Drug intelligence / Profile preview

mechlorethamine

Development stage
Approved
Lead developer
Recordati
Modality
Small Molecules
Administration
Intravenous, Topical, Intracavitary
01

Overview

Mechlorethamine is a small molecule alkylating agent and one of the earliest chemotherapy drugs developed. It is also known as nitrogen mustard and was originally derived from chemical warfare agents. Mechlorethamine exerts its antineoplastic effects by alkylating DNA, leading to cross-linking and strand breaks that inhibit DNA replication and transcription, ultimately causing cell death. This mechanism targets rapidly dividing cells such as cancer cells but can also affect normal proliferating cells. Mechlorethamine has been used in the treatment of Hodgkin's lymphoma, non-Hodgkin's lymphoma, mycosis fungoides (cutaneous T-cell lymphoma), chronic lymphocytic leukemia (CLL), chronic myelogenous leukemia (CML), polycythemia vera, lung cancer, and malignant effusions caused by tumors. It is available in both intravenous formulations (historically under the brand name Mustargen) and topical gel formulations for cutaneous T-cell lymphoma (Valchlor/Ledaga). The drug is a vesicant with significant potential for tissue damage if extravasation occurs during IV administration[1][3][4][5][8].

Brand names
MustargenValchlorLedaga
Other names
nitrogen mustardchlormethinemustinebis(2-chloroethyl)methylaminemethylbis(2-chloroethyl)amineβ,β'-dichlorodiethyl-N-methylamine
02

Targets

DNA

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