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pemetrexed + trametinib
- Development stage
- Preclinical
- Lead developer
- Eli Lilly
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Pemetrexed + trametinib is a combination of two small molecule chemotherapeutic agents used in oncology, particularly for cancers such as non-small cell lung cancer. Pemetrexed is an antifolate antineoplastic agent that inhibits folate-dependent enzymes essential for DNA and purine synthesis, thereby blocking cell replication. Trametinib is a selective inhibitor of MEK1 and MEK2 kinases in the MAPK/ERK pathway, leading to decreased tumor cell proliferation and survival. This combination targets different aspects of cancer cell growth: pemetrexed disrupts nucleotide synthesis while trametinib blocks oncogenic signaling pathways[1][3][6][8]. Pemetrexed was developed by Eli Lilly and Company; trametinib was originally developed by Japan Tobacco and later by GlaxoSmithKline.
- Brand names
- MekinistSpexotras
- Other names
- pemetrexed disodium (for pemetrexed)trametinib dimethyl sulfoxide (for trametinib)
02
Targets
MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)GART (GAR transformylase)KSR1 (Kinase suppressor of Ras 1)ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)KSR2 (Kinase suppressor of Ras 2)DHFR (Dihydrofolate reductase)ABCB1 (P-glycoprotein)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)TS (Thymidylate synthase)
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