CGT4255

CGT4255 is a potent, selective, orally bioavailable small molecule inhibitor that targets mutant forms of HER2 (also known as ErbB2), while sparing wild-type EGFR. It is being developed by Cogent Biosciences for the treatment of solid tumors driven by oncogenic HER2 mutations, including those with brain metastases. Preclinical data demonstrate that CGT4255 has low nanomolar potency against both wild-type and mutant ErbB2, with over 100-fold selectivity versus wild-type EGFR. The compound exhibits best-in-class brain penetration properties (up to 80% in preclinical models) and induces tumor regression in multiple HER2-mutant tumor models, including intracranial models. Its favorable pharmacokinetic profile includes high oral bioavailability and long half-life across species.