bortezomib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
proteasome inhibitors 391 179324-69-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • LDP-341
  • PS-341
  • bortezomib
  • velcade
  • radiciol
A pyrazine and boronic acid derivative that functions as a reversible PROTEASOME INHIBITOR. It is used as an ANTINEOPLASTIC AGENT in the treatment of MULTIPLE MYELOMA and MANTLE CELL LYMPHOMA.
  • Molecular weight: 384.24
  • Formula: C19H25BN4O4
  • CLOGP: 0.78
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 4
  • TPSA: 124.44
  • ALOGS: -3.86
  • ROTB: 9

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 3.30 mg/mL Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.08 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 10 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 19 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.17 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 18 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 14, 2019 EMA FRESENIUS KABI DEUTSCHLAND GMBH
Aug. 22, 2019 PMDA Janssen Pharmaceutical K.K.
May 13, 2003 FDA MILLENNIUM PHARMS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Neuropathy peripheral 2838.08 35.17 714 7075 10718 2339578
Plasma cell myeloma 2703.47 35.17 643 7146 7490 2342806
Thrombocytopenia 1122.30 35.17 393 7396 18738 2331558
Diarrhoea 1088.21 35.17 591 7198 82973 2267323
Disease progression 1078.91 35.17 371 7418 16724 2333572
Pneumonia 951.87 35.17 456 7333 48840 2301456
Platelet count decreased 926.87 35.17 325 7464 15488 2334808
Pyrexia 771.43 35.17 407 7382 53301 2296995
Sepsis 686.19 35.17 272 7517 18216 2332080
Anaemia 645.40 35.17 314 7475 34478 2315818
Vomiting 588.62 35.17 378 7411 71224 2279072
Nausea 583.89 35.17 447 7342 111742 2238554
Neutropenia 508.45 35.17 230 7559 21318 2328978
Dehydration 491.51 35.17 227 7562 22068 2328228
Constipation 479.19 35.17 221 7568 21408 2328888
Plasma cell myeloma recurrent 477.16 35.17 90 7699 275 2350021
Hypotension 469.83 35.17 248 7541 32188 2318108
Fatigue 461.66 35.17 348 7441 84525 2265771
Febrile neutropenia 434.15 35.17 169 7620 10713 2339583
Acute kidney injury 418.31 35.17 219 7570 27903 2322393
Herpes zoster 409.12 35.17 157 7632 9568 2340728
Pancytopenia 394.53 35.17 160 7629 11292 2339004
White blood cell count decreased 390.38 35.17 182 7607 18026 2332270
Asthenia 377.22 35.17 245 7544 46681 2303615
Plasmacytoma 355.94 35.17 71 7718 313 2349983
Off label use 324.13 35.17 267 7522 73331 2276965
Haemoglobin decreased 323.83 35.17 160 7629 17991 2332305
Septic shock 318.54 35.17 120 7669 6934 2343362
Pleural effusion 317.90 35.17 138 7651 11530 2338766
Atrial fibrillation 314.79 35.17 144 7645 13624 2336672
Hyponatraemia 309.78 35.17 141 7648 13184 2337112
Dyspnoea 300.27 35.17 263 7526 78470 2271826
Hypokalaemia 296.72 35.17 128 7661 10526 2339770
Neutrophil count decreased 283.05 35.17 108 7681 6459 2343837
Tumour lysis syndrome 278.19 35.17 70 7719 1005 2349291
Renal failure 277.27 35.17 142 7647 17207 2333089
Malignant neoplasm progression 271.36 35.17 125 7664 12003 2338293
Oedema peripheral 264.40 35.17 153 7636 23610 2326686
Orthostatic hypotension 258.86 35.17 82 7707 2797 2347499
Syncope 254.89 35.17 133 7656 16742 2333554
Infection 249.41 35.17 134 7655 17895 2332401
Rash 226.62 35.17 199 7590 59359 2290937
Decreased appetite 224.52 35.17 148 7641 28743 2321553
Product use in unapproved indication 221.36 35.17 106 7683 11094 2339202
Posterior reversible encephalopathy syndrome 216.18 35.17 69 7720 2411 2347885
Abdominal pain 212.66 35.17 153 7636 34221 2316075
Respiratory failure 205.26 35.17 107 7682 13421 2336875
Polyneuropathy 204.19 35.17 61 7728 1702 2348594
Plasma cell leukaemia 201.83 35.17 39 7750 140 2350156
Colitis 196.93 35.17 78 7711 5148 2345148
Hypoaesthesia 192.96 35.17 118 7671 20097 2330199
Urinary tract infection 191.39 35.17 136 7653 29806 2320490
Dizziness 189.69 35.17 179 7610 58486 2291810
Back pain 189.11 35.17 138 7651 31521 2318775
Peripheral sensory neuropathy 188.76 35.17 51 7738 979 2349317
Bone marrow failure 177.01 35.17 74 7715 5612 2344684
Drug ineffective 175.96 35.17 223 7566 101401 2248895
Myelodysplastic syndrome 173.90 35.17 59 7730 2501 2347795
Multiple organ dysfunction syndrome 171.52 35.17 79 7710 7562 2342734
