Drug intelligence / Profile preview

telaglenastat + pembrolizumab + carboplatin + pemetrexed

Development stage
Unknown
Lead developer
Calithera Biosciences, Inc
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
Intravenous
01

Overview

This is a **combination regimen** consisting of four agents: - **Telaglenastat**: a small molecule inhibitor of glutaminase, impeding cancer cell metabolism. - **Pembrolizumab**: a humanized monoclonal antibody targeting PD-1 (Programmed Death-1), thereby enhancing T-cell–mediated anti-tumor immune responses. - **Carboplatin**: a platinum-based chemotherapy agent, functioning as a DNA crosslinker that causes DNA damage in rapidly dividing cells. - **Pemetrexed**: a multi-targeted antifolate chemotherapeutic that disrupts folate-dependent metabolic processes necessary for DNA replication and cell division. The combination is designed to target advanced cancer (such as non-squamous non-small cell lung cancer [NSCLC]), integrating immunotherapy, chemotherapy, and metabolic blockade. Pembrolizumab plus pemetrexed and carboplatin is an approved standard of care for first-line treatment of metastatic non-squamous NSCLC without EGFR or ALK genomic aberrations[1][5][2][3][4]. Telaglenastat is under investigation in clinical trials for augmenting standard regimens with metabolic inhibition.

Other names
telaglenastatCB-839CB839CB 839pembrolizumabMK-3475MK3475MK 3475KEYTRUDAcarboplatinpemetrexedALIMTA
02

Targets

GART (GAR transformylase)GLS1 (Glutaminase 1)DHFR (Dihydrofolate reductase)DNATS (Thymidylate synthase)PDCD1 (Programmed cell death protein 1 receptor)

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