KBP-2205 is a highly selective second-generation poly(ADP-ribose) polymerase 1 (PARP1) inhibitor, developed based on innovative molecular design, featuring precise targeting and excellent drugability properties. Preclinical study results demonstrated that KBP-2205 effectively mitigates the risk of hematological toxicity caused by inhibition of PARP2 , exhibiting a superior therapeutic window. In various homologous recombination repair (HRD)-deficient tumor models, KBP-2205 demonstrates potent antitumor activity. Its high oral bioavailability and favorable pharmacokinetic profile support a once-daily dosing regimen.

KBP-2205 has currently initiated Phase 1/2 clinical studies, designed to evaluate its safety, pharmacokinetic profile, and preliminary efficacy in patients with advanced solid tumors. Given its precise targeting mechanism, superior DNA-trapping activity, and optimized therapeutic window, this agent holds promise for providing a safer and more durable targeted therapeutic option for cancer patients with BRCA mutations or other HRD characteristics . especially having significant clinical value for those who are resistant to traditional PARP inhibitors or sensitive to hematological toxicity .

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