General Information of Drug (ID: DMNO38U)

Drug Name
Bortezomib
Synonyms
179324-69-7; Velcade; Bortezomib (PS-341); UNII-69G8BD63PP; N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE; MLN-341; [(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid; [(1R)-3-Methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl)amino]propyl]amino]butyl]boronic acid; CHEMBL325041; 69G8BD63PP; Boronic acid,; DPBA; PROSCRIPT BORONIC ACID; LPD 341; LPD-341; VELCADE (TN); Velcade (TN); Pyz-Phe-boroLeu; Bortezomib(JAN/USAN/INN); Velcade, MG-341, PS-341, Bortezomib; N-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-Nalpha-(pyrazin-2-ylcarbonyl)-L-phenylalaninamide; Bortezomib (Proteasome inhibitor); Peptide boronate
Indication
Disease Entry ICD 11 Status REF
Leukemia N.A. Approved [1]
Lung cancer 2C25.0 Approved [1]
Lymphoproliferative syndrome N.A. Approved [1]
MALT lymphoma N.A. Approved [1]
Mantle cell lymphoma 2A85.5 Approved [2]
Minimally invasive lung adenocarcinoma N.A. Approved [1]
Multiple myeloma 2A83 Approved [3]
Nodal marginal zone lymphoma 2A85.0 Approved [1]
Plasma cell myeloma 2A83.1 Approved [1]
Recurrent adult burkitt lymphoma 2A85.6 Approved [1]
Non-hodgkin lymphoma 2B33.5 Phase 3 [3]
B-cell neoplasm N.A. Investigative [1]
Colon cancer 2B90.Z Investigative [1]
Gastric cancer 2B72 Investigative [1]
⏷ Show the Full List of Indication(s)
Therapeutic Class
Anticancer Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski):
0
Molecular Weight 384.2
Logarithm of the Partition Coefficient Not Available
Rotatable Bond Count 9
Hydrogen Bond Donor Count 4
Hydrogen Bond Acceptor Count 6
ADMET Property
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 57 mcg/L [4]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 1: high solubility and high permeability [5]
Clearance
The total body clearance of drug is 102-112 L/h [4]
Half-life
The concentration or amount of drug in body reduced by one-half in 40 - 193 hours [4]
Metabolism
The drug is metabolized via the CYP3A4, CYP2C19, and CYP1A2 [4]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.0836 micromolar/kg/day [6]
Unbound Fraction
The unbound fraction of drug in plasma is 0.17% [7]
Vd
Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 10 L/kg [7]
Water Solubility
The ability of drug to dissolve in water is measured as 3.3 mg/mL [5]
Chemical Identifiers
Formula
C19H25BN4O4
IUPAC Name
[(1R)-3-methyl-1-[[(2S)-3-phenyl-2-(pyrazine-2-carbonylamino)propanoyl]amino]butyl]boronic acid
Canonical SMILES
B([C@H](CC(C)C)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)(O)O
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
InChIKey
GXJABQQUPOEUTA-RDJZCZTQSA-N
Cross-matching ID
PubChem CID
387447
ChEBI ID
CHEBI:52717
CAS Number
179324-69-7
DrugBank ID
DB00188
TTD ID
D0SH3I
VARIDT ID
DR01331
INTEDE ID
DR0221
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Cationic trypsinogen (PRSS1) TT2WR1T TRY1_HUMAN Inhibitor [8]
Kallikrein-related peptidase (KLK) TT5L2VC NOUNIPROTAC Inhibitor [8]
Proteasome (PS) TTU7ZMG NOUNIPROTAC Modulator [9]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [10]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4)
Main DME
DE4LYSA CP3A4_HUMAN Substrate [11]
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [12]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Substrate [13]
Mephenytoin 4-hydroxylase (CYP2C19)
Main DME
DEGTFWK CP2CJ_HUMAN Substrate [12]
Cytochrome P450 1A2 (CYP1A2)
Main DME
DEJGDUW CP1A2_HUMAN Substrate [14]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
14-3-3 protein epsilon OT3WQXNA 1433E_HUMAN Gene/Protein Processing [15]
14-3-3 protein sigma (SFN) OTLJCZ1U 1433S_HUMAN Gene/Protein Processing [15]
14-3-3 protein zeta/delta OT2TKG9P 1433Z_HUMAN Gene/Protein Processing [15]
2-oxoglutarate dehydrogenase complex component E1 (OGDH) OTHGTQWF ODO1_HUMAN Gene/Protein Processing [15]
26S proteasome non-ATPase regulatory subunit 12 (PSMD12) OTWICA51 PSD12_HUMAN Gene/Protein Processing [15]
26S proteasome non-ATPase regulatory subunit 13 (PSMD13) OTNQ351N PSD13_HUMAN Gene/Protein Processing [15]
26S proteasome non-ATPase regulatory subunit 7 (PSMD7) OT7PZZ4K PSMD7_HUMAN Gene/Protein Processing [15]
