tianeptine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
	2650	72797-41-2

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tianeptine monosodium
tianeptine sodium
stablon
tianeptine
coaxil

Molecular weight: 436.95
Formula: C21H25ClN2O4S
CLOGP: 1.52
LIPINSKI: 0
HAC: 6
HDO: 2
TPSA: 86.71
ALOGS: -5.03
ROTB: 8

Drug dosage:

Dose	Unit	Route
37.50	mg	O

ADMET properties:

Property	Value	Reference
BA (Bioavailability)	99 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.30 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	2.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.05 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.40 hours	Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,IKBKB,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK14,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CG,PIM2,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,ZAP70	42
kinase-selectivity-class	AXL,EIF2AK3,GRK2,MAP2K6,MAPK7,PDK4,STK33,TEK	8
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

None

FDA Adverse Event Reporting System (Female)

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
Persistent genital arousal disorder	162.65	42.46	24	1291	676	90626456
Overdose	77.28	42.46	40	1275	157669	90469463
Drug interaction	75.90	42.46	48	1267	276405	90350727
Intentional overdose	61.36	42.46	29	1286	93805	90533327
Disturbance in sexual arousal	59.99	42.46	9	1306	283	90626849
Suicide attempt	54.54	42.46	25	1290	75374	90551758
Perineal pain	53.77	42.46	9	1306	574	90626558
Female reproductive tract disorder	52.98	42.46	9	1306	627	90626505
Genital pain	51.41	42.46	9	1306	749	90626383
Crush syndrome	44.50	42.46	7	1308	302	90626830

FDA Adverse Event Reporting System (Male)

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
Serotonin syndrome	93.06	48.46	28	606	25817	42594884
Stress cardiomyopathy	73.60	48.46	15	619	2770	42617931

FDA Adverse Event Reporting System (Geriatric)

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
Persistent genital arousal disorder	144.74	36.16	22	1829	654	110586794
Serotonin syndrome	109.36	36.16	40	1811	59113	110528335
Overdose	61.99	36.16	42	1809	233752	110353696
Drug interaction	48.20	36.16	50	1801	500133	110087315
Stress cardiomyopathy	45.89	36.16	15	1836	15791	110571657
Crush syndrome	41.77	36.16	7	1844	388	110587060
Disturbance in sexual arousal	41.58	36.16	7	1844	399	110587049
Female reproductive tract disorder	40.10	36.16	7	1844	495	110586953

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N06AX14	NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Other antidepressants
MeSH PA	D000928	Antidepressive Agents
MeSH PA	D000929	Antidepressive Agents, Tricyclic
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D011619	Psychotropic Drugs
CHEBI has role	CHEBI:35469	antidepressant
CHEBI has role	CHEBI:35474	anxiolytic drug
CHEBI has role	CHEBI:35476	antipsychotic agent
CHEBI has role	CHEBI:55322	μ-opioid receptor agonist
CHEBI has role	CHEBI:65191	second generation antipsychotic

Related Drugs by ATC class:

N06AX Other antidepressants 28 drugs

agomelatine bifemelane brexanolone bupropion desvenlafaxine dextromethorphan duloxetine esketamine gepirone levomilnacipran medifoxamine mianserin show all 28 →

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

None

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.76	acidic
pKa2	6.85	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN		Ki	6.42		PDSP

External reference:

ID	Source
D02575	KEGG_DRUG
30123-17-2	SECONDARY_CAS_RN
C0076652	UMLSCUI
CHEBI:91749	CHEBI
CHEMBL1289110	ChEMBL_ID
DB09289	DRUGBANK_ID
C050504	MESH_SUPPLEMENTAL_RECORD_UI
7558	IUPHAR_LIGAND_ID
4906	INN_ID
0T493YFU8O	UNII
68870	PUBCHEM_CID
38252	RXNORM
005515	NDDF
005516	NDDF
1172815007	SNOMEDCT_US
703713005	SNOMEDCT_US
703714004	SNOMEDCT_US

Pharmaceutical products:

None