Bortezomib
DRACPC ID DRACPC0017
Active Ingredients Bortezomib
Description A dipeptide boronic acid analogue with antineoplastic activity. Bortezomib reversibly inhibits the 26S proteasome, a large protease complex that degrades ubiquinated proteins. By blocking the targeted proteolysis normally performed by the proteasome, bortezomib disrupts various cell signaling pathways, leading to cell cycle arrest, apoptosis, and inhibition of angiogenesis. Specifically, the agent inhibits nuclear factor (NF)-kappaB, a protein that is constitutively activated in some cancers, thereby interfering with NF-kappaB-mediated cell survival, tumor growth, and angiogenesis. In vivo, bortezomib delays tumor growth and enhances the cytotoxic effects of radiation and chemotherapy.
Synonyms [(1R)-3-Methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl)amino]propyl]amino]butyl]boronic Acid; LDP 341; MLN341; PS-341; PS341; Velcade; Bortezomib
Type Small Molecule
Disease Multiple myeloma, Mantle cell lymphoma
Classification
Proteasome inhibitor Peptide and derivative
Structure Information
Molecular Formula C19H25BN4O4
Molecular Weight 384.2
Active Sequence Not available
Sequence Length Not available
Modification Not available
IUPAC Name [(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid
InChI InChI=1S/C19H25BN4O4/c1-13(2)10-17(20(27)28)24-18(25)15(11-14-6-4-3-5-7-14)23-19(26)16-12-21-8-9-22-16/h3-9,12-13,15,17,27-28H,10-11H2,1-2H3,(H,23,26)(H,24,25)/t15-,17-/m0/s1
InChI_Key GXJABQQUPOEUTA-RDJZCZTQSA-N
SMILES CC(C)C[C@@H](B(O)O)NC([C@@H](NC(C1=NC=CN=C1)=O)CC2=CC=CC=C2)=O
External Codes
PubChem CID 387447
DrugBank Accession Number DB00188
NCI Thesaurus Code C1851
UNII 69G8BD63PP GSRS
CAS 179324-69-7
Drug approval
Drug indication
Bortezomib is indicated for the treatment of adults with multiple myeloma, also used to treat mantle cell lymphoma in patients who have already received at least one other type of treatment and is being studied in the treatment of other types of cancer.
| Drug Name | Strength | Dosage Form/Route | Company | Marketing Status | Drug ID | Approval year |
|---|---|---|---|---|---|---|
| Velcade | 3.5mg/vial | Injectable; Intravenous, Subcutaneous | Takeda Pharms Usa | Prescription | NDA: 021602 | 2003 |
| Bortezomib | 3.5mg/vial | Injectable; Intravenous, Subcutaneous | Apotex | Prescription | ANDA: 205533 | 2022 |
| Bortezomib | 3.5mg/vial | Injectable; Intravenous, Subcutaneous | Baxter Hlthcare Corp | Prescription | ANDA: 213823 | 2022 |
| Bortezomib | 3.5mg/vial | Injectable; Intravenous, Subcutaneous | Eugia Pharma | Prescription | ANDA: 212825 | 2022 |
| Bortezomib | 3.5mg/vial | Injectable; Intravenous, Subcutaneous | Fresenius Kabi Usa | Prescription | ANDA: 209659 | 2022 |
| Bortezomib | 3.5mg/vial | Injectable; Intravenous, Subcutaneous | Pharmascience Inc | Prescription | ANDA: 208392 | 2022 |
| Bortezomib | 3.5mg/vial | Injectable; Intravenous, Subcutaneous | Qilu Pharm Hainan | Prescription | ANDA: 210824 | 2022 |
| Bortezomib | 3.5mg/vial | Injectable; Intravenous, Subcutaneous | Teva Pharms Usa | Prescription | ANDA: 205857 | 2022 |
| Bortezomib | 3.5mg/vial | Injectable; Intravenous, Subcutaneous | Zydus Pharms | Prescription | ANDA: 210204 | 2022 |
| Bortezomib Accord | 1mg; 3.5mg | Injectable; Intravenous, Subcutaneous | Accord Healthcare S.L.U. | Prescription | EMEA/H/C/003984 | 2015 |
| Bortezomib Hospira | 3.5mg | Injectable; Intravenous, Subcutaneous | Pfizer Europe Ma Eeig | Prescription | EMEA/H/C/004207 | 2016 |
| Bortezomib Sun | 3.5mg | Solution; Intravenous, Subcutaneous | Sun Pharmaceutical Industries (Europe) Bv | Prescription | EMEA/H/C/004076 | 2016 |
| Bortezomib Fresenius Kabi | 3.5mg | Powder; Intravenous, Subcutaneous | Fresenius Kabi Deutschland Gmbh | Prescription | EMEA/H/C/005074 | 2019 |
| Velcade | 1mg; 3.5mg | Injectable; Intravenous, Subcutaneous | Janssen-Cilag International Nv | Prescription | EMEA/H/C/000539 | 2004 |
| ClinicalTrials.gov Identifier | Title | Condition or disease | Phase | Purpose |
|---|---|---|---|---|
| NCT03129828 | Ibrutinib (Imbruvica®), Bortezomib (Velcade®) s.c., Rituximab, CHOP for the Treatment of Elderly Patients (Age 61-80 Years) With CD20+ Diffuse Large B-cell Lymphoma, IPI ≥ 2 | Diffuse Large B Cell Lymphoma | Phase 1/2 | Treatment |
| NCT02356458 | Combination of Ibrutinib and Bortezomib Followed by Ibrutinib Maintenance to Treat Patients With Relapsed and Refractory Mantle Cell Lymphoma; a Multicenter Phase I/II Trial. | Mantle Cell Lymphoma | Phase 1/2 | Treatment |
| NCT02613598 | Phase I Dose Escalation Study to Determine the Maximum Tolerated Dose of the Combination of Ruxolitinib and Bortezomib in Patients With Relapsed or Refractory Lymphoma | Hodgkin's Lymphoma; Lymphoma, Non-Hodgkin | Phase 1 | Treatment |
| NCT01736943 | Phase II Trial of the Combination of Subcutaneous (SQ) Bortezomib and Pegylated Liposomal Doxorubicin (PLD or Doxil or LipoDox) for the Treatment of Patients With Relapsed/Refractory Acute Myelogenous Leukemia (AML) | Acute Myelogenous Leukemia | Phase 2 | Treatment |
| NCT03345303 | Bortezomib in Treating Patients With Intrahepatic Cholangiocellular Carcinoma Featuring PTEN Deficiency | Intrahepatic Cholangiocarcinoma | Phase 3 | Treatment |
More clinical information is obtained from ClinicalTrials.gov.
