DX126-262

DX126-262 is a next-generation HER2-targeted antibody-drug conjugate (ADC) developed for the treatment of HER2-positive cancers. It consists of a recombinant humanized anti-HER2 monoclonal antibody (DX-CHO9, IgG1) conjugated via a cysteine thiol linkage to Tub114, a novel hydrophilic analogue of Tubulysin B—a potent tubulin inhibitor. The average drug-to-antibody ratio is approximately 3.5–3.8[1][3][6]. Upon binding to HER2 on tumor cells, the ADC is internalized and degraded by proteases, releasing Tub114-cys inside the cell. This payload binds to tubulin and inhibits its polymerization, disrupting cell division and leading to tumor cell death[1][6]. Preclinical studies show that DX126-262 has superior antitumor efficacy compared with existing ADCs like Kadcyla (T-DM1), with improved safety due to reduced off-target toxicity and lower risk of interstitial pneumonitis or hepatotoxicity[6]. Clinical trials have demonstrated significant activity in multiple HER2-positive solid tumors including breast cancer, gastric cancer, non-small cell lung cancer, transitional cell carcinoma, and gastroesophageal junction adenocarcinoma[2][4].

Other names

Recombinant Humanized Anti-Her2 Monoclonal Antibody-Tub114 Conjugate for Intravenous Injection