Drug intelligence / Profile preview

cisplatin + nimustine + temozolomide

Development stage
Unknown
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination chemotherapy regimen consisting of three small-molecule alkylating agents—cisplatin, nimustine (also known as ACNU), and temozolomide. Each drug has a distinct but complementary mechanism of action targeting DNA in cancer cells, leading to cell death. Cisplatin forms DNA crosslinks that inhibit DNA replication and transcription; nimustine is a nitrosourea that alkylates and carbamoylates DNA and RNA; temozolomide methylates guanine residues in DNA, resulting in cytotoxicity. This combination has been studied primarily for the treatment of newly diagnosed glioblastoma, where it is used as neoadjuvant chemotherapy (cisplatin + nimustine) prior to radiotherapy followed by adjuvant temozolomide[1]. The rationale for combining these agents is to exploit their synergistic effects on tumor cell killing while attempting to overcome resistance mechanisms seen with single-agent therapy. However, this regimen has shown significant toxicity concerns[1].

02

Targets

DNAN7-G (DNA guanine-N7 adduct)

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