antifungal Agent.
2015-11-15
Isavuconazole: Pharmacology, Pharmacodynamics, and Current Clinical Experience with a New Triazole Antifungal Agent.
2015-11
Isavuconazole activity against Aspergillus lentulus, Neosartorya udagawae, and Cryptococcus gattii, emerging fungal pathogens with reduced azole susceptibility.
2013-09
In vitro activity of isavuconazole against 208 Aspergillus flavus isolates in comparison with 7 other antifungal agents: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
2011-12
In vitro antifungal susceptibilities and amplified fragment length polymorphism genotyping of a worldwide collection of 350 clinical, veterinary, and environmental Cryptococcus gattii isolates.
2010-12
Isavuconazole: a comprehensive review of spectrum of activity of a new triazole.
2010-11
Antifungal susceptibility, serotyping, and genotyping of clinical Cryptococcus neoformans isolates collected during 18 years in a single institution in Madrid, Spain.
2010-11
Microsatellite typing and susceptibilities of serial Cryptococcus neoformans isolates from Cuban patients with recurrent cryptococcal meningitis.
2010-10-04
In vitro activity of isavuconazole against 140 reference fungal strains and 165 clinically isolated yeasts from Japan.
2010-10
Chromatographic and electrophoretic techniques used in the analysis of triazole antifungal agents-a review.
2010-09-15
Opportunistic fungi: a view to the future.
2010-09
In vitro antifungal activities of isavuconazole and comparators against rare yeast pathogens.
2010-09
[Recent advances in the study of new antifungal lead compounds].
2010-08
Rhinocladiella aquaspersa, proven agent of verrucous skin infection and a novel type of chromoblastomycosis.
2010-08
In vitro activities of eight antifungal drugs against 55 clinical isolates of Fonsecaea spp.
2010-04
Novel triazole antifungal drugs: focus on isavuconazole, ravuconazole and albaconazole.
2010-02
Clinical safety and tolerability issues in use of triazole derivatives in management of fungal infections.
2010
New triazoles and echinocandins: mode of action, in vitro activity and mechanisms of resistance.
2009-10
Comparison of adverse events between oral and intravenous formulations of antimicrobial agents: a systematic review of the evidence from randomized trials.
2009-10
New generation azole antifungals in clinical investigation.
2009-09
In vitro activity of isavuconazole against Trichosporon, Rhodotorula, Geotrichum, Saccharomyces and Pichia species.
2009-07
In vitro antifungal activity of isavuconazole against 345 mucorales isolates collected at study centers in eight countries.
2009-06
In vitro activities of isavuconazole against opportunistic filamentous and dimorphic fungi.
2009-02
Efficacy of isavuconazole, voriconazole and fluconazole in temporarily neutropenic murine models of disseminated Candida tropicalis and Candida krusei.
2009-01
Antifungal susceptibilities among different serotypes of Cryptococcus gattii and Cryptococcus neoformans.
2009-01
Cryptococcus gattii: An Emerging Cause of Fungal Disease in North America.
2009
New and investigational triazole agents for the treatment of invasive fungal infections.
2008-12
Isavuconazole: a new and promising antifungal triazole for the treatment of invasive fungal infections.
2008-12
Investigational antimicrobial drugs for bloodstream infections.
2008-08
New and emerging treatments for fungal infections.
2008-01
Drug evaluation: BAL-8557--a novel broad-spectrum triazole antifungal.
2006-08
Multiple-dose pharmacokinetics and safety of the new antifungal triazole BAL4815 after intravenous infusion and oral administration of its prodrug, BAL8557, in healthy volunteers.
2006-01
Single-ascending-dose pharmacokinetics and safety of the novel broad-spectrum antifungal triazole BAL4815 after intravenous infusions (50, 100, and 200 milligrams) and oral administrations (100, 200, and 400 milligrams) of its prodrug, BAL8557, in healthy volunteers.
2006-01
In vitro activity of a new triazole BAL4815, the active component of BAL8557 (the water-soluble prodrug), against Aspergillus spp.
2006-01
Patents

Patents

06300353
8
20040176432
6
20050038038
6
20050038075
6
20070027322
6
20080015157
7
20080139674
6
20080146679
6

