Drug intelligence / Profile preview

lomustine + carmustine + streptozotocin

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

- **lomustine + carmustine + streptozotocin** is an investigational or non-standard combination of three nitrosourea alkylating agents—lomustine, carmustine, and streptozotocin—used primarily in research and potentially in oncology regimens for aggressive or refractory cancers. Each of the three agents acts as a DNA alkylator, causing cross-linking and breaking of DNA strands which leads to inhibition of DNA, RNA, and protein synthesis and subsequent cell apoptosis. Nitrosoureas are lipid-soluble and cross the blood-brain barrier, making combinations attractive for treating central nervous system tumors. Lomustine and carmustine are synthetic nitrosoureas used mainly for brain tumors and lymphomas; streptozotocin is naturally occurring and used in pancreatic cancer and as a diabetogenic agent in research. The mechanism centers on alkylation at the O6 position of guanine residues in DNA, and additional protein carbamoylation effects. The specific combination does not have a unique brand name or structured approval but may be considered in advanced experimental oncology settings for synergistic cytotoxicity. - Lomustine is principally used for **brain tumors** (primary and metastatic), Hodgkin’s and non-Hodgkin’s lymphoma, melanoma, and various solid tumors[1][2][5][9]. - Carmustine is primarily utilized in **high-grade gliomas**, including glioblastoma, as well as lymphomas and some other solid tumors[3][7]. - Streptozotocin is mainly indicated for **pancreatic neuroendocrine tumors**, and is notable for its selective action on pancreatic beta cells[6][7].

02

Targets

SLC2A2 (Solute carrier family 2 facilitated glucose transporter member 2)

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