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Carfilzomib A Kind Of Epoxy Ketone Proteasome Inhibitor

Shanghai Chiral Chemicals Inc | Updated: Oct 23, 2017

Kafi bortezomib is a kind of epoxy ketone proteasome inhibitor, which can be selectively and irreversibly combined with the structural proteasome and the immune protease body.

July 20, 2012, the United States Food and Drug Administration (FDA) approved by the priority approval process Onyx (Onyx) pharmaceutical company developed by the bortezomib Injection (carfilzomib) listed sales, product name: Kyprolis, used for single drug treatment has been at least two treatments previously, Patients with multiple myeloma, including Boron bortezomib (Bortezomib/velcade) and an immunosuppressive agent, were treated with evidence of progression of the disease within 60d after the last 1 treatments were completed.

Multiple Myeloma (MM) is a malignant plasma cell disease that occurs in B lymphocytes, it is characterized by the cloning and proliferation of malignant plasma cells in the microenvironment of bone marrow, the single protein in blood or urine and related organ dysfunction. The second most common blood-system tumor in the world, which accounts for about 1% of tumor disease and 13% of blood tumors. In Western countries, the incidence of 5.6 cases per year/100,000 people.

Kafi Bortezomib is the second proteasome inhibitor that has been approved globally since Boron bortezomib, the first multiple myeloma drug (proteasome inhibitor) approved by the FDA in recent years, and the main role of proteasome is to degrade the unwanted or damaged proteins of cells, This effect is achieved by interrupting the chemical reaction of the peptide bond. Representative drugs are: Boron for bortezomib, card non-bortezomib). Kafi bortezomib (carfilzomib) is a new generation of protease inhibitors by intravenous administration, selectively targeting the proteasome in blood tumor cells, and avoiding the toxic side effects of inhibiting the formation of proteasome in non malignant cells.

Non-bortezomib (carfilzomib) is a peptide based epoxy matrix inhibitor that is irreversibly coupled to the 20S protease body containing threonine N-terminal active site and 26S protease in vivo proteolytic core granules. Carfilzomib has a proliferation-resistant and apoptotic activity in the body and in the hematology of granular cells. In animals, carfilzomib inhibits protease activity in blood and tissue and in multiple myeloma, hematology and solid tumor models to delay tumor growth.

Adverse reactions: The most common adverse reactions observed in clinical trials (incidence ≥30%) of Kafi bortezomib therapy are fatigue, anemia, nausea, thrombocytopenia, dyspnea, diarrhea and fever; the most common serious adverse reactions (45%) are pneumonia, acute renal failure, fever and congestive heart failure.

To assess the safety and efficacy of the drug, a study included 266 patients who had received at least 2 treatments (including boron bortezomib and thalidomide) before. Evaluate the total or partial disappearance of a patient's tumor after treatment (overall efficiency). The results showed that the overall effective rate of patients was 23% and the median remission time was 7.8 months.

The common adverse effects of bortezomib (Carfilzomib) were observed in more than 30% subjects, including fatigue, blood cell count and low platelet count, dyspnea, diarrhea and fever. Severe adverse reactions, including heart failure and dyspnea, should be closely monitored and discontinued if serious adverse reactions occur.

The pharmacological effects, indications, mechanisms, indications and adverse reactions of multiple myeloma (MM) in the treatment of drug-bortezomib (Carfilzomib) were edited and collated by Chemicalbook's Xiao Nan.


Shanghai Chiral Chemicals Inc