Drug intelligence / Profile preview

altretamine

Development stage
Phase 1
Lead developer
National Cancer Institute
Modality
Small Molecules
Administration
Oral
01

Overview

Altretamine is an oral antineoplastic (anticancer) agent classified as an alkylating agent. It is primarily used for the palliative treatment of persistent or recurrent ovarian cancer, especially after failure of first-line therapies such as cisplatin and/or other alkylating agents[1][2][3][4][5]. Altretamine works by interfering with the growth of cancer cells, leading to their destruction. Its precise mechanism of action is not fully understood but involves metabolic activation via N-demethylation to produce weakly alkylating species (such as formaldehyde), which can form covalent adducts with DNA and proteins, potentially causing DNA cross-linking and cell death[3][5][6]. The drug is less toxic than some other agents used in refractory ovarian cancer. Altretamine was approved by the FDA in 1990[5].

Brand names
Hexalen
Other names
hexamethylmelamine
02

Targets

DNA

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