title: Ridaforolimus: a promising drug in the treatment of soft-tissue sarcoma and other malignancies.
abstract: Ridaforolimus (deforolimus; AP23573; MK-8669) is a novel sirolimus derivative manufactured by ARIAD Pharmaceuticals and acquired by Merck. It is a small-molecule kinase inhibitor of the mTOR in clinical development for the treatment of cancer. Both intravenous and oral formulations of the agent are being tested in cancer clinical trials. In preclinical and clinical studies, ridaforolimus exhibited significant antitumor activity with acceptable safety and tolerability. With single-agent ridaforolimus, mucositis and myelosuppression were dose-limiting toxicities. In advanced soft-tissue sarcoma, single-agent ridaforolimus was associated with a 29% clinical benefit rate and 2% partial response rate. A Phase III trial has recently been reported to have met its primary end point.
authors: NCIC Clinical Trials Group, 10 Stuart St, Queen's University, Kingston, ON, K7L 3N6, Canada.
authors: Janet E
authors: JE
authors: Dancey
authors: Jose
authors: J
authors: Monzon
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D017277:Drug Approval / Q000331:legislation & jurisprudence; D004353:Drug Evaluation, Preclinical; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology; D012509:Sarcoma / Q000188:drug therapy* / Q000201:enzymology; D020123:Sirolimus / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D058570:TOR Serine-Threonine Kinases / Q000037:antagonists & inhibitors; D016896:Treatment Outcome
chemical_list: D000970:Antineoplastic Agents; C515074:ridaforolimus; D058570:TOR Serine-Threonine Kinases; D020123:Sirolimus