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

Details

Stereochemistry RACEMIC
Molecular Formula C16H25NO2
Molecular Weight 263.3752
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DESVENLAFAXINE

SMILES

CN(C)CC(C1=CC=C(O)C=C1)C2(O)CCCCC2

InChI

InChIKey=KYYIDSXMWOZKMP-UHFFFAOYSA-N
InChI=1S/C16H25NO2/c1-17(2)12-15(13-6-8-14(18)9-7-13)16(19)10-4-3-5-11-16/h6-9,15,18-19H,3-5,10-12H2,1-2H3

HIDE SMILES / InChI
Molecular Formula C16H25NO2
Molecular Weight 263.3752
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/16675639 | http://adisinsight.springer.com/drugs/800000550

Desvenlafaxine is a dual serotonin and norepinephrine reuptake inhibitor in vitro and in vivo that demonstrates good brain-to-plasma ratios. Desvenlafaxine has demonstrated antidepressant effects in preclinical studies. Pfizer is developing an oral, extended-release formulation of desvenlafaxine for the treatment of major depressive disorder. Desvenlafaxine has been registered and is available on the market for the treatment of major depressive disorder in adults.

CNS Activity

Originator

Approval Year

2008
174
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8504
 40.2 nM [Ki]
Inhibitor
8504
 558.4 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
PRISTIQ

Approved Use

PRISTIQ (DESVENLAFAXINE SUCCINATE), a selective serotonin and norepinephrine reuptake inhibitor, is indicated for the treatment of major depressive disorder.

Launch Date

2014
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
39.6 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/19142106/
75 mg single, oral
dose: 75 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DESVENLAFAXINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
591 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/19142106/
75 mg single, oral
dose: 75 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DESVENLAFAXINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
10.9 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/19142106/
75 mg single, oral
dose: 75 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DESVENLAFAXINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
70%
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/19142106/
75 mg single, oral
dose: 75 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
DESVENLAFAXINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
750 mg single, oral
MTD
Dose: 750 mg
Route: oral
Route: single
Dose: 750 mg
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
healthy, 23.95
Health Status: healthy
Age Group: 23.95
Sex: M
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Other AEs: Vomiting...
Other AEs:
Vomiting (27%)
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
900 mg single, oral
Highest studied dose
Dose: 900 mg
Route: oral
Route: single
Dose: 900 mg
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
healthy, 27.5 ± 9.0
Health Status: healthy
Age Group: 27.5 ± 9.0
Sex: M
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
DLT: Vomiting...
Other AEs: Nausea...
Dose limiting toxicities:
Vomiting (67%)
Other AEs:
Nausea (severe, 33%)
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
healthy, 32.9 ± 4.7
Health Status: healthy
Age Group: 32.9 ± 4.7
Sex: M
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
DLT: Orthostatic hypotension...
Dose limiting toxicities:
Orthostatic hypotension (67%)
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
3500 mg single, oral
Overdose
Dose: 3500 mg
Route: oral
Route: single
Dose: 3500 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/27622824
healthy, 33
Health Status: healthy
Age Group: 33
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/27622824
Disc. AE: Serotonin syndrome...
AEs leading to
discontinuation/dose reduction:
Serotonin syndrome
Sources:
https://pubmed.ncbi.nlm.nih.gov/27622824
450 mg 1 times / day multiple, oral
MTD
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
healthy, 34.9 ± 7.4
Health Status: healthy
Age Group: 34.9 ± 7.4
Sex: M
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Other AEs: Nausea...
Other AEs:
Nausea (67%)
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Disc. AE: Suicidal ideation, Serotonin syndrome...
AEs leading to
discontinuation/dose reduction:
Suicidal ideation
Serotonin syndrome
Neuroleptic malignant syndrome
Blood pressure increased
Bleeding
Glaucoma
Mania
Hypomania
Cardiovascular disease, unspecified
Unspecified cerebrovascular disease
Elevated cholesterol
Elevated triglycerides
Seizure
Hyponatremia
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Other AEs: Lightheadedness, Sickness/nausea...
Other AEs:
Lightheadedness (below serious, 11 patient)
Sickness/nausea (below serious, 11 patient)
Drowsiness (below serious, 7 patients)
Insomnia (below serious, 5 patients)
Decreased appetite (below serious, 6 patients)
Indigestion (below serious, 4 patients)
Soft stools (below serious, 5 patients)
Dry mouth (below serious, 3 patients)
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Other AEs: Sleep decreased, Daytime sleepiness...
Other AEs:
Sleep decreased (below serious, 10 patients)
Daytime sleepiness (below serious, 9 patients)
Headache (below serious, 9 patients)
Nausea (below serious, 9 patients)
Dry mouth (below serious, 7 patients)
Agitation (below serious, 5 patients)
Dizziness (below serious, 5 patients)
Sweating (below serious, 5 patients)
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
AEs

