PIK3CA mutant-selective degrader

Venquis Therapeutics' PIK3CA mutant-selective degrader is an investigational small molecule protein degrader designed to selectively target and degrade mutant forms of the p110α catalytic subunit of PI3-kinase alpha (PIK3CA) while sparing the wild-type protein. Built on the proprietary Chemically Induced Protein Degrader (CIPD) platform, the drug utilizes a direct, non-covalent binding mechanism that is distinct from traditional PROTACs or molecular glues. By specifically degrading mutant PIK3CA, the therapy aims to provide therapeutic benefit while minimizing on-target toxicities, such as hyperglycemia, which are commonly associated with the inhibition of wild-type PIK3CA involved in normal glucose metabolism. The program is currently in the IND-enabling stage of development for the treatment of breast cancer, cervical cancer, and other PIK3CA-mutant solid tumors.

Other names

CIPDChemically Induced Protein Degrader