26S proteasome regulatory subunit 6B (PSMC4) OTS3XN41 PRS6B_HUMAN Gene/Protein Processing [15]
5'-nucleotidase (NT5E) OT7J5LT6 5NTD_HUMAN Gene/Protein Processing [15]
5-hydroxytryptamine receptor 2B (HTR2B) OTM1AD9J 5HT2B_HUMAN Gene/Protein Processing [15]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Bortezomib
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Carfilzomib DM48K0X Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Carfilzomib. Multiple myeloma [2A83] [16]
Thalidomide DM70BU5 Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Thalidomide. Multiple myeloma [2A83] [16]
Elotuzumab DMEYHG9 Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Elotuzumab. Multiple myeloma [2A83] [16]
Coadministration of a Drug Treating the Disease Different from Bortezomib (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Bortezomib and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [17]
Metreleptin DM1NOEK Minor Increased metabolism of Bortezomib caused by Metreleptin mediated induction of CYP450 enzyme. Acute diabete complication [5A2Y] [18]
Thioguanine DM7NKEV Moderate Increased risk of hepatotoxicity by the combination of Bortezomib and Thioguanine. Acute myeloid leukaemia [2A60] [19]
Ivosidenib DM8S6T7 Minor Increased metabolism of Bortezomib caused by Ivosidenib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [18]
Arn-509 DMT81LZ Major Increased metabolism of Bortezomib caused by Arn-509 mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [18]
Mitotane DMU1GX0 Major Increased metabolism of Bortezomib caused by Mitotane mediated induction of CYP450 enzyme. Adrenal cancer [2D11] [18]
Metronidazole DMTIVEN Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Metronidazole. Amoebiasis [1A36] [16]
Bedaquiline DM3906J Moderate Increased risk of hepatotoxicity by the combination of Bortezomib and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [20]
Butalbital DM9J04X Minor Increased metabolism of Bortezomib caused by Butalbital mediated induction of CYP450 enzyme. Anxiety disorder [6B00-6B0Z] [18]
Methylphenobarbital DMDSWAG Minor Increased metabolism of Bortezomib caused by Methylphenobarbital mediated induction of CYP450 enzyme. Anxiety disorder [6B00-6B0Z] [18]
Clobazam - Lundbeck DMW1OQ0 Minor Decreased metabolism of Bortezomib caused by Clobazam - Lundbeck mediated inhibition of CYP450 enzyme. Anxiety disorder [6B00-6B0Z] [21]
Cilostazol DMZMSCT Moderate Decreased metabolism of Bortezomib caused by Cilostazol mediated inhibition of CYP450 enzyme. Arterial occlusive disease [BD40] [22]
Voriconazole DMAOL2S Moderate Decreased metabolism of Bortezomib caused by Voriconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [23]
Posaconazole DMUL5EW Moderate Decreased metabolism of Bortezomib caused by Posaconazole mediated inhibition of CYP450 enzyme. Aspergillosis [1F20] [23]
Zafirlukast DMHNQOG Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Zafirlukast. Asthma [CA23] [16]
Roflumilast DMPGHY8 Moderate Additive immunosuppressive effects by the combination of Bortezomib and Roflumilast. Asthma [CA23] [18]
Oritavancin DM28D05 Minor Increased metabolism of Bortezomib caused by Oritavancin mediated induction of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [18]
Tindamax DM3OWT4 Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Tindamax. Bacterial infection [1A00-1C4Z] [16]
Erythromycin DM4K7GQ Moderate Decreased metabolism of Bortezomib caused by Erythromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [23]
Clarithromycin DM4M1SG Moderate Decreased metabolism of Bortezomib caused by Clarithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [23]
Chloramphenicol DMFXEWT Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Chloramphenicol. Bacterial infection [1A00-1C4Z] [16]
Linezolid DMGFPU2 Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Linezolid. Bacterial infection [1A00-1C4Z] [16]
Troleandomycin DMUZNIG Moderate Decreased metabolism of Bortezomib caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [23]
Telithromycin DMZ4P3A Moderate Decreased metabolism of Bortezomib caused by Telithromycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [23]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Bortezomib and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [24]
