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RX BIN: 015558RX PCN: HTGroup ID: DDN6600Card Holder ID: DDN6600
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2019 Price of Bortezomib

Velcade 3.5 mg vial

price without discount in nearest pharmacy. Price may vary.

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Bortezomib volume of distribution

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2018 Statistics

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Discount Cards 16,000+


Clients Benefit 29%


Total savings $4,735,080

What is Bortezomib

Bortezomib (originally PS-341 and marketed as Velcade by Millennium Pharmaceuticals) is the first therapeutic proteasome inhibitor to be tested in humans. The boron atom within bortezomib catalytically binds the active site of the 26S proteasome with high affinity and specificity, thereby resulting in cell cycle arrest and apoptosis. In normal cells, the proteasome is involved in degradation of ubiquitylated proteins that have been tagged for destruction because they are damaged or unneeded by the cell. However, in cancerous cells, proteasome activity degrades pro-apoptotic proteins such as p53 that would normally result in programmed cell death of the dysfunctional cells. Proteasome inhibitors such as bortezomib interrupt this process, resulting in destruction of cancerous cells. Bortezomib is approved in the U.S. for treating relapsed multiple myeloma and mantle cell lymphoma. In multiple myeloma, complete clinical responses have been obtained in patients with otherwise refractory or rapidly advancing disease.

Bortezomib mechanism of action

Bortezomib is a reversible inhibitor of the chymotrypsin-like activity of the 26S proteasome in mammalian cells. The 26S proteasome is a large protein complex that degrades ubiquitinated proteins. The active site of the proteasome has chymotrypsin-like, trypsin-like, and postglutamyl peptide hydrolysis activity. The 26S proteasome degrades various proteins critical to cancer cell survival, such as cyclins, tumor suppressors, BCL-2, and cyclin-dependent kinase inhibitors. Inhibition of these degradations sensitizes cells to apoptosis. Bortezomib is a potent inhibitor of 26S proteasome, which sensitizes activity in dividing multiple myeloma and leukemic cells, thus inducing apoptosis. In addition, bortezomib appears to increase the sensitivity of cancer cells to traditional anticancer agents (e.g., gemcitabine, cisplatin, paclitaxel, irinotecan, and radiation).

Dosage forms of Bortezomib

Powder for solution for injectionIntravenous use, Subcutaneous use3.5 mg
Injection, powder, lyophilized, for solutionintravenous; subcutaneous3.5 mg/1
Powder for solutionintravenous; subcutaneous3.5 mg

Prescription Generics


International Brands

Act Bortezomib


((1R)-3-methyl-1-({(2S)-3-phenyl-2-((pyrazin-2-ylcarbonyl)amino)propanoyl}amino)butyl)boronic acid N-((1R)-1-(DIHYDROXYBORYL)-3-methylbutyl)-N-(pyrazin-2-ylcarbonyl)-L-phenylalaninamide


Actavis Pharma Company

CAS number






Affected organisms

Humans and other mammals

Indication of Bortezomib

For treatment of multiple myeloma in patients who have not been successfully treated with at least two previous therapies.

Toxicity of Bortezomib

Cardiovascular safety pharmacology studies in monkeys show that lethal IV doses are associated with decreases in blood pressure, increases in heart rate, increases in contractility, and ultimately terminal hypotension. In monkeys, doses of 3.0 mg/m sup 2 /sup and greater (approximately twice the recommended clinical dose) resulted in progressive hypotension starting at 1 hour and progressing to death by 12 to 14 hours following drug administration.

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