Drugs R D. 2010;10(3):165-78. doi: 10.2165/11586010-000000000-00000.
Ridaforolimus (AP23573; MK 8669) is an analog of sirolimus and a small molecule inhibitor of the mammalian target of rapamycin for the treatment of cancer. Both intravenous and oral formulations of the compound are being tested in clinical trials for the treatment of soft-tissue and bone sarcomas. It is in phase III development for sarcoma in the EU and US, and phase II for breast cancer, endometrial cancer, non-small cell lung cancer, and prostate cancer in the US and other markets in the world. This review discusses the key development milestones and therapeutic trials of this drug.
瑞达福罗莫司(AP23573;MK 8669)是西罗莫司的类似物,也是一种用于治疗癌症的雷帕霉素哺乳动物靶蛋白的小分子抑制剂。该化合物的静脉内和口服制剂都正在临床试验中用于软组织肉瘤和骨肉瘤的治疗。它正在欧盟和美国的肉瘤 III 期开发中,在美国和世界其他市场的乳腺癌、子宫内膜癌、非小细胞肺癌和前列腺癌的 II 期开发中。本文讨论了该药物的关键开发里程碑和治疗试验。