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gemcitabine + trametinib
- Development stage
- Unknown
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Gemcitabine + trametinib is a combination of two small molecule anticancer drugs used in clinical research for the treatment of advanced solid tumors, including pancreatic cancer. Gemcitabine is a nucleoside analog that inhibits DNA synthesis by incorporating into DNA and causing masked chain termination, leading to apoptosis in rapidly dividing cells[1]. Trametinib is an orally bioavailable, selective inhibitor of mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2, which are key components of the RAS/RAF/MEK/ERK signaling pathway often dysregulated in cancers[8][4]. The combination has been studied particularly for tumors with RAS mutations such as pancreatic cancer, aiming to enhance antitumor efficacy by targeting both DNA synthesis and oncogenic signaling pathways[5].
- Brand names
- Mekinist + gemcitabineSpexotras + gemcitabine
- Other names
- none
02
Targets
MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)DNAMEK1 (Dual specificity mitogen-activated protein kinase kinase 1)
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