DGIdb - BORTEZOMIB Drug Record

BORTEZOMIB chembl:CHEMBL325041 ApprovedAntineoplasticImmunotherapy

Alternate Names:

BORTEZOMIB HYDRATE
VELCADE
LDP-341
BORTEZOMIB
NSC-681239
PS-341
PS 341
N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE
VELCADE®
PEPTIDE BORONATE
[(1R)-3-METHYL-1-({(2S)-3-PHENYL-2-[(PYRAZIN-2-YLCARBONYL)AMINO]PROPANOYL}AMINO)BUTYL]BORONIC ACID
drugbank:00188
rxcui:358258
chembl:CHEMBL325041
chemidplus:179324-69-7
pubchem.compound:387447

Drug Info:

Year of Approval	2003
Drug Class	antineoplastic agents
FDA Approval	Multiple myeloma, Mantle cell lymphoma
Drug Class	Small molecule inhibitor
Drug Categories	cytochrome p-450 cyp1a2 inhibitors (moderate)
Drug Categories	boronic acids
Drug Categories	boron compounds
Drug Categories	acids
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antineoplastic agent
Drug Categories	cardiotoxic antineoplastic agents
Drug Categories	cytochrome p-450 cyp1a2 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2c19 inhibitors (weak)
Drug Categories	cytochrome p-450 cyp2c9 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	hepatotoxic agents
Drug Categories	immunosuppressive agents
Drug Categories	narrow therapeutic index drugs
Drug Categories	oatp1b3 inhibitors
Drug Categories	p-glycoprotein substrates
Drug Categories	p-glycoprotein substrates with narrow therapeutic index
Drug Categories	potential qtc-prolonging agents
Drug Categories	proteasome inhibitors
Drug Categories	qtc prolonging agents

(17 More Sources)

Publications:

Kawamura S et al., 2014, Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates., J Med Chem
Kumar et al., 2012, The GATA2 transcriptional network is requisite for RAS oncogene-driven non-small cell lung cancer., Cell
Pearse et al., 2005, A neurotrophin axis in myeloma: TrkB and BDNF promote tumor-cell survival., Blood
Chauhan et al., 2004, 2-Methoxyestardiol and bortezomib/proteasome-inhibitor overcome dexamethasone-resistance in multiple myeloma cells by modulating Heat Shock Protein-27., Apoptosis
Blackburn C et al., 2010, Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome., Bioorg Med Chem Lett
Fernández et al., 2005, Differential regulation of noxa in normal melanocytes and melanoma cells by proteasome inhibition: therapeutic implications., Cancer Res.
Kawamura S et al., 2013, Potent proteasome inhibitors derived from the unnatural cis-cyclopropane isomer of Belactosin A: synthesis, biological activity, and mode of action., J Med Chem
Pikman et al., 2017, Synergistic Drug Combinations with a CDK4/6 Inhibitor in T-cell Acute Lymphoblastic Leukemia., Clin. Cancer Res.
Duechler et al., 2005, In vitro cytotoxic effect of proteasome inhibitor bortezomib in combination with purine nucleoside analogues on chronic lymphocytic leukaemia cells., Eur. J. Haematol.
Meißner T et al., 2017, Metastatic triple-negative breast cancer patient with <i>TP53</i> tumor mutation experienced 11 months progression-free survival on bortezomib monotherapy without adverse events after ending standard treatments with grade 3 adverse events., Cold Spring Harb Mol Case Stud
Shringarpure et al., 2006, Gene expression analysis of B-lymphoma cells resistant and sensitive to bortezomib., Br. J. Haematol.
Bodoor et al., 2010, FGFR3 mutational status and protein expression in patients with bladder cancer in a Jordanian population., Cancer Epidemiol
Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
Guan et al., 2009, Bortezomib therapeutic effect is associated with expression of FGFR3 in multiple myeloma cells., Anticancer Res.
Otsuka et al., 2011, Constitutively active FGFR3 with Lys650Glu mutation enhances bortezomib sensitivity in plasma cell malignancy., Anticancer Res.
Chell et al., 2013, Tumour cell responses to new fibroblast growth factor receptor tyrosine kinase inhibitors and identification of a gatekeeper mutation in FGFR3 as a mechanism of acquired resistance., Oncogene
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
Qing et al., 2009, Antibody-based targeting of FGFR3 in bladder carcinoma and t(4;14)-positive multiple myeloma in mice., J. Clin. Invest.
Favis R et al., 2011, Genetic variation associated with bortezomib-induced peripheral neuropathy., Pharmacogenet Genomics
Nawrocki et al., 2005, Bortezomib inhibits PKR-like endoplasmic reticulum (ER) kinase and induces apoptosis via ER stress in human pancreatic cancer cells., Cancer Res.
Janku et al., 2011, PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitors., Mol. Cancer Ther.
Jung et al., 2001, Flavopiridol increases sensitization to gemcitabine in human gastrointestinal cancer cell lines and correlates with down-regulation of ribonucleotide reductase M2 subunit., Clin. Cancer Res.
Ngo BT et al., 2010, Monitoring bortezomib therapy in multiple myeloma: screening of cyclin D1, D2, and D3 via reliable real-time polymerase chain reaction and association with clinico-pathological features and outcome., Leuk Lymphoma

