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

Stem definition	Drug id	CAS RN
serotonin and/or norepinephrine reuptake inhibitors, fluoxetine derivatives	972	116539-59-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: yentreve cymbalta duloxetine (S)-Duloxetine duloxetine hydrochloride duloxetine HCl	A thiophene derivative and selective NEUROTRANSMITTER UPTAKE INHIBITOR for SEROTONIN and NORADRENALINE (SNRI). It is an ANTIDEPRESSIVE AGENT and ANXIOLYTIC, and is also used for the treatment of pain in patients with DIABETES MELLITUS and FIBROMYALGIA. Molecular weight: 297.42 Formula: C18H19NOS CLOGP: 4.26 LIPINSKI: 0 HAC: 2 HDO: 1 TPSA: 21.26 ALOGS: -5 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

yentreve
cymbalta
duloxetine
(S)-Duloxetine
duloxetine hydrochloride
duloxetine HCl

A thiophene derivative and selective NEUROTRANSMITTER UPTAKE INHIBITOR for SEROTONIN and NORADRENALINE (SNRI). It is an ANTIDEPRESSIVE AGENT and ANXIOLYTIC, and is also used for the treatment of pain in patients with DIABETES MELLITUS and FIBROMYALGIA.

Molecular weight: 297.42
Formula: C18H19NOS
CLOGP: 4.26
LIPINSKI: 0
HAC: 2
HDO: 1
TPSA: 21.26
ALOGS: -5
ROTB: 6

Status: OFP

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

Drug dosage:

Dose	Unit	Route
60	mg	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	8.57 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	50 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	2.88 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
t_half (Half-life)	12 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.04 %	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Aug. 3, 2004	FDA	LILLY

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
Drug withdrawal syndrome	4079.64	10.00	2008	236838	25186	63224990
Dysphoria	3522.88	10.00	1129	237717	3837	63246339
Affect lability	2782.04	10.00	1174	237672	9977	63240199
Irritability	2255.42	10.00	1434	237412	30260	63219916
Suicidal ideation	2034.84	10.00	1765	237081	60656	63189520
Agitation	1774.72	10.00	1603	237243	58154	63192022
Sensory disturbance	1314.97	10.00	751	238095	12921	63237255
Hyperhidrosis	1288.74	10.00	1798	237048	106038	63144138
Vertigo	1216.80	10.00	1306	237540	58581	63191595
Paraesthesia	1186.48	10.00	2121	236725	154845	63095331

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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
Drug withdrawal syndrome	1270.43	11.19	691	75471	19143	34861626
Dysphoria	1218.65	11.19	368	75794	1934	34878835
Affect lability	1145.29	11.19	393	75769	3290	34877479
Suicidal ideation	772.19	11.19	666	75496	39722	34841047
Irritability	649.80	11.19	491	75671	24199	34856570
Sensory disturbance	553.58	11.19	270	75892	5907	34874862
Agitation	470.59	11.19	602	75560	56797	34823972
Vertigo	467.37	11.19	411	75751	25125	34855644
Paraesthesia	452.27	11.19	625	75537	63547	34817222
Insomnia	435.92	11.19	798	75364	103109	34777660

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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
Drug withdrawal syndrome	980.01	9.93	798	222573	33920	79487097
Suicidal ideation	861.96	9.93	1066	222305	75274	79445743
Serotonin syndrome	838.52	9.93	818	222553	44209	79476808
Completed suicide	569.92	9.93	1746	221625	244021	79276996
Hyperhidrosis	489.93	9.93	1216	222155	150276	79370741
Dysphoria	474.18	9.93	242	223129	4492	79516525
Affect lability	402.98	9.93	298	223073	10961	79510056
Irritability	361.16	9.93	508	222863	40636	79480381
Tremor	352.41	9.93	1163	222208	168920	79352097
Anxiety	346.06	9.93	1496	221875	247016	79274001

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FDA Adverse Event Reporting System (Pediatric)

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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
Telangiectasia congenital	30.47	28.20	9	373	18	89392
Liver disorder	29.80	28.20	8	374	9	89401

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Pharmacologic Action:

