Bortezomib

Highest phase reached

Approved

www.ebi.ac.uk

Drug type

Small molecule

www.ebi.ac.uk

Listing at source: Listed

Highest phase reached: Approved
www.ebi.ac.uk

Drug type: Small molecule
www.ebi.ac.uk

Drug name: Bortezomib
www.ebi.ac.uk

Molecular weight: 384.25
www.ebi.ac.uk

Structure (SMILES): CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)c1cnccn1)B(O)O
www.ebi.ac.uk

abt 888 bortezomib
boronic acid 1r 3 methyl 1 2s 1 oxo 3 phenyl 2 pyrazinylcarbonyl amino propyl amino butyl
BORONIC ACID, ((1R)-3-METHYL-1-(((2S)-1-OXO-3-PHENYL-2-((PYRAZINYLCARBONYL)AMINO)PROPYL)AMINO)BUTYL)-
bortezomib
Bortezomib
BORTEZOMIB
Bortezomib (BTZ)
Bortezomib (drug)
bortezomib (optimized retreatment)
Bortezomib (PS-341)
bortezomib (standard retreatment)
BORTEZOMIB [EMA EPAR]
BORTEZOMIB [HSDB]
bortezomib [INN]
BORTEZOMIB [JAN]
BORTEZOMIB [MART.]
BORTEZOMIB [MI]
BORTEZOMIB [ORANGE BOOK]
BORTEZOMIB [USAN]
BORTEZOMIB [VANDF]
Bortezomib [WHO-DD]
Bortezomib 3.5 MG
bortezomib accord
BORTEZOMIB ACCORD
bortezomib ema epar

And 31 more, listed on the interactive page.

CAS registry numbers

179324-69-7

ChEMBL ID: CHEMBL325041
www.ebi.ac.uk

InChIKey: GXJABQQUPOEUTA-RDJZCZTQSA-N
www.ebi.ac.uk

PubChem compound IDs

387447

RxNorm IDs (RxCUI)

358258

FDA ingredient codes (UNII)

69G8BD63PP

L01XG01
L01XX32

Sources for recorded values

www.ebi.ac.uk

Applicant: TAKEDA PHARMS USA
Approval date: 13 May 2003
Application number: NDA021602

Status: Authorised
Status date: 26 Apr 2004
Authorisation date: 26 Apr 2004
Approved indications: Velcade as monotherapy or in combination with pegylated liposomal doxorubicin or dexamethasone is indicated for the treatment of adult patients with progressive multiple myeloma who have received at least 1 prior therapy and who have already undergone or are unsuitable for haematopoietic stem cell transplantation. Velcade in combination with melphalan and prednisone is indicated for the treatment of adult patients with previously untreated multiple myeloma who are not eligible for high dose chemotherapy with haematopoietic stem cell transplantation. Velcade in combination with dexamethasone, or with dexamethasone and thalidomide, is indicated for the induction treatment of adult patients with previously untreated multiple myeloma who are eligible for high dose chemotherapy with haematopoietic stem cell transplantation. Velcade in combination with rituximab, cyclophosphamide, doxorubicin and prednisone is indicated for the treatment of adult patients with previously untreated mantle cell lymphoma who are unsuitable for haematopoietic stem cell transplantation.
Product number: EMEA/H/C/000539
Authorisation holder: Janssen-Cilag International NV
Priority medicines scheme: No
Generic: No
Biosimilar: No
Generic medicines: 3
Biosimilar medicines: 0
Advanced therapy: No
Conditional approval: No
Additional monitoring: No
Accelerated assessment: No
Exceptional circumstances: No

Therapeutic areas

Multiple Myeloma

European medicines record

www.ema.europa.eu

Patents: 4
Designations: 4
Earliest recorded loss of exclusivity: 23 Sept 2042
First in class: Yes
Fast track: Yes
Breakthrough designation: No
Orphan designation: No
Priority review: Yes
Orphan exclusivity: No
Accelerated approval: Yes

Pharmacology name: bortezomib
Type: Synthetic organic
Drug name stem: -zomib
Approval recorded by Guide to Pharmacology: Yes

Action
Inhibition
Action type
Inhibitor
Target
proteasome 20S subunit beta 5
Gene symbol
PSMB5
Protein identifier
P28074
Median affinity
7.7
Affinity units
pIC50
Primary target
Yes
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
A5LHX3
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
O00231
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
O00232
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
O00487
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
O14818
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
O43242
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P17980
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P20618
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P25786
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P25787
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P25788
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P25789
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P28062
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P28065
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P28066
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P28070
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P28072
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P28074
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P35998
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P40306
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P43686
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P48556
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P49720
Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome
Protein identifier
P49721

And 14 more, listed on the interactive page.

