CAS number：179324-69-7
molecular formula：C19H25BN4O4
molecular weight：384.24
EINECS number：605-854-3

English synonyms

Boronic acid, B-[(1R)-3-Methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(2-pyrazinylcarbonyl)aMino]propyl]aMino]bu;MG-341 PS-341;BortezoMib Base;BortezoMib-D8;bortezoMib(other);MLM341;BortezoMib R;VELCADE(BORTEZOMIB)

Related categories

Signal transduction pathway kinase inhibitors; scientific research reagents; raw materials; anti-tumor drugs; anti-tumor; raw material intermediates - raw materials; Inhibitors; proteases; anti-malarial drugs; intermediates; pharmaceutical raw materials; anti-tumor products; small molecule inhibitors; small molecule inhibitors, natural products; Intermediates; Material intermediates and additives; Raw materials; Impurity reference substances;
Boron Derivatives; Inhibitors; Intermediates & Fine Chemicals; Pharmaceuticals; Pepetides; Proteasome Inhibitors; Apis; Inhibitor; Final material; API; peptides; Chemicals; scientific research raw materials; chemical reagents; reference substances

Introduction

Bortezomib is a new type of targeted drug for myeloma. The discovery of this drug has attracted widespread attention in the medical field. Its mechanism of action won the Nobel Prize in Chemistry in 2004 and the highest honor in the pharmaceutical industry - the International Galen Award in 2006 ( Prix Galien, known as "a revolution in cancer treatment and a major advance in the treatment of multiple myeloma".

Chemical properties

Use

●  Bortezomib is the first proteasome inhibitor approved by the FDA for multiple myeloma, a blood cancer. Reversible inhibitor of the 26S proteasome, a barrel-shaped polyprotein particle found in the nucleus and cytoplasm of all eukaryotic cells. Targets the ubiquitin-proteasome pathway.

●  Bortezomib is the first proteasome inhibitor to be used clinically. The proteasome is present in all eukaryotic cells and degrades more than 80% of the proteins in the cell. It reversibly inhibits the function of proteasome, thereby inhibiting protein degradation, leading to protein accumulation and cell apoptosis. Since multiple myeloma (MM) continuously replicates and secretes myeloma proteins, it is more sensitive to proteasome than normal cells and can be used as a second-line treatment for MM and mantle cell lymphoma.

●  Bortezomib is the first proteasome inhibitor approved by the FDA for multiple myeloma, a blood cancer. Reversible inhibitor of the 26S proteasome, a barrel-shaped polyprotein particle found in the nucleus and cytoplasm of all eukaryotic cells. Targets the ubiquitin-proteasome pathway.

Production method

API Active Pharmaceutical Ingredients
Obtained from natural medicine. Natural medicine is an important part of medicine. For example, artemisinin, an effective antimalarial ingredient isolated from the traditional Chinese medicine Artemisia annua.
Take existing drugs as first-comers.
1) Discover the active ingredients of the drug from the side effects of the drug. For example, the phenothiazine antipsychotic chlorpromazine and its analogs are developed from the sedative side effects of the similarly structured antihistamine promethazine.
2) Obtained through drug metabolism research. For example, the metabolites of antidepressants imipramine and amitriptyline, norimipramine and noramitriptyline, have stronger antidepressant effects than the original drug; oxazepam is the active metabolite of diazepam.
3) Leading with existing breakthrough drugs. For example, the research on lansoprazole and other prazols is based on omeprazole, which is more active than omeprazole.
Obtained by screening with pharmacological model. Through combinatorial chemistry, a large number of chemical libraries with different structures are constructed without separation of mixtures. Through high-throughput screening, the components are found to have pharmaceutical activity and then separated, and the structure of the active compound is determined.
Designed according to physiological and pathological mechanisms. For example: the study of fluorouracil takes the nucleotide uracil synthesized from DNA or RNA as the lead compound, and replaces the hydrogen at position 5 with fluorine, making it a metabolic antagonist of the normal metabolites of the organism, and is used as an antitumor drug