Blood lactate dehydrogenase increased 170.76 35.17 63 7726 3421 2346875
Confusional state 168.14 35.17 116 7673 24228 2326068
Death 167.28 35.17 195 7594 81273 2269023
Cardiac failure 164.59 35.17 89 7700 12005 2338291
Deep vein thrombosis 161.74 35.17 90 7699 12842 2337454
Mucosal inflammation 159.29 35.17 67 7722 5157 2345139
Blood creatinine increased 153.11 35.17 81 7708 10452 2339844
Hypoxia 151.15 35.17 68 7721 6159 2344137
General physical health deterioration 148.98 35.17 88 7701 14051 2336245
Inappropriate antidiuretic hormone secretion 148.17 35.17 51 7738 2258 2348038
Lung disorder 148.13 35.17 67 7722 6145 2344151
Electrolyte imbalance 146.45 35.17 49 7740 1988 2348308
Haematotoxicity 137.81 35.17 41 7748 1126 2349170
Atelectasis 136.25 35.17 46 7743 1919 2348377
Hypercalcaemia 134.90 35.17 49 7740 2543 2347753
Cardiac failure congestive 130.99 35.17 85 7704 16016 2334280
Renal impairment 130.99 35.17 72 7717 10020 2340276
Respiratory tract infection 130.64 35.17 54 7735 3975 2346321
Haematocrit decreased 130.35 35.17 55 7734 4263 2346033
Chest pain 125.01 35.17 103 7686 28034 2322262
Muscular weakness 122.05 35.17 79 7710 14818 2335478
Fall 119.24 35.17 126 7663 46973 2303323
Hypoalbuminaemia 118.22 35.17 38 7751 1356 2348940
Pulmonary oedema 116.62 35.17 60 7729 7303 2342993
Paraesthesia 115.49 35.17 89 7700 21999 2328297
Aspartate aminotransferase increased 113.55 35.17 71 7718 12541 2337755
Lower respiratory tract infection 112.13 35.17 53 7736 5371 2344925
Weight decreased 111.91 35.17 97 7692 28274 2322022
Pain 107.03 35.17 136 7653 61721 2288575
Hypocalcaemia 105.79 35.17 46 7743 3837 2346459
Therapy non-responder 105.65 35.17 58 7731 8046 2342250
Cytomegalovirus infection 103.92 35.17 41 7748 2672 2347624
Stem cell transplant 99.41 35.17 25 7764 357 2349939
Pulmonary embolism 99.20 35.17 75 7714 18008 2332288
C-reactive protein increased 99.13 35.17 51 7738 6204 2344092
Pneumonia fungal 99.02 35.17 25 7764 363 2349933
Product use issue 98.34 35.17 64 7725 12105 2338191
Condition aggravated 96.25 35.17 94 7695 31885 2318411
Autonomic neuropathy 95.20 35.17 20 7769 119 2350177
Alanine aminotransferase increased 94.72 35.17 66 7723 13966 2336330
Ileus paralytic 94.12 35.17 28 7761 768 2349528
Cellulitis 93.55 35.17 56 7733 9145 2341151
Chills 93.13 35.17 68 7721 15484 2334812
Neurotoxicity 91.55 35.17 35 7754 2095 2348201
Ileus 90.88 35.17 35 7754 2137 2348159
Hypophosphataemia 90.04 35.17 29 7760 1041 2349255
Bone pain 89.51 35.17 54 7735 8942 2341354
Leukopenia 88.25 35.17 56 7733 10140 2340156
Malaise 87.96 35.17 117 7672 55468 2294828
Chalazion 87.74 35.17 17 7772 62 2350234
Tachycardia 87.66 35.17 67 7722 16342 2333954
Bacteraemia 87.38 35.17 32 7757 1698 2348598
Lung infiltration 85.96 35.17 34 7755 2230 2348066
Hyperglycaemia 83.72 35.17 42 7747 4843 2345453
Hypophagia 82.40 35.17 39 7750 3961 2346335
Peripheral sensorimotor neuropathy 81.60 35.17 18 7771 139 2350157
Amyloidosis 81.40 35.17 20 7769 258 2350038
Staphylococcal infection 80.29 35.17 42 7747 5284 2345012
Cardiomyopathy 78.89 35.17 34 7755 2773 2347523
Blood sodium decreased 78.85 35.17 35 7754 3065 2347231
Neuralgia 78.72 35.17 34 7755 2788 2347508
Peripheral motor neuropathy 77.84 35.17 19 7770 238 2350058
Blood potassium decreased 77.60 35.17 41 7748 5264 2345032
Acute respiratory distress syndrome 76.83 35.17 35 7754 3257 2347039
Acute myeloid leukaemia 76.74 35.17 33 7756 2677 2347619
Cough 73.92 35.17 83 7706 33034 2317262
Pathological fracture 73.69 35.17 26 7763 1238 2349058
Hyperviscosity syndrome 72.93 35.17 14 7775 48 2350248
Pulmonary mycosis 72.26 35.17 16 7773 126 2350170
Metabolic acidosis 70.18 35.17 40 7749 5958 2344338
Blood alkaline phosphatase increased 69.55 35.17 41 7748 6504 2343792
Injection site erythema 69.36 35.17 74 7715 27813 2322483
Hypertension 68.75 35.17 73 7716 27288 2323008
Clostridium difficile colitis 67.82 35.17 28 7761 2051 2348245
Cardiomegaly 67.26 35.17 29 7760 2367 2347929
Lymphopenia 66.59 35.17 29 7760 2425 2347871
Infusion related reaction 65.90 35.17 46 7743 9750 2340546
Hyperkalaemia 65.48 35.17 38 7751 5855 2344441
Enterococcal sepsis 65.47 35.17 15 7774 140 2350156
Large intestinal ulcer perforation 63.59 35.17 10 7779 4 2350292
