Tianeptine

Summary

Tianeptine (CHEMBL1289110) is a phase-3 clinical-stage small molecule (ATC N06AX14); indicated across 3 conditions including bipolar disorder and depressive disorder.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: N06AX14
• Indications: 3 conditions
• Clinical trials: 8
• Chemistry: 437 Da · C21H25ClN2O4S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1289110
Name	Tianeptine
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	68870
ChEBI	CHEBI:190008
ATC	N06AX14
Molecular formula	C21H25ClN2O4S
Molecular weight	437
InChIKey	JICJBGPOMZQUBB-UHFFFAOYSA-N

SMILES: CN1C2=CC=CC=C2C(C3=C(S1(=O)=O)C=C(C=C3)Cl)NCCCCCCC(=O)O

IUPAC name: 7-[(3-chloro-6-methyl-5,5-dioxo-11H-benzo[c][2,1]benzothiazepin-11-yl)amino]heptanoic acid

ChEBI definition: A member of the class of dibenzothiazepines that is 3-chloro-6-methyl-6,11-dihydrodibenzo[c,f][1,2]thiazepine 5,5-dioxide substituted by a (6-carboxyhexyl)amino group at position 11.

Also known as: Gas station heroin, Jnj-39823277, JNJ-39823277, S-1574, Stablon, Tianeptina, Tianeptine, TPI-1062, tianeptine, TIANEPTINE, Tianeptine (sodium salt)

Parent form; salt/anhydrous children: CHEMBL2361572

Patent coverage: 1,378 distinct patent families (5,440 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 5,402 (99%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Mu-type opioid receptor, D(3) dopamine receptor, Delta-type opioid receptor, Nuclear receptor subfamily 1 group I member 2.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 4 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
OPRM1	5.58	AC50	2600	nM	CHEMBL_ACT_25147313

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

3 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
bipolar disorder	3	MONDO:0004985	MONDO:0004985
depressive disorder	3	MONDO:0002050	MONDO:0002009
nervous system disorder	2	MONDO:0005071	EFO:0000618

Clinical trials

Total trials: 8.

Phase distribution

Phase	Trials
Not specified	3
PHASE4	2
PHASE3	1
PHASE2	1
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01309776	PHASE4	COMPLETED	Comparison of Tianeptine Versus Escitalopram Patients Major Depressive Disorder
NCT04249596	PHASE4	TERMINATED	Tianeptine for Treatment Resistant Depression
NCT00879372	PHASE3	UNKNOWN	Efficacy of Adjunctive Tianeptine in the Treatment of Bipolar Depression
NCT06012552	PHASE2	RECRUITING	Randomized, Double-blind, Placebo-controlled Trial of the Efficacy and Safety of Tianeptine in the Treatment of Covid Fog Symptoms in Patients After COVID-19.
NCT02103985	PHASE1	COMPLETED	A Study of Effect of Food on the Pharmacokinetics of a Single JNJ-39823277 (TPI-1062) Dose in Healthy Participants
NCT04145076	Not specified	UNKNOWN	Brain Response to Serotonergic Medications in ASD
NCT04446039	Not specified	COMPLETED	Non-interventional, Retrospective Cohort Study to Explore Antidepressant Treatment in Korea
NCT05935059	Not specified	COMPLETED	The Efficacy of Tianeptine Versus Pregabalin on Acute and Chronic Post Mastectomy Pain After Breast Cancer Surgery.

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 1 clinical and 2 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).