Eribulin DM1DX4Q Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Eribulin. Breast cancer [2C60-2C6Y] [16]
Ixabepilone DM2OZ3G Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Ixabepilone. Breast cancer [2C60-2C6Y] [16]
Tucatinib DMBESUA Moderate Decreased metabolism of Bortezomib caused by Tucatinib mediated inhibition of CYP450 enzyme. Breast cancer [2C60-2C6Y] [23]
Alpelisib DMEXMYK Moderate Increased metabolism of Bortezomib caused by Alpelisib mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [25]
Cabazitaxel DMPAZHC Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Cabazitaxel. Breast cancer [2C60-2C6Y] [16]
Trastuzumab Emtansine DMU1LXS Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Trastuzumab Emtansine. Breast cancer [2C60-2C6Y] [16]
Atorvastatin DMF28YC Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Atorvastatin. Cardiovascular disease [BA00-BE2Z] [16]
Secobarbital DM14RF5 Minor Increased metabolism of Bortezomib caused by Secobarbital mediated induction of CYP450 enzyme. Chronic insomnia [7A00] [18]
Phenylbutazone DMAYL0T Minor Increased metabolism of Bortezomib caused by Phenylbutazone mediated induction of CYP450 enzyme. Chronic pain [MG30] [18]
Oxaliplatin DMQNWRD Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Oxaliplatin. Colorectal cancer [2B91] [16]
Mifepristone DMGZQEF Moderate Decreased metabolism of Bortezomib caused by Mifepristone mediated inhibition of CYP450 enzyme. Cushing syndrome [5A70] [17]
Lumacaftor DMCLWDJ Major Increased metabolism of Bortezomib caused by Lumacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [23]
Nefazodone DM4ZS8M Moderate Decreased metabolism of Bortezomib caused by Nefazodone mediated inhibition of CYP450 enzyme. Depression [6A70-6A7Z] [23]
Griseofulvin DMK54YG Minor Increased metabolism of Bortezomib caused by Griseofulvin mediated induction of CYP450 enzyme. Dermatophytosis [1F28] [18]
PMID28454500-Compound-96 DM2A75P Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and PMID28454500-Compound-96. Discovery agent [N.A.] [16]
Citalopram derivative 1 DMITX1G Minor Decreased metabolism of Bortezomib caused by Citalopram derivative 1 mediated inhibition of CYP450 enzyme. Discovery agent [N.A.] [21]
Diazepam DM08E9O Minor Decreased metabolism of Bortezomib caused by Diazepam mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [21]
Primidone DM0WX6I Major Increased metabolism of Bortezomib caused by Primidone mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [18]
Felbamate DM1V5ZS Minor Increased metabolism of Bortezomib caused by Felbamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [18]
Oxcarbazepine DM5PU6O Minor Increased metabolism of Bortezomib caused by Oxcarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [18]
Mephenytoin DM5UGDK Minor Decreased metabolism of Bortezomib caused by Mephenytoin mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [21]
Valproate DMCFE9I Minor Decreased metabolism of Bortezomib caused by Valproate mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [26]
Cenobamate DM8KLU9 Minor Increased metabolism of Bortezomib caused by Cenobamate mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [18]
Stiripentol DMMSDOY Moderate Decreased metabolism of Bortezomib caused by Stiripentol mediated inhibition of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [27]
Fosphenytoin DMOX3LB Major Increased metabolism of Bortezomib caused by Fosphenytoin mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [18]
Rufinamide DMWE60C Minor Increased metabolism of Bortezomib caused by Rufinamide mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [18]
Phenobarbital DMXZOCG Major Increased metabolism of Bortezomib caused by Phenobarbital mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [18]
Carbamazepine DMZOLBI Major Increased metabolism of Bortezomib caused by Carbamazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [18]
Eslicarbazepine DMZREFQ Minor Increased metabolism of Bortezomib caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [18]
Tazemetostat DMWP1BH Minor Increased metabolism of Bortezomib caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [18]
