ixazomib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
proteasome inhibitors 5067 1072833-77-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ixazomib
  • ixazomib citrate
  • MLN2238
  • MLN9708
  • ninlaro
an oral proteasome inhibitor with antineoplastic activity; MLN2238 is the biologically active form of MLN9708
  • Molecular weight: 361.03
  • Formula: C14H19BCl2N2O4
  • CLOGP: 1.10
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 4
  • TPSA: 98.66
  • ALOGS: -4.47
  • ROTB: 7
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.43 mg O

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 3.61 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.50 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.01 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 97 hours Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
March 30, 2017 PMDA Takeda Pharmaceutical Company Limited
Nov. 21, 2016 EMA Takeda Pharma A/S
Nov. 20, 2015 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
Diarrhoea 1031.78 23.16 1320 25586 937870 89663671
Neuropathy peripheral 827.16 23.16 511 26395 136459 90465082
Death 670.55 23.16 747 26159 455804 90145737
Platelet count decreased 386.43 23.16 322 26584 136647 90464894
Thrombocytopenia 376.67 23.16 382 26524 208343 90393198
Pneumonia 298.49 23.16 612 26294 637447 89964094
Constipation 256.27 23.16 363 26543 280032 90321509
Plasma cell myeloma recurrent 249.60 23.16 79 26827 4149 90597392
Product physical issue 246.40 23.16 84 26822 5576 90595965
Off label use 240.25 23.16 793 26113 1101459 89500082
Plasma cell myeloma 234.80 23.16 148 26758 40680 90560861
Nausea 213.99 23.16 767 26139 1109549 89491992
Adverse event 191.82 23.16 204 26702 117214 90484327
Product dose omission issue 191.16 23.16 324 26582 291363 90310178
White blood cell count decreased 180.76 23.16 235 26671 166874 90434667
No adverse event 159.43 23.16 144 26762 67838 90533703
Full blood count decreased 149.42 23.16 99 26807 29590 90571951
Cytopenia 120.13 23.16 71 26835 17378 90584163
Neutrophil count decreased 107.50 23.16 119 26787 71413 90530128
Neutropenia 105.96 23.16 217 26689 224687 90376854
Vomiting 102.16 23.16 483 26423 787810 89813731
Fatigue 89.40 23.16 616 26290 1153407 89448134
COVID-19 86.78 23.16 169 26737 168674 90432867
Infusion related reaction 83.97 23.16 12 26894 416768 90184773
Dehydration 83.85 23.16 181 26725 194266 90407275
Glossodynia 82.31 23.16 3 26903 321776 90279765
Laboratory test abnormal 81.49 23.16 80 26826 41774 90559767
Condition aggravated 76.23 23.16 41 26865 595504 90006037
Cataract 71.09 23.16 97 26809 71995 90529546
Hepatic enzyme increased 69.00 23.16 12 26894 360724 90240817
Back pain 68.12 23.16 228 26678 316947 90284594
Wound 67.84 23.16 6 26900 302974 90298567
Light chain analysis increased 67.26 23.16 23 26883 1539 90600002
Haemorrhoidal haemorrhage 62.86 23.16 31 26875 5292 90596249
Accidental exposure to product 61.09 23.16 69 26837 42297 90559244
Plasmacytoma 61.00 23.16 25 26881 2768 90598773
Treatment failure 60.61 23.16 9 26897 303919 90297622
Pericarditis 58.75 23.16 6 26900 270145 90331396
Wheezing 58.29 23.16 3 26903 238077 90363464
Therapeutic product effect decreased 58.25 23.16 7 26899 277564 90323977
Influenza 57.01 23.16 127 26779 139137 90462404
