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

Details

Stereochemistry RACEMIC
Molecular Formula C16H25NO2.C4H6O4.H2O
Molecular Weight 399.4785
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DESVENLAFAXINE SUCCINATE

SMILES

O.OC(=O)CCC(O)=O.CN(C)CC(C1=CC=C(O)C=C1)C2(O)CCCCC2

InChI

InChIKey=PWPDEXVGKDEKTE-UHFFFAOYSA-N
InChI=1S/C16H25NO2.C4H6O4.H2O/c1-17(2)12-15(13-6-8-14(18)9-7-13)16(19)10-4-3-5-11-16;5-3(6)1-2-4(7)8;/h6-9,15,18-19H,3-5,10-12H2,1-2H3;1-2H2,(H,5,6)(H,7,8);1H2

HIDE SMILES / InChI
Molecular Formula H2O
Molecular Weight 18.0153
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula C4H6O4
Molecular Weight 118.088
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
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
8297
 40.2 nM [Ki]
Inhibitor
8297
 558.4 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
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
Page: 28
healthy, 23.95
n = 11
Health Status: healthy
Age Group: 23.95
Sex: M
Population Size: 11
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Page: 28
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
Page: 28
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
Page: 28
healthy, 27.5 ± 9.0
n = 6
Health Status: healthy
Age Group: 27.5 ± 9.0
Sex: M
Population Size: 6
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Page: 28
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
Page: 28
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
Page: 28
healthy, 32.9 ± 4.7
n = 9
Health Status: healthy
Age Group: 32.9 ± 4.7
Sex: M
Population Size: 9
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Page: 28
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
Page: 28
3500 mg single, oral
Overdose
Dose: 3500 mg
Route: oral
Route: single
Dose: 3500 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/27622824
Page: p.6
healthy, 33
n = 1
Health Status: healthy
Age Group: 33
Sex: F
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/27622824
Page: p.6
Disc. AE: Serotonin syndrome...
AEs leading to
discontinuation/dose reduction:
Serotonin syndrome
Sources:
https://pubmed.ncbi.nlm.nih.gov/27622824
Page: p.6
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
Page: 28
healthy, 34.9 ± 7.4
n = 9
Health Status: healthy
Age Group: 34.9 ± 7.4
Sex: M
Population Size: 9
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Page: 28
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
Page: 28
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
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Major depressive disorder
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Page: p.1
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
Page: p.1
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
n = 30
Health Status: unhealthy
Condition: Social Anxiety Disorder
Population Size: 30
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 (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
n = 30
Health Status: unhealthy
Condition: Chronic Depression
Population Size: 30
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
Page: 28
healthy, 23.95
n = 11
Health Status: healthy
Age Group: 23.95
Sex: M
Population Size: 11
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Page: 28
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
Page: 28
healthy, 27.5 ± 9.0
n = 6
Health Status: healthy
Age Group: 27.5 ± 9.0
Sex: M
Population Size: 6
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Page: 28
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
Page: 28
healthy, 27.5 ± 9.0
n = 6
Health Status: healthy
Age Group: 27.5 ± 9.0
Sex: M
Population Size: 6
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Page: 28
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
Page: 28
healthy, 32.9 ± 4.7
n = 9
Health Status: healthy
Age Group: 32.9 ± 4.7
Sex: M
Population Size: 9
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Page: 28
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
Page: p.6
healthy, 33
n = 1
Health Status: healthy
Age Group: 33
Sex: F
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/27622824
Page: p.6
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
Page: 28
healthy, 34.9 ± 7.4
n = 9
Health Status: healthy
Age Group: 34.9 ± 7.4
Sex: M
Population Size: 9
Sources:
https://www.longdom.org/open-access/pharmacokinetics-pharmacodynamics-and-safety-of-desvenlafaxine-a-serotonin-norepinephrine-reuptake-inhibitor-jbb.1000130.pdf
Page: 28
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
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Major depressive disorder
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Page: p.1
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
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Major depressive disorder
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Page: p.1
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
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Major depressive disorder
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Page: p.1
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
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Major depressive disorder
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Page: p.1
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
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Major depressive disorder
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Page: p.1
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
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Major depressive disorder
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Page: p.1
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
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Major depressive disorder
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Page: p.1
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
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Major depressive disorder
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Page: p.1
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
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Major depressive disorder
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Page: p.1
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
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Major depressive disorder
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Page: p.1
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
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Major depressive disorder
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Page: p.1
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
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Major depressive disorder
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Page: p.1
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
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Major depressive disorder
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Page: p.1
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
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Major depressive disorder
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021992s030lbl.pdf
Page: p.1
Lightheadedness below serious, 11 patient
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
n = 30
Health Status: unhealthy
Condition: Social Anxiety Disorder
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Sickness/nausea below serious, 11 patient
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
n = 30
Health Status: unhealthy
Condition: Social Anxiety Disorder
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Dry mouth below serious, 3 patients
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
n = 30
Health Status: unhealthy
Condition: Social Anxiety Disorder
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Indigestion below serious, 4 patients
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
n = 30
Health Status: unhealthy
Condition: Social Anxiety Disorder
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Insomnia below serious, 5 patients
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
n = 30
Health Status: unhealthy
Condition: Social Anxiety Disorder
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Soft stools below serious, 5 patients
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
n = 30
Health Status: unhealthy
Condition: Social Anxiety Disorder
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Decreased appetite below serious, 6 patients
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
n = 30
Health Status: unhealthy
Condition: Social Anxiety Disorder
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Drowsiness below serious, 7 patients
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
unhealthy
n = 30
Health Status: unhealthy
Condition: Social Anxiety Disorder
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01316302
Sleep decreased below serious, 10 patients
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
n = 30
Health Status: unhealthy
Condition: Chronic Depression
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Agitation below serious, 5 patients
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
n = 30
Health Status: unhealthy
Condition: Chronic Depression
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Dizziness below serious, 5 patients
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
n = 30
Health Status: unhealthy
Condition: Chronic Depression
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Sweating below serious, 5 patients
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
n = 30
Health Status: unhealthy
Condition: Chronic Depression
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Dry mouth below serious, 7 patients
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
n = 30
Health Status: unhealthy
Condition: Chronic Depression
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Daytime sleepiness below serious, 9 patients
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
n = 30
Health Status: unhealthy
Condition: Chronic Depression
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Headache below serious, 9 patients
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
n = 30
Health Status: unhealthy
Condition: Chronic Depression
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Nausea below serious, 9 patients
100 mg 1 times / day steady, oral (max)
Dose: 100 mg, 1 times / day
Route: oral
Route: steady
Dose: 100 mg, 1 times / day
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
unhealthy
n = 30
Health Status: unhealthy
Condition: Chronic Depression
Population Size: 30
Sources:
https://clinicaltrials.gov/ct2/show/NCT01537068
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737

