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bortezomib + melphalan
- Development stage
- Unknown
- Lead developer
- Millennium Pharmaceuticals
- Modality
- Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Intravenous, Subcutaneous, Oral
01
Overview
Bortezomib + melphalan is a combination regimen used primarily in the treatment of multiple myeloma. Bortezomib is a small molecule proteasome inhibitor that blocks the 26S proteasome, leading to accumulation of proteins within cancer cells and subsequent apoptosis. Melphalan is an alkylating agent that cross-links DNA strands, inhibiting DNA and RNA synthesis and causing cell death in both dividing and non-dividing tumor cells. The combination exploits bortezomib’s ability to sensitize myeloma cells to DNA-damaging agents like melphalan, potentially overcoming chemoresistance and enhancing anti-myeloma activity. This regimen is especially used for patients who are not eligible for high-dose therapy with stem cell transplantation[1][2][3][4][5][6].
- Brand names
- Boruzu
- Other names
- Velcade-Melphalanbortezomib-melphalan conditioning regimen
02
Targets
DNAPSMB5 (Proteasome subunit beta Type-5)
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