Impaired healing 54.19 23.16 4 26902 234195 90367346
Monoclonal immunoglobulin increased 52.19 23.16 14 26892 407 90601134
Product packaging quantity issue 51.55 23.16 19 26887 1583 90599958
Product use in unapproved indication 51.11 23.16 18 26888 336218 90265323
Product packaging issue 51.10 23.16 19 26887 1622 90599919
Drug hypersensitivity 50.92 23.16 38 26868 463571 90137970
Cardiac failure 49.55 23.16 104 26802 109392 90492149
Anaemia 49.01 23.16 221 26685 352581 90248960
Discomfort 48.52 23.16 11 26895 274324 90327217
N-terminal prohormone brain natriuretic peptide decreased 46.41 23.16 8 26898 22 90601519
Paraesthesia 45.99 23.16 171 26735 250155 90351386
Asthenia 45.90 23.16 293 26613 533458 90068083
Hypertension 45.89 23.16 41 26865 457491 90144050
COVID-19 pneumonia 45.54 23.16 40 26866 18137 90583404
Drug interaction 45.21 23.16 13 26893 276440 90325101
Musculoskeletal stiffness 44.85 23.16 16 26890 296516 90305025
Body dysmorphic disorder 43.19 23.16 12 26894 399 90601142
Monoclonal immunoglobulin present 42.96 23.16 18 26888 2106 90599435
Arthropathy 42.87 23.16 28 26878 366214 90235327
Herpes zoster 41.78 23.16 89 26817 94555 90506986
Irritable bowel syndrome 41.67 23.16 6 26900 207442 90394099
Injury 41.34 23.16 5 26901 197344 90404197
Muscle spasms 41.31 23.16 166 26740 251717 90349824
Rash 40.61 23.16 387 26519 795713 89805828
Injection site pain 40.08 23.16 3 26903 173696 90427845
Adverse drug reaction 39.67 23.16 99 26807 116602 90484939
Myelosuppression 39.65 23.16 63 26843 53528 90548013
Plasma cell myeloma refractory 39.50 23.16 14 26892 1042 90600499
Urinary tract infection 38.41 23.16 186 26720 305446 90296095
Ill-defined disorder 37.96 23.16 5 26901 184886 90416655
Blood cholesterol increased 37.46 23.16 8 26898 208004 90393537
Burning sensation 36.89 23.16 67 26839 63385 90538156
Hypersensitivity 36.47 23.16 49 26857 454628 90146913
Osteoarthritis 36.34 23.16 7 26899 195723 90405818
Product blister packaging issue 36.00 23.16 10 26896 332 90601209
Cardiac amyloidosis 35.98 23.16 13 26893 1023 90600518
Migraine 34.95 23.16 7 26899 190385 90411156
Rash macular 34.89 23.16 44 26862 30236 90571305
Arthralgia 34.04 23.16 118 26788 778404 89823137
Mobility decreased 33.90 23.16 16 26890 250718 90350823
Renal failure 33.40 23.16 100 26806 130907 90470634
Drug ineffective 33.30 23.16 258 26648 1384040 89217501
Peripheral swelling 33.16 23.16 223 26683 412883 90188658
COVID-19 immunisation 32.49 23.16 14 26892 1755 90599786
Alopecia 32.47 23.16 61 26845 495010 90106531
Polyneuropathy 32.23 23.16 34 26872 19307 90582234
Pain 31.94 23.16 170 26736 996171 89605370
Blood potassium decreased 31.12 23.16 53 26853 47674 90553867
Fall 30.62 23.16 246 26660 481564 90119977
Hypokalaemia 30.55 23.16 97 26809 131019 90470522
Neoplasm skin 30.41 23.16 16 26890 3126 90598415
Therapy partial responder 30.25 23.16 35 26871 22008 90579533
Vitiligo 30.13 23.16 14 26892 2096 90599445
Ageusia 29.93 23.16 30 26876 16046 90585495
Liver injury 29.82 23.16 7 26899 170560 90430981
Joint ankylosis 29.61 23.16 12 26894 1291 90600250
Bone pain 29.35 23.16 60 26846 61923 90539618
Asthma 29.02 23.16 18 26888 242142 90359399
VIth nerve paresis 26.85 23.16 6 26900 79 90601462
Dry skin 26.11 23.16 71 26835 88002 90513539
Skin discolouration 26.02 23.16 47 26859 44268 90557273
