JAB-2485

JAB-2485 is a highly selective, orally bioavailable small-molecule inhibitor of Aurora kinase A (AURKA), developed by Jacobio Pharma for the treatment of various solid tumors. Mechanistically, JAB-2485 binds to and inhibits AURKA, disrupting mitotic spindle assembly and chromosome segregation, leading to cell cycle arrest in the G2/M phase and induction of apoptosis in tumor cells overexpressing AURKA[1][2][3][4]. Preclinical studies demonstrate that JAB-2485 exhibits subnanomolar potency against AURKA with approximately 1,500-fold selectivity over related kinases (AURKB/AURKC), resulting in strong antitumor activity and favorable safety profiles compared to less selective inhibitors[3][4][6]. The drug is being investigated for use in estrogen receptor-positive breast cancer, triple-negative breast cancer, small cell lung cancer (especially those with retinoblastoma gene loss), neuroblastoma, and other solid tumors with ARID1A mutations[2][3][4]. As of 2024, JAB-2485 is undergoing Phase 1/2 clinical trials in the US and China for these indications[6][7].

Other names

aurora a kinase inhibitor jab-2485