Drug intelligence / Profile preview

adriamycin + lomustine + methotrexate

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

Overview

This is a combination chemotherapy regimen consisting of three cytotoxic agents: - Adriamycin (doxorubicin), an anthracycline antibiotic that intercalates DNA and inhibits topoisomerase II, leading to inhibition of DNA replication and RNA synthesis. - Lomustine (CCNU), a nitrosourea alkylating agent that causes cross-linking of DNA and RNA, resulting in inhibition of cancer cell replication. - Methotrexate, an antimetabolite and antifolate drug that inhibits dihydrofolate reductase, blocking the synthesis of tetrahydrofolate required for purine and thymidylate synthesis. This combination has been used in the treatment of various cancers, particularly lung cancer (including non-small cell lung cancer and small cell lung cancer) as part of multi-agent regimens. The drugs act synergistically to target rapidly dividing tumor cells through different mechanisms. Toxicities include myelosuppression, gastrointestinal side effects, alopecia, mucositis/stomatitis, cardiotoxicity (from doxorubicin), nephrotoxicity/hepatotoxicity (from methotrexate), and delayed bone marrow suppression (from lomustine)[1][2][7].

02

Targets

DHFR (Dihydrofolate reductase)DNA

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