Joint swelling 25.71 23.16 71 26835 503229 90098312
Blood immunoglobulin G increased 25.59 23.16 14 26892 2958 90598583
Swelling 25.44 23.16 54 26852 419004 90182537
Headache 25.02 23.16 152 26754 862594 89738947
Hypoglossal nerve paresis 24.85 23.16 6 26900 113 90601428
Paraproteinaemia 24.71 23.16 7 26899 250 90601291
Unevaluable event 24.68 23.16 52 26854 54796 90546745
Vulvovaginal mycotic infection 24.60 23.16 18 26888 6296 90595245
Bone lesion 24.29 23.16 18 26888 6419 90595122
Neutrophil count abnormal 23.80 23.16 15 26891 4113 90597428

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 583.45 19.94 478 24278 101375 42495204
Death 534.59 19.94 965 23791 470220 42126359
Pneumonia 404.81 19.94 806 23950 421343 42175236
Diarrhoea 327.29 19.94 780 23976 460069 42136510
Adverse event 269.45 19.94 169 24587 23471 42573108
Platelet count decreased 249.36 19.94 352 24404 138229 42458350
Plasma cell myeloma recurrent 243.34 19.94 100 24656 5657 42590922
Plasma cell myeloma 228.07 19.94 202 24554 47376 42549203
Thrombocytopenia 226.73 19.94 400 24356 189879 42406700
Product physical issue 219.22 19.94 79 24677 3120 42593459
Off label use 217.28 19.94 834 23922 637501 41959078
Full blood count decreased 178.38 19.94 124 24632 20436 42576143
Light chain analysis increased 155.77 19.94 53 24703 1761 42594818
No adverse event 145.22 19.94 144 24612 38877 42557702
Fatigue 136.62 19.94 556 24200 435085 42161494
Product dose omission issue 135.03 19.94 285 24471 154080 42442499
Drug interaction 133.37 19.94 5 24751 266994 42329585
Peripheral swelling 128.79 19.94 206 24550 90064 42506515
Constipation 118.70 19.94 279 24477 162012 42434567
White blood cell count decreased 112.14 19.94 217 24539 110179 42486400
Laboratory test abnormal 106.90 19.94 96 24660 22882 42573697
Rash 97.43 19.94 367 24389 276587 42319992
Influenza 95.72 19.94 147 24609 62028 42534551
COVID-19 78.93 19.94 194 24562 115754 42480825
Adverse drug reaction 75.99 19.94 101 24655 37333 42559246
Plasma cell myeloma refractory 71.73 19.94 28 24728 1382 42595197
Back pain 64.62 19.94 205 24551 141571 42455008
Product use in unapproved indication 62.82 19.94 15 24741 184441 42412138
Toxicity to various agents 61.67 19.94 28 24728 229108 42367471
Accidental exposure to product 59.28 19.94 66 24690 20327 42576252
Cytopenia 58.54 19.94 61 24695 17436 42579143
Respiratory tract infection 53.38 19.94 71 24685 26251 42570328
Neutropenia 51.72 19.94 241 24515 199190 42397389
Respiratory tract infection bacterial 50.91 19.94 24 24732 1885 42594694
Condition aggravated 50.87 19.94 46 24710 260708 42335871
Neutrophil count abnormal 47.96 19.94 26 24730 2745 42593834
Lower respiratory tract infection 46.74 19.94 85 24671 41121 42555458
Plasmacytoma 46.68 19.94 30 24726 4334 42592245
Respiratory tract infection viral 45.56 19.94 27 24729 3379 42593200
Product packaging issue 45.28 19.94 17 24739 754 42595825
Muscle spasms 43.43 19.94 129 24627 85915 42510664
Tachycardia 41.46 19.94 5 24751 101082 42495497
Hypertension 39.68 19.94 24 24732 167180 42429399
Product packaging quantity issue 39.16 19.94 18 24738 1335 42595244
Nasopharyngitis 38.71 19.94 122 24634 83874 42512705
Monoclonal immunoglobulin present 38.06 19.94 17 24739 1179 42595400
Nausea 36.02 19.94 370 24386 396429 42200150
