KBP-2205 is a small molecule drug with global intellectual property rights, independently discovered by Keythera Pharmaceuticals. Its primary clinical indications are advanced malignant solid tumors, including breast cancer, ovarian cancer, pancreatic cancer, prostate cancer, etc., with homologous recombination repair defects or BRCA gene mutations.

KBP-2205 is a second-generation PARP inhibitor. Based on the principle of synthetic lethality, PARP inhibitors have a good antitumor effect on malignant tumors with mutations in genes related to DNA homologous recombination repair (HRR). Second-generation PARP inhibitors can reduce the myelosuppression caused by first-generation PARP inhibitors, alleviating hematological toxicity such as anemia, and thus offer better safety profiles. Second-generation PARP inhibitors also offer more possibilities for combination therapy, especially with drugs that also have myelosuppressive effects, including chemotherapy drugs and some targeted anticancer drugs, thereby expanding the clinical application of PARP inhibitors.

Preclinical studies show that KBP-2205 selectively induces PARP1 trapping and can cause tumor cell death only in cells with BRCA1/2 mutations, but has no effect on the growth of BRCA1/2 wild-type cells. KBP-2205 has demonstrated good pharmacokinetic characteristics and safety profiles  in animals. It has also shown significant tumor inhibitory effects in CDX and PDX animal models of ovarian and breast cancers, with some animals achieved complete tumor regression. This effect lasts even 2-7 weeks after drug discontinuation. KBP-2205 is expected to become a new generation of PARP-targeted anticancer drugs in the future.

Back to List