Drug intelligence / Profile preview

MK-2206 + carboplatin + paclitaxel

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

Overview

MK-2206 + carboplatin + paclitaxel is an investigational combination therapy consisting of MK-2206, an oral allosteric inhibitor of all AKT isoforms (pan-AKT inhibitor), combined with the chemotherapeutic agents carboplatin (a platinum-based DNA crosslinker) and paclitaxel (a microtubule stabilizer). MK-2206 blocks AKT signaling, a key pathway in cancer survival and resistance, by inhibiting phosphorylation of AKT at both Thr308 and Ser473 residues and demonstrating high selectivity for AKT over other kinases. Carboplatin induces DNA damage by creating DNA adducts, while paclitaxel promotes microtubule assembly and blocks cell division. This triple-drug combination has been tested in early-phase clinical trials for enhanced efficacy, particularly in high-risk breast cancer populations, with MK-2206 administered orally and carboplatin and paclitaxel by intravenous infusion. Merck developed MK-2206[1][2][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)DNATUBB (Tubulin (alpha and beta subunits))

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