Tolazamide

Summary

Tolazamide (CHEMBL817) is an approved small-molecule hypoglycemic agent (ATC A10BB05); indicated across 2 conditions including diabetes mellitus and type 2 diabetes mellitus.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: A10BB05
• Indications: 2 conditions
• Chemistry: 311.4 Da · C14H21N3O3S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL817
Name	Tolazamide
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	5503
ChEBI	CHEBI:9613
ATC	A10BB05
Molecular formula	C14H21N3O3S
Molecular weight	311.4
InChIKey	OUDSBRTVNLOZBN-UHFFFAOYSA-N

SMILES: CC1=CC=C(C=C1)S(=O)(=O)NC(=O)NN2CCCCCC2

IUPAC name: 1-(azepan-1-yl)-3-(4-methylphenyl)sulfonylurea

ChEBI definition: An N-sulfonylurea that is 1-tosylurea in which a hydrogen attached to the nitrogen at position 3 is replaced by an azepan-1-yl group. A hypoglycemic agent, it is used for the treatment of type 2 diabetes mellitus.

Pharmacological roles (ChEBI): hypoglycemic agent, potassium channel blocker.

Also known as: NSC-70762, Tolazamida, Tolazamide, Tolinase, U-17835, tolazamide, SID11111870, SID26747047, SID26751566, SID50104182, SID855941, SID90340862

Patent coverage: 5,726 distinct patent families (23,556 SureChEMBL compound mentions), from 1 matched compound structure(s). 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: 14 (assay-derived). Sample: Microtubule-associated protein tau, Lysine-specific demethylase 4E, Fructose-bisphosphate aldolase, 4’-phosphopantetheinyl transferase ffp, Endonuclease 4, Alpha-galactosidase A, Lysosomal alpha-glucosidase, Muscarinic acetylcholine receptor M1, Nuclear factor NF-kappa-B p105 subunit, Cytochrome P450 3A4.

Bioactivity

ChEMBL activities: 6 potent at pChembl ≥ 5 of 19 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P08482	7.95	Potency	11.2	nM	CHEMBL_ACT_4811363
P0A6C1	6.95	Potency	112.2	nM	CHEMBL_ACT_4084739
ALDH1A1	6.55	Potency	281.8	nM	CHEMBL_ACT_4136067
P12530	5.29	IC50	5106	nM	CHEMBL_ACT_7808725
GLA	5.25	Potency	5623	nM	CHEMBL_ACT_4829035
ALOX12	5.15	Potency	7080	nM	CHEMBL_ACT_4532165

Target pathways

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

Indications & clinical

Indications

2 indications (2 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
diabetes mellitus	4	MONDO:0005015	EFO:0000400
type 2 diabetes mellitus	4	MONDO:0005148	MONDO:0005148

Clinical trials

Total trials: 0.

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

PharmGKB dosing guidelines (1) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):

Guideline	Source	Gene(s)	Dosing	Recommendation
Annotation of CPIC Guideline for chlorpropamide, dabrafenib, gliclazid	CPIC	G6PD

Related molecules

Related molecules

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