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

Details

Stereochemistry ABSOLUTE
Molecular Formula C22H18FN7O
Molecular Weight 415.423
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of IDELALISIB

SMILES

CC[C@H](NC1=NC=NC2=C1N=CN2)C3=NC4=C(C(=O)N3C5=CC=CC=C5)C(F)=CC=C4

InChI

InChIKey=IFSDAJWBUCMOAH-HNNXBMFYSA-N
InChI=1S/C22H18FN7O/c1-2-15(28-20-18-19(25-11-24-18)26-12-27-20)21-29-16-10-6-9-14(23)17(16)22(31)30(21)13-7-4-3-5-8-13/h3-12,15H,2H2,1H3,(H2,24,25,26,27,28)/t15-/m0/s1

HIDE SMILES / InChI
Molecular Formula C22H18FN7O
Molecular Weight 415.423
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including http://link.springer.com/article/10.1007/s40265-014-0285-6

Idelalisib is a first-in-class selective inhibitor of adenosine-5'-triphosphate (ATP) binding to PI3Kdelta kinase, resulting in inhibition of the P13K signalling pathway in malignant B cells. The compound is approved for the treatment of several types of blood cancer. Idelalisib is intended to be used in combination with rituximab as second or subsequent line therapy for the treatment of chronic lymphocytic leukaemia. The drug may cause fatal and/or severe diarrhea or colitis, hepatotoxicity, pneumonitis and intestinal perforation.

CNS Activity

CNS Penetrant
2588
Curator's Comment: Ibrutinib can cross the blood-brain barrier (1–7% of the dose found in cerebral spinal fluid).

Originator

Approval Year

2014
503
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2849
 2.5 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
ZYDELIG

Approved Use

Indicated for the treatment of patients with: 1) relapsed chronic lymphocytic leukemia (CLL), in combination with rituximab, in patients for whom rituximab alone would be considered appropriate therapy due to other co-morbidities; 2) relapsed follicular B-cell non-Hodgkin lymphoma (FL) in patients who have received at least two prior systemic therapies; 3) relapsed small lymphocytic lymphoma (SLL) in patients who have received at least two prior systemic therapies.

Launch Date

2014
Primary
Approved
8583
ZYDELIG

Approved Use

Indicated for the treatment of patients with: 1) relapsed chronic lymphocytic leukemia (CLL), in combination with rituximab, in patients for whom rituximab alone would be considered appropriate therapy due to other co-morbidities; 2) relapsed follicular B-cell non-Hodgkin lymphoma (FL) in patients who have received at least two prior systemic therapies; 3) relapsed small lymphocytic lymphoma (SLL) in patients who have received at least two prior systemic therapies.

Launch Date

2014
Primary
Approved
8583
ZYDELIG

Approved Use

Indicated for the treatment of patients with: 1) relapsed chronic lymphocytic leukemia (CLL), in combination with rituximab, in patients for whom rituximab alone would be considered appropriate therapy due to other co-morbidities; 2) relapsed follicular B-cell non-Hodgkin lymphoma (FL) in patients who have received at least two prior systemic therapies; 3) relapsed small lymphocytic lymphoma (SLL) in patients who have received at least two prior systemic therapies.

