MK-2206 + bicalutamide

MK-2206 + bicalutamide is a combination therapy investigated for the treatment of prostate cancer, particularly in patients with rising PSA levels after primary therapy. MK-2206 is an orally active, potent, and highly selective allosteric inhibitor of Akt (protein kinase B), targeting Akt1, Akt2, and Akt3. Unlike ATP-competitive inhibitors, MK-2206 binds to the pleckstrin homology (PH) domain, inducing a conformational change that prevents Akt translocation to the plasma membrane and its subsequent activation. This inhibition disrupts the PI3K/AKT/mTOR signaling pathway, a key driver of cell survival and proliferation in many cancers, including prostate cancer. Bicalutamide is a non-steroidal androgen receptor (AR) antagonist that blocks the action of androgens, which are essential for prostate cancer growth. The combination is designed to overcome resistance to androgen deprivation by simultaneously inhibiting the compensatory Akt survival pathway.

Other names

Akt inhibitor MK2206MK-2206 and bicalutamideMK2206 and bicalutamideMK 2206 and bicalutamide