Myocardial ischaemia 62.26 35.17 27 7762 2235 2348061
Spinal cord compression 61.89 35.17 19 7770 581 2349715
Pneumonitis 61.30 35.17 32 7757 4007 2346289
Hordeolum 61.22 35.17 17 7772 362 2349934
Kaposi's sarcoma 61.01 35.17 16 7773 272 2350024
Pain in extremity 60.34 35.17 85 7704 42455 2307841
Mesenteric abscess 60.03 35.17 10 7779 10 2350286
Loss of consciousness 59.85 35.17 57 7732 18710 2331586
Gastrointestinal fungal infection 59.21 35.17 12 7777 58 2350238
Toxic skin eruption 59.03 35.17 26 7763 2234 2348062
Nasal abscess 58.93 35.17 11 7778 31 2350265
Shock 58.71 35.17 31 7758 3973 2346323
Interstitial lung disease 58.02 35.17 39 7750 7773 2342523
Somnolence 57.82 35.17 62 7727 23423 2326873
Vision blurred 57.44 35.17 50 7739 14618 2335678
Staphylococcal bacteraemia 57.41 35.17 18 7771 591 2349705
Blood calcium decreased 56.92 35.17 25 7764 2133 2348163
Pulmonary hypertension 56.85 35.17 33 7756 5085 2345211
Mental status changes 56.78 35.17 34 7755 5548 2344748
Pneumonia pneumococcal 55.93 35.17 15 7774 279 2350017
Urosepsis 55.68 35.17 24 7765 1957 2348339
Disease recurrence 54.26 35.17 28 7761 3423 2346873
Ejection fraction decreased 53.70 35.17 26 7763 2775 2347521
Dialysis 53.61 35.17 24 7765 2143 2348153
Candida infection 53.07 35.17 26 7763 2847 2347449
Productive cough 53.06 35.17 32 7757 5289 2345007
Oedema 53.00 35.17 41 7748 10162 2340134
Varicella zoster virus infection 53.00 35.17 15 7774 343 2349953
Hypomagnesaemia 52.80 35.17 25 7764 2539 2347757
Clostridium bacteraemia 52.62 35.17 10 7779 32 2350264
Sinus polyp 52.56 35.17 11 7778 64 2350232
Monoclonal immunoglobulin present 52.37 35.17 12 7777 112 2350184
Blood pressure decreased 52.14 35.17 39 7750 9197 2341099
Enterocolitis 51.72 35.17 18 7771 822 2349474
Tremor 51.65 35.17 55 7734 20606 2329690
Respiratory distress 51.54 35.17 31 7758 5098 2345198
Febrile bone marrow aplasia 51.37 35.17 18 7771 839 2349457
Herpes simplex 51.16 35.17 19 7770 1048 2349248
Cardiac amyloidosis 50.69 35.17 11 7778 78 2350218
Tricuspid valve incompetence 49.64 35.17 21 7768 1635 2348661
Oxygen saturation decreased 49.56 35.17 35 7754 7551 2342745
Drug reaction with eosinophilia and systemic symptoms 49.45 35.17 31 7758 5487 2344809
Mucosal erosion 49.13 35.17 13 7776 229 2350067
Supraventricular tachycardia 48.90 35.17 22 7767 1987 2348309
Rash maculo-papular 48.78 35.17 28 7761 4224 2346072
Gastrointestinal haemorrhage 47.90 35.17 42 7747 12393 2337903
Abdominal pain upper 46.90 35.17 54 7735 22046 2328250
Sinusitis 46.72 35.17 47 7742 16479 2333817
Mantle cell lymphoma 46.29 35.17 11 7778 122 2350174
Protein total increased 46.24 35.17 14 7775 408 2349888
Oral fungal infection 46.21 35.17 14 7775 409 2349887
Abdominal distension 45.90 35.17 38 7751 10373 2339923
Toxicity to various agents 45.75 35.17 65 7724 32689 2317607
Atrial flutter 45.22 35.17 18 7771 1199 2349097
Pericardial effusion 44.92 35.17 26 7763 3983 2346313
Insomnia 44.92 35.17 57 7732 25730 2324566
Blood urea increased 44.75 35.17 25 7764 3580 2346716
Performance status decreased 44.63 35.17 15 7774 616 2349680
Urinary retention 44.36 35.17 25 7764 3642 2346654
Blood glucose increased 44.34 35.17 40 7749 12250 2338046
Chronic kidney disease 44.27 35.17 26 7763 4092 2346204
Mitral valve incompetence 43.90 35.17 22 7767 2528 2347768
Neoplasm progression 43.79 35.17 27 7762 4641 2345655
Red blood cell count decreased 43.42 35.17 26 7763 4240 2346056
Dysphagia 42.93 35.17 40 7749 12765 2337531
Gait disturbance 42.74 35.17 52 7737 22493 2327803
Oesophagitis 42.66 35.17 20 7769 1986 2348310
Gastrointestinal disorder 42.37 35.17 34 7755 8883 2341413
Congestive cardiomyopathy 42.00 35.17 16 7773 947 2349349
Therapeutic response decreased 41.99 35.17 31 7758 7164 2343132
Fluid overload 41.91 35.17 22 7767 2784 2347512
Epilepsy 41.41 35.17 26 7763 4613 2345683
Cardiotoxicity 41.37 35.17 17 7772 1230 2349066
Bronchopulmonary aspergillosis 41.35 35.17 16 7773 988 2349308
Asthma 41.16 35.17 37 7752 11277 2339019
Stevens-Johnson syndrome 40.88 35.17 25 7764 4234 2346062
Meningitis cryptococcal 40.79 35.17 11 7778 209 2350087
Acute coronary syndrome 40.72 35.17 18 7771 1559 2348737
Guillain-Barre syndrome 40.13 35.17 14 7775 644 2349652
