CHK1 inhibitor ADC

CHK1 inhibitor ADC is a first-in-class antibody-drug conjugate (ADC) developed by Cancentus in collaboration with the University of Bern, the University of Geneva, and the University of Basel. The ADC consists of a trastuzumab variant containing five engineered cysteines for site-specific conjugation, linked via a proprietary cleavable linker to a novel checkpoint kinase 1 (CHK1) inhibitor payload. This payload targets oncogene-induced DNA replication stress, a key vulnerability unique to cancer cells, thereby offering enhanced selectivity and a wider therapeutic window compared to traditional ADC payloads like TOP1 inhibitors or microtubule inhibitors. In preclinical studies, the CHK1 inhibitor ADC demonstrated potent HER2-dependent antitumor efficacy in vitro and in vivo, including in trastuzumab deruxtecan-resistant breast cancer models, without causing significant systemic toxicity or body weight loss.

Other names

CHK1 antibody-drug conjugateCHK-1 antibody-drug conjugateCHK 1 antibody-drug conjugateCHK1i ADCCHK-1i ADCCHK 1i ADCHER2-targeting CHK1 inhibitor ADCHER-2-targeting CHK1 inhibitor ADCHER 2-targeting CHK1 inhibitor ADC