tpx-4589

TPX-4589 is a **humanized IgG1 antibody-drug conjugate (ADC)** targeting the tight junction protein **Claudin 18.2 (CLDN18.2)**, a protein overexpressed in various gastrointestinal cancers, including gastric, gastroesophageal junction, and pancreatic cancers[1][3][5][9]. The drug consists of a monoclonal antibody specific for CLDN18.2 conjugated via a valine-citrulline-p-aminobenzyl (MC-VC-PAB) cleavable linker to the cytotoxic payload **Monomethyl auristatin E (MMAE)**[1][9]. The mechanism involves **binding to CLDN18.2-expressing tumor cells**, followed by internalization and release of MMAE, leading to **microtubule inhibition, mitosis arrest, and apoptosis**[3]. TPX-4589 has demonstrated potent preclinical and clinical efficacy and safety in both high- and low-expressing CLDN18.2 tumor models and is advancing in multiple late-phase trials for gastrointestinal cancers including gastric, gastroesophageal junction, biliary tract, pancreatic, and other solid tumors[2][3][5][6][8][9]. Development was initiated by LaNova Medicines, with subsequent development and commercialization rights in certain territories licensed to Turning Point Therapeutics[3][5].

Other names

tpx-4589tpx4589tpx 4589lm-302lm302lm 302bms-986476bms986476bms 986476