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pemetrexed + gemcitabine
- Development stage
- Unknown
- Lead developer
- Eli Lilly
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
Pemetrexed + gemcitabine is a combination chemotherapy regimen consisting of two antimetabolite agents used primarily in the treatment of various solid tumors, most notably non-small cell lung cancer (NSCLC) and malignant pleural mesothelioma. Pemetrexed is a multitargeted antifolate that inhibits several folate-dependent enzymes involved in nucleotide synthesis—specifically thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT)—thereby disrupting DNA and RNA synthesis essential for tumor cell replication[1][5][2]. Gemcitabine is a nucleoside analog that interferes with DNA synthesis by incorporating into DNA strands during replication, leading to chain termination and apoptosis. The combination has demonstrated synergistic anti-tumor effects in preclinical models and clinical studies for advanced or metastatic NSCLC as well as other cancers such as Group 3 medulloblastoma[8][2]. Both drugs are administered intravenously.
- Brand names
- GemzarAlimta
- Other names
- pemetrexed disodium + gemcitabine hydrochloride
02
Targets
GART (GAR transformylase)DNA polymerase familyDHFR (Dihydrofolate reductase)RNR (Ribonucleotide reductase)TS (Thymidylate synthase)
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