desvenlafaxine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	4380	93413-62-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: desvenlafaxine desvenlafaxine succinate pristiq DVS-233 desvenlafaxine fumarate	The exact mechanism of the antidepressant action of desvenlafaxine is unknown, but is thought to be related to the potentiation of serotonin and norepinephrine in the central nervous system, through inhibition of their reuptake. Non-clinical studies have shown that desvenlafaxine is a potent and selective serotonin and norepinephrine reuptake inhibitor (SNRI). Molecular weight: 263.38 Formula: C16H25NO2 CLOGP: 2.68 LIPINSKI: 0 HAC: 3 HDO: 2 TPSA: 43.70 ALOGS: -2.27 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

desvenlafaxine
desvenlafaxine succinate
pristiq
DVS-233
desvenlafaxine fumarate

The exact mechanism of the antidepressant action of desvenlafaxine is unknown, but is thought to be related to the potentiation of serotonin and norepinephrine in the central nervous system, through inhibition of their reuptake. Non-clinical studies have shown that desvenlafaxine is a potent and selective serotonin and norepinephrine reuptake inhibitor (SNRI).

Molecular weight: 263.38
Formula: C16H25NO2
CLOGP: 2.68
LIPINSKI: 0
HAC: 3
HDO: 2
TPSA: 43.70
ALOGS: -2.27
ROTB: 4

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
50	mg	O

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	8.40 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	572 mg/mL	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	5.42 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	45 %	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	4.90 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	3.50 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.70 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Feb. 29, 2008	FDA	WYETH PHARMS INC

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product residue present	772.21	14.53	199	24197	3780	63460846
Drug withdrawal syndrome	652.65	14.53	280	24116	26914	63437712
Suicidal ideation	375.23	14.53	256	24140	62165	63402461
Withdrawal syndrome	306.81	14.53	151	24245	19846	63444780
Feeling abnormal	292.16	14.53	321	24075	148071	63316555
Crying	281.90	14.53	150	24246	23193	63441433
Anxiety	246.43	14.53	357	24039	217184	63247442
Irritability	216.84	14.53	141	24255	31553	63433073
Insomnia	212	14.53	331	24065	214921	63249705
Dizziness	157.79	14.53	440	23956	429485	63035141

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product residue present	228.17	22.39	61	6812	2685	34947373
Serotonin syndrome	184.02	22.39	86	6787	19847	34930211
Drug withdrawal syndrome	166.01	22.39	80	6793	19754	34930304
Suicidal ideation	124.88	22.39	85	6788	40303	34909755
Anxiety	100.18	22.39	110	6763	99318	34850740
Suicide attempt	73.22	22.39	61	6812	39055	34911003
Hyperhidrosis	73.15	22.39	82	6791	75610	34874448
Overdose	70.39	22.39	88	6785	90971	34859087
Sexual dysfunction	57.48	22.39	27	6846	6276	34943782
Major depression	55.77	22.39	24	6849	4548	34945510

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Withdrawal syndrome	287.74	14.44	140	20506	26714	79697028
Suicidal ideation	238.02	14.44	180	20466	76160	79647582
Drug withdrawal syndrome	237.42	14.44	134	20512	34584	79689158
Feeling abnormal	223.24	14.44	239	20407	158960	79564782
Product residue present	191.96	14.44	60	20586	3476	79720266
Anxiety	191.35	14.44	276	20370	248236	79475506
Crying	190.92	14.44	101	20545	22942	79700800
Serotonin syndrome	169.39	14.44	119	20527	44908	79678834
Irritability	134.79	14.44	100	20546	41044	79682698
Overdose	125.01	14.44	193	20453	184013	79539729

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N06AX23	NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Other antidepressants
CHEBI has role	CHEBI:35469	antidepressants
CHEBI has role	CHEBI:49103	drug metabolites
CHEBI has role	CHEBI:83399	marine xenobiotic metabolites
FDA EPC	N0000175749	Serotonin and Norepinephrine Reuptake Inhibitor
FDA MoA	N0000000102	Norepinephrine Uptake Inhibitors
FDA MoA	N0000000109	Serotonin Uptake Inhibitors
FDA MoA	N0000182137	Cytochrome P450 2D6 Inhibitors
MeSH PA	D000928	Antidepressive Agents
MeSH PA	D002491	Central Nervous System Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Major depressive disorder	indication	370143000
Generalized anxiety disorder	off-label use	21897009	DOID:14320
Social phobia	off-label use	25501002	DOID:11257
Menopausal flushing	off-label use	198436008
Neuropathic pain	off-label use	247398009
Panic disorder	off-label use	371631005	DOID:594
Ocular hypertension	contraindication	4210003	DOID:9282
Suicidal thoughts	contraindication	6471006
Hypercholesterolemia	contraindication	13644009
Bipolar disorder	contraindication	13746004	DOID:3312

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.79	acidic
pKa2	9.33	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN	INHIBITOR	Ki	7.33	WOMBAT-PK	CHEMBL
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN	INHIBITOR	Ki	6.28	WOMBAT-PK	CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	7.22	CHEMBL

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External reference:

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ID	Source
012574	NDDF
012575	NDDF
015249	NDDF
125017	PUBCHEM_CID
132507	MMSL
200628	MMSL
25184	MMSL
339716	MMSL
386750-22-7	SECONDARY_CAS_RN
38906	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Desvenlafaxine	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0400	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	ANDA	30 sections
Desvenlafaxine	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0400	TABLET, FILM COATED, EXTENDED RELEASE	50 mg	ORAL	ANDA	30 sections
Desvenlafaxine	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0401	TABLET, FILM COATED, EXTENDED RELEASE	100 mg	ORAL	ANDA	30 sections
Desvenlafaxine	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0401	TABLET, FILM COATED, EXTENDED RELEASE	100 mg	ORAL	ANDA	30 sections
Desvenlafaxine	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0603	TABLET, FILM COATED, EXTENDED RELEASE	25 mg	ORAL	ANDA	30 sections
Desvenlafaxine	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0603	TABLET, FILM COATED, EXTENDED RELEASE	25 mg	ORAL	ANDA	30 sections
Desvenlafaxine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3659	TABLET, EXTENDED RELEASE	50 mg	ORAL	ANDA	30 sections
Desvenlafaxine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3659	TABLET, EXTENDED RELEASE	50 mg	ORAL	ANDA	30 sections
Desvenlafaxine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3660	TABLET, EXTENDED RELEASE	100 mg	ORAL	ANDA	30 sections
Desvenlafaxine	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3660	TABLET, EXTENDED RELEASE	100 mg	ORAL	ANDA	30 sections

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