Itraconazole DMCR1MV Moderate Decreased metabolism of Bortezomib caused by Itraconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [23]
Terbinafine DMI6HUW Minor Decreased metabolism of Bortezomib caused by Terbinafine mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [21]
Clotrimazole DMMFCIH Moderate Decreased metabolism of Bortezomib caused by Clotrimazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [23]
Ketoconazole DMPZI3Q Moderate Decreased metabolism of Bortezomib caused by Ketoconazole mediated inhibition of CYP450 enzyme. Fungal infection [1F29-1F2F] [23]
Omeprazole DM471KJ Minor Decreased metabolism of Bortezomib caused by Omeprazole mediated inhibition of CYP450 enzyme. Gastro-oesophageal reflux disease [DA22] [21]
Pantoprazole DMSVOCZ Minor Decreased metabolism of Bortezomib caused by Pantoprazole mediated inhibition of CYP450 enzyme. Gastro-oesophageal reflux disease [DA22] [21]
Colchicine DM2POTE Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Colchicine. Gout [FA25] [16]
Sulfinpyrazone DMEV954 Minor Increased metabolism of Bortezomib caused by Sulfinpyrazone mediated induction of CYP450 enzyme. Gout [FA25] [18]
Boceprevir DMBSHMF Moderate Decreased metabolism of Bortezomib caused by Boceprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [23]
Telaprevir DMMRV29 Moderate Decreased metabolism of Bortezomib caused by Telaprevir mediated inhibition of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [23]
Telbivudine DMSWUGE Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Telbivudine. Hepatitis virus infection [1E50-1E51] [16]
Isoniazid DM5JVS3 Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Isoniazid. HIV-infected patients with tuberculosis [1B10-1B14] [16]
Rifampin DMA8J1G Major Increased metabolism of Bortezomib caused by Rifampin mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [23]
Rifapentine DMCHV4I Major Increased metabolism of Bortezomib caused by Rifapentine mediated induction of CYP450 enzyme. HIV-infected patients with tuberculosis [1B10-1B14] [18]
Brentuximab vedotin DMWLC57 Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Brentuximab vedotin. Hodgkin lymphoma [2B30] [28]
Indinavir DM0T3YH Moderate Decreased metabolism of Bortezomib caused by Indinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [23]
Delavirdine DM3NF5G Moderate Decreased metabolism of Bortezomib caused by Delavirdine mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [23]
Fosamprenavir DM4W9B3 Moderate Decreased metabolism of Bortezomib caused by Fosamprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [23]
Stavudine DM6DEK9 Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Stavudine. Human immunodeficiency virus disease [1C60-1C62] [16]
Nevirapine DM6HX9B Minor Increased metabolism of Bortezomib caused by Nevirapine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [18]
Cobicistat DM6L4H2 Moderate Decreased metabolism of Bortezomib caused by Cobicistat mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [23]
Efavirenz DMC0GSJ Minor Increased metabolism of Bortezomib caused by Efavirenz mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [18]
Saquinavir DMG814N Moderate Decreased metabolism of Bortezomib caused by Saquinavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [23]
Etravirine DMGV8QU Minor Increased metabolism of Bortezomib caused by Etravirine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [18]
Zalcitabine DMH7MUV Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Zalcitabine. Human immunodeficiency virus disease [1C60-1C62] [16]
Didanosine DMI2QPE Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Didanosine. Human immunodeficiency virus disease [1C60-1C62] [16]
Amprenavir DMLMXE0 Moderate Decreased metabolism of Bortezomib caused by Amprenavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [23]
Atazanavir DMSYRBX Moderate Decreased metabolism of Bortezomib caused by Atazanavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [23]
Ritonavir DMU764S Moderate Decreased metabolism of Bortezomib caused by Ritonavir mediated inhibition of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [23]
Fluvastatin DM4MDJY Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Fluvastatin. Hyper-lipoproteinaemia [5C80] [16]