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Source	Code	Description
ATC	N06AX21	NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Other antidepressants
CHEBI has role	CHEBI:35469	antidepressants
FDA EPC	N0000175749	Serotonin and Norepinephrine Reuptake Inhibitor
FDA MoA	N0000000102	Norepinephrine Uptake Inhibitors
FDA MoA	N0000000109	Serotonin Uptake Inhibitors
MeSH PA	D000700	Analgesics
MeSH PA	D000928	Antidepressive Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D015259	Dopamine Agents
MeSH PA	D049990	Membrane Transport Modulators

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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
Generalized anxiety disorder	indication	21897009	DOID:14320
Female stress incontinence	indication	60241006	DOID:724
Fibromyalgia	indication	203082005	DOID:631
Major depressive disorder	indication	370143000
Diabetic peripheral neuropathy	indication	424736006
Chronic Musculoskeletal Pain	indication
Osteoarthritis	off-label use	396275006
Suicidal thoughts	contraindication	6471006
Alcoholism	contraindication	7200002
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	8.7	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 20MG BASE	CYMBALTA	LILLY	N021427	Aug. 3, 2004	RX	CAPSULE, DELAYED REL PELLETS	ORAL	April 20, 2023	NEW PATIENT POPULATION
EQ 30MG BASE	CYMBALTA	LILLY	N021427	Aug. 3, 2004	RX	CAPSULE, DELAYED REL PELLETS	ORAL	April 20, 2023	NEW PATIENT POPULATION
EQ 60MG BASE	CYMBALTA	LILLY	N021427	Aug. 3, 2004	RX	CAPSULE, DELAYED REL PELLETS	ORAL	April 20, 2023	NEW PATIENT POPULATION

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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	9.62	CHEMBL	CHEMBL
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN	INHIBITOR	Ki	8.22	CHEMBL	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	5.30	PDSP
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	6.30	IUPHAR
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	5.68	PDSP
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	ANTAGONIST	Ki	6	IUPHAR
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN	ANTAGONIST	Ki	6.40	IUPHAR
5-hydroxytryptamine receptor 7	GPCR	P34969	5HT7R_HUMAN		Ki	5.65	PDSP
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	5.64	PDSP
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN		Ki	5.40	PDSP

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External reference:

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ID	Source
29E	PDB_CHEM_ID
008705	NDDF
008707	NDDF
136434-34-9	SECONDARY_CAS_RN
18760	MMSL
202	IUPHAR_LIGAND_ID
208014	MMSL
33554	MMSL
4021477	VANDF
407032004	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Cymbalta	HUMAN PRESCRIPTION DRUG LABEL	1	0002-3235	CAPSULE, DELAYED RELEASE	20 mg	ORAL	NDA	36 sections
Cymbalta	HUMAN PRESCRIPTION DRUG LABEL	1	0002-3235	CAPSULE, DELAYED RELEASE	20 mg	ORAL	NDA	36 sections
Cymbalta	HUMAN PRESCRIPTION DRUG LABEL	1	0002-3240	CAPSULE, DELAYED RELEASE	30 mg	ORAL	NDA	36 sections
Cymbalta	HUMAN PRESCRIPTION DRUG LABEL	1	0002-3240	CAPSULE, DELAYED RELEASE	30 mg	ORAL	NDA	36 sections
Cymbalta	HUMAN PRESCRIPTION DRUG LABEL	1	0002-3270	CAPSULE, DELAYED RELEASE	60 mg	ORAL	NDA	36 sections
Cymbalta	HUMAN PRESCRIPTION DRUG LABEL	1	0002-3270	CAPSULE, DELAYED RELEASE	60 mg	ORAL	NDA	36 sections
Duloxetine	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2890	CAPSULE, DELAYED RELEASE PELLETS	20 mg	ORAL	ANDA	29 sections
Duloxetine	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2891	CAPSULE, DELAYED RELEASE PELLETS	30 mg	ORAL	ANDA	29 sections
Duloxetine	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2892	CAPSULE, DELAYED RELEASE PELLETS	60 mg	ORAL	ANDA	29 sections
Duloxetine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7043	CAPSULE, DELAYED RELEASE	20 mg	ORAL	ANDA	31 sections

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