Busulfan

Busulfan injection is indicated for use in combination with cyclophosphamide as a conditioning regimen prior to allogeneic hematopoietic progenitor cell transplantation for chronic myelogenous leukemia. Busulfan injection is an alkylating drug indicated for: Use in combination with cyclophosphamide as a conditioning regimen prior to allogeneic hematopoietic progenitor cell transplantation for chronic myelogenous leukemia (CML). (1)

12.1 Mechanism of Action Busulfan is a bifunctional alkylating agent in which two labile methanesulfonate groups are attached to opposite ends of a four-carbon alkyl chain. In aqueous media, busulfan hydrolyzes to release the methanesulfonate groups. This produces reactive carbonium ions that can alkylate DNA. DNA damage is thought to be responsible for much of the cytotoxicity of busulfan.

Clinical clearance of Busulfan (Alkylating Drug) relies on predominantly hepatic biotransformation with renal elimination of polar busulfan conjugates with a Steady-state plasma equilibrium reached over 9–16 hour t½ intervals for Busulfan half-life; patients absorbing at Complete (~100%) parenteral systemic delivery for Busulfan (6 mg/mL Injection) bioavailability typically observe target onset around rapid intravascular/parenteral onset within 15–45 minutes after busulfan administration.

FDA clinical labeling for Busulfan restricts administration in busulfan injection is contraindicated in patients with a history of hypersensitivity to any of its components.; busulfan injection is contraindicated in patients with a history of hypersensitivity to any of its components. across 6 mg/mL Injection, 6 mg/mL Injection, Solution, Concentrate, 6 mg/mL Injection, Solution, 2 mg/1 Tablet, Film Coated, with self-reported patient tracking dominated by nausea (12.3% of reports), headache (10.9% of reports), diarrhea (9.6% of reports).