Sample Use Guides

In Vivo Use Guide
Loading Dose: 372 mg isavuconazonium sulfate (equivalent to 200 mg of isavuconazole) every 8 hours for 6 doses (48 hours) via oral (2 capsules) or intravenous administration (1 reconstituted vial) Maintenance Dose: 372 mg isavuconazonium sulfate (equivalent to 200 mg of isavuconazole) once daily via oral (2 capsules) or intravenous administration (1 reconstituted vial) starting 12 to 24 hours after the last loading dose.
Route of Administration: Other
In Vitro Use Guide
Isavuconazole exhibited MIC50 values of 1–4 ug/ mL and MIC90 values of 4–16 ug/mL, against Mucorales isolates. MIC90 against Aspergillus fumigatus was 0.5–2 ug/ml, MIC90 against Aspergillus terreus was 0.5–4 ug/ml, MIC90 against Aspergillus flavus was 1–16 ug/ml, MIC90 against Aspergillus niger was 2–4 ug/ml.
Substance Class Chemical
Created
by admin
on Wed Apr 02 07:52:38 GMT 2025
Edited
by admin
on Wed Apr 02 07:52:38 GMT 2025
Record UNII
60UTO373KE
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BAL-4815
Preferred Name English
Isavuconazole
INN   MI   WHO-DD  
INN  
Official Name English
4-(2-((2R,3R)-3-(2,5-DIFLUOROPHENYL)-3-HYDROXY-4-(1H-1,2,4-TRIAZOL-1-YL)BUTAN-2-YL)-1,3-THIAZOL-4-YL)BENZONITRILE
Systematic Name English
ISAVUCONAZOLE [MI]
Common Name English
isavuconazole [INN]
Common Name English
Isavuconazole [WHO-DD]
Common Name English
Classification Tree Code System Code
WHO-ATC J02AC05
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
NCI_THESAURUS C514
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
NDF-RT N0000175487
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
Code System Code Type Description
WIKIPEDIA
ISAVUCONAZOLE
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY
DAILYMED
60UTO373KE
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY
EPA CompTox
DTXSID2058251
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY
NCI_THESAURUS
C64543
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY
ChEMBL
CHEMBL409153
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY
NDF-RT
N0000187061
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY Organic Cation Transporter 2 Inhibitors [MoA]
CAS
241479-67-4
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY
INN
8783
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY
EVMPD
SUB128138
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY
DRUG BANK
DB11633
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY
NDF-RT
N0000185503
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY P-Glycoprotein Inhibitors [MoA]
RXCUI
1720882
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY RxNorm
CHEBI
85979
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY
MERCK INDEX
m6419
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY Merck Index
NDF-RT
N0000182141
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY Cytochrome P450 3A4 Inhibitors [MoA]
FDA UNII
60UTO373KE
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY
PUBCHEM
6918485
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY
SMS_ID
100000153839
Created by admin on Wed Apr 02 07:52:39 GMT 2025 , Edited by admin on Wed Apr 02 07:52:39 GMT 2025
PRIMARY
Related Record Type Details
CYTOCHROME P450 3A5
METABOLIC ENZYME -> SUBSTRATE
Structure of Isavuconazole
EXCRETED UNCHANGED
FECAL
CYTOCHROME P450 2C19
METABOLIC ENZYME -> INHIBITOR
CYTOCHROME P450 3A4
METABOLIC ENZYME -> INHIBITOR
CYTOCHROME P450 2C8
METABOLIC ENZYME -> INDUCER
CYTOCHROME P450 2C8
METABOLIC ENZYME -> INHIBITOR
CYTOCHROME P450 2D6
METABOLIC ENZYME -> INHIBITOR
ASPERGILLUS FUMIGATUS
TARGET ORGANISM->INHIBITOR
CANDIDA TROPICALIS
TARGET ORGANISM->INHIBITOR
MIC
CYTOCHROME P450 2C9
METABOLIC ENZYME -> INHIBITOR
CYTOCHROME P450 2B6
METABOLIC ENZYME -> INDUCER
CANDIDA ALBICANS
TARGET ORGANISM->INHIBITOR
MIC
CYTOCHROME P450 2C9
METABOLIC ENZYME -> INDUCER
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Structure of Isavuconazole
EXCRETED UNCHANGED
URINE
ISSATCHENKIA ORIENTALIS WHOLE
TARGET ORGANISM->INHIBITOR
MIC
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
RHIZOPUS ARRHIZUS
TARGET ORGANISM->INHIBITOR
CANDIDA PARAPSILOSIS
TARGET ORGANISM->INHIBITOR
MIC
ASPERGILLUS FLAVUS
TARGET ORGANISM->INHIBITOR
CYTOCHROME P450 3A4
METABOLIC ENZYME -> INDUCER
CYTOCHROME P450 3A5
METABOLIC ENZYME -> INDUCER
Related Record Type Details
Structure of Isavuconazonium
PRODRUG -> METABOLITE ACTIVE
Related Record Type Details
Structure of Isavuconazole
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC INTRAVENOUS ADMINISTRATION

ORAL BIOAVAILABILITY PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC INTRAVENOUS ADMINISTRATION

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