Cyclopropane is the smallest cyclic compound with unique structural features and physicochemical properties, which is widely used in the design of small molecule drugs. In drug design, it is often used to increase activity, fix conformation and improve PK and water solubility. The introduction of cyclopropyl groups into drugs can change various properties of molecules, such as improving metabolic stability; increasing biological activity; enhancing drug efficacy; limiting polypeptide conformation and slowing down its hydrolysis; reducing plasma clearance; improving drug dissociation and many more. Cyclopropane rings are widely found in marketed drugs, including cardiovascular drugs, central nervous system (CNS) drugs, anticancer drugs, autoimmune and anti-inflammatory drugs.
On August 21, 2023, Exelixis and Ipsen announced that the global phase 3 CONTACT-02 study of cabozantinib (Cabometyx ®) in combination with atezolizumab for metastatic castration-resistant prostate cancer (mCRPC) met the primary endpoint of progression-free survival (PFS) in an interim analysis.
Prostate cancer is the fourth most common cancer worldwide and the second most common cancer among men. At present, the drugs approved for the treatment of CRPC are basically AR inhibitors or PARP inhibitors, and the combination therapy of Cabozantinib + Atezolizumab is expected to become a new treatment option for such patients. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.