Erythema 39.74 35.17 53 7736 25106 2325190
Cryptococcosis 39.68 35.17 10 7779 144 2350152
Seizure 39.35 35.17 52 7737 24414 2325882
Hepatitis C 38.77 35.17 17 7772 1444 2348852
Failure to thrive 38.76 35.17 15 7774 927 2349369
Drug intolerance 38.74 35.17 39 7750 13678 2336618
Sinus tachycardia 38.41 35.17 22 7767 3303 2346993
Blood culture positive 38.39 35.17 14 7775 733 2349563
Upper respiratory tract infection 38.38 35.17 32 7757 8819 2341477
Metabolic encephalopathy 38.12 35.17 13 7776 558 2349738
Salmonella sepsis 37.88 35.17 8 7781 49 2350247
Stomatitis 37.80 35.17 33 7756 9677 2340619
Drug resistance 37.57 35.17 20 7769 2604 2347692
Acute respiratory failure 37.52 35.17 21 7768 3017 2347279
Staphylococcal sepsis 36.97 35.17 15 7774 1050 2349246
Immunosuppression 36.92 35.17 15 7774 1054 2349242
Influenza 36.84 35.17 37 7752 12941 2337355
Full blood count decreased 36.83 35.17 22 7767 3571 2346725
Hepatitis B 36.79 35.17 14 7775 826 2349470
Protein urine present 36.50 35.17 13 7776 636 2349660
Skin exfoliation 36.17 35.17 26 7763 5764 2344532
Device related infection 36.15 35.17 21 7768 3238 2347058
Circulatory collapse 36.12 35.17 22 7767 3698 2346598
Haemodialysis 36.06 35.17 18 7771 2051 2348245
Liver disorder 36.00 35.17 27 7762 6387 2343909
Chronic obstructive pulmonary disease 35.79 35.17 28 7761 7049 2343247
Neutropenic sepsis 35.76 35.17 16 7773 1426 2348870
Urinary tract infection bacterial 35.56 35.17 12 7777 499 2349797
Blood albumin decreased 35.42 35.17 17 7772 1778 2348518
Fungal infection 35.32 35.17 24 7765 4865 2345431
Transplant rejection 35.17 35.17 15 7774 1191 2349105

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Neuropathy peripheral 3212.42 32.08 885 9304 8368 1728224
Plasma cell myeloma 2816.21 32.08 813 9376 9201 1727391
Pneumonia 1396.64 32.08 741 9448 45441 1691151
Thrombocytopenia 1352.89 32.08 571 9618 20678 1715914
Disease progression 1124.01 32.08 472 9717 16791 1719801
Platelet count decreased 1025.93 32.08 437 9752 16086 1720506
Pyrexia 945.91 32.08 577 9612 45823 1690769
Diarrhoea 940.94 32.08 607 9582 53245 1683347
Plasma cell myeloma recurrent 588.63 32.08 128 10061 358 1736234
Anaemia 560.71 32.08 352 9837 29105 1707487
Fatigue 539.21 32.08 424 9765 50357 1686235
Sepsis 499.08 32.08 282 9907 19156 1717436
Asthenia 489.51 32.08 344 9845 34326 1702266
Hypotension 489.14 32.08 324 9865 29330 1707262
Neutropenia 479.77 32.08 269 9920 17991 1718601
Constipation 471.78 32.08 249 9940 14751 1721841
Febrile neutropenia 471.70 32.08 226 9963 10874 1725718
Polyneuropathy 460.29 32.08 136 10053 1619 1734973
Off label use 458.79 32.08 345 9844 38226 1698366
Dyspnoea 452.07 32.08 387 9802 51672 1684920
Orthostatic hypotension 442.49 32.08 155 10034 3276 1733316
Tumour lysis syndrome 434.45 32.08 130 10059 1621 1734971
Dehydration 428.36 32.08 247 9942 17411 1719181
Atrial fibrillation 414.09 32.08 229 9960 14882 1721710
Pleural effusion 405.55 32.08 204 9985 10906 1725686
Herpes zoster 381.38 32.08 150 10039 4423 1732169
Acute kidney injury 376.54 32.08 295 9894 34649 1701943
Pancytopenia 375.21 32.08 195 9994 11162 1725430
Renal failure 371.86 32.08 236 9953 19781 1716811
Septic shock 362.20 32.08 171 10018 7938 1728654
Malignant neoplasm progression 348.28 32.08 200 9989 13958 1722634
Haemoglobin decreased 346.03 32.08 213 9976 16901 1719691
Nausea 332.84 32.08 324 9865 50872 1685720
White blood cell count decreased 324.02 32.08 186 10003 12963 1723629
Plasmacytoma 311.42 32.08 77 10112 432 1736160
Infection 304.93 32.08 175 10014 12185 1724407
Respiratory failure 304.50 32.08 185 10004 14320 1722272
Decreased appetite 277.24 32.08 211 9978 23660 1712932
Syncope 265.11 32.08 168 10021 14001 1722591
Vomiting 260.74 32.08 249 9940 38066 1698526
Peripheral sensory neuropathy 248.88 32.08 72 10117 789 1735803
General physical health deterioration 239.03 32.08 153 10036 12965 1723627
Blood creatinine increased 232.90 32.08 154 10035 13792 1722800
Product use in unapproved indication 231.13 32.08 133 10056 9289 1727303
Cardiac failure 224.68 32.08 145 10044 12457 1724135
Oedema peripheral 222.35 32.08 156 10033 15394 1721198
Neutrophil count decreased 219.59 32.08 111 10078 5970 1730622
Hypoaesthesia 215.36 32.08 129 10060 9706 1726886