Lovastatin DM9OZWQ Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Lovastatin. Hyper-lipoproteinaemia [5C80] [16]
Mipomersen DMGSRN1 Major Increased risk of hepatotoxicity by the combination of Bortezomib and Mipomersen. Hyper-lipoproteinaemia [5C80] [29]
Rosuvastatin DMMIQ7G Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Rosuvastatin. Hyper-lipoproteinaemia [5C80] [16]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Bortezomib and BMS-201038. Hyper-lipoproteinaemia [5C80] [30]
Hydralazine DMU8JGH Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Hydralazine. Hypertension [BA00-BA04] [16]
Conivaptan DM1V329 Moderate Decreased metabolism of Bortezomib caused by Conivaptan mediated inhibition of CYP450 enzyme. Hypo-osmolality/hyponatraemia [5C72] [31]
Pirfenidone DM6VZFQ Minor Decreased metabolism of Bortezomib caused by Pirfenidone mediated inhibition of CYP450 enzyme. Idiopathic interstitial pneumonitis [CB03] [21]
Lesinurad DMUR64T Minor Increased metabolism of Bortezomib caused by Lesinurad mediated induction of CYP450 enzyme. Inborn purine/pyrimidine/nucleotide metabolism error [5C55] [18]
Auranofin DMWE2N4 Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Auranofin. Inflammatory arthropathy [FA2Z] [16]
Amobarbital DM0GQ8N Minor Increased metabolism of Bortezomib caused by Amobarbital mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [18]
Butabarbital DMC5AST Minor Increased metabolism of Bortezomib caused by Butabarbital mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [18]
Pentobarbital DMFNH7L Minor Increased metabolism of Bortezomib caused by Pentobarbital mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [18]
Quazepam DMY4D87 Minor Decreased metabolism of Bortezomib caused by Quazepam mediated inhibition of CYP450 enzyme. Insomnia [7A00-7A0Z] [21]
Nelarabine DMB6VEG Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Nelarabine. Leukaemia [2A60-2B33] [16]
Glycerol phenylbutyrate DMDGRQO Moderate Decreased metabolism of Bortezomib caused by Glycerol phenylbutyrate mediated inhibition of CYP450 enzyme. Liver disease [DB90-DB9Z] [18]
Denosumab DMNI0KO Moderate Additive myelosuppressive effects by the combination of Bortezomib and Denosumab. Low bone mass disorder [FB83] [32]
Brigatinib DM7W94S Minor Increased metabolism of Bortezomib caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [18]
Ceritinib DMB920Z Moderate Decreased metabolism of Bortezomib caused by Ceritinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [23]
PF-06463922 DMKM7EW Moderate Increased metabolism of Bortezomib caused by PF-06463922 mediated induction of CYP450 enzyme. Lung cancer [2C25] [17]
Osimertinib DMRJLAT Minor Increased metabolism of Bortezomib caused by Osimertinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [18]
Selpercatinib DMZR15V Moderate Decreased metabolism of Bortezomib caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [33]
Chloroquine DMSI5CB Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Chloroquine. Malaria [1F40-1F45] [16]
Hydroxychloroquine DMSIVND Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Hydroxychloroquine. Malaria [1F40-1F45] [16]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Bortezomib and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [34]
Cladribine DM3JDRP Major Additive myelosuppressive effects by the combination of Bortezomib and Cladribine. Mature B-cell leukaemia [2A82] [18]
Idelalisib DM602WT Moderate Increased risk of hepatotoxicity by the combination of Bortezomib and Idelalisib. Mature B-cell leukaemia [2A82] [35]
Clofarabine DMCVJ86 Moderate Increased risk of hepatotoxicity by the combination of Bortezomib and Clofarabine. Mature B-cell lymphoma [2A85] [36]
Vincristine DMINOX3 Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Vincristine. Mature B-cell lymphoma [2A85] [16]
Teniposide DMLW57T Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Teniposide. Mature B-cell lymphoma [2A85] [16]
Ponatinib DMYGJQO Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Ponatinib. Mature B-cell lymphoma [2A85] [16]
Vemurafenib DM62UG5 Minor Increased metabolism of Bortezomib caused by Vemurafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [18]