Illness 34.26 19.94 56 24700 24874 42571705
Rhabdomyolysis 34.21 19.94 3 24753 78016 42518563
Product blister packaging issue 33.83 19.94 9 24747 125 42596454
Therapy partial responder 31.71 19.94 48 24708 19973 42576606
Full blood count increased 30.98 19.94 14 24742 998 42595581
Haemoglobin abnormal 29.75 19.94 24 24732 4940 42591639
Asthenia 29.43 19.94 270 24486 280523 42316056
Keratopathy 29.06 19.94 12 24744 686 42595893
COVID-19 pneumonia 28.96 19.94 48 24708 21565 42575014
Hypotension 28.94 19.94 67 24689 257564 42339015
Malaise 28.63 19.94 216 24540 211940 42384639
Herpes zoster 28.49 19.94 67 24689 38810 42557769
Insomnia 27.77 19.94 139 24617 118114 42478465
Light chain disease 27.49 19.94 8 24748 157 42596422
Polyneuropathy 27.12 19.94 43 24713 18618 42577961
Morganella infection 26.99 19.94 11 24745 608 42595971
Monoclonal immunoglobulin increased 26.75 19.94 10 24746 438 42596141
Abdominal pain 26.15 19.94 44 24712 190427 42406152
Protein total increased 25.80 19.94 17 24739 2561 42594018
Bronchial haemorrhage 25.63 19.94 11 24745 693 42595886
Intentional product misuse 25.53 19.94 3 24753 61897 42534682
Bradycardia 25.32 19.94 9 24747 85475 42511104
Thrombosis 24.95 19.94 92 24664 68419 42528160
Laryngeal cancer metastatic 24.45 19.94 6 24750 59 42596520
Musculoskeletal chest pain 23.91 19.94 31 24725 11173 42585406
JC virus CSF test positive 23.75 19.94 7 24749 144 42596435
Paraproteinaemia 23.74 19.94 9 24747 410 42596169
Spinal pain 23.32 19.94 24 24732 6758 42589821
Headache 23.23 19.94 67 24689 239302 42357277
Hospitalisation 23.15 19.94 95 24661 74235 42522344
Upper respiratory tract infection 22.96 19.94 65 24691 42108 42554471
Overdose 22.42 19.94 17 24739 105247 42491332
Paraesthesia 22.18 19.94 93 24663 73366 42523213
Neutrophil count decreased 22.13 19.94 84 24672 63331 42533248
Unevaluable event 21.84 19.94 56 24700 34232 42562347
Cataract 21.62 19.94 52 24704 30552 42566027
Seizure 21.46 19.94 23 24733 120538 42476041
Otitis externa bacterial 21.42 19.94 4 24752 8 42596571
Cryptosporidiosis infection 21.31 19.94 10 24746 777 42595802
Hypoaesthesia 21.21 19.94 90 24666 71373 42525206
Cellulitis enterococcal 21.16 19.94 6 24750 107 42596472
Chillblains 20.98 19.94 5 24751 43 42596536
Oxygen saturation decreased 20.59 19.94 6 24750 64681 42531898
Blood immunoglobulin G increased 20.56 19.94 11 24745 1131 42595448
Hypoglycaemia 20.09 19.94 5 24751 59849 42536730
Ageusia 20.07 19.94 29 24727 11576 42585003

FDA Adverse Event Reporting System (Geriatric)

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 974.35 19.33 634 33385 178643 110376637
Diarrhoea 833.12 19.33 1348 32671 1138157 109417123
Pneumonia 676.86 19.33 1065 32954 875649 109679631
Platelet count decreased 552.33 19.33 501 33518 229942 110325338
Thrombocytopenia 485.56 19.33 566 33453 348319 110206961
Off label use 459.27 19.33 1243 32776 1498942 109056338
Death 424.22 19.33 764 33255 698105 109857175
Plasma cell myeloma 334.64 19.33 220 33799 62716 110492564
Plasma cell myeloma recurrent 332.24 19.33 112 33907 6930 110548350
Product physical issue 249.08 19.33 83 33936 4953 110550327
Product dose omission issue 219.26 19.33 371 33648 321411 110233869
White blood cell count decreased 217.26 19.33 308 33711 229082 110326198
