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BAY2965501 + pembrolizumab + platinum-based chemotherapy

Development stage
Unknown
Lead developer
Bayer
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

**BAY2965501 + pembrolizumab + platinum-based chemotherapy** is a **combination investigational cancer therapy** currently tested in phase 1 clinical trials for advanced solid tumors such as non-small cell lung cancer, gastric cancer, melanoma, and renal cancers. It combines: - **BAY2965501**, a first-in-human, orally available small molecule inhibitor of diacylglycerol kinase zeta (DGKζ), which activates T-cells and enhances anti-cancer immune responses by overcoming immunosuppression within the tumor microenvironment[1][2][6][8]. - **Pembrolizumab**, a monoclonal antibody checkpoint inhibitor targeting PD-1, which prevents engagement with PD-L1/L2, leading to increased T-cell mediated immune attack on cancer cells[1][3][7][9]. - **Platinum-based chemotherapy**, a class of cytotoxic agents (usually cisplatin, carboplatin, or oxaliplatin) that cross-link DNA and induce cancer cell death[1]. The combination aims to synergistically enhance immune-mediated tumor killing by simultaneously activating T-cells, relieving immune checkpoints, and increasing cancer cell susceptibility to immune attack and cytotoxicity. Development is led by Bayer, with dose escalation and expansion cohorts focused on advanced solid tumors unresponsive to standard therapy[1][2][3][4][5][6][8].

Other names
diacylglycerol kinase zeta inhibitor BAY 2965501pembrolizumabplatinum-based chemotherapy
02

Targets

DGKZ (Diacylglycerol kinase zeta)DNAPDCD1 (Programmed cell death protein 1 receptor)

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