Drug intelligence / Profile preview

CH-2-102

Development stage
Preclinical
Lead developer
Indian Institute of Technology Hyderabad
Modality
Small Molecules
Administration
Intravenous
01

Overview

CH-2-102 is a novel small molecule tubulin polymerization inhibitor developed for the treatment of melanoma. It acts by directly binding the colchicine site on tubulin, thereby suppressing microtubule polymerization, inducing G2 phase cell cycle arrest, and showing high anti-tumor activity in both human (A375) and murine (B16-F10) melanoma cell lines. Unlike paclitaxel and related agents, CH-2-102 is effective against drug-resistant melanoma cells due to its distinct binding site and is not a substrate for P-glycoprotein. It demonstrates higher potency than colchicine and a previous generation inhibitor (QW-296). CH-2-102 has also been formulated into pH-sensitive nanoparticles for enhanced delivery and tumor regression in animal models of lung metastasis from melanoma[1].

02

Targets

TUBB (Tubulin (alpha and beta subunits))

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