Launch Date

2014
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2258.8 ng/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01282424
150 mg 2 times / day multiple, oral
dose: 150 mg
route of administration: oral
experiment type: multiple
co-administered:
IDELALISIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
2647.5 ng/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01282424
150 mg single, oral
dose: 150 mg
route of administration: oral
experiment type: single
co-administered:
IDELALISIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
1953 ng/mL
OTHER GOV
https://www.ema.europa.eu/en/documents/product-information/zydelig-epar-product-information_en.pdf
150 mg 2 times / day steady-state, oral
dose: 150 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
IDELALISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
9293.39 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01282424
150 mg 2 times / day multiple, oral
dose: 150 mg
route of administration: oral
experiment type: multiple
co-administered:
IDELALISIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
9094.76 ng*h/mL
Clinical Trial
https://clinicaltrials.gov/ct2/show/NCT01282424
150 mg single, oral
dose: 150 mg
route of administration: oral
experiment type: single
co-administered:
IDELALISIB plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
10439 ng × h/mL
OTHER GOV
https://www.ema.europa.eu/en/documents/product-information/zydelig-epar-product-information_en.pdf
150 mg 2 times / day steady-state, oral
dose: 150 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
IDELALISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
8.2 h
OTHER GOV
https://www.ema.europa.eu/en/documents/product-information/zydelig-epar-product-information_en.pdf
150 mg 2 times / day steady-state, oral
dose: 150 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
IDELALISIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Other AEs: Diarrhea, Pneumonia...
Other AEs:
Diarrhea (grade 3, 25%)
Pneumonia (grade 3, 25%)
Edema peripheral (grade 3, 25%)
AST increased (grade 3, 50%)
ALT increased (grade 3, 50%)
Absolute neutrophil count decreased (grade 3, 50%)
Platelets decreased (grade 3, 50%)
Vomiting (all grades, 25%)
Rash (all grades, 25%)
Chills (all grades, 25%)
Fatigue (all grades, 25%)
Constipation (all grades, 25%)
Nausea (all grades, 25%)
Insomnia (all grades, 25%)
Edema peripheral (all grades, 25%)
Arterial pressure NOS increased (all grades, 25%)
Bilirubin increased (all grades, 25%)
Glucose increased (all grades, 25%)
Glucose decreased (all grades, 25%)
Hemoglobin decreased (all grades, 25%)
Pyrexia (all grades, 25%)
Night sweats (all grades, 25%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
unhealthy, 71 years (range: 47 - 92 years)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
Disc. AE: Hepatotoxicity, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Hepatotoxicity (10%)
Diarrhea (10%)
Colitis (10%)
Transaminases increased (15%)
Diarrhea (15%)
Colitis (15%)
Rash (15%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
Other AEs: Hepatotoxicity, Diarrhea...
Other AEs:
Hepatotoxicity (serious|grade 5, 14%)
Diarrhea (serious|grade 5, 14%)
Colitis (serious|grade 5, 14%)
Pneumonitis (serious|grade 5)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Arterial pressure NOS increased all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Bilirubin increased all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Chills all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Constipation all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Edema peripheral all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Fatigue all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Glucose decreased all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Glucose increased all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Hemoglobin decreased all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Insomnia all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Nausea all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Night sweats all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Pyrexia all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Rash all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Vomiting all grades, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Diarrhea grade 3, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Edema peripheral grade 3, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Pneumonia grade 3, 25%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
ALT increased grade 3, 50%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
AST increased grade 3, 50%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Absolute neutrophil count decreased grade 3, 50%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Platelets decreased grade 3, 50%
350 mg 2 times / day multiple, oral
Highest studied dose
Dose: 350 mg, 2 times / day
Route: oral
Route: multiple
Dose: 350 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
unhealthy, 64 years (range: 32-91 years)
Health Status: unhealthy
Age Group: 64 years (range: 32-91 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/24615776
Colitis 10%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
unhealthy, 71 years (range: 47 - 92 years)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
Diarrhea 10%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
unhealthy, 71 years (range: 47 - 92 years)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
Hepatotoxicity 10%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
unhealthy, 71 years (range: 47 - 92 years)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
Colitis 15%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
unhealthy, 71 years (range: 47 - 92 years)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
Diarrhea 15%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
unhealthy, 71 years (range: 47 - 92 years)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
Rash 15%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
unhealthy, 71 years (range: 47 - 92 years)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
Transaminases increased 15%
Disc. AE
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
unhealthy, 71 years (range: 47 - 92 years)
Health Status: unhealthy
Age Group: 71 years (range: 47 - 92 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
Pneumonitis serious|grade 5
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
Colitis serious|grade 5, 14%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
Diarrhea serious|grade 5, 14%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
Hepatotoxicity serious|grade 5, 14%
150 mg 2 times / day steady, oral
Recommended
Dose: 150 mg, 2 times / day
Route: oral
Route: steady
Dose: 150 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205858lbl.pdf
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:82701
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:82701
ChemicalBook
CB32538915
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB32538915
ChemicalBook
CB62638450
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB62638450
eMolecules
36516858
https://www.emolecules.com/cgi-bin/more?vid=36516858
MolPort
MolPort-016-633-355
https://www.molport.com/shop/molecule-link/MolPort-016-633-355
MolPort
MolPort-042-652-833
https://www.molport.com/shop/molecule-link/MolPort-042-652-833
Selleck Chemicals
CAL-101
http://www.selleckchem.com/products/CAL-101.html
ZINC
ZINC000013986658
http://zinc15.docking.org/substances/ZINC000013986658
PubMed

