Drug intelligence / Profile preview

trametinib + pemetrexed + cisplatin

Development stage
Preclinical
Lead developer
Novartis
Modality
Small Molecules
Administration
Intravenous, Oral (for Trametinib Only)
01

Overview

Trametinib + pemetrexed + cisplatin** refers to a combination regimen using three distinct chemotherapy and targeted therapy agents: - **Trametinib** is a selective inhibitor of MEK1 and MEK2, components of the MAPK/ERK pathway, used in cancers with BRAF mutations, including some non-small cell lung cancers[4]. - **Pemetrexed** is an antifolate chemotherapy that disrupts folate-dependent metabolic processes essential for cell replication, often used for malignant pleural mesothelioma and non-squamous non-small cell lung cancer, particularly in combination with a platinum drug like cisplatin[1][2][3][5][6]. - **Cisplatin** is a platinum-based chemotherapy that forms DNA crosslinks and induces apoptosis in rapidly dividing cells and is widely used in many solid tumors, notably in lung cancer and mesothelioma, both as monotherapy and in combination (most commonly with pemetrexed)[1][2][3][5]. While combinations of **pemetrexed + cisplatin** are established and FDA-approved for advanced non-squamous NSCLC and malignant pleural mesothelioma, the combination specifically including **trametinib** is not an established, widely approved regimen but has been investigated in clinical trials for various advanced and refractory tumors, with interest in synergistic effects from targeted MEK inhibition alongside cytotoxic chemotherapy.

02

Targets

TS (Thymidylate synthase)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)DHFR (Dihydrofolate reductase)DNAGART (GAR transformylase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)

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