Open Targets mechanisms

Mechanism
26S proteasome inhibitor
Action type
Inhibitor
Target
26S proteasome

Action type
Inhibitor
Gene symbol
PSMB1
Protein identifier
P20618
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
PSMA1
Protein identifier
P25786
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
PSMB8
Protein identifier
P28062
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
PSMB5
Protein identifier
P28074
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
PSMB2
Protein identifier
P49721
Organism
Homo sapiens
Target development level
Clinical

Condition
Leukemia, Biphenotypic, Acute
Highest recorded phase
2
Condition identifier
EFO:0000094
Subject identifier
D015456
Condition
Leukemia, Lymphocytic, Chronic, B-Cell
Highest recorded phase
2
Condition identifier
EFO:0000095
Subject identifier
D015451
Condition
Lymphoma, Follicular
Highest recorded phase
2
Condition identifier
EFO:0000096
Subject identifier
D008224
Condition
Hodgkin Disease
Highest recorded phase
2
Condition identifier
EFO:0000183
Subject identifier
D006689
Condition
Lymphoma, B-Cell, Marginal Zone
Highest recorded phase
2
Condition identifier
EFO:0000191
Subject identifier
D018442
Condition
Myelodysplastic Syndromes
Highest recorded phase
2
Condition identifier
EFO:0000198
Subject identifier
D009190
Condition
Neoplasms, Plasma Cell
Highest recorded phase
2
Condition identifier
EFO:0000200
Subject identifier
D054219
Condition
Leukemia, Biphenotypic, Acute
Highest recorded phase
2
Condition identifier
EFO:0000209
Subject identifier
D015456
Condition
Lymphoma, T-Cell, Peripheral
Highest recorded phase
2
Condition identifier
EFO:0000211
Subject identifier
D016411
Condition
Precursor Cell Lymphoblastic Leukemia-Lymphoma
Highest recorded phase
3
Condition identifier
EFO:0000220
Subject identifier
D054198
Condition
Leukemia, Myeloid, Acute
Highest recorded phase
3
Condition identifier
EFO:0000222
Subject identifier
D015470
Condition
Leukemia, Promyelocytic, Acute
Highest recorded phase
2
Condition identifier
EFO:0000224
Subject identifier
D015473
Condition
Carcinoma, Adenoid Cystic
Highest recorded phase
2
Condition identifier
EFO:0000231
Subject identifier
D003528
Condition
Immunoblastic Lymphadenopathy
Highest recorded phase
1
Condition identifier
EFO:0000255
Subject identifier
D007119
Condition
Breast Neoplasms
Highest recorded phase
2
Condition identifier
EFO:0000305
Subject identifier
D001943
Condition
Burkitt Lymphoma
Highest recorded phase
1
Condition identifier
EFO:0000309
Subject identifier
D002051
Condition
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Highest recorded phase
2
Condition identifier
EFO:0000339
Subject identifier
D015464
Condition
Lymphoma, Large B-Cell, Diffuse
Highest recorded phase
3
Condition identifier
EFO:0000403
Subject identifier
D016403
Condition
Adenocarcinoma, Follicular
Highest recorded phase
2
Condition identifier
EFO:0000501
Subject identifier
D018263
Condition
Glioblastoma
Highest recorded phase
2
Condition identifier
EFO:0000519
Subject identifier
D005909
Condition
Immune System Diseases
Highest recorded phase
2
Condition identifier
EFO:0000540
Subject identifier
D007154
Condition
Leukemia
Highest recorded phase
3
Condition identifier
EFO:0000565
Subject identifier
D007938
Condition
Adenocarcinoma of Lung
Highest recorded phase
2
Condition identifier
EFO:0000571
Subject identifier
D000077192
Condition
Lymphoma
Highest recorded phase
3
Condition identifier
EFO:0000574
Subject identifier
D008223
Condition
Mesothelioma
Highest recorded phase
2
Condition identifier
EFO:0000588
Subject identifier
D008654

And 82 more, listed on the interactive page.