PubMed

TitleDatePubMed
Clinical drug interaction profile of idelalisib in healthy subjects.
2015-08
Idelalisib, an inhibitor of phosphatidylinositol 3-kinase p110δ, for relapsed/refractory chronic lymphocytic leukemia.
2014-05-29
Idelalisib, a selective inhibitor of phosphatidylinositol 3-kinase-δ, as therapy for previously treated indolent non-Hodgkin lymphoma.
2014-05-29
Idelalisib and rituximab in relapsed chronic lymphocytic leukemia.
2014-03-13
Induction of prolonged early G1 arrest by CDK4/CDK6 inhibition reprograms lymphoma cells for durable PI3Kδ inhibition through PIK3IP1.
2013-06-15
Simultaneous inhibition of pan-phosphatidylinositol-3-kinases and MEK as a potential therapeutic strategy in peripheral T-cell lymphomas.
2013-01
The PI3-kinase delta inhibitor idelalisib (GS-1101) targets integrin-mediated adhesion of chronic lymphocytic leukemia (CLL) cell to endothelial and marrow stromal cells.
2013
CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability.
2011-01-13
Patents

Patents

07932260
1
08207153
1
08779131
1
20080275067
2

Sample Use Guides

In Vivo Use Guide
The recommended dose is 150 mg taken orally, twice daily
Route of Administration: Oral
In Vitro Use Guide
Treatment of primary CLL cells (n =14) co-cultured with HS5 stromal cells with 100 nM idelalisib results in decreased AKT phosphorylation and inhibition of BCR mediated signaling pathways.
Substance Class Chemical
Created
by admin
on Mon Mar 31 20:52:32 GMT 2025
Edited
by admin
on Mon Mar 31 20:52:32 GMT 2025
Record UNII
YG57I8T5M0
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
idelalisib [INN]
Preferred Name English
IDELALISIB
DASH   INN   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
CAL-101
Code English
GS-1101
Code English
4(3H)-QUINAZOLINONE, 5-FLUORO-3-PHENYL-2-((1S)-1-(1H-PURIN-6-YLAMINO)PROPYL)-
Systematic Name English
ZYDELIG
Brand Name English
IDELALISIB [JAN]
Common Name English
IDELALISIB [ORANGE BOOK]
Common Name English
5-FLUORO-3-PHENYL-2-((S)-1-(9H-PURIN-6-YLAMINO)-PROPYL)-3H-QUINAZOLIN-4-ONE
Systematic Name English
IDELALISIB [VANDF]
Common Name English
IDELALISIB [MI]
Common Name English
4(3H)-QUINAZOLINONE, 5-FLUORO-3-PHENYL-2-((1S)-1-(9H-PURIN-6-YLAMINO)PROPYL)-
Systematic Name English
Idelalisib [WHO-DD]
Common Name English
IDELALISIB [USAN]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 405913
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
EMA ASSESSMENT REPORTS ZYDELIG (AUTHORIZED: LYMPHOMA, NON-HODGKIN)
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
NCI_THESAURUS C129825
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
FDA ORPHAN DRUG 405813
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
WHO-ATC L01XX47
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
NDF-RT N0000175605
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
FDA ORPHAN DRUG 405613
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
FDA ORPHAN DRUG 412613
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
EMA ASSESSMENT REPORTS ZYDELIG (AUTHORIZED: LEUKEMIA, LYMPHOCYTIC, CHRONIC, B-CELL)
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
FDA ORPHAN DRUG 405713
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
EU-Orphan Drug EU/3/13/1160
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
FDA ORPHAN DRUG 347511
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
NCI_THESAURUS C2152
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
FDA ORPHAN DRUG 412513
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
Code System Code Type Description
DRUG BANK
DB09054
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
NDF-RT
N0000175082
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY Kinase Inhibitors [MoA]
SMS_ID
100000151771
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
RXCUI
1544460
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY RxNorm
LACTMED
Idelalisib
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
MERCK INDEX
m11752
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
EVMPD
SUB126168
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
CAS
870281-82-6
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
CHEBI
82701
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
EPA CompTox
DTXSID701007266
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
NDF-RT
N0000190114
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY Cytochrome P450 3A Inhibitors [MoA]
NCI_THESAURUS
C78825
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
WIKIPEDIA
Idelalisib
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
IUPHAR
6741
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
DAILYMED
YG57I8T5M0
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
FDA UNII
YG57I8T5M0
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
DRUG CENTRAL
4878
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
INN
9624
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
ChEMBL
CHEMBL2216870
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
USAN
AB-74
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
PUBCHEM
11625818
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
NCI_THESAURUS
C78825
Created by admin on Mon Mar 31 20:52:32 GMT 2025 , Edited by admin on Mon Mar 31 20:52:32 GMT 2025
PRIMARY
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Related Record Type Details
Structure of IDELALISIB
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
blood-to-plasma ratio PHARMACOKINETIC
Structure of IDELALISIB
Volume of Distribution PHARMACOKINETIC
Structure of IDELALISIB
Tmax PHARMACOKINETIC
Structure of IDELALISIB
NIH
NCATS
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ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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