ASP9521

ASP9521 is a first-in-class, selective, orally bioavailable small molecule inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; also known as aldo-keto reductase 1C3 or AKR1C3). It was developed by Astellas Pharma for the treatment of castration-resistant prostate cancer and functions by inhibiting the conversion of androstenedione to testosterone and other androgens. Preclinical studies demonstrated anti-tumor activity in vitro and in vivo. In addition to its primary action on AKR1C3, ASP9521 has shown moderate inhibitory activity against carbonyl reductase 1 (CBR1), suggesting a potential dual mechanism that may help overcome anthracycline resistance and cardiotoxicity. Despite favorable pharmacokinetics and safety profiles observed in early clinical trials, no significant clinical efficacy was seen in patients with metastatic castration-resistant prostate cancer, leading to discontinuation of its development[5][6][8].

Other names

1126084-37-4