Drug intelligence / Profile preview

lalotasate

Development stage
Unknown
Lead developer
Shanxi Zhendong Pharmaceutical
Modality
Small Molecules
Administration
Intravenous
01

Overview

Lalotasate is a novel taxane derivative developed by Shanxi Zhendong Pharmaceutical for the treatment of advanced solid tumors. It is specifically formulated as a lipid microsphere injection, a drug delivery system designed to improve the solubility and stability of the taxane moiety while potentially reducing the systemic toxicities and hypersensitivity reactions often associated with traditional solvent-based taxane formulations (such as those containing Cremophor EL). Mechanistically, lalotasate acts as a microtubule stabilizer; it binds to the beta-subunit of tubulin, promoting microtubule assembly and inhibiting depolymerization. This stabilization leads to cell cycle arrest, particularly in the G2/M phase, and ultimately triggers apoptosis in rapidly proliferating cancer cells. Lalotasate has been evaluated in Phase 1 clinical trials in China to determine its safety, tolerability, and maximum tolerated dose in patients with advanced malignancies who have failed standard therapies.

Other names
lalotasate lipid microsphere injection
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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