Ipilimumab DMJTIYK Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Ipilimumab. Melanoma [2C30] [16]
Dabrafenib DMX6OE3 Minor Increased metabolism of Bortezomib caused by Dabrafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [18]
Propranolol DM79NTF Minor Decreased metabolism of Bortezomib caused by Propranolol mediated inhibition of CYP450 enzyme. Migraine [8A80] [21]
Exjade DMHPRWG Minor Increased metabolism of Bortezomib caused by Exjade mediated induction of CYP450 enzyme. Mineral absorption/transport disorder [5C64] [18]
Flibanserin DM70DTN Minor Decreased metabolism of Bortezomib caused by Flibanserin mediated inhibition of CYP450 enzyme. Mood disorder [6A60-6E23] [21]
Tecfidera DM2OVDT Moderate Additive immunosuppressive effects by the combination of Bortezomib and Tecfidera. Multiple sclerosis [8A40] [37]
Siponimod DM2R86O Major Additive immunosuppressive effects by the combination of Bortezomib and Siponimod. Multiple sclerosis [8A40] [17]
Fingolimod DM5JVAN Major Additive immunosuppressive effects by the combination of Bortezomib and Fingolimod. Multiple sclerosis [8A40] [38]
Ocrelizumab DMEZ2KH Moderate Additive immunosuppressive effects by the combination of Bortezomib and Ocrelizumab. Multiple sclerosis [8A40] [39]
Ozanimod DMT6AM2 Major Additive immunosuppressive effects by the combination of Bortezomib and Ozanimod. Multiple sclerosis [8A40] [18]
Carisoprodol DMWR1JC Minor Decreased metabolism of Bortezomib caused by Carisoprodol mediated inhibition of CYP450 enzyme. Musculoskeletal disorder [FA00-FC0Z] [21]
Rifabutin DM1YBHK Major Increased metabolism of Bortezomib caused by Rifabutin mediated induction of CYP450 enzyme. Mycobacterium infection [1B10-1B21] [18]
Bexarotene DMOBIKY Minor Increased metabolism of Bortezomib caused by Bexarotene mediated induction of CYP450 enzyme. Mycosis fungoides [2B01] [18]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Bortezomib caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [18]
Nilotinib DM7HXWT Moderate Decreased metabolism of Bortezomib caused by Nilotinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [40]
Omacetaxine mepesuccinate DMPU2WX Moderate Additive myelosuppressive effects by the combination of Bortezomib and Omacetaxine mepesuccinate. Myeloproliferative neoplasm [2A20] [41]
Modafinil DMYILBE Minor Increased metabolism of Bortezomib caused by Modafinil mediated induction of CYP450 enzyme. Narcolepsy [7A20] [18]
Carboplatin DMG281S Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Carboplatin. Ovarian cancer [2C73] [16]
Levodopa DMN3E57 Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Levodopa. Parkinsonism [8A00] [16]
Abametapir DM2RX0I Moderate Decreased metabolism of Bortezomib caused by Abametapir mediated inhibition of CYP450 enzyme. Pediculosis [1G00] [42]
Esomeprazole DM7BN0X Minor Decreased metabolism of Bortezomib caused by Esomeprazole mediated inhibition of CYP450 enzyme. Peptic ulcer [DA61] [21]
Dapsone DM4LT8A Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Dapsone. Pneumonia [CA40] [16]
Lonafarnib DMGM2Z6 Moderate Decreased metabolism of Bortezomib caused by Lonafarnib mediated inhibition of CYP450 enzyme. Premature ageing appearance [LD2B] [23]
Enzalutamide DMGL19D Major Increased metabolism of Bortezomib caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [18]
Bosentan DMIOGBU Minor Increased metabolism of Bortezomib caused by Bosentan mediated induction of CYP450 enzyme. Pulmonary hypertension [BB01] [18]
Tocilizumab DM7J6OR Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Tocilizumab. Rheumatoid arthritis [FA20] [16]
Canakinumab DM8HLO5 Moderate Additive immunosuppressive effects by the combination of Bortezomib and Canakinumab. Rheumatoid arthritis [FA20] [43]
Rilonacept DMGLUQS Moderate Additive immunosuppressive effects by the combination of Bortezomib and Rilonacept. Rheumatoid arthritis [FA20] [43]
Golimumab DMHZV7X Major Additive immunosuppressive effects by the combination of Bortezomib and Golimumab. Rheumatoid arthritis [FA20] [44]
Dexamethasone DMMWZET Minor Increased metabolism of Bortezomib caused by Dexamethasone mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [18]
Nafcillin DMN9RPO Minor Increased metabolism of Bortezomib caused by Nafcillin mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [18]