BORTEZOMIB PMAIP1

Interaction Score: 1.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16024631

Sources:
NCI
BORTEZOMIB PSMD1

Interaction Score: 0.95

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

Trial Name Velcade

PMIDs:
24524217

Sources:
DTC MyCancerGenome TdgClinicalTrial ChemblInteractions TEND
BORTEZOMIB PSMD2

Interaction Score: 0.95

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction 26S proteosome inhibitor

Trial Name Velcade

PMIDs:
24524217

Sources:
DTC MyCancerGenome TdgClinicalTrial ChemblInteractions TEND
BORTEZOMIB PSMB1

Interaction Score: 0.74

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Velcade

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions TEND
BORTEZOMIB CAPN1

Interaction Score: 0.63

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20875739

Sources:
DTC
BORTEZOMIB PSMC4

Interaction Score: 0.63

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMD7

Interaction Score: 0.63

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMC6

Interaction Score: 0.63

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMD12

Interaction Score: 0.63

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMD6

Interaction Score: 0.63

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMC1

Interaction Score: 0.63

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMD13

Interaction Score: 0.63

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction 26S proteosome inhibitor

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMD8

Interaction Score: 0.63

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMD3

Interaction Score: 0.63

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMD11

Interaction Score: 0.63

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMC2

Interaction Score: 0.63

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMB5

Interaction Score: 0.52

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Velcade

Direct Interaction? True

PMIDs:
24524217 23547757

Sources:
DTC DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology
BORTEZOMIB PSMB4

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMB7

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMB6

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMC5

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMA6

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMA2

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMD4

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction 26S proteosome inhibitor

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMA1

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMC3

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMA5

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMB10

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMA8

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMB3

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB SEM1

Interaction Score: 0.47

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC ChemblInteractions
BORTEZOMIB PSMB2

Interaction Score: 0.47

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

Trial Name Velcade

PMIDs:
24524217

Sources:
DTC MyCancerGenome TdgClinicalTrial ChemblInteractions TEND
BORTEZOMIB ADRM1

Interaction Score: 0.47

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC ChemblInteractions
BORTEZOMIB GATA2

Interaction Score: 0.47

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy bortezomib + fasudil

Indication/Tumor Type non-small cell lung carcinoma

Response Type sensitive

PMIDs:
22541434

Sources:
JAX-CKB CIViC
BORTEZOMIB PSMB9

Interaction Score: 0.42

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMA4

Interaction Score: 0.42

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMA3

Interaction Score: 0.42

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMA7

Interaction Score: 0.42

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSMB11

Interaction Score: 0.38

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC ChemblInteractions
BORTEZOMIB PSMD10P1

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB PIPSL

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB PSMF1

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB CTSL

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20875739

Sources:
DTC
BORTEZOMIB PSME4

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB PSME2

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB PSMD5

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB PSMD10

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB F12

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20875739

Sources:
DTC
BORTEZOMIB PSMB8

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction 26S proteosome inhibitor

