tasisulam + docetaxel

Tasisulam + docetaxel is a combination chemotherapy regimen that was investigated for the treatment of advanced solid tumors. Tasisulam (LY573636) is a synthetic acylsulfonamide small molecule that functions as a molecular glue, inducing the degradation of the splicing factor RBM39 by facilitating its interaction with the E3 ubiquitin ligase substrate receptor DCAF15. Additionally, tasisulam has been shown to inhibit VEGF-induced angiogenesis and trigger the intrinsic apoptotic pathway. Docetaxel is a well-established taxane that promotes microtubule assembly and inhibits disassembly, leading to cell cycle arrest in the G2/M phase. The development of this combination by Eli Lilly was halted during Phase 1b clinical trials due to significant safety concerns, particularly severe hematologic toxicities including grade 4 neutropenia and thrombocytopenia.

Other names

tasisulam sodium + docetaxelLY573636 + docetaxel