inducer
781

inhibitor
1587
inhibitor
1767
substrate
1217

inhibitor
1852

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2A6
707

CYP2C8
911

CYP2C19
1478

P-gp
1461
P-gp
1537

UGT1A1
418

UGT1A3
422

UGT2B4
249

UGT2B15
203

UGT2B17
213
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1692
 no
CYP2A6
739
 no
CYP2C19
1553
 no
CYP2C8
965
 no
CYP2C9
1819
 no
CYP3A4
1925
 no
CYP3A4
1925
 no
P-gp
1650
 no
CYP2D6
1891
 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
1737
 minor
yes (co-administration study)
Comment: ketoconazole increased Cmax by 1.08-fold and AUC by 1.43-fold
Page: 62.0
P-gp
1537
 no
CYP2D6
1217
 yes
UGT1A1
418
 yes
UGT1A3
422
 yes
UGT2B15
203
 yes
UGT2B17
213
 yes
UGT2B4
249
 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
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
Aaron Chemicals
AR006GN3
http://www.aaronchem.com/93413-62-8
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
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
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
1062607-49-1
https://www.bocsci.com/rac-o-desmethyl-venlafaxine-d10-cas-1062607-49-1-item-482669.html
BOC Sciences
1062605-69-9
https://www.bocsci.com/rac-o-desmethyl-venlafaxine-d6-cas-1062605-69-9-item-482681.html
BioChemPartner
BCP28517
http://www.biochempartner.com/93413-62-8-BCP28517
BioCrick
BCC5038
http://www.biocrick.com/Desvenlafaxine-BCC5038.html
CSNpharm
CSN10736
https://www.csnpharm.com/products/desvenlafaxine.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
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
Finetech
FT-0654519
http://www.finetechnology-ind.com/prod/detail/pub/93413-62-8.html
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
Lab Network
LN00175672
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00175672
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
OChem
22266
http://www.ocheminc.com/index.php?act=psearch&pid=413D628
Oakwood
79439
http://www.oakwoodchemical.com/ProductsList.aspx?CategoryID=-2&txtSearch=64613&ExtHyperLink=1
Parchem
27061
http://www.parchem.com/chemical-supplier-distributor/4-2-Dimethyamino-1-1-hydroxycyclohexyl-ethyl-phenol-017061.aspx
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
Sigma-Aldrich
93867_SIAL
https://www.sigmaaldrich.com/catalog/product/sial/93867?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
abcr GmbH
AB436252
http://www.abcr.com/shop/en/AB436252
eNovation Chemicals
D383107
http://www.enovationchem.com/productDetails.asp?productID=D383107
iChemical
EBD51027
http://www.ichemical.com/chemicals/cas-93413-62-8
PubMed

