Drug intelligence / Profile preview

leucovorin + methotrexate + vinblastine + prednisone

Development stage
Unknown
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Oral, Intrathecal, Intramuscular
01

Overview

This is a combination chemotherapy regimen consisting of four drugs: - **Leucovorin** (folinic acid): A reduced form of folic acid used to "rescue" normal cells from the toxic effects of methotrexate and to enhance the efficacy or reduce toxicity of other chemotherapeutics. - **Methotrexate**: An antimetabolite and antifolate agent that inhibits dihydrofolate reductase, blocking DNA synthesis and cell replication, particularly in rapidly dividing cancer cells. - **Vinblastine**: A vinca alkaloid that binds tubulin, inhibiting microtubule formation during mitosis, leading to cell cycle arrest and apoptosis in dividing cells. - **Prednisone**: A synthetic glucocorticoid corticosteroid with anti-inflammatory and immunosuppressive properties; it also induces apoptosis in certain cancerous lymphoid cells. This combination is designed for synergistic cytotoxicity against malignant cells by targeting different pathways involved in cell division and survival. Leucovorin is specifically included to mitigate methotrexate toxicity. While combinations involving subsets of these drugs are well established (e.g., vinblastine plus prednisone for lymphomas), this exact four-drug regimen may be considered investigational or off-label for specific cancers such as refractory breast cancer or certain hematologic malignancies[1][2][5].

02

Targets

GR (Glucocorticoid receptor)DHFR (Dihydrofolate reductase)TUBB (Tubulin (alpha and beta subunits))

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