Condition identifier
EFO_0000191
Highest recorded phase
2
Condition identifier
EFO_0000198
Highest recorded phase
2
Condition identifier
EFO_0000220
Highest recorded phase
2
Condition identifier
EFO_0000222
Highest recorded phase
2
Condition identifier
EFO_0000403
Highest recorded phase
3
Condition identifier
EFO_0000565
Highest recorded phase
2
Condition identifier
EFO_0000574
Highest recorded phase
3
Condition identifier
EFO_0000616
Highest recorded phase
2
Condition identifier
EFO_0000685
Condition identifier
EFO_0000691
Highest recorded phase
2
Condition identifier
EFO_0000707
Highest recorded phase
1
Condition identifier
EFO_0001378
Condition identifier
EFO_0003060
Highest recorded phase
2
Condition identifier
EFO_0004256
Highest recorded phase
2
Condition identifier
EFO_0005952
Highest recorded phase
3
Condition identifier
EFO_0007160
Highest recorded phase
3
Condition identifier
EFO_0007183
Highest recorded phase
2
Condition identifier
EFO_0009441
Highest recorded phase
2
Condition identifier
EFO_0010134
Highest recorded phase
3
Condition identifier
EFO_0010673
Highest recorded phase
2
Condition identifier
EFO_1000355
Highest recorded phase
2
Condition identifier
EFO_1001469
Condition identifier
EFO_1001875
Condition identifier
EFO_1001938
Highest recorded phase
2
Condition identifier
EFO_1001941
Highest recorded phase
2

And 158 more, listed on the interactive page.

Event
disease progression
Reports
683
Reporting signal score
415.578
Event
drug hypersensitivity
Reports
34
Reporting signal score
343.533
Event
febrile neutropenia
Reports
553
Reporting signal score
344.333
Event
headache
Reports
196
Reporting signal score
376.321
Event
neuropathy peripheral
Reports
2,710
Reporting signal score
4,913.79
Event
neutropenia
Reports
913
Reporting signal score
396.54
Event
peripheral sensory neuropathy
Reports
210
Reporting signal score
339.863
Event
plasma cell myeloma
Reports
2,222
Reporting signal score
5,889.42
Event
plasma cell myeloma recurrent
Reports
296
Reporting signal score
814.524
Event
plasmacytoma
Reports
139
Reporting signal score
355.743
Event
platelet count decreased
Reports
751
Reporting signal score
424.561
Event
pneumonia
Reports
1,133
Reporting signal score
345.162
Event
polyneuropathy
Reports
384
Reporting signal score
655.647
Event
thrombocytopenia
Reports
1,429
Reporting signal score
1,227.38

NCT00004002
clinicaltrials.gov
NCT00006098
clinicaltrials.gov
NCT00030875
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NCT00038571
clinicaltrials.gov
NCT00045695
clinicaltrials.gov
NCT00066508
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NCT00093769
clinicaltrials.gov
NCT00182637
clinicaltrials.gov
NCT00217503
clinicaltrials.gov
NCT00262860
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NCT00265928
clinicaltrials.gov
NCT00290706
clinicaltrials.gov
NCT00295932
clinicaltrials.gov
NCT00298779
clinicaltrials.gov
NCT00334438
clinicaltrials.gov
NCT00372905
clinicaltrials.gov
NCT00376961
clinicaltrials.gov
NCT00377052
clinicaltrials.gov
NCT00428142
clinicaltrials.gov
NCT00428545
clinicaltrials.gov
NCT00439556
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NCT00513955
clinicaltrials.gov
NCT00515138
clinicaltrials.gov
NCT00598169
clinicaltrials.gov
NCT00634179
clinicaltrials.gov

And 476 more, listed on the interactive page.

Prodrug: No
Chirality: Single enantiomer
Inorganic: No
Heavy atoms: 28
Molecular formula: C19H25BN4O4
Monoisotopic mass: 384.1968855
Natural product: Yes

0143-9098
0409-1700
0409-1703
0409-1704
25021-262
31722-303
43598-426
51817-586
55150-337
63020-049
63323-821
68001-534
68001-540
68001-541
68083-650
68083-651
70069-836
70511-161
70511-162
71288-118
72205-183
72338-200
72603-270
75007-501
83090-008

And 7 more, listed on the interactive page.

