Ridaforolimus (Deforolimus, AP23573)
Ridaforolimus (previously known as deforolimus and as AP23573) is an inhibitor of mTOR originally being developed by Ariad and more recetnly acquired by Merck. Phase I-II trials have been completed.
NCI drug Dictionary definition: Deforolimus is a small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Deforolimus binds to and inhibits the mammalian target of rapamycin (mTOR), which may result in cell cycle arrest and,consequently, the inhibition of tumor cell growth and proliferation. Upregulated in some tumors, mTOR is a serine/threonine kinase involved in regulating cellular proliferation, motility, and survival that is located downstream of the PI3K/Akt signaling pathway.
For information at the site of the manufacturer click here.
A Phase III trial, called the SUCCEED trial, is ongoingfor patients with metastatic sarcoma but no longer recruiting. Preliminary results were presented at ASCO 2011, as shown in the following link.
Results of the phase III, placebo-controlled trial (SUCCEED) evaluating the mTOR inhibitor ridaforolimus (R) as maintenance therapy in advanced sarcoma patients (pts) following clinical benefit from prior standard cytotoxic chemotherapy (CT). SP Chawla et al, J Clin Oncol 29: 2011 (suppl; abstr 10005)
A combination trial with an IGF-1R monoclonal mntibody is also now open:
A Combination Study With MK8669 (Deforolimus) and MK0646 in Patients With Advanced Cancer