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

Structure

 

Show IUPAC/InChI/SMILES

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.





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