Recorded assays: 3,908
Active assays: 1,833

Confirmatory
Other
Screening
Summary

Antineoplastic Agents
id.nlm.nih.gov

Oral bioavailability

Median: 28.5
Mean: 28.5
Minimum: 11
Maximum: 46
Unit: %
Assays: 2
Standard deviation: 24.7487
Summary method: median
Censored results excluded: 0
Other units excluded: 0
Unknown units excluded: 0

Measurement types

Related records

Trials (1,292)

17-N-Allylamino-17-Demethoxygeldanamycin and Bortezomib in Treating Patients With Relapsed or Refractory Hematologic Cancer
2015-09: a Phase II Randomized, Open-label Study of Anti-signaling Lymphocytic Activation Molecule Monoclonal Antibody During Maintenance Therapy
2015-12: A Study Exploring the Use of Early and Late Consolidation/Maintenance Therapy
2017-03: A Single-Arm, Open-label Study of Anti-Signaling Lymphocytic Activation Molecule F7 (Anti-SLAMF7) Monoclonal Antibody (mAb) Therapy After Autologous Stem Cell Transplant in Patients With Multiple Myeloma
3T MRI Biomarkers of Glioma Treatment Response
5-fluorouracil Plus Panitumumab (Anti-EGFR) and Sotorasib (KRAS G12C Inhibitor) in First-line Treatment of Patients Non-eligible for a Doublet/Triplet Chemotherapy With Advanced Unresectab
A 24 Week, Multicenter, Prospective, Open-labeled, Single-arm, Exploratory Phase 4 Clinical Trial to Evaluate the Safety and Efficacy of Lobeglitazone in Decreasing Intrahepatic Fat Contents in Type 2 Diabetes With NAFLD
A Clinical Study on the Whole-course Management (BCD-KPD-AutoHSCT) Scheme for Patients With RIMM
A Clinical Study to Assess the Safety and Activity of SRT501 Alone or in Combination With Bortezomib in Patients With Multiple Myeloma
A Clinical Study to Evaluate the Safety and the Pharmacokinetics of UI068 in Healthy Adult Volunteers Under Fed Conditions
A Combination of Zarnestra With Velcade for Patients With Relapsed Multiple Myeloma
A Comparative Study of Oral Gabapentin, Oral Alprazolam and Intravenous Dexmedetomidine on Perioperative Anxiety and Pain During Posterior Segment Eye Surgery Under Peribulbar Block : a Randomized, Double-blind Study.
A Comparison of Desflurane vs. Sevoflurane and the Time to Awakening and the Incidence and Severity of Cough
A Comparison of Propofol Based Total Intravenous Anesthesia and Sevoflurane Based Balanced Anesthesia on Renal Protection During Lung Transplantation Under Extracorporeal Membrane Oxygenation - A Prospective, Randomized Trial
A Dose Escalation Study of the Histone Deacetylase Inhibitor (HDACi) JNJ 26481585 in Combination With VELCADE (Bortezomib) and Dexamethasone for Patients With Relapsed Multiple Myeloma
A Dose Finding Phase I Trial of the Combination of Topotecan and PS-341, a Novel Proteasome Inhibitor, in Advanced Malignancies
A Drug-drug Interaction Study of DP-R213
A FIH Study to Investigate the Safety, Tolerability and PK of P218
A Japan Phase I/II Study of Bortezomib in Relapsed or Refractory Multiple Myeloma Patients
A Multicenter Phase I Study Evaluating the Addition of Bortezomib to an Established Acute Graft Versus Host Disease Prophylaxis Regimen in Pediatric Allogeneic Hematopoietic Stem Cell Transplant Patients

In development for (32)

Acute lymphoblastic leukemia Phase 2
Acute myeloid leukemia Phase 2
Autoimmune encephalitis Phase 2
Autoimmune thrombocytopenic purpura Phase 3
B-cell neoplasm Phase 2
B-cell non-Hodgkin lymphoma Phase 2
Breast cancer Phase 2
Bronchiolitis obliterans syndrome Phase 2
Chronic graft versus host disease Phase 2
Colorectal cancer Phase 2
Diffuse large B-cell lymphoma Phase 3
Follicular lymphoma Phase 2
Gastric cancer Phase 2
Graft versus host disease Phase 2
Hematopoietic and lymphoid cell neoplasm Phase 2
Intrahepatic cholangiocarcinoma Phase 3
Kidney cancer Phase 2
Leukemia Phase 2
Lung cancer Phase 2
Lymphoma Phase 3

Bortezomib

Development status

Names and chemistry

Other names (56)

Identifiers

ATC classification codes (2)

Regulatory information

United States

European Union

Therapeutic areas

Other regulatory facts

Pharmacology

Drug classification

Mechanisms of action (39)

Open Targets mechanisms

DrugCentral mechanisms (5)

Investigated indications (107)

Open Targets indications (183)

Reported adverse events (14)

Trial references (501)

Chemical properties

National Drug Codes

Evidence counts

Active assay types (4)

Pharmacologic actions

Biological measurements

Observed measurements

Oral bioavailability

Measurement types

Related records

Trials (1,292)

In development for (32)

Other linked conditions (4)