Drug intelligence / Profile preview

mechlorethamine (Actelion Pharmaceuticals Ltd)

Development stage
Approved
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Topical
01

Overview

Mechlorethamine, also known as chlormethine or nitrogen mustard, is a bifunctional alkylating agent and a nitrogen analog of mustard gas. In its topical gel formulation (marketed as Valchlor or Ledaga), it is specifically indicated for the treatment of stage IA and IB mycosis fungoides-type cutaneous T-cell lymphoma (MF-CTCL) in patients who have received prior skin-directed therapy. The drug acts by forming covalent bonds with DNA, specifically cross-linking guanine residues at the N7 position. This DNA damage inhibits replication and transcription, ultimately triggering apoptosis in malignant T-cells. While historically used intravenously as part of the MOPP regimen for Hodgkin lymphoma, the gel formulation provides a localized delivery system that minimizes systemic absorption and associated toxicities such as myelosuppression.

Brand names
ValchlorLedagaMustargen
Other names
chlormethinenitrogen mustardmustinemechlorethamine hydrochloride
02

Targets

DNA

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