Melarsoprol

Summary

Melarsoprol (CHEMBL166) is a phase-3 clinical-stage small molecule (ATC P01CD01); indicated across 2 conditions including trypanosomiasis and leishmaniasis.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: P01CD01
• Indications: 2 conditions
• Clinical trials: 1
• Chemistry: 398.3 Da · C12H15AsN6OS2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL166
Name	Melarsoprol
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	10311
ATC	P01CD01
Molecular formula	C12H15AsN6OS2
Molecular weight	398.3
InChIKey	JCYZMTMYPZHVBF-UHFFFAOYSA-N

SMILES: C1C(S[As](S1)C2=CC=C(C=C2)NC3=NC(=NC(=N3)N)N)CO

IUPAC name: [2-[4-[(4,6-diamino-1,3,5-triazin-2-yl)amino]phenyl]-1,3,2-dithiarsolan-4-yl]methanol

Also known as: Mel b, Melarsoprol, RP 3854, RP-3854, melarsoprol, melarsporol, MELARSOPROL, Melarosoprol

Patent coverage: 1,570 distinct patent families (6,457 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: 6 (assay-derived). Sample: Muscarinic acetylcholine receptor M1, Prostaglandin G/H synthase 1, Sodium-dependent dopamine transporter, 3’,5’-cyclic-AMP phosphodiesterase 4A, Adenosine receptor A3, Gamma-aminobutyric acid receptor subunit alpha-1.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
ADORA3	5.72	AC50	1918	nM	CHEMBL_ACT_25198784

Target pathways

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

Indications & clinical

Indications

2 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
trypanosomiasis	3	MONDO:0000940	DOID:10113
leishmaniasis	3	MONDO:0011989	EFO:0005044

Clinical trials

Total trials: 1.

Phase distribution

Phase	Trials
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00330148	PHASE3	TERMINATED	Randomized Clinical Trial of Three Drug Combinations for Late-Stage Gambiense Human African Trypanosomiasis

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

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