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RX BIN: 015558
RX PCN: HT
Group ID: DDN6600
Card Holder ID: DDN6600

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2018 Price of Bortezomib

Velcade 3.5 mg vial

$1590.0

vial

* price without discount in nearest pharmacy. Price may vary.

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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

FormRouteStrength
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

false

International Brands

Act Bortezomib

Synonyms

((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

Manufacturers

Actavis Pharma Company

CAS number

179324-69-7

UNII

69G8BD63PP

State

solid

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.

RX24 Drugs Disclaimer: before buying a Bortezomib on prescription, consult your healthcare provider. Content on this page is provided for informational purposes only. Any use of this information is at your own risk.

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