The proteasome is an enzyme, which is a central component of protein degradation machinery in eukaryotic cells, both transformed and normal cells depend on the function of the proteasome to control the expression of proteins linked to cell survival and proliferation. Proteasome inhibitors block the action of proteasomes, thereby preventing the degradation of pro-apoptotic factors such as the p53 protein, permitting action of programmed cell death in neoplastic cells depending on the suppression of pro-apoptotic pathways. Proteasome inhibitors are used in the treatment of multiple myeloma, mantle-cell lymphoma, and Waldenstorm’s macroglobulinemia. Takeda Pharmaceutical, Onyx Pharmaceuticals, Celegene Corporation, Amgen, GSK, and Bristol-Myers Squibb are some of the major players in the market for proteasome inhibitors. Additionally, there are drug molecules in pipeline of various pharmaceutical companies for proteasome inhibitors.
Key Market Developments:
Approved Drug Molecules and Brand Names for Proteasome Inhibitors:
Drugs under the Pipeline for Proteasome Inhibitors:
Clinical Activity and Developments of Proteasome Inhibitors:
Currently, there are about 12 drug products in proteasome inhibitors, including 3 approved drugs and 9 drug molecules in pipeline of pharmaceutical companies.
Molecule Name |
Number of Studies |
Marizomib (NPI-0052) |
14 |
Oprozomib (ONX 0912) |
9 |
Zetomipzomib (KZR-616) |
8 |
Delanzomib (CEP-18770) |
3 |
TQB3602 |
2 |
FHND6091 |
1 |
GSK3494245 |
1 |
LXE408 |
1 |
VLX1570 |
1 |
Proteasome inhibitors are primarily used for the treatment of cancer diseases. Bortezomib has been marketed for the treatment of multiple myeloma, mantle-cell lymphoma, and Waldenstorm’s macroglobulinemia, registered for B-cell lymphoma. It is in phase-III for diffuse large B cell lymphoma, and in phase-II for amyloid light-chain amyloidosis, glioma, graft-versus--host disease, hodgkin’s disease, myelodysplastic syndromes, non-small cell lung cancer, and others. Carfilzomib is in phase-II for prostate cancer, renal cell carcinoma, mantle-cell lymphoma, and others. Marizomib is in phase-III for glioblastoma, in phase-II for ependymoma, in phase-I for diffuse intrinsic pontine glioma. Zetmipzomib is in phase-II for dermatomyositis, lupus nephritis, polymyositis, and systemic lupus erythematosus, and in phase-I for autoimmune hepatitis.
Velcade (Bortezomib), Kyprolis (Carfilzomib), and Ninlaro (Ixazomib) are the approved proteasome inhibitors in the market.
Takeda Pharmaceutical, Onyx Pharmaceuticals, Celgene Corporation, Amgen, GSK, and Bristol-Myers Squibb are some of the major market players in proteasome inhibitors.
Major indications for proteasome inhibitors are multiple myeloma, mantle-cell lymphoma, and Waldenstorm’s macroglobulinemia.
There are a total of 9 molecules in the Phase-I, II, III clinical development for proteasome inhibitors.