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busulfan + melphalan
- Development stage
- Unknown
- Lead developer
- GSK
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Busulfan + melphalan is a chemotherapy combination regimen composed of two alkylating agents, busulfan and melphalan. This combination is primarily used as a conditioning regimen before hematopoietic stem cell transplantation (SCT), especially in the treatment of high-risk neuroblastoma and multiple myeloma[1][8]. Both drugs work by alkylating DNA, leading to cross-linking and disruption of DNA replication and transcription, ultimately causing cell death. Busulfan forms guanine-adenine intrastrand crosslinks via SN2 reactions after hydrolysis releases reactive carbonium ions[4][6]. Melphalan binds at the N7 position of guanine to induce inter-strand DNA cross-links[2][5]. The combination exploits their complementary mechanisms to maximize cytotoxicity against malignant cells prior to transplant. Developers: - GlaxoSmithKline (for busulfan/Myleran) - Aspen Pharmacare (for melphalan/Alkeran) Manufacturers: - Otsuka Pharmaceutical (busulfan/Busulfex) - Aspen Pharmacare (melphalan/Alkeran) - Fresenius Kabi (busulfan)
- Other names
- BuMelbusulfan/melphalan regimen
02
Targets
DNA
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