Drug intelligence / Profile preview

6-mercaptopurine + carmustine

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination of two chemotherapeutic agents, 6-mercaptopurine and carmustine. - **6-mercaptopurine** is an antimetabolite that inhibits purine nucleotide synthesis by competing with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRT), leading to inhibition of DNA and RNA synthesis[3]. - **Carmustine** (also known as BCNU) is a nitrosourea alkylating agent that cross-links DNA and RNA, inhibiting their function and leading to cell death. It may also inhibit key enzymatic processes by carbamoylation of amino acids in proteins[4]. The combination has been studied primarily in the treatment of malignant gliomas (including glioblastoma multiforme) as part of chemoradiotherapy regimens, but did not show significant survival benefit over carmustine alone in randomized trials[2].

Other names
6-MP + BCNU
02

Targets

DNAHPRT1 (Hypoxanthine-guanine phosphoribosyltransferase)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)PPAT (Amidophosphoribosyltransferase)GSR (Glutathione reductase)

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