Product Description
Aliase: Bortezomib
Purity: 99%
Appearance:White powder
Brand: Tianhua
Grade: EP, USP, CP, JP,BP
Usage: Bortezomib is the first proteasome inhibitor to be approved b the US FDA for multiple myeloma, a blood cancer. A reversible
inhibitor of the 26S proteasome-a barrel-shaped multiprotein particle found in the nucleus and cytosol of all eukaryotic cells. T
AI Product Description
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Bortezomib, commercially known as Velcade, is a potent proteasome inhibitor widely utilized in the treatment of hematologic malignancies. Its chemical identity is defined by the molecular formula C20H30BN4O6 and the CAS Registry Number 179324-69-7. Structurally, it features a boronic acid moiety linked to a dipeptide backbone, which allows for specific and reversible binding to the catalytic chymotrypsin-like site of the 26S proteasome. This unique mechanism distinguishes it from earlier non-specific inhibitors, offering high selectivity against cancer cells while minimizing toxicity to normal tissues.
The primary clinical application of Bortezomib involves the management of multiple myeloma and mantle cell lymphoma. In multiple myeloma, it is indicated as a monotherapy for patients who have received at least one prior therapy, or in combination with dexamethasone, melphalan, and prednisone for newly diagnosed cases. For mantle cell lymphoma, it serves as a single-agent treatment for patients who have received at least one prior therapy. By inhibiting the proteasome, Bortezomib prevents the degradation of pro-apoptotic proteins such as p53 and IκBα, leading to an accumulation of these proteins within the cell. This accumulation triggers cell cycle arrest and induces apoptosis, effectively halting tumor growth.
Beyond its established indications, research continues to explore its efficacy in other solid tumors and autoimmune disorders, though results remain variable. The drug is typically administered intravenously or subcutaneously, with careful monitoring required for side effects like peripheral neuropathy, thrombocytopenia, and gastrointestinal disturbances. Despite these challenges, Bortezomib remains a cornerstone therapy in oncology, significantly improving progression-free survival and overall response rates in refractory blood cancers. Its development marked a paradigm shift in targeting intracellular protein degradation pathways, paving the way for subsequent generations of targeted therapies. As a first-in-class agent, it revolutionized the treatment landscape for multiple myeloma, transforming what was once a fatal diagnosis into a manageable chronic condition for many patients worldwide.