AEs

AESignificanceDosePopulation
Vomiting 27%
750 mg single, oral
MTD
Dose: 750 mg
Route: oral
Route: single
Dose: 750 mg
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
healthy, 23.95
Health Status: healthy
Age Group: 23.95
Sex: M
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Vomiting 67%
DLT
900 mg single, oral
Highest studied dose
Dose: 900 mg
Route: oral
Route: single
Dose: 900 mg
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
healthy, 27.5 ± 9.0
Health Status: healthy
Age Group: 27.5 ± 9.0
Sex: M
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Nausea severe, 33%
900 mg single, oral
Highest studied dose
Dose: 900 mg
Route: oral
Route: single
Dose: 900 mg
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
healthy, 27.5 ± 9.0
Health Status: healthy
Age Group: 27.5 ± 9.0
Sex: M
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Orthostatic hypotension 67%
DLT
600 mg 1 times / day multiple, oral
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
healthy, 32.9 ± 4.7
Health Status: healthy
Age Group: 32.9 ± 4.7
Sex: M
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Serotonin syndrome Disc. AE
3500 mg single, oral
Overdose
Dose: 3500 mg
Route: oral
Route: single
Dose: 3500 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/27622824
healthy, 33
Health Status: healthy
Age Group: 33
Sex: F
Sources:
https://pubmed.ncbi.nlm.nih.gov/27622824
Nausea 67%
450 mg 1 times / day multiple, oral
MTD
Dose: 450 mg, 1 times / day
Route: oral
Route: multiple
Dose: 450 mg, 1 times / day
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
healthy, 34.9 ± 7.4
Health Status: healthy
Age Group: 34.9 ± 7.4
Sex: M
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Bleeding Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Blood pressure increased Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Cardiovascular disease, unspecified Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Elevated cholesterol Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Elevated triglycerides Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Glaucoma Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Hypomania Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Hyponatremia Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Mania Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Neuroleptic malignant syndrome Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Seizure Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Serotonin syndrome Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Suicidal ideation Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Unspecified cerebrovascular disease Disc. AE
50 mg 1 times / day multiple, oral
Recommended
Dose: 50 mg, 1 times / day
Route: oral
Route: multiple
Dose: 50 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Lightheadedness below serious, 11 patient
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Sickness/nausea below serious, 11 patient
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Dry mouth below serious, 3 patients
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Indigestion below serious, 4 patients
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Insomnia below serious, 5 patients
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Soft stools below serious, 5 patients
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Decreased appetite below serious, 6 patients
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Drowsiness below serious, 7 patients
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Sleep decreased below serious, 10 patients
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Agitation below serious, 5 patients
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Dizziness below serious, 5 patients
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Sweating below serious, 5 patients
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Dry mouth below serious, 7 patients
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Daytime sleepiness below serious, 9 patients
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Headache below serious, 9 patients
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Nausea below serious, 9 patients
100 mg 1 times / day steady, oral
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
Health Status: unhealthy
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946

inducer
1087

inhibitor
2252
inhibitor
2438
substrate
1388

inhibitor
2507

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
2153

CYP2A6
879

CYP2C8
1057

CYP2C19
2057

P-gp
1741
P-gp
2052

UGT1A1
479

UGT1A3
470

UGT2B4
278

UGT2B15
236

UGT2B17
237
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
2333
 no
CYP2A6
911
 no
CYP2C19
2141
 no
CYP2C8
1117
 no
CYP2C9
2497
 no
CYP3A4
2633
 no
CYP3A4
2633
 no
P-gp
1932
 no
CYP2D6
2546
 weak
likely (co-administration study)
Comment: "coadministration with desipramine showed desipramine increased Cmax 25% and AUC 17% and ""clinical significance of changes in desipramine Cmax is not clear""; desvenlaxafine is not an inhibitor of the CYP P450 isozymes except a possible inhibiton of CYP1A2"
Page: 4, 41
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1946
 minor
yes (co-administration study)
Comment: ketoconazole increased Cmax by 1.08-fold and AUC by 1.43-fold
Page: 62.0
P-gp
2052
 no
CYP2D6
1388
 yes
UGT1A1
479
 yes
UGT1A3
470
 yes
UGT2B15
236
 yes
UGT2B17
237
 yes
UGT2B4
278
 yes
Sourcing

