basroparib

Basroparib (STP1002) is a novel, orally active small molecule inhibitor that selectively targets tankyrase 1 and 2 (TNKS1/2), members of the poly(ADP-ribose) polymerase (PARP) enzyme family[1][3][4]. By inhibiting tankyrase activity, basroparib stabilizes AXIN proteins and antagonizes the Wnt/β-catenin signaling pathway, which is implicated in tumorigenesis—particularly in cancers with APC mutations such as colorectal cancer[4][5]. Preclinical studies have demonstrated antitumor efficacy without significant on-target gastrointestinal toxicity. Basroparib has shown selective inhibition of TNKS1/2 over PARP1/2 and suppresses Wnt-mediated cancer stemness, a mechanism associated with resistance to other targeted therapies like MEK inhibitors in KRAS-mutated colorectal cancer[5]. The drug was developed by ST Pharm and has completed phase 1 clinical trials for advanced-stage solid tumors including colorectal carcinoma, gastric carcinoma, and hepatocellular carcinoma[5][8].