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cisplatin + cyclophosphamide + etoposide + lomustine + methotrexate + thiotepa + vincristine

Development stage
Preclinical
Modality
Small Molecules
Administration
Intravenous, Oral, Intrathecal, Intramuscular, Intravesical, Subcutaneous
01

Overview

This is a multi-agent chemotherapy regimen composed of seven cytotoxic drugs: cisplatin, cyclophosphamide, etoposide, lomustine, methotrexate, thiotepa, and vincristine. Each component has a distinct mechanism of action targeting rapidly dividing cancer cells through various pathways: - Cisplatin is a platinum-based compound that forms DNA crosslinks and inhibits DNA synthesis. - Cyclophosphamide is an alkylating agent that interferes with DNA replication by forming covalent bonds with DNA. - Etoposide inhibits topoisomerase II, leading to double-strand breaks in DNA. - Lomustine (CCNU) is a nitrosourea alkylating agent causing interstrand crosslinks in DNA and RNA. - Methotrexate inhibits dihydrofolate reductase (DHFR), blocking folic acid metabolism required for nucleotide synthesis. - Thiotepa is an alkylating agent that crosslinks DNA strands to prevent cell division. - Vincristine binds tubulin and disrupts microtubule formation during mitosis. This combination may be used in the treatment of certain aggressive or refractory cancers where multi-drug regimens are indicated. The specific indications depend on clinical protocols but can include some pediatric brain tumors or relapsed/refractory malignancies. The regimen leverages multiple mechanisms to maximize cytotoxicity against tumor cells while attempting to minimize resistance.

02

Targets

TUBB (Tubulin (alpha and beta subunits))TOP2A (DNA topoisomerase II)DNADHFR (Dihydrofolate reductase)

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