Drug ineffective 209.63 32.08 284 9905 63517 1673075
Hypercalcaemia 197.09 32.08 73 10116 1813 1734779
Hyponatraemia 196.90 32.08 118 10071 8882 1727710
Ileus paralytic 189.70 32.08 60 10129 907 1735685
Autonomic neuropathy 188.55 32.08 41 10148 114 1736478
Hypoxia 186.94 32.08 99 10090 5864 1730728
Fall 185.01 32.08 177 10012 27037 1709555
Deep vein thrombosis 183.81 32.08 117 10072 9803 1726789
Blood lactate dehydrogenase increased 177.78 32.08 82 10107 3593 1732999
Pulmonary oedema 172.26 32.08 97 10092 6489 1730103
Lung disorder 171.88 32.08 89 10100 5030 1731562
Ileus 171.85 32.08 71 10118 2375 1734217
Myelodysplastic syndrome 170.47 32.08 77 10112 3212 1733380
Paraesthesia 168.53 32.08 113 10076 10338 1726254
Pain in extremity 166.65 32.08 141 10048 18331 1718261
Multiple organ dysfunction syndrome 163.77 32.08 106 10083 9136 1727456
Weight decreased 162.21 32.08 152 10037 22601 1713991
Bone marrow failure 162.03 32.08 86 10103 5114 1731478
Colitis 161.74 32.08 80 10109 4100 1732492
Pulmonary embolism 159.16 32.08 119 10070 12940 1723652
Dizziness 159.08 32.08 182 10007 34179 1702413
Back pain 158.50 32.08 131 10058 16482 1720110
Confusional state 157.17 32.08 145 10044 21133 1715459
Acute myeloid leukaemia 156.98 32.08 71 10118 2970 1733622
Rash 156.10 32.08 191 9998 38502 1698090
Hypokalaemia 148.30 32.08 87 10102 6287 1730305
Infusion related reaction 148.18 32.08 88 10101 6505 1730087
Cytomegalovirus infection 142.20 32.08 68 10121 3233 1733359
Death 140.49 32.08 282 9907 87161 1649431
Renal impairment 138.53 32.08 107 10082 12207 1724385
Pain 138.41 32.08 150 10039 26507 1710085
Plasma cell leukaemia 137.93 32.08 33 10156 157 1736435
Chills 136.83 32.08 104 10085 11583 1725009
Cellulitis 134.16 32.08 82 10107 6386 1730206
Product use issue 127.03 32.08 88 10101 8483 1728109
Muscular weakness 123.94 32.08 93 10096 10156 1726436
Aspartate aminotransferase increased 122.13 32.08 94 10095 10662 1725930
Lower respiratory tract infection 120.81 32.08 64 10125 3787 1732805
Bacteraemia 116.76 32.08 50 10139 1830 1734762
Chest pain 115.63 32.08 119 10070 19795 1716797
Blood urea increased 114.04 32.08 66 10123 4645 1731947
Abdominal pain 113.35 32.08 122 10067 21368 1715224
Enterococcal infection 113.29 32.08 40 10149 861 1735731
Interstitial lung disease 112.84 32.08 86 10103 9610 1726982
Amyloidosis 112.84 32.08 32 10157 324 1736268
Condition aggravated 111.43 32.08 120 10069 21030 1715562
Clostridium difficile colitis 107.39 32.08 45 10144 1559 1735033
Spinal compression fracture 102.99 32.08 37 10152 839 1735753
Neuralgia 102.88 32.08 42 10147 1360 1735232
Atrial flutter 102.29 32.08 46 10143 1896 1734696
Cough 101.24 32.08 109 10080 19088 1717504
Alanine aminotransferase increased 101.02 32.08 89 10100 12189 1724403
Staphylococcal infection 100.98 32.08 61 10128 4646 1731946
Leukopenia 100.39 32.08 76 10113 8404 1728188
Stem cell transplant 100.03 32.08 31 10158 436 1736156
Urinary tract infection 98.68 32.08 81 10108 10072 1726520
Respiratory distress 98.35 32.08 62 10127 5095 1731497
C-reactive protein increased 98.08 32.08 65 10124 5820 1730772
Bone pain 97.39 32.08 53 10136 3309 1733283
Hypoalbuminaemia 94.53 32.08 40 10149 1420 1735172
Therapy non-responder 94.37 32.08 65 10124 6201 1730391
Oxygen saturation decreased 92.93 32.08 62 10127 5613 1730979
Ejection fraction decreased 92.89 32.08 45 10144 2200 1734392
Malaise 92.60 32.08 129 10060 29436 1707156
Pneumonitis 92.50 32.08 54 10135 3861 1732731
Mucosal inflammation 91.94 32.08 55 10134 4114 1732478
Dyspnoea exertional 89.45 32.08 54 10135 4107 1732485
Cardiac failure congestive 88.13 32.08 91 10098 15179 1721413
Herpes zoster disseminated 86.56 32.08 22 10167 140 1736452
Small intestinal obstruction 85.92 32.08 40 10149 1787 1734805
Haematocrit decreased 85.58 32.08 53 10136 4220 1732372
Diverticulitis 85.47 32.08 43 10146 2282 1734310
Hypophosphataemia 85.23 32.08 36 10153 1272 1735320
Blood culture positive 84.40 32.08 31 10158 750 1735842
Rib fracture 84.14 32.08 39 10150 1725 1734867
Acute respiratory distress syndrome 83.94 32.08 49 10140 3502 1733090
Neutropenic sepsis 83.89 32.08 37 10152 1455 1735137
Device related infection 83.22 32.08 42 10147 2244 1734348
Neurotoxicity 82.02 32.08 40 10149 1984 1734608
