Drug intelligence / Profile preview

gemcitabine + pemetrexed + paclitaxel + 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, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of gemcitabine, pemetrexed, and paclitaxel. Each component is a small molecule antineoplastic agent with distinct mechanisms of action: - Gemcitabine is a nucleoside analog that inhibits DNA synthesis by incorporating into DNA and inhibiting ribonucleotide reductase. - Pemetrexed is an antifolate that inhibits several folate-dependent enzymes involved in the de novo biosynthesis of thymidine and purine nucleotides, primarily targeting thymidylate synthase. - Paclitaxel stabilizes microtubules and prevents their depolymerization, thereby inhibiting cell division. These agents are commonly used in the treatment of various solid tumors, particularly non-small cell lung cancer (NSCLC), either as monotherapies or in two-drug combinations. There are clinical studies evaluating combinations such as gemcitabine plus pemetrexed or gemcitabine plus paclitaxel for advanced NSCLC[1][3]. However, there is no evidence supporting the use of all three drugs together in a single regimen or any established protocol involving "gemcitabine + pemetrexed + paclitaxel + gemcitabine" as one combination. The name also appears to redundantly list "gemcitabine" twice.

02

Targets

DNA polymerase familyTUBB (Tubulin (alpha and beta subunits))RNR (Ribonucleotide reductase)TS (Thymidylate synthase)

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