Sourcing

Vendor/AggregatorIDURL
001 Chemical
NO11197
https://www.001chemical.com/chem/93413-62-8
3B Scientific (Wuhan) Corp
3B3-032554
http://www.3bsc.com/index/pro_info.php?id=53818
AA Blocks
AA006FVB
http://www.aablocks.com/goods/Goods/detail?id=AA006FVB
Aaron Chemicals
AR006GN3
http://www.aaronchem.com/93413-62-8
abcr GmbH
AB436252
http://www.abcr.com/shop/en/AB436252
AbMole Bioscience
M2623
http://www.abmole.com/products/desvenlafaxine.html
Acadechem
ACDS-019021
http://www.acadechemical.com/product/93720
Achemica
ACMC-20ek0k
http://www.achemica.com/prodinfo/?id=146430
Achemo Scientific Limited
AC-72716
http://www.achemo.com/search/?Keyword= 93413-62-8
Achemtek
0104-022788
http://www.achemtek.com/93413-62-8
Acros Organics
AC461570010
https://www.fishersci.com/shop/products/desvenlafaxine-97-acros-organics-1/AC461570010
Acros Organics
AC461570050
https://www.fishersci.com/shop/products/desvenlafaxine-97-acros-organics/AC461570050
AEchem Scientific Corp., USA
AE1-014851
http://www.aechemsc.com/info_products/AE1-014851.php
AHH Chemical co.,ltd
MT-49703
http://www.ahhchemical.com/product/MT-49703.html
AK Scientific, Inc. (AKSCI)
J10126
http://www.aksci.com/item_detail.php?cat=J10126
AK Scientific, Inc. (AKSCI)
X4688
http://www.aksci.com/item_detail.php?cat=X4688
Alfa Chemistry
AP93413628
https://reagents.alfa-chemistry.com/product/o-desmethylvenlafaxine-solution-cas-93413-62-8-18710.html
Alsachim
1487
http://www.alsachim.com/product-C2083-glo.bal-view.html
Ark Pharm
AK-72949
http://www.arkpharminc.com/products/93413-62-8.html
AstaTech, Inc.
35693
http://www.astatechinc.com/CPSResult.php?CRNO=36104
Aurum Pharmatech LLC
S-2830
http://www.Aurumpharmatech.com/Product/ProductDetails/S_2830
BioChemPartner
BCP28517
http://www.biochempartner.com/93413-62-8-BCP28517
BioCrick
BCC5038
http://www.biocrick.com/Desvenlafaxine-BCC5038.html
BLD Pharm
BD123273
http://www.bldpharm.com/products/93413-62-8.html
BOC Sciences
1020719-35-0
https://isotope.bocsci.com/product/d-l-o-desmethyl-venlafaxine-d6-cas-1020719-35-0-347354.html
BOC Sciences
1062605-69-9
https://www.bocsci.com/rac-o-desmethyl-venlafaxine-d6-cas-1062605-69-9-item-482681.html
BOC Sciences
1062607-49-1
https://www.bocsci.com/rac-o-desmethyl-venlafaxine-d10-cas-1062607-49-1-item-482669.html
Chem Scene
CS-2818
http://www.chemscene.com/93413-62-8.html
Chemenu
CM117133
http://www.chemenu.com/products/CM117133
Chemspace
CSSB00015191201
https://chem-space.com/CSSB00015191201
Clearsynth
CS-O-01279
https://www.clearsynth.com/en/CSO01279.html
Clearsynth
CS-O-08430
https://www.clearsynth.com/en/CSO08430.html
Clearsynth
CS-O-08431
https://www.clearsynth.com/en/CSO08431.html
Clearsynth
CS-T-88511
https://www.clearsynth.com/en/CST88511.html
CSNpharm
CSN10736
https://www.csnpharm.com/products/desvenlafaxine.html
eNovation Chemicals
D383107
http://www.enovationchem.com/productDetails.asp?productID=D383107
Finetech
FT-0654519
http://www.finetechnology-ind.com/prod/detail/pub/93413-62-8.html
Finetech
FT-0666245
http://www.finetechnology-ind.com/prod/detail/pub/142761-11-3.html
Finetech
FT-0666246
http://www.finetechnology-ind.com/prod/detail/pub/142761-12-4.html
iChemical
EBD51027
http://www.ichemical.com/chemicals/cas-93413-62-8
Lab Network
LN00175672
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00175672
LGC Standards
DRE-A17907100AL-100
https://www.lgcstandards.com/US/en/p/DRE-A17907100AL-100
LGC Standards
DRE-C17907100
https://www.lgcstandards.com/US/en/p/DRE-C17907100
LGC Standards
LGCAMP0393.01-02
https://www.lgcstandards.com/US/en/p/LGCAMP0393.01-02
LGC Standards
LGCFOR0393.01
https://www.lgcstandards.com/US/en/p/LGCFOR0393.01
LGC Standards
MM0393.01
https://www.lgcstandards.com/US/en/p/MM0393.01
Matrix Scientific
76092
https://www.matrixscientific.com/076092.html
MedChem Express
HY-B0602
https://www.medchemexpress.com/desvenlafaxine.html
Molcore
CS11197
https://www.molcore.com/product/93413-62-8
Oakwood
79439
http://www.oakwoodchemical.com/ProductsList.aspx?CategoryID=-2&txtSearch=64613&ExtHyperLink=1
OChem
22266
http://www.ocheminc.com/index.php?act=psearch&pid=413D628
Parchem
27061
http://www.parchem.com/chemical-supplier-distributor/4-2-Dimethyamino-1-1-hydroxycyclohexyl-ethyl-phenol-017061.aspx
Sigma-Aldrich
93867_SIAL
https://www.sigmaaldrich.com/catalog/product/sial/93867?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich
V-007_CERILLIAN
https://www.sigmaaldrich.com/catalog/product/cerillian/v007?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich
V-045_CERILLIAN
https://www.sigmaaldrich.com/catalog/product/cerillian/v045?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sinfoo Biotech
S003364
http://www.sinfoobiotech.com/product/1006762
Smolecule
S525732
http://www.smolecule.com/products/s525732
Synblock Inc
SB17444
http://www.synblock.com/product/93413-62-8.html
Syncom
SIC-020075
http://syncom.nl/product/SIC-020075
Synthink Research Chemicals
SA22713
https://synthinkchemicals.com/product/venlafaxine-o-desmethyl/
THE BioTek
bt-267069
https://www.thebiotek.com/product/inhibitors/bt-267069
THE BioTek
bt-305496
https://www.thebiotek.com/product/others/bt-305496
VladaChem
VL278427-1G
https://www.vladachem.com/product.php?products=93413-62-8
Wuhan Atomole Chemicals Co., Ltd.
AT-19352
http://www.atomole.com/en/products-view.asp?id=8635
PubMed