PubMed

TitleDatePubMed
Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor.
2006 Aug
[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 Jun
Desvenlafaxine succinate identifies novel antagonist binding determinants in the human norepinephrine transporter.
2007 Nov
Desvenlafaxine succinate for major depressive disorder: a critical review of the evidence.
2008 Dec
Desvenlafaxine succinate monohydrate.
2008 May
Desvenlafaxine and venlafaxine exert minimal in vitro inhibition of human cytochrome P450 and P-glycoprotein activities.
2009
Comparison of the pharmacokinetics of venlafaxine extended release and desvenlafaxine in extensive and poor cytochrome P450 2D6 metabolizers.
2009 Feb
Desvenlafaxine, a serotonin-norepinephrine uptake inhibitor for major depressive disorder, neuropathic pain and the vasomotor symptoms associated with menopause.
2009 Jan
Discontinuation symptoms and taper/poststudy-emergent adverse events with desvenlafaxine treatment for major depressive disorder.
2009 Nov
Efficacy, safety, and tolerability of Desvenlafaxine 50 mg/d for the treatment of major depressive disorder:a systematic review of clinical trials.
2010
Short-term efficacy and safety of desvenlafaxine in a randomized, placebo-controlled study of perimenopausal and postmenopausal women with major depressive disorder.
2010 Aug
Assessment of infant dose through milk in a lactating woman taking amisulpride and desvenlafaxine for treatment-resistant depression.
2010 Dec
Clinical utility of desvenlafaxine 50 mg/d for treating MDD: a review of two randomized placebo-controlled trials for the practicing physician.
2010 Jan
Desvenlafaxine in the treatment of major depressive disorder.
2011 Dec
Influence of CYP2D6 genotype on the disposition of the enantiomers of venlafaxine and its major metabolites in postmortem femoral blood.
2012 Jan 10
Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.
2013 Jun 13
Syndrome of inappropriate antidiuretic hormone secretion associated with desvenlafaxine.
2014 Apr
Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis.
2015 May 18
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 Fri Dec 15 15:25:49 GMT 2023
Edited
by admin
on Fri Dec 15 15:25:49 GMT 2023
Record UNII
ZB22ENF0XR
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DESVENLAFAXINE SUCCINATE
DASH   MART.   ORANGE BOOK   USAN  
USAN  
Official Name English
WY-45233
Code English
Desvenlafaxine succinate monohydrate [WHO-DD]
Common Name English
DESVENLAFAXINE SUCCINATE [USAN]
Common Name English
DESVENLAFAXINE SUCCINATE MONOHYDRATE
MI  
Common Name English
DVS
Common Name English
O-DESMETHYL VENLAFAXINE SUCCINATE
Common Name English
BUTANEDIOIC ACID, COMPOUND WITH 4-(2-(DIMETHYLAMINO)-1-(1-HYDROXYCYCLOHEXYL)ETHYL)PHENOL (1:1), MONOHYDRATE
Common Name English
DVS-233
Code English
DESVENLAFAXINE SUCCINATE [USP MONOGRAPH]
Common Name English
DESVENLAFAXINE SUCCINATE HYDRATE
JAN  
Common Name English
DESVENLAFAXINE SUCCINATE [ORANGE BOOK]
Common Name English
PRISTIQ
Brand Name English
DESVENLAFAXINE SUCCINATE [MART.]
Common Name English
DESVENLAFAXINE SUCCINATE [USP-RS]
Common Name English
DESVENLAFAXINE SUCCINATE HYDRATE [JAN]
Common Name English
DESVENLAFAXINE SUCCINATE MONOHYDRATE [MI]
Common Name English
O-DESMETHYLVENLAFAXINE SUCCINATE MONOHYDRATE
Common Name English
BUTANEDIOIC ACID, COMPD. WITH 4-(2-(DIMETHYLAMINO)-1-(1-HYDROXYCYCLOHEXYL)ETHYL)PHENOL, HYDRATE (1:1:1)
Common Name English
1-[(1RS)-2-(Dimethylamino)-1-(4-hydroxyphenyl)ethyl]cyclohexanol hydrogen butanedioate monohydrate
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C265
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
Code System Code Type Description
RS_ITEM_NUM
1175773
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
PRIMARY
ChEMBL
CHEMBL1118
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
PRIMARY
EPA CompTox
DTXSID70959511
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
PRIMARY
NCI_THESAURUS
C61704
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
PRIMARY
SMS_ID
100000135810
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
PRIMARY
DRUG BANK
DBSALT000045
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
PRIMARY
CAS
386750-22-7
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
PRIMARY
RXCUI
683693
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
PRIMARY RxNorm
EVMPD
SUB72084
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
PRIMARY
PUBCHEM
6918664
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
PRIMARY
EVMPD
SUB27750
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
PRIMARY
DAILYMED
ZB22ENF0XR
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
PRIMARY
FDA UNII
ZB22ENF0XR
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
PRIMARY
USAN
OO-67
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
PRIMARY
MERCK INDEX
m4207
Created by admin on Fri Dec 15 15:25:49 GMT 2023 , Edited by admin on Fri Dec 15 15:25:49 GMT 2023
PRIMARY Merck Index
Related Record Type Details
Structure of DESVENLAFAXINE SUCCINATE ANHYDROUS
ANHYDROUS->SOLVATE
Structure of DESVENLAFAXINE
PARENT -> SALT/SOLVATE
Related Record Type Details
Structure of N,O-DIDESMETHYLVENLAFAXINE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of RAC DEHYDRO-O-DESMETHYL VENLAFAXINE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of TRIDESMETHYLVENLAFAXINE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of VENLAFAXINE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of HORDENINE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Related Record Type Details
Structure of DESVENLAFAXINE
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