Drug intelligence / Profile preview

ridaforolimus

Development stage
Phase 3
Lead developer
Merck
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Ridaforolimus is a non-prodrug analog of rapamycin (sirolimus) and a potent small-molecule inhibitor of the mammalian target of rapamycin (mTOR), a central regulator of protein synthesis, cell proliferation, cell cycle progression, and cell survival. It belongs to the macrolide lactam class and is structurally related to other mTOR inhibitors such as sirolimus and everolimus. Ridaforolimus has been investigated primarily for its antineoplastic activity in various cancers including soft tissue sarcoma, bone sarcoma (osteosarcoma), endometrial cancer, ovarian cancer, prostate cancer, breast cancer (including HER2 positive), renal cell carcinoma, non-small cell lung cancer (NSCLC), and solid tumors. It also serves as the active pharmaceutical ingredient in drug-eluting coronary stents for the treatment of coronary artery disease by inhibiting neointimal hyperplasia following stent placement[1][3][5][6][7][8].

Brand names
EluNIR
Other names
JenzylNirSupreme
02

Targets

mTOR (Mammalian target of rapamycin kinase)

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