PubMed

TitleDatePubMed
Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis.
2015-05-18
Syndrome of inappropriate antidiuretic hormone secretion associated with desvenlafaxine.
2014-04
Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.
2013-06-13
Influence of CYP2D6 genotype on the disposition of the enantiomers of venlafaxine and its major metabolites in postmortem femoral blood.
2012-01-10
Desvenlafaxine in the treatment of major depressive disorder.
2011-12
Assessment of infant dose through milk in a lactating woman taking amisulpride and desvenlafaxine for treatment-resistant depression.
2010-12
Short-term efficacy and safety of desvenlafaxine in a randomized, placebo-controlled study of perimenopausal and postmenopausal women with major depressive disorder.
2010-08
Clinical utility of desvenlafaxine 50 mg/d for treating MDD: a review of two randomized placebo-controlled trials for the practicing physician.
2010-01
Efficacy, safety, and tolerability of Desvenlafaxine 50 mg/d for the treatment of major depressive disorder:a systematic review of clinical trials.
2010
Discontinuation symptoms and taper/poststudy-emergent adverse events with desvenlafaxine treatment for major depressive disorder.
2009-11
Comparison of the pharmacokinetics of venlafaxine extended release and desvenlafaxine in extensive and poor cytochrome P450 2D6 metabolizers.
2009-02
Desvenlafaxine, a serotonin-norepinephrine uptake inhibitor for major depressive disorder, neuropathic pain and the vasomotor symptoms associated with menopause.
2009-01
Desvenlafaxine and venlafaxine exert minimal in vitro inhibition of human cytochrome P450 and P-glycoprotein activities.
2009
Desvenlafaxine succinate for major depressive disorder: a critical review of the evidence.
2008-12
Desvenlafaxine succinate monohydrate.
2008-05
Desvenlafaxine succinate identifies novel antagonist binding determinants in the human norepinephrine transporter.
2007-11
Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor.
2006-08
[Trazodone for the treatment of behavioral and psychological symptoms of dementia (BPSD) in Alzheimer's disease: a retrospective study focused on the aggression and negativism in caregiving situations].
2006-06
Patents

