Drug intelligence / Profile preview

ridaforolimus + MK-2206

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

Overview

Ridaforolimus + MK-2206 is a combination therapy consisting of two investigational small molecule inhibitors: ridaforolimus, an inhibitor of the mammalian target of rapamycin (mTOR), and MK-2206, an inhibitor of protein kinase B (Akt). The combination was designed to more effectively block the PI3K/Akt/mTOR signaling pathway, commonly dysregulated in cancers, particularly in advanced solid tumors with PI3K pathway dependency such as breast and prostate cancer. Clinical studies have shown the combination can be tolerated in advanced cancer patients and may provide clinical benefit, such as partial and complete responses in biomarker-selected breast cancer populations. The approach exploits complementary mechanisms to overcome compensatory resistance seen with pathway inhibition at a single node. Both compounds were developed by Merck (Merck Sharp & Dohme). Clinical development has primarily targeted solid tumors, especially breast and castration-resistant prostate cancers with specific molecular markers[1][4][5].

02

Targets

mTOR (Mammalian target of rapamycin kinase)AKT (RAC-alpha serine/threonine-protein kinase)

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