Tasisulam

Summary

Tasisulam (CHEMBL2110587) is a phase-3 clinical-stage small-molecule angiogenesis inhibitor targeting RBM39; indicated across 12 conditions including sarcoma and metastatic melanoma.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 1 (RBM39)
• Indications: 12 conditions
• Clinical trials: 5
• Chemistry: 415.1 Da · C11H6BrCl2NO3S2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2110587
Name	Tasisulam
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	10160238
ChEBI	CHEBI:231621
Molecular formula	C11H6BrCl2NO3S2
Molecular weight	415.1
InChIKey	WWONFUQGBVOKOF-UHFFFAOYSA-N

SMILES: C1=CC(=C(C=C1Cl)Cl)C(=O)NS(=O)(=O)C2=CC=C(S2)Br

IUPAC name: N-(5-bromothiophen-2-yl)sulfonyl-2,4-dichlorobenzamide

ChEBI definition: A thiophene substituted by a 2,4-dichlorobenzamide-N-sulfonyl and bromo groups at positions 2 and 4, respectively. It induces tumour cell apoptosis via ROS induction and mitochondrial membrane potential loss and currently in clinical development for the treatment of cancer.

Pharmacological roles (ChEBI): angiogenesis inhibitor, antineoplastic agent, apoptosis inducer.

Also known as: LY-573636, Ly573636, Tasisulam, TASISULAM, TASISULAM (LY573636), Tasisulam (LY573636)

Parent form; salt/anhydrous children: CHEMBL2103823

Patent coverage: 79 distinct patent families (187 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 119 (64%) 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

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
RBM39	RNA binding motif protein 39	Binding		99.9% (common-essential)	Q14498

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): RBM39.

Top Reactome pathways

2 total, by targets touching each:

Pathway	Targets	Genes
mRNA Splicing - Major Pathway	1	RBM39
mRNA Polyadenylation	1	RBM39

Dominant GO biological processes

GO term	Targets
RNA processing	1
mRNA processing	1
RNA splicing	1
regulation of mRNA splicing, via spliceosome	1

Indications & clinical

Indications

12 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
sarcoma	2	MONDO:0005089	EFO:0000691
metastatic melanoma	2	MONDO:0005191	EFO:0002617
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060
fallopian tube neoplasm	2	MONDO:0021092	MONDO:0002158
breast neoplasm	2	MONDO:0021100	MONDO:0007254
ovarian cancer	2	MONDO:0008170	MONDO:0008170
acute myeloid leukemia	1	MONDO:0018874	EFO:0000222
essential thrombocythemia	1	MONDO:0005029	EFO:0000479
lymphoma	1	MONDO:0005062	EFO:0000574
neoplasm	1	MONDO:0005070	EFO:0000616
renal cell carcinoma	1	MONDO:0005086	EFO:0000681

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 5.

Phase distribution

Phase	Trials
PHASE1	4
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00383292	PHASE2	COMPLETED	A Study of Tasisulam in Treating Participants With Malignant Melanoma
NCT01185548	PHASE1	TERMINATED	A Drug Interaction Study of Tasisulam in Patients With Advanced Cancer or Lymphoma
NCT01209832	PHASE1	TERMINATED	A Tasisulam and Midazolam Drug Interaction Study in Cancer Patients
NCT01215916	PHASE1	COMPLETED	A Phase 1 Study in Patients With Solid Tumors
NCT01284335	PHASE1	TERMINATED	A Safety Study in Participants With Advanced Solid Tumors

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

1 molecules share ≥1 primary target. Top 1 by shared-target count:

Molecule	Source	Status	Shared targets
MOLIBRESIB	ChEMBL	Phase 2	RBM39