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB PSME2P2

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB PSMD10P3

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB PSMD9

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB PSME3

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB PSMD10P2

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB PSMC1P1

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB PSMC3IP

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB PSMD4P1

Interaction Score: 0.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB PRSS3

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20875739

Sources:
DTC
BORTEZOMIB PSMD14

Interaction Score: 0.23

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions
BORTEZOMIB BCL2L2

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15813915

Sources:
NCI
BORTEZOMIB KLK4

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
BORTEZOMIB PSME1

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenome
BORTEZOMIB PRSS2

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20875739

Sources:
DTC
BORTEZOMIB CTSB

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20875739

Sources:
DTC
BORTEZOMIB HSPB2

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15004512

Sources:
NCI
BORTEZOMIB PRB2

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
BORTEZOMIB PLAT

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20875739

Sources:
DTC
BORTEZOMIB FGFR3

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

Clinical Status preclinical

Pathway activation

Variant Effect gain-of-function

PMIDs:
20542753 26619011 19331127 21273588 22869148 25157968 19381019

Sources:
CGI DoCM
BORTEZOMIB E2F1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11489836

Sources:
NCI
BORTEZOMIB NOTCH1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
28151717

Sources:
JAX-CKB
BORTEZOMIB CTLA4

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21228734

Sources:
PharmGKB
BORTEZOMIB CCND1

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20578819

Sources:
CIViC
BORTEZOMIB RB1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Ribociclib + Bortezomib

Indication/Tumor Type T-cell adult acute lymphocytic leukemia

Response Type sensitive

PMIDs:
28151717

Sources:
JAX-CKB
BORTEZOMIB XIAP

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15813915

Sources:
NCI
BORTEZOMIB DDIT3

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16357160

Sources:
NCI
BORTEZOMIB PLG

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20875739

Sources:
DTC
BORTEZOMIB HSPA4

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16846475

Sources:
NCI
BORTEZOMIB PRSS1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20875739

Sources:
DTC TTD
BORTEZOMIB NFKB2

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC TTD
BORTEZOMIB BDNF

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15657181

Sources:
NCI
BORTEZOMIB F2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20875739

Sources:
DTC
BORTEZOMIB BAX

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC
BORTEZOMIB BCL2

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC
BORTEZOMIB KRAS

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical

Response Type sensitive

PMIDs:
22541434

Sources:
JAX-CKB
BORTEZOMIB PIK3CA

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Bortezomib + Temsirolimus + Topotecan

Indication/Tumor Type small intestine adenocarcinoma

Response Type resistant

PMIDs:
21216929

Sources:
JAX-CKB
BORTEZOMIB NFKB1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
ClearityFoundationClinicalTrial
BORTEZOMIB FLT3

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
None found

Sources:
MyCancerGenomeClinicalTrial
BORTEZOMIB TP53

Interaction Score: 0.0

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
28679691

Sources:
TALC CIViC
BORTEZOMIB NFE2L2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
BORTEZOMIB AR

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

TEND: BORTEZOMIB
- Version: 01-August-2011
Alternate Names:

BORTEZOMIB Primary Drug Name

Drug Info:

Drug Class antineoplastic agents

Year of Approval 2003

Publications:
MyCancerGenome: BORTEZOMIB
- Version: 20-Jun-2017
Alternate Names:

LDP341 Development Name

MLN341 Development Name

PS-341 Development Name

Drug Info:

Drug Class Small molecule inhibitor

FDA Approval Multiple myeloma, Mantle cell lymphoma

Publications:
DrugBank: DB00188
- Version: 5.1.7
Alternate Names:

BORTEZOMIB DrugBank Drug Name

179324-69-7 CAS Number

Act Bortezomib Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:
TdgClinicalTrial: BORTEZOMIB
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small Molecule

FDA Approval approved

Publications:

DTC: BORTEZOMIB

Version: 02-September-2020

Alternate Names:

CHEMBL325041 ChEMBL Drug ID

Drug Info:

Publications:

Kawamura S et al., 2014, Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates., J Med Chem

Blackburn C et al., 2010, Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome., Bioorg Med Chem Lett

Kawamura S et al., 2013, Potent proteasome inhibitors derived from the unnatural cis-cyclopropane isomer of Belactosin A: synthesis, biological activity, and mode of action., J Med Chem

NCI: PS-341

Version: 14-September-2017

Alternate Names:

C1851 NCI drug code

Drug Info:

Publications:

Jung et al., 2001, Flavopiridol increases sensitization to gemcitabine in human gastrointestinal cancer cell lines and correlates with down-regulation of ribonucleotide reductase M2 subunit., Clin. Cancer Res.