Patents

08329952
8
EP2455076A1
8
US20120087986
8
US8779005
8
WO2011141791A2
8

Sample Use Guides

In Vivo Use Guide
Recommended dose: 50 mg once daily with or without food.
Route of Administration: Oral
In Vitro Use Guide
Unknown
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:27:57 GMT 2025
Edited
by admin
on Mon Mar 31 18:27:57 GMT 2025
Record UNII
NG99554ANW
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
D-VENIZ
Preferred Name English
DESVENLAFAXINE
INN   MI   ORANGE BOOK   VANDF   WHO-DD  
INN  
Official Name English
DESVENLAFAXINE [USP-RS]
Common Name English
desvenlafaxine [INN]
Common Name English
NEWVEN
Common Name English
MDD-XR
Common Name English
DESVENLAFAXINE [USP MONOGRAPH]
Common Name English
O-DESMETHYLVENLAFAXINE
Common Name English
DESVENLAFAXINE [MI]
Common Name English
DESVENLAFAXINE [ORANGE BOOK]
Common Name English
DESVENLAFAXINE [VANDF]
Common Name English
Desvenlafaxine [WHO-DD]
Common Name English
Classification Tree Code System Code
LIVERTOX 286
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
NDF-RT N0000175749
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
WHO-ATC N06AX23
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
NDF-RT N0000000102
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
NCI_THESAURUS C265
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
WHO-VATC QN06AX23
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
NDF-RT N0000000109
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
Code System Code Type Description
NCI_THESAURUS
C61703
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
RS_ITEM_NUM
1175751
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
WIKIPEDIA
DESVENLAFAXINE
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
MESH
C086816
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
CHEBI
83527
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
PUBCHEM
125017
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
DRUG BANK
DB06700
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
NDF-RT
N0000182137
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY Cytochrome P450 2D6 Inhibitors [MoA]
DRUG CENTRAL
4380
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
LACTMED
Desvenlafaxine
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
MERCK INDEX
m4207
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY Merck Index
CAS
93413-62-8
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
CAS
130198-07-1
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
SUPERSEDED
INN
8361
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
EPA CompTox
DTXSID40869118
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
DAILYMED
NG99554ANW
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
IUPHAR
7158
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
EVMPD
SUB25380
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
SMS_ID
100000089362
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
FDA UNII
NG99554ANW
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
HSDB
7993
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
RXCUI
734064
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY RxNorm
ChEMBL
CHEMBL1118
Created by admin on Mon Mar 31 18:27:57 GMT 2025 , Edited by admin on Mon Mar 31 18:27:57 GMT 2025
PRIMARY
Related Record Type Details
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
Structure of DESVENLAFAXINE
EXCRETED UNCHANGED
AMOUNT EXCRETED
URINE
Structure of DESVENLAFAXINE, (-)-
ENANTIOMER -> RACEMATE
Structure of DESVENLAFAXINE SUCCINATE
SALT/SOLVATE -> PARENT
Structure of DESVENLAFAXINE SUCCINATE ANHYDROUS
SALT/SOLVATE -> PARENT
Structure of DESVENLAFAXINE FUMARATE
SALT/SOLVATE -> PARENT
SODIUM-DEPENDENT SEROTONIN TRANSPORTER
TARGET -> INHIBITOR
IC50
Structure of DESVENLAFAXINE HYDROCHLORIDE
SALT/SOLVATE -> PARENT
Structure of DESVENLAFAXINE, (+)-
ENANTIOMER -> RACEMATE
Structure of DESVENLAFAXINE FUMARATE MONOHYDRATE
SALT/SOLVATE -> PARENT
Structure of DESVENLAFAXINE BENZOATE
SALT/SOLVATE -> PARENT
SODIUM-DEPENDENT NORADRENALINE TRANSPORTER
TARGET->WEAK INHIBITOR
IC50
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
Structure of VENLAFAXINE
PARENT -> METABOLITE ACTIVE
MAJOR
Structure of DESVENLAFAXINE-O-GLUCURONIDE
METABOLITE INACTIVE -> PARENT
Structure of N,O-DIDESMETHYLVENLAFAXINE
METABOLITE INACTIVE -> PARENT
Structure of TOLUDESVENLAFAXINE
PRODRUG -> METABOLITE ACTIVE
Structure of N,O-DIDESMETHYLVENLAFAXINE-GLUCURONIDE
METABOLITE INACTIVE -> PARENT
Related Record Type Details
Structure of VENLAFAXINE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of RAC DEHYDRO-O-DESMETHYL VENLAFAXINE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of N-nitroso-desmethyl-desvenlafaxine
IMPURITY -> PARENT
Related Record Type Details
Structure of DESVENLAFAXINE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC STEADY-STATE

INTRAVENOUS ADMINISTRATION

Tmax PHARMACOKINETIC ORAL ADMINISTRATION

ORAL BIOAVAILABILITY PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC ORAL ADMINISTRATION

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