An Expert Report on Carmustine (BCNU): Pharmacology, Clinical Applications, and Evolving Therapeutic Landscape

Executive Summary

Carmustine, a nitrosourea alkylating agent identified by the DrugBank ID DB00262, represents a cornerstone in the chemotherapeutic management of central nervous system (CNS) malignancies. For nearly five decades, its clinical utility has been fundamentally defined by its high lipophilicity, which facilitates penetration of the blood-brain barrier (BBB)—a characteristic that distinguishes it from many other cytotoxic agents. This report provides an exhaustive analysis of Carmustine, synthesizing its physicochemical properties, multifaceted mechanism of action, complex pharmacokinetics, clinical efficacy, and extensive safety profile.

The drug operates primarily through the alkylation and subsequent cross-linking of DNA and RNA, a process that physically obstructs replication and transcription, leading to cancer cell death. This direct cytotoxic assault is synergistically amplified by Carmustine's ability to inhibit key cellular defense and repair pathways, including glutathione reductase and O6-methylguanine-DNA methyltransferase (MGMT), effectively disarming the cell while damaging it.