apomine

Apomine (SR-45023A) is a synthetic gem-diphosphonate small molecule developed by Genzyme (now Sanofi) that was investigated for the treatment of postmenopausal osteoporosis and advanced solid tumors. Unlike traditional nitrogen-containing bisphosphonates that primarily act as antiresorptive agents by inhibiting osteoclast activity, Apomine was characterized as an anabolic agent capable of stimulating new bone formation. In the context of oncology, Apomine exhibits antineoplastic activity by inducing apoptosis in various cancer cell lines, a process thought to be mediated by the inhibition of the mevalonate pathway and the subsequent depletion of isoprenoid intermediates required for the prenylation of small GTP-binding proteins like Ras. Clinical development reached Phase I/II for osteoporosis and Phase I for metastatic solid tumors, but the program is no longer active.

Brand names

Apomine

Other names

tetraisopropyl 2-(3,5-di-tert-butyl-4-hydroxyphenyl)ethyl-1,1-biphosphonate