Drug intelligence / Profile preview

cyclophosphamide + mesna

Development stage
Unknown
Lead developer
ASTA
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Cyclophosphamide + mesna is a combination therapy used primarily in oncology and hematology. Cyclophosphamide is an alkylating agent of the nitrogen mustard type that requires hepatic activation to form its active metabolites, which cross-link DNA strands, leading to inhibition of DNA synthesis and cell death. It is widely used as an antineoplastic and immunosuppressive agent[2][10]. Mesna (sodium 2-mercaptoethane sulfonate) is a synthetic sulfhydryl compound administered alongside high-dose cyclophosphamide to prevent hemorrhagic cystitis—a potentially severe bladder toxicity caused by the urotoxic metabolite acrolein produced during cyclophosphamide metabolism[1][5][6][8]. Mesna acts as a uroprotective agent by binding and detoxifying acrolein in the urinary tract, thereby reducing or preventing bladder irritation and bleeding without interfering with the antitumor efficacy of cyclophosphamide[6][8]. This combination is standard for regimens involving high-dose cyclophosphamide, such as those used in bone marrow transplantation or certain cancer protocols.

02

Targets

DNA

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