Bortezomib CAS 179324-69-7 API

 

Bortezomib is a modified dipeptidyl boronic acid. The material is provided as a mannitol boronic ester which, in reconstituted form, consists of the mannitol ester in equilibrium with its hydrolysis product, the monomeric boronic acid. The drug substance exists in its cyclic anhydride form as a trimeric boroxine.

 

The chemical name for bortezomib, the monomeric boronic acid, is [(1R)-3-methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl) amino]propyl]amino]butyl] boronic acid.

 

The molecular weight is 384.24. The molecular formula is C19H25BN4O4. The solubility of bortezomib, as the monomeric boronic acid, in water is 3.3 to 3.8 mg/mL in a pH range of 2 to 6.5.

 

 

 

 

Sold under the brand name Velcade among others, Bortezomib is an anti-cancer medication used for treating multiple myeloma and mantle cell lymphoma. This includes multiple myeloma in those who have and have not previously received treatment.

 

Given by injection, Bortezomib is generally used together with other medications.

 

As a generic medication on the World Health Organization's List of Essential Medicines, Bortezomib was approved for medical use in the United States in 2003 and in the European Union in 2004.

 

 

Bortezomib for Injection is indicated for the treatment of patients with multiple myeloma who have received at least 1 prior therapy.

 

Bortezomib for Injection is indicated for the treatment of patients with mantle cell

lymphoma who have received at least 1 prior therapy.

 

 

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 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.

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