Drug intelligence / Profile preview

tasisulam

Development stage
Phase 3
Lead developer
Eli Lilly
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
01

Overview

Tasisulam is a small molecule acylsulfonamide anticancer agent developed by Eli Lilly. It functions primarily as an apoptosis stimulant, inducing programmed cell death in cancer cells through activation of the intrinsic (mitochondrial) pathway, leading to cytochrome c release and caspase-dependent cell death. Tasisulam also inhibits mitotic progression and induces vascular normalization in tumors. It was investigated for various cancers including melanoma (with orphan drug status for malignant melanoma), breast cancer, ovarian cancer, non-small cell lung cancer, renal cancer, soft tissue sarcoma, lymphoma, and other solid tumors. Clinical development was discontinued after safety concerns arose during phase III trials in metastatic melanoma due to hematologic toxicity and drug accumulation in some patients[1][2][7][8].

Other names
tasisulam sodiumN-(2,4-Dichlorobenzoyl)-5-bromothiophene-2-sulfonamideN-(5-Bromothiophen-2-ylsulfonyl)-2,4-dichlorobenzamide
02

Targets

RBM39 (RNA-binding motif protein 39)DCAF15 (DDB1- and CUL4-associated factor 15 ubiquitin ligase complex)

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