Bortezomib

• Antineoplastic Agents
• Protease Inhibitors
• ATC:L01XX32

• Velcade

• No information avaliable

C₁₉H₂₅BN₄O₄

http://www.rxlist.com/cgi/generic3/velcade.htm

Bortezomib FDA

No information avaliable

384.237 g/mol

No information avaliable

The solubility of bortezomib, as the monomeric boronic acid, is 3.3 to 3.8 mg/mL in a pH range of 2 to 6.5.

Solid

No information avaliable

Powder for intravenous injection solution (each single dose vial contains 3.5 mg of bortezomib)

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

Bortezomib is a drug that inhibits the mammalian 26S proteasome. The ubiquitin-proteasome pathway plays an essential role in regulating the intracellular concentration of specific proteins, thereby maintaining homeostasis within cells. Inhibition of the 26S proteasome prevents this targeted proteolysis, which can affect multiple signaling cascades within the cell. This disruption of normal homeostatic mechanisms can lead to cell death. Experiments have demonstrated that bortezomib is cytotoxic to a variety of cancer cell types in vitro. Bortezomib causes a delay in tumor growth in vivo in nonclinical tumor models, including multiple myeloma. Tumor cells, that is, rapidly dividing cells, appear to be more sensitive to proteasome inhibition.

No information avaliable

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/m² 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.

No information avaliable

Humans and other mammals