Drug intelligence / Profile preview

M2698 + trastuzumab

Development stage
Phase 1
Lead developer
Merck KGaA
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
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Overview

M2698 + trastuzumab is a combination therapy consisting of M2698, an orally available small molecule dual inhibitor of p70S6K and AKT (specifically Akt 1/3), and trastuzumab, a monoclonal antibody targeting the human epidermal growth factor receptor 2 (HER2). M2698 inhibits two key nodes in the PI3K/AKT/mTOR (PAM) pathway, which is implicated in tumor progression and resistance to therapy. Trastuzumab binds to HER2 receptors on cancer cells, inhibiting their proliferation. The combination has demonstrated antitumor activity in patients with advanced breast cancer resistant to multiple standard therapies and shows promise for overcoming treatment resistance. Preclinical studies also support its efficacy in HER2-positive gastric cancer models[1][2][3].

02

Targets

AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)AKT3 (RAC-gamma serine/threonine-protein kinase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)RPS6KB1 (Ribosomal protein S6 kinase beta-1)

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