Temsirolimus is an ester analog of rapamycin. Temsirolimus binds to and inhibits the mammalian target of rapamycin (mTOR), resulting in decreased expression of mRNAs necessary for cell cycle progression and arresting cells in the G1 phase of the cell cycle. mTOR is a serine/threonine kinase which plays a role in the PI3K/AKT pathway that is upregulated in some tumors. Temsirolimus (CCI-779) is an intravenous drug for the treatment of renal cell carcinoma (RCC), developed by Wyeth Pharmaceuticals and approved by the U.S. Food and Drug Administration (FDA) in late May 2007, and was also approved by the European Medicines Agency (EMEA) on November 2007.
Gu, Jianxin; Ruppen, Mark E.; Raveendranath, Panolil; Chew, Warren; Shaw, Chia-Cheng. Production of rapamycin 42-ester with 2,2-bis(hydroxymethyl)propionic acid (CCI-779) and its proline analog. Assignee Wyeth, USA. US 20050234086. (2005).
Chew, Warren; Shaw, Chia-cheng. Preparation of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779). Assignee Wyeth, USA. US 20050033046. (2005).
Gupta, Nitin; Handa, Vishal; Pal, Abir Kumar; Singh, Hemant Kumar; Lahiri, Saswata; Dubey, Sushil Kumar. Process for the preparation of temsirolimus and its intermediates. Assignee Fresenius Kabi Oncology Limited, India. US 20110184167. (2011).
Song, Honghai; Tang, Long; Chen, Wei; Li, Zheng; Li, Jinzhou; Sun, Zhicun; Feng, Jiajin. Process for the preparation of temsirolimus from rapamycin. Assignee Tianjin Weijie Technology Co., Ltd., Peop. Rep. China. US 20130296572. (2013).
Lee, Kwang-Chung; Lee, Ting-Huei; Tung, Yen-Shih; Kao, Chia-Chen; Lee, Tzu-Ai. Process for preparation of temsirolimus. Assignee Chunghwa Chemical Synthesis & Biotech Co., Ltd., Taiwan. US 20100249415. (2010).
Cao, Kangping; Sun, Jian; Xie, Yipeng; Liu, Yanxia. Separation and purification method of temsirolimus. Assignee Sichuan Hairong Pharmaceutical Co., Ltd., Yangtze River Pharmaceutical Group, Peop. Rep. China. CN 109851626. (2019).
He, Zhengquan; Tian, Shan; Huang, Yan. Preparation method of Temsirolimus. Assignee Sichuan Moer Biopharmaceutical Co., Ltd., Peop. Rep. China. CN 107722037. (2018).