Leflunomide DMR8ONJ Major Additive immunosuppressive effects by the combination of Bortezomib and Leflunomide. Rheumatoid arthritis [FA20] [45]
Anthrax vaccine DM9GSWY Moderate Antagonize the effect of Bortezomib when combined with Anthrax vaccine. Sepsis [1G40-1G41] [46]
Telotristat ethyl DMDIYFZ Moderate Increased metabolism of Bortezomib caused by Telotristat ethyl mediated induction of CYP450 enzyme. Small intestine developmental anomaly [DA90] [18]
Vinblastine DM5TVS3 Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Vinblastine. Solid tumour/cancer [2A00-2F9Z] [16]
Docetaxel DMDI269 Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Docetaxel. Solid tumour/cancer [2A00-2F9Z] [16]
Trabectedin DMG3Y89 Moderate Increased risk of hepatotoxicity by the combination of Bortezomib and Trabectedin. Solid tumour/cancer [2A00-2F9Z] [18]
Armodafinil DMGB035 Minor Increased metabolism of Bortezomib caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [18]
Etoposide DMNH3PG Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Etoposide. Solid tumour/cancer [2A00-2F9Z] [16]
Epirubicin DMPDW6T Moderate Increased risk of hepatotoxicity by the combination of Bortezomib and Epirubicin. Solid tumour/cancer [2A00-2F9Z] [17]
Cisplatin DMRHGI9 Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Cisplatin. Solid tumour/cancer [2A00-2F9Z] [16]
Taxol DMUOT9V Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Taxol. Solid tumour/cancer [2A00-2F9Z] [16]
Vinorelbine DMVXFYE Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Vinorelbine. Solid tumour/cancer [2A00-2F9Z] [16]
Disulfiram DMCL2OK Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Disulfiram. Substance abuse [6C40] [16]
Naltrexone DMUL45H Moderate Increased risk of hepatotoxicity by the combination of Bortezomib and Naltrexone. Substance abuse [6C40] [47]
Warfarin DMJYCVW Minor Decreased metabolism of Bortezomib caused by Warfarin mediated inhibition of CYP450 enzyme. Supraventricular tachyarrhythmia [BC81] [21]
Anagrelide DMSQ8MD Moderate Decreased metabolism of Bortezomib caused by Anagrelide mediated inhibition of CYP450 enzyme. Thrombocytosis [3B63] [17]
Clopidogrel DMOL54H Moderate Decreased metabolism of Bortezomib caused by Clopidogrel mediated inhibition of CYP450 enzyme. Thrombosis [DB61-GB90] [48]
Azathioprine DMMZSXQ Moderate Additive myelosuppressive effects by the combination of Bortezomib and Azathioprine. Transplant rejection [NE84] [17]
Ethambutol DMR87LC Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Ethambutol. Tuberculosis [1B10-1B12] [16]
Nitrofurantoin DM7PQIK Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Nitrofurantoin. Urinary tract infection [GC08] [16]
Elagolix DMB2C0E Minor Increased metabolism of Bortezomib caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [18]
Secnidazole DMJ18YL Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Secnidazole. Vaginal discharge [MF3A] [16]
Amiodarone DMUTEX3 Moderate Increased risk of peripheral neuropathy by the combination of Bortezomib and Amiodarone. Ventricular tachyarrhythmia [BC71] [16]
Valganciclovir DMS2IUH Moderate Additive myelosuppressive effects by the combination of Bortezomib and Valganciclovir. Virus infection [1A24-1D9Z] [17]
⏷ Show the Full List of 171 DDI Information of This Drug

References

1 Bortezomib FDA Label
2 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
3 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6391).
4 FDA Approved Drug Products: Bortezomib for Injection, for subcutaneous or intravenous use
5 BDDCS applied to over 900 drugs
6 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
7 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
8 Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin. J Med Chem. 1995 Apr 28;38(9):1511-22.
9 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
10 CNS uptake of bortezomib is enhanced by P-glycoprotein inhibition: implications for spinal muscular atrophy. Neurobiol Dis. 2016 Apr;88:118-24.
11 Relative contributions of the five major human cytochromes P450, 1A2, 2C9, 2C19, 2D6, and 3A4, to the hepatic metabolism of the proteasome inhibitor bortezomib. Drug Metab Dispos. 2005 Nov;33(11):1723-8.