Hyperglycaemia 78.76 32.08 54 10135 5111 1731481
Cardiac arrest 77.95 32.08 87 10102 15843 1720749
Atelectasis 77.71 32.08 38 10151 1896 1734696
Cardiac amyloidosis 77.65 32.08 19 10170 101 1736491
Basal cell carcinoma 77.10 32.08 41 10148 2442 1734150
Respiratory tract infection 76.95 32.08 41 10148 2452 1734140
Abdominal distension 76.80 32.08 58 10131 6386 1730206
Hypophagia 76.76 32.08 46 10143 3451 1733141
Lung infiltration 76.64 32.08 39 10150 2120 1734472
Cardiomegaly 76.62 32.08 40 10149 2294 1734298
Epistaxis 75.98 32.08 64 10125 8242 1728350
Fluid overload 75.52 32.08 38 10151 2017 1734575
Hiccups 74.65 32.08 34 10155 1443 1735149
Tachycardia 74.19 32.08 76 10113 12552 1724040
Bronchitis 73.99 32.08 53 10136 5379 1731213
Blood alkaline phosphatase increased 73.79 32.08 52 10137 5143 1731449
Hypocalcaemia 73.15 32.08 43 10146 3113 1733479
Bronchopulmonary aspergillosis 72.75 32.08 34 10155 1532 1735060
Bacterial infection 72.33 32.08 36 10153 1866 1734726
Injection site erythema 72.08 32.08 51 10138 5076 1731516
Pneumocystis jirovecii pneumonia 71.91 32.08 39 10150 2417 1734175
Dysphagia 70.51 32.08 67 10122 10101 1726491
Gastrointestinal haemorrhage 68.22 32.08 77 10112 14190 1722402
Loss of consciousness 67.27 32.08 78 10111 14797 1721795
Light chain analysis increased 67.02 32.08 18 10171 146 1736446
Diverticular perforation 66.84 32.08 23 10166 457 1736135
Neurogenic bladder 65.76 32.08 20 10169 263 1736329
Dialysis 64.40 32.08 36 10153 2368 1734224
Mental status changes 64.36 32.08 51 10138 6024 1730568
Lymphopenia 64.34 32.08 34 10155 1999 1734593
Hepatitis B 63.75 32.08 30 10159 1373 1735219
Blood sodium decreased 63.07 32.08 35 10154 2269 1734323
Urinary retention 63.04 32.08 48 10141 5347 1731245
Spinal cord compression 62.62 32.08 24 10165 655 1735937
Insomnia 61.62 32.08 78 10111 16198 1720394
Upper respiratory tract infection 60.53 32.08 42 10147 4051 1732541
Acute respiratory failure 60.21 32.08 37 10152 2903 1733689
Influenza 59.54 32.08 51 10138 6716 1729876
Peripheral sensorimotor neuropathy 58.66 32.08 17 10172 187 1736405
Compression fracture 58.14 32.08 20 10169 397 1736195
Gait inability 58.08 32.08 38 10151 3325 1733267
Failure to thrive 57.62 32.08 26 10163 1079 1735513
Immunosuppression 57.02 32.08 24 10165 840 1735752
Neoplasm progression 56.63 32.08 37 10152 3230 1733362
Pleuritic pain 56.47 32.08 20 10169 434 1736158
Haemodialysis 56.34 32.08 34 10155 2582 1734010
Delirium 56.08 32.08 48 10141 6314 1730278
Oesophagitis 55.40 32.08 29 10160 1672 1734920
Pulmonary fibrosis 55.10 32.08 33 10156 2471 1734121
Hepatic failure 55.03 32.08 46 10143 5857 1730735
Inappropriate antidiuretic hormone secretion 54.65 32.08 29 10160 1719 1734873
Oedema 54.38 32.08 49 10140 6899 1729693
Blood pressure decreased 54.17 32.08 51 10138 7595 1728997
Clostridium difficile infection 54.14 32.08 29 10160 1752 1734840
Lymphocyte count decreased 53.71 32.08 31 10158 2167 1734425
Parainfluenzae virus infection 53.42 32.08 16 10173 199 1736393
Cachexia 53.28 32.08 24 10165 992 1735600
Escherichia sepsis 52.99 32.08 21 10168 628 1735964
Encephalopathy 52.87 32.08 40 10149 4412 1732180
Adenocarcinoma of colon 52.74 32.08 19 10170 434 1736158
Liver disorder 52.71 32.08 44 10145 5592 1731000
Guillain-Barre syndrome 52.48 32.08 23 10166 890 1735702
Peripheral swelling 52.37 32.08 51 10138 7920 1728672
Blood calcium decreased 52.17 32.08 26 10163 1351 1735241
Cytopenia 51.93 32.08 23 10166 913 1735679
Gait disturbance 51.60 32.08 63 10126 12607 1723985
Peripheral motor neuropathy 51.04 32.08 16 10173 234 1736358
Hyperviscosity syndrome 50.87 32.08 12 10177 53 1736539
Performance status decreased 50.27 32.08 21 10168 721 1735871
Sudden death 50.23 32.08 33 10156 2907 1733685
Intestinal obstruction 49.55 32.08 35 10154 3472 1733120
Second primary malignancy 49.21 32.08 23 10166 1036 1735556
Squamous cell carcinoma of skin 48.68 32.08 24 10165 1218 1735374
Chronic obstructive pulmonary disease 48.60 32.08 43 10146 5910 1730682
Protein total increased 48.30 32.08 17 10172 362 1736230
Pathological fracture 47.98 32.08 19 10170 567 1736025
Blood albumin decreased 47.77 32.08 26 10163 1622 1734970
Rash pruritic 47.62 32.08 37 10152 4245 1732347
Cardio-respiratory arrest 47.57 32.08 52 10137 9241 1727351
