Drug intelligence / Profile preview

lomustine + doxorubicin + bleomycin + dacarbazine

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of **lomustine**, **doxorubicin**, **bleomycin**, and **dacarbazine**. Each of these agents is a cytotoxic drug that acts via distinct mechanisms and is used primarily to treat cancer; such combinations are designed to exploit drug synergy, minimize resistance, and maximize tumor cell kill. There is precedent for regimens combining three of these agents (e.g., B-CAVe, which substitutes vinblastine for dacarbazine), but no widely recognized regimen or standard protocol uses all four of these specific drugs together in a single regimen. Each drug works as follows: - **Lomustine** is an alkylating nitrosourea that causes DNA strand cross-linking and breaks, inhibiting DNA and RNA synthesis. - **Doxorubicin** is an anthracycline that intercalates DNA, inhibits topoisomerase II, and generates free radicals, leading to DNA damage and cell death. - **Bleomycin** is an antitumor antibiotic that induces DNA strand breaks via free radical formation. - **Dacarbazine** is an alkylating agent that methylates DNA, leading to inhibition of DNA synthesis and function. Combination therapy with related drugs is used to treat Hodgkin lymphoma and other cancers, but this exact four-drug combination does not appear to be standard or widely used clinically.

02

Targets

TOP2A (DNA topoisomerase II)DNA

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