12 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
13 Investigation of drug-drug interaction potential of bortezomib in vivo in female Sprague-Dawley rats and in vitro in human liver microsomes. Drug Metab Dispos. 2006 Apr;34(4):702-8.
14 Human metabolism of the proteasome inhibitor bortezomib: identification of circulating metabolites. Drug Metab Dispos. 2005 Jun;33(6):771-7.
15 The proapoptotic effect of zoledronic acid is independent of either the bone microenvironment or the intrinsic resistance to bortezomib of myeloma cells and is enhanced by the combination with arsenic trioxide. Exp Hematol. 2011 Jan;39(1):55-65.
16 Argov Z, Mastaglia FL "Drug-induced peripheral neuropathies." Br Med J 1 (1979): 663-6. [PMID: 219931]
17 Cerner Multum, Inc. "Australian Product Information.".
18 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
19 Product Information. Aubagio (teriflunomide). Genzyme Corporation, Cambridge, MA.
20 Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
21 Product Information. Velcade (bortezomib). Millennium Pharmaceuticals Inc, Cambridge, MA.
22 Hedaya MA, El-Afify DR, El-Maghraby GM "The effect of ciprofloxacin and clarithromycin on sildenafil oral bioavailability in human volunteers." Biopharm Drug Dispos 27 (2006): 103-10. [PMID: 16372380]
23 Pekol T, Daniels JS, Labutti J, et al "Human metabolism of the proteasome inhibitor bortezomib: identification of circulating metabolites." Drug Metab Dispos 33 (2005): 771-7. [PMID: 15764713]
24 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
25 Product Information. Piqray (alpelisib). Novartis Pharmaceuticals, East Hanover, NJ.
26 Bodiford AB, Kessler FO, Fermo JD, Ragucci KR "Elevated international normalized ratio with the consumption of grapefruit and use of warfarin." SAGE Open Med Case Rep 0 (2013): 1-3. [PMID: 27489634]
27 EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports.".
28 Product Information. Accolate (zafirlukast). Zeneca Pharmaceuticals, Wilmington, DE.
29 Product Information. Kynamro (mipomersen). Genzyme Corporation, Cambridge, MA.
30 Product Information. Juxtapid (lomitapide). Aegerion Pharmaceuticals Inc, Cambridge, MA.
31 Product Information. Vaprisol (conivaptan). Cumberland Pharmaceuticals Inc, Nashville, TN.
32 Product Information. Prolia (denosumab). Amgen USA, Thousand Oaks, CA.
33 Product Information. Retevmo (selpercatinib). Lilly, Eli and Company, Indianapolis, IN.
34 Al-Nawakil C, Willems L, Mauprivez C, et.al "Successful treatment of l-asparaginase-induced severe acute hepatotoxicity using mitochondrial cofactors." Leuk Lymphoma 55 (2014): 1670-4. [PMID: 24090500]
35 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
36 Product Information. Clolar (clofarabine). sanofi-aventis, Bridgewater, NJ.
37 Product Information. Vumerity (diroximel fumarate). Alkermes, Inc, Cambridge, MA.
38 Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
39 Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA.
40 Product Information. Tasigna (nilotinib). Novartis Pharmaceuticals, East Hanover, NJ.
41 Product Information. Synribo (omacetaxine). Teva Pharmaceuticals USA, North Wales, PA.
42 Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
43 Product Information. Arcalyst (rilonacept). Regeneron Pharmaceuticals Inc, Tarrytown, NY.
44 Product Information. Cimzia (certolizumab). UCB Pharma Inc, Smyrna, GA.
45 Product Information. Arava (leflunomide). Hoechst Marion-Roussel Inc, Kansas City, MO.
46 CDC. Centers for Disease Control and Prevention/ "Recommendations of the advisory committtee on immunization practices (ACIP): use of vaccines and immune globulins in persons with altered immunocompetence." MMWR Morb Mortal Wkly Rep 42(RR-04) (1993): 1-18. [PMID: 20300058]
47 Product Information. ReVia (naltrexone). DuPont Pharmaceuticals, Wilmington, DE.
48 Collet JP, Hulot JS, Pena A, et al. "Cytochrome P450 2C19 polymorphism in young patients treated with clopidogrel after myocardial infarction: a cohort study." Lancet 373 (2009): 309-17. [PMID: 19108880]