Lethargy 47.26 32.08 46 10143 7138 1729454
Pulmonary alveolar haemorrhage 47.12 32.08 23 10166 1142 1735450
Blood bilirubin increased 47.04 32.08 43 10146 6167 1730425
Fluid retention 46.96 32.08 35 10154 3774 1732818
Musculoskeletal chest pain 46.79 32.08 24 10165 1326 1735266
Hypertension 46.67 32.08 75 10114 19373 1717219
Pericarditis 46.63 32.08 25 10164 1513 1735079
Pneumonia bacterial 46.58 32.08 23 10166 1171 1735421
Refusal of treatment by patient 46.53 32.08 23 10166 1174 1735418
Disseminated intravascular coagulation 46.33 32.08 34 10155 3580 1733012
Spinal pain 46.10 32.08 19 10170 630 1735962
Nocardiosis 46.10 32.08 18 10171 517 1736075
Hyperkalaemia 45.80 32.08 49 10140 8498 1728094
Body temperature increased 45.62 32.08 30 10159 2647 1733945
Squamous cell carcinoma 44.69 32.08 26 10163 1845 1734747
Pseudomonas infection 44.67 32.08 23 10166 1281 1735311
Encephalitis 44.63 32.08 22 10167 1116 1735476
Clostridial infection 44.48 32.08 19 10170 690 1735902
Gastrointestinal disorder 44.25 32.08 37 10152 4711 1731881
H1N1 influenza 44.21 32.08 14 10175 212 1736380
Pneumocystis jirovecii infection 44.11 32.08 15 10174 287 1736305
Capillary leak syndrome 43.83 32.08 15 10174 293 1736299
Pericardial effusion 43.70 32.08 32 10157 3358 1733234
Rash maculo-papular 43.37 32.08 33 10156 3670 1732922
Blood calcium increased 43.06 32.08 18 10171 619 1735973
Prostate cancer 43.01 32.08 36 10153 4590 1732002
Waldenstrom's macroglobulinaemia 43.01 32.08 11 10178 72 1736520
Hypogammaglobulinaemia 43.00 32.08 18 10171 621 1735971
Acute febrile neutrophilic dermatosis 42.50 32.08 15 10174 322 1736270
Supraventricular tachycardia 42.09 32.08 24 10165 1639 1734953
Abdominal pain upper 42.05 32.08 53 10136 10948 1725644
Acute lymphocytic leukaemia 41.84 32.08 17 10172 543 1736049
Herpes simplex 41.35 32.08 18 10171 685 1735907
Vision blurred 41.15 32.08 46 10143 8377 1728215
Pneumonia aspiration 40.93 32.08 37 10152 5229 1731363
Arrhythmia 40.46 32.08 39 10150 5977 1730615
International normalised ratio increased 39.99 32.08 45 10144 8254 1728338
Prothrombin time prolonged 39.97 32.08 23 10166 1598 1734994
Productive cough 39.86 32.08 31 10158 3560 1733032
Therapeutic product effect incomplete 39.85 32.08 37 10152 5411 1731181
Cerebral aspergillosis 39.79 32.08 12 10177 153 1736439
Therapeutic response decreased 39.55 32.08 37 10152 5463 1731129
Injection site rash 39.49 32.08 21 10168 1250 1735342
Somnolence 39.40 32.08 64 10125 16675 1719917
Staphylococcal bacteraemia 39.33 32.08 18 10171 772 1735820
Chest X-ray abnormal 39.32 32.08 17 10172 636 1735956
Chalazion 39.28 32.08 9 10180 34 1736558
Pulmonary haemorrhage 38.97 32.08 23 10166 1676 1734916
Acidosis 38.95 32.08 22 10167 1475 1735117
Mantle cell lymphoma 38.89 32.08 14 10175 319 1736273
Candida infection 38.46 32.08 24 10165 1934 1734658
Muscle spasms 38.23 32.08 52 10137 11569 1725023
Graft versus host disease 38.20 32.08 22 10167 1531 1735061
Blood potassium decreased 37.37 32.08 25 10164 2270 1734322
Progressive multifocal leukoencephalopathy 37.10 32.08 22 10167 1617 1734975
VIth nerve paralysis 36.83 32.08 12 10177 200 1736392
Presyncope 35.98 32.08 26 10163 2672 1733920
Cystitis haemorrhagic 35.77 32.08 16 10173 650 1735942
No adverse event 35.62 32.08 34 10155 5148 1731444
Rectal haemorrhage 35.53 32.08 35 10154 5507 1731085
Large intestine perforation 35.23 32.08 19 10170 1163 1735429
Blood uric acid increased 35.14 32.08 18 10171 991 1735601
Injection site reaction 35.11 32.08 28 10161 3334 1733258
Rash erythematous 35.10 32.08 30 10159 3935 1732657
Dizziness postural 35.03 32.08 17 10172 833 1735759
Sputum culture positive 34.79 32.08 12 10177 240 1736352
General physical condition abnormal 34.75 32.08 16 10173 696 1735896
Acute pulmonary oedema 34.71 32.08 19 10170 1198 1735394
Staphylococcal sepsis 34.57 32.08 19 10170 1208 1735384
Haematemesis 34.50 32.08 31 10158 4346 1732246
Aplasia 34.49 32.08 14 10175 446 1736146
Blood immunoglobulin G increased 34.41 32.08 11 10178 172 1736420
Enterocolitis 34.09 32.08 17 10172 884 1735708
Lung consolidation 33.87 32.08 15 10174 595 1735997
Optic neuropathy 33.67 32.08 13 10176 362 1736230
Nervous system disorder 33.53 32.08 24 10165 2430 1734162
