Drug intelligence / Profile preview

MK-2206 + docetaxel

Development stage
Phase 1
Lead developer
Merck
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

MK-2206 + docetaxel is a combination therapy of MK-2206, an orally active allosteric inhibitor of Akt (protein kinase B), and docetaxel, a cytotoxic taxane chemotherapeutic. MK-2206 inhibits Akt isoforms (Akt1, Akt2, Akt3) by binding allosterically, suppressing signaling through the PI3K/Akt pathway involved in cell proliferation and survival. Docetaxel stabilizes microtubules, disrupting cell division and inducing apoptosis. The combination aims to enhance antitumor efficacy, showing synergistic or additive effects in preclinical breast, prostate, and other cancer models, and has been evaluated in early phase clinical trials in solid tumors, particularly breast cancer[1][3].

02

Targets

AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)AKT2 (Rac-beta serine/threonine-protein kinase)AKT3 (RAC-gamma serine/threonine-protein kinase)TUBB (Tubulin (alpha and beta subunits))

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