Drug intelligence / Profile preview

carmustine + methotrexate

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

Overview

Carmustine + methotrexate is a combination chemotherapy regimen consisting of two small molecule antineoplastic agents. Carmustine (also known as BCNU) is a nitrosourea alkylating agent that exerts its effect primarily by alkylating DNA and RNA, leading to inhibition of DNA replication and transcription, as well as carbamoylation of proteins which can inhibit key enzymatic processes. Methotrexate is an antimetabolite and antifolate agent that inhibits dihydrofolate reductase, thereby blocking the synthesis of tetrahydrofolate required for purine and thymidylate synthesis, ultimately inhibiting DNA synthesis and cell division. This combination has been used particularly in patients with brain metastases from breast cancer after whole brain radiotherapy, where it has shown clinical activity with manageable toxicity profiles[1][2]. Both drugs are also individually approved for use in various cancers.

Other names
BCNU + MTXcarmustine and methotrexate combination
02

Targets

DHFR (Dihydrofolate reductase)GSR (Glutathione reductase)HMGB1 (High mobility group protein B1)DNA

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