Pseudomonal sepsis 33.34 32.08 13 10176 372 1736220
Haematotoxicity 33.11 32.08 17 10172 941 1735651
Cytomegalovirus chorioretinitis 33.08 32.08 13 10176 380 1736212
Chronic kidney disease 32.90 32.08 30 10159 4287 1732305
Blood potassium increased 32.87 32.08 24 10165 2506 1734086
Liver function test abnormal 32.76 32.08 34 10155 5692 1730900
Procalcitonin increased 32.63 32.08 10 10179 135 1736457
Hypercapnic coma 32.30 32.08 7 10182 19 1736573

Pharmacologic Action:

SourceCodeDescription
ATC L01XX32 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Other antineoplastic agents
FDA MoA N0000175075 Proteasome Inhibitors
MeSH PA D000970 Antineoplastic Agents
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35820 antiprotozoal drug
CHEBI has role CHEBI:52726 proteasome inhibitor

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Multiple myeloma indication 109989006 DOID:9538
Mantle cell lymphoma indication 443487006
Orthostatic hypotension contraindication 28651003
Dehydration contraindication 34095006
Low blood pressure contraindication 45007003
Chronic heart failure contraindication 48447003
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Interstitial pneumonia contraindication 64667001
Adult respiratory distress syndrome contraindication 67782005 DOID:11394
Pulmonary hypertension contraindication 70995007 DOID:6432
Diabetes mellitus contraindication 73211009 DOID:9351
Intestinal obstruction contraindication 81060008 DOID:8437
Prolonged QT interval contraindication 111975006
Pneumonia contraindication 233604007 DOID:552
Disease of liver contraindication 235856003 DOID:409
Syncope contraindication 271594007
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Peripheral nerve disease contraindication 302226006
Neutropenic disorder contraindication 303011007 DOID:1227
Breastfeeding (mother) contraindication 413712001
Posterior reversible encephalopathy syndrome contraindication 450886002
Chemotherapy-Induced Hyperuricemia contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.39 acidic
pKa2 12.09 acidic
pKa3 13.65 acidic
pKa4 2.9 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
3.5MG/VIAL VELCADE MILLENNIUM PHARMS N021602 May 13, 2003 RX INJECTABLE INTRAVENOUS, SUBCUTANEOUS Oct. 8, 2021 TREATMENT OF PATIENTS WITH MANTLE CELL LYMPHOMA WHO HAVE NOT RECEIVED AT LEAST 1 PRIOR THERAPY
3.5MG/VIAL VELCADE MILLENNIUM PHARMS N021602 May 13, 2003 RX INJECTABLE INTRAVENOUS, SUBCUTANEOUS April 8, 2022 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Proteasome subunit beta type-2 Enzyme INHIBITOR IC50 6.23 CHEMBL CHEMBL
Proteasome subunit beta type-1 Enzyme INHIBITOR IC50 7.28 CHEMBL CHEMBL
Proteasome subunit beta type-8 Enzyme INHIBITOR IC50 8.09 CHEMBL CHEMBL
Proteasome subunit beta type-5 Enzyme INHIBITOR Ki 9.26 CHEMBL CHEMBL
Proteasome subunit alpha type-1 Enzyme INHIBITOR Ki 9.21 WOMBAT-PK CHEMBL
Lysosomal protective protein Enzyme IC50 5.04 CHEMBL
Chymase Enzyme IC50 5.92 CHEMBL
Chymotrypsinogen B Enzyme Ki 6.49 CHEMBL
Nuclear factor NF-kappa-B complex Unclassified IC50 8.01 CHEMBL
Neutrophil elastase Enzyme Ki 5.64 CHEMBL
26S proteasome non-ATPase regulatory subunit 1 Cytosolic other Ki 7.74 WOMBAT-PK
Cytochrome P450 2C19 Enzyme Ki 4.74 WOMBAT-PK
PH and SEC7 domain-containing protein 1 Unclassified Ki 7.74 WOMBAT-PK
Prothrombin Enzyme Ki 4.89 CHEMBL
Cathepsin G Enzyme Ki 6.20 CHEMBL
Alpha-chymotrypsin Unclassified Ki 5.62 CHEMBL

External reference:

IDSource
D000069286 MESH_DESCRIPTOR_UI
4021393 VUID
N0000148811 NUI
C1176309 UMLSCUI
D03150 KEGG_DRUG
69G8BD63PP UNII
8331 INN_ID
398907002 SNOMEDCT_US
358258 RXNORM
d04871 MMSL
17263 MMSL
407097007 SNOMEDCT_US
4021393 VANDF
009985 NDDF
233935 MMSL
CHEMBL325041 ChEMBL_ID
DB00188 DRUGBANK_ID
BO2 PDB_CHEM_ID
CHEBI:52717 CHEBI
6391 IUPHAR_LIGAND_ID
387447 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Bortezomib HUMAN PRESCRIPTION DRUG LABEL 1 43598-865 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 3.50 mg INTRAVENOUS NDA 17 sections
VELCADE HUMAN PRESCRIPTION DRUG LABEL 1 63020-049 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 3.50 mg INTRAVENOUS NDA 19 sections
Bortezomib HUMAN PRESCRIPTION DRUG LABEL 1 63323-721 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 1 mg INTRAVENOUS NDA 18 sections