everolimus + capecitabine

Everolimus + capecitabine is an all-oral combination therapy investigated for the treatment of metastatic breast cancer. Everolimus is a small molecule inhibitor of the mammalian target of rapamycin (mTOR), a serine/threonine kinase that plays a central role in regulating cell growth, proliferation, and survival by integrating signals from nutrients and growth factors. Capecitabine is an oral fluoropyrimidine carbamate that functions as a prodrug; it is converted in a three-step enzymatic process to 5-fluorouracil (5-FU) within the body, with the final conversion often occurring preferentially in tumor tissues. Once converted, 5-FU inhibits thymidylate synthase and incorporates into RNA and DNA, leading to cell cycle arrest and apoptosis. This specific combination was evaluated in a Phase I pilot study led by Stanford University to determine the safety, tolerability, and maximum tolerated dose in patients with HER2-negative metastatic breast cancer who had previously received chemotherapy.

Brand names

AfinitorXeloda

Other names

everolimus + capecitabineRAD001 + capecitabine