Drug intelligence / Profile preview

amg 193 + carboplatin + pemetrexed + pembrolizumab

Development stage
Phase 1
Lead developer
Amgen
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

This is an experimental **combination therapy** consisting of AMG 193, carboplatin, pemetrexed, and pembrolizumab. - **AMG 193** is a second-generation, MTA-cooperative, selective PRMT5 inhibitor, designed to induce synthetic lethality in tumors with MTAP deletion by inhibiting PRMT5, making these genetically altered cells vulnerable while sparing normal cells[1][3][5][7]. - **Carboplatin** is a platinum-based chemotherapy that crosslinks DNA and inhibits DNA synthesis and function. - **Pemetrexed** is an antifolate antineoplastic agent that interrupts folate-dependent metabolic processes essential for cell replication. - **Pembrolizumab** is a humanized monoclonal antibody that blocks the programmed cell death protein 1 (PD-1) receptor, enhancing antitumor immunity[2][4][6][8][10]. This combination is being evaluated in clinical trials for advanced solid tumors, particularly those with MTAP deletion, and in settings such as non–small cell lung cancer where pembrolizumab, pemetrexed, and platinum chemotherapy (carboplatin) are already approved[2][4][6][8].

02

Targets

DNADHFR (Dihydrofolate reductase)PDCD1 (Programmed cell death protein 1 receptor)TS (Thymidylate synthase)PRMT5 (Protein arginine N-methyltransferase 5)

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