General
Preferred name
DESVENLAFAXINE
Synonyms
DESVENLAFAXINE SUCCINATE ()
WY 45233 succinate ()
O-Desmethylvenlafaxine succinate hydrate ()
O-Desmethylvenlafaxine ()
Desvenlafaxine succinate hydrate ()
O-Desmethylvenlafaxine succinate ()
Desvenalfaxine succinate ()
desmethylvenlafaxine ()
DESVENLAFAXINE FUMARATE ()
WY 45233 Succinate ()
WY45233 ()
Desvenlafaxine succinate anhydrous ()
Dvs anhydrous ()
DVS-233 ()
Pristiq ()
Desvenlafaxine succinate monohydrate ()
O-desmethyl venlafaxine succinate ()
WY-45233 ()
Newven ()
ODV ()
Khedezla ()
D-veniz ()
Mdd-xr ()
Desvenlafaxine ()
O-desmethylvenlafaxine fumarate ()
Desvenlafaxine fumarate anhydrous ()
(±)-O-Desmethyl Venlafaxine ()
(±)-O-Desmethyl Venlafaxine-d6 ()
Desvenlafaxine (succinate hydrate) ()
P&D ID
PD009285
CAS
386750-22-7
93413-62-8
448904-47-0
1062605-69-9
Tags
natural product
drug
available
Approved by
FDA
First approval
2008
2013
Drug Status
investigational
approved
Drug indication
Major depressive disorder
Fibromyalgia
Menopause symptom
Max Phase
Phase 4
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
ABSORPTION
Oral bioavailability is approximately 80%[A6997,A6991,A6996] and is unaffected by food. Peak plasma concentration is reached in 7.5 hours[A6996].
PHARMACODYNAMICS
Desvenlafaxine is a selective serotonin and norepinephrine reuptake inhibitor[A6990,A6991,Label]. It lacks significant activity on muscarinic-cholinergic, H1-histaminergic, or α1-adrenergic receptors in vitro. Desvenlafaxine does not appear to exert activity against calcium, chloride, potassium and sodium ion channels and also lacks monoamine oxidase (MAO) inhibitory activity[A6991]. It was also shown to lack significant activity again the cardiac potassium channel, hERG, in vitro[A36975]. Compared to other SNRIs, desvenlafaxine undergoes simple metabolism, has a low risk of drug-drug interactions and does not have to be extensively titrated to reach a therapeutic dose[Label].
MOA
Desvenlafaxine, the active metabolite of venlafaxine, is a selective serotonin and norepinephrine reuptake inhibitor[A6990,A6991,Label]. Desvenlafaxine inhibits neurotransmitter reuptake in serotonin, norepinephrine, and dopamine transporters[A6991]. Desvenlafaxine inhibits serotonin transporters with 10 times the affinity of norepinephrine transporters, and dopamine transporters with the lowest affinity[A6991]. In vitro, desvenlafaxine has no inhibition of monoamine oxidase, and almost no affinity for muscarinic, cholinergic, H1-histaminergic, and alpha1-adrenergic receptors[A6991].
HALF-LIFE
The mean terminal half life is 11.1 hours and may be prolonged in patients with renal and/or moderate to severe hepatic impairment[A6991].
INDICATION
Desvenlafaxine is indicated for the treatment of major depressive disorder in adults[A6990,A6991,Label].
ROE
Desvenlafaxine is mainly excreted in the urine[A6991]. 45% of the dose is unchanged in the urine, 19% is excreted as a glucuronide metabolite, and <5% is excreted as N,O-didesmethylvenlafaxine[A6991]. No dosage adjustment is necessary for gender, ethnicity, food, or combination with other psychotropics[A6997].
TOXICITY
Desvenlafaxine is excreted in breast milk and as a result, nursing mothers must either stop the drug or stop breast feeding depending on the risks and benefit to mother and child[Label,A6988].
METABOLISM
Desvenlafaxine also undergoes oxidative N-demethylation via cytochrome P450 3A4 to a minor extent[A6991]. CYP2D6 is not involved with the metabolism of desvenlafaxine[A6991].
DESCRIPTION
Desvenlafaxine belongs to the group of serotonin–norepinephrine reuptake inhibitors (SNRIs) which are antidepressants. Desvenlafaxine is the major active metabolite of .
(GtoPdb)
DESCRIPTION
Dual serotonin/noradrenalin re-uptake inhibitor
(Tocriscreen Plus)
DESCRIPTION
WY 45233 succinate is an inhibitor of serotonin and noradrenalin reuptake (SNRI) used in the treatment of major depressive disorder (MDD). WY 45233 succinate inhibits [3H]5-HT and [3H]NE uptake (IC50 = 47.3 and 531.3 nM).
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
24
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
ChEMBL Approved Drugs
ChEMBL Drugs
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
Enamine BioReference Compounds
Guide to Pharmacology
Ki Database
LSP-MoA library (Laboratory of Systems Pharmacology)
NCATS Inxight Approved Drugs
Other bioactive compounds
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
The Spectrum Collection
Tocriscreen Plus
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
83
Molecular Weight
263.19
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
2
Rotatable Bonds
4
Ring Count
2
Aromatic Ring Count
1
cLogP
2.73
TPSA
43.7
Fraction CSP3
0.62
Chiral centers
1.0
Largest ring
6.0
QED
0.88
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Transporters
Target
Serotonin Transporter
5-HT
Norepinephrine (NE)
SNRI
Adrenergic Receptor,Serotonin Transporter
Pathway
GPCR/G protein
Neuroscience
MOA
5-HT Receptor
VGSC Target
Nav1.5
Source data