Chauhan et al., 2004, 2-Methoxyestardiol and bortezomib/proteasome-inhibitor overcome dexamethasone-resistance in multiple myeloma cells by modulating Heat Shock Protein-27., Apoptosis

NCI: BORTEZOMIB

Version: 14-September-2017

Alternate Names:

C1851 NCI drug code

Drug Info:

Publications:

Duechler et al., 2005, In vitro cytotoxic effect of proteasome inhibitor bortezomib in combination with purine nucleoside analogues on chronic lymphocytic leukaemia cells., Eur. J. Haematol.

Nawrocki et al., 2005, Bortezomib inhibits PKR-like endoplasmic reticulum (ER) kinase and induces apoptosis via ER stress in human pancreatic cancer cells., Cancer Res.

Pearse et al., 2005, A neurotrophin axis in myeloma: TrkB and BDNF promote tumor-cell survival., Blood

JAX-CKB: Bortezomib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Janku et al., 2011, PIK3CA mutations in patients with advanced cancers treated with PI3K/AKT/mTOR axis inhibitors., Mol. Cancer Ther.

Pikman et al., 2017, Synergistic Drug Combinations with a CDK4/6 Inhibitor in T-cell Acute Lymphoblastic Leukemia., Clin. Cancer Res.

CGI: Bortezomib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Guan et al., 2009, Bortezomib therapeutic effect is associated with expression of FGFR3 in multiple myeloma cells., Anticancer Res.

Otsuka et al., 2011, Constitutively active FGFR3 with Lys650Glu mutation enhances bortezomib sensitivity in plasma cell malignancy., Anticancer Res.

JAX-CKB: bortezomib
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:

Kumar et al., 2012, The GATA2 transcriptional network is requisite for RAS oncogene-driven non-small cell lung cancer., Cell

DoCM: BORTEZOMIB

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Qing et al., 2009, Antibody-based targeting of FGFR3 in bladder carcinoma and t(4;14)-positive multiple myeloma in mice., J. Clin. Invest.

MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn

Chell et al., 2013, Tumour cell responses to new fibroblast growth factor receptor tyrosine kinase inhibitors and identification of a gatekeeper mutation in FGFR3 as a mechanism of acquired resistance., Oncogene

PharmGKB: bortezomib
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Favis R et al., 2011, Genetic variation associated with bortezomib-induced peripheral neuropathy., Pharmacogenet Genomics

CIViC: BORTEZOMIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Kumar et al., 2012, The GATA2 transcriptional network is requisite for RAS oncogene-driven non-small cell lung cancer., Cell

Meißner T et al., 2017, Metastatic triple-negative breast cancer patient with <i>TP53</i> tumor mutation experienced 11 months progression-free survival on bortezomib monotherapy without adverse events after ending standard treatments with grade 3 adverse events., Cold Spring Harb Mol Case Stud

Ngo BT et al., 2010, Monitoring bortezomib therapy in multiple myeloma: screening of cyclin D1, D2, and D3 via reliable real-time polymerase chain reaction and association with clinico-pathological features and outcome., Leuk Lymphoma

TTD: PS-341
- Version: 2020.06.01
Alternate Names:

D03AJX TTD Drug ID

Drug Info:

Publications:
TALC: BORTEZOMIB
- Version: 12-May-2016
Alternate Names:

BORTEZOMIB Primary Drug Name

BORTEZOMIB Drug Generic Name

VELCADE Drug Trade Name

Drug Info:

Publications:
TTD: Bortezomib
- Version: 2020.06.01
Alternate Names:

D0SH3I TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178103007
- Version: 29-September-2020
Alternate Names:

BORTEZOMIB GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblInteractions: CHEMBL325041
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL325041
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: BORTEZOMIB
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
ClearityFoundationClinicalTrial: BORTEZOMIB
- Version: 15-June-2013
Alternate Names:

Drug Info:

Publications:

Mechanism of Interaction	26S proteosome inhibitor
Direct Interaction	yes
Trial Name	Velcade

Novel drug target	Established target
Trial Name	Velcade
Direct Interaction	yes

combination therapy	bortezomib + fasudil
Indication/Tumor Type	non-small cell lung carcinoma
Response Type	sensitive

Clinical Status	preclinical
Pathway	activation
Variant Effect	gain-of-function

Evidence Type	Actionable
Approval Status	Preclinical - Cell culture
Response Type	sensitive

combination therapy	Ribociclib + Bortezomib
Indication/Tumor Type	T-cell adult acute lymphocytic leukemia
Response Type	sensitive

combination therapy	Bortezomib + Temsirolimus + Topotecan
Indication/Tumor Type	small intestine adenocarcinoma
Response Type	resistant

LDP341	Development Name
MLN341	Development Name
PS-341	Development Name

BORTEZOMIB	DrugBank Drug Name
179324-69-7	CAS Number
Act Bortezomib	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

BORTEZOMIB	Primary Drug Name
BORTEZOMIB	Drug Generic Name
VELCADE	Drug Trade Name

BORTEZOMIB Drug Record

BORTEZOMIB chembl:CHEMBL325041 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16024631

Sources: NCI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction 26S proteosome inhibitor Direct Interaction yes Trial Name Velcade

PMIDs: 24524217

Sources: DTC MyCancerGenome TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction 26S proteosome inhibitor Trial Name Velcade

PMIDs: 24524217

Sources: DTC MyCancerGenome TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name Velcade Direct Interaction yes

PMIDs: 24524217

Sources: DTC DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20875739

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction 26S proteosome inhibitor Direct Interaction yes

PMIDs: 24524217

Sources: DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction 26S proteosome inhibitor Direct Interaction yes

PMIDs: 24524217

Sources: DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction 26S proteosome inhibitor Direct Interaction yes

PMIDs: 24524217

Sources: DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction 26S proteosome inhibitor Direct Interaction yes

PMIDs: 24524217

Sources: DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction 26S proteosome inhibitor Direct Interaction yes

PMIDs: 24524217

Sources: DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction 26S proteosome inhibitor Direct Interaction yes

PMIDs: 24524217

Sources: DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction 26S proteosome inhibitor

PMIDs: 24524217

Sources: DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction 26S proteosome inhibitor Direct Interaction yes

PMIDs: 24524217

Sources: DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction 26S proteosome inhibitor Direct Interaction yes

PMIDs: 24524217

Sources: DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction 26S proteosome inhibitor Direct Interaction yes

PMIDs: 24524217

Sources: DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction 26S proteosome inhibitor Direct Interaction yes

PMIDs: 24524217

Sources: DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name Velcade Direct Interaction? True

PMIDs: 24524217 23547757

Sources: DTC DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction 26S proteosome inhibitor Direct Interaction yes

PMIDs: 24524217

Sources: DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction 26S proteosome inhibitor Direct Interaction yes

PMIDs: 24524217

Interaction Types & Directionality:

n/a

PMIDs:
16024631

Sources:
NCI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

Trial Name Velcade

PMIDs:
24524217

Sources:
DTC MyCancerGenome TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction 26S proteosome inhibitor

Trial Name Velcade

PMIDs:
24524217

Sources:
DTC MyCancerGenome TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Velcade

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

n/a

PMIDs:
20875739

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction 26S proteosome inhibitor

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Velcade

Direct Interaction? True

PMIDs:
24524217 23547757

Sources:
DTC DrugBank MyCancerGenome TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes

PMIDs:
24524217

Sources:
DTC MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction 26S proteosome inhibitor

Direct Interaction yes