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epirubicin + methotrexate + vinorelbine
- Development stage
- Unknown
- Lead developer
- Pierre Fabre
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
Epirubicin + methotrexate + vinorelbine is a combination chemotherapy regimen, often referred to as VEM. It consists of three cytotoxic agents: - Epirubicin, an anthracycline antibiotic that intercalates DNA and inhibits topoisomerase II, leading to DNA strand breaks and apoptosis. - Methotrexate, an antimetabolite that inhibits dihydrofolate reductase (DHFR), blocking folic acid metabolism and thus DNA synthesis. - Vinorelbine, a vinca alkaloid that disrupts microtubule assembly by binding tubulin, inhibiting mitosis. This combination has been studied primarily as neoadjuvant or primary chemotherapy for locally advanced or operable breast cancer. Clinical trials have shown high response rates with manageable toxicity profiles. The regimen aims to downstage tumors before surgery and increase the rate of breast conservation[1][2][3].
- Other names
- vinorelbine + epirubicin + methotrexateVEM regimen
02
Targets
TOP2A (DNA topoisomerase II)DHFR (Dihydrofolate reductase)TUBB (Tubulin (alpha and beta subunits))
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