Drug intelligence / Profile preview

exemestane + ridaforolimus

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Exemestane + ridaforolimus is an investigational oral combination therapy evaluated primarily for the treatment of estrogen receptor (ER)-positive advanced or metastatic breast cancer in postmenopausal women. Exemestane is a steroidal aromatase inhibitor that irreversibly blocks the conversion of androgens to estrogens, thereby reducing estrogen levels and limiting growth stimulation in hormone-dependent breast cancer. Ridaforolimus is a small molecule inhibitor of mammalian target of rapamycin (mTOR), a key regulator of cell growth, proliferation, and survival; by inhibiting mTOR signaling, it can suppress tumor cell proliferation and angiogenesis. The combination was studied to determine if dual targeting of hormonal signaling (via exemestane) and mTOR pathway (via ridaforolimus) would improve outcomes compared to monotherapy or other combinations. Clinical trials found that this combination did not significantly improve progression-free survival compared to other regimens such as everolimus plus exemestane or monotherapy with exemestane alone; toxicity was also notable[2][3]. Development has not progressed beyond phase II.

02

Targets

Mechanistic target of rapamycin complex 1CYP19A1 (Aromatase)

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