Constipation 205.77 19.33 383 33636 357403 110197877
Light chain analysis increased 154.05 19.33 48 33971 2307 110552973
Full blood count decreased 153.23 19.33 105 33914 31994 110523286
COVID-19 145.32 19.33 266 33753 244794 110310486
Neutrophil count decreased 144.46 19.33 182 33837 120759 110434521
No adverse event 124.95 19.33 133 33886 73706 110481574
Plasma cell myeloma refractory 123.44 19.33 39 33980 1962 110553318
Neutropenia 120.63 19.33 318 33701 374302 110180978
Nausea 112.81 19.33 706 33313 1234984 109320296
Rash 107.72 19.33 518 33501 820446 109734834
Drug interaction 106.59 19.33 14 34005 500169 110055111
Fatigue 99.47 19.33 676 33343 1215282 109339998
Influenza 94.46 19.33 179 33840 168922 110386358
Cytopenia 89.09 19.33 74 33945 30042 110525238
Plasmacytoma 86.74 19.33 39 33980 5223 110550057
Neutrophil count abnormal 81.31 19.33 37 33982 5095 110550185
Respiratory tract infection 79.53 19.33 104 33915 71513 110483767
COVID-19 pneumonia 77.61 19.33 75 33944 37068 110518212
Anaemia 72.86 19.33 347 33672 546739 110008541
Condition aggravated 70.88 19.33 73 33946 734763 109820517
Therapy partial responder 66.68 19.33 69 33950 36992 110518288
Back pain 66.06 19.33 257 33762 370739 110184541
Polyneuropathy 65.68 19.33 64 33955 31948 110523332
Drug hypersensitivity 65.28 19.33 29 33990 454061 110101219
Hypertension 65.23 19.33 38 33981 510046 110045234
Respiratory tract infection viral 64.66 19.33 33 33986 5845 110549435
Cataract 62.58 19.33 98 33921 79387 110475893
Product use in unapproved indication 62.09 19.33 30 33989 447347 110107933
Hepatic enzyme increased 61.54 19.33 12 34007 320880 110234400
Cardiac failure 61.01 19.33 160 33859 187466 110367814
Dehydration 60.19 19.33 206 33813 279305 110275975
Respiratory tract infection bacterial 60.15 19.33 24 33995 2392 110552888
Infusion related reaction 55.31 19.33 24 33995 381138 110174142
Myelosuppression 54.06 19.33 101 33918 94239 110461041
Treatment failure 53.93 19.33 10 34009 277224 110278056
Toxicity to various agents 53.14 19.33 42 33977 480513 110074767
Glossodynia 53.00 19.33 4 34015 222000 110333280
Arthropathy 52.56 19.33 12 34007 287510 110267770
Musculoskeletal stiffness 52.53 19.33 11 34008 279811 110275469
Product packaging quantity issue 52.31 19.33 20 33999 1779 110553501
Pain 51.10 19.33 139 33880 954816 109600464
Rash macular 50.63 19.33 61 33958 38625 110516655
Herpes zoster 50.03 19.33 106 33913 108273 110447007
Product blister packaging issue 49.14 19.33 13 34006 345 110554935
Wheezing 47.98 19.33 10 34009 255220 110300060
Laboratory test abnormal 47.37 19.33 63 33956 44016 110511264
Neoplasm skin 47.31 19.33 22 33997 3182 110552098
Accidental exposure to product 47.01 19.33 67 33952 49941 110505339
Product packaging issue 46.52 19.33 18 34001 1653 110553627
Monoclonal immunoglobulin increased 46.32 19.33 14 34005 607 110554673
Peripheral swelling 45.78 19.33 245 33774 403789 110151491
Therapeutic product effect decreased 45.05 19.33 10 34009 244306 110310974
Headache 43.84 19.33 133 33886 882244 109673036
COVID-19 immunisation 43.60 19.33 16 34003 1270 110554010
Injection site pain 43.06 19.33 3 34016 177919 110377361
Alopecia 41.43 19.33 31 33988 364722 110190558
Blood immunoglobulin G increased 40.79 19.33 21 33998 3787 110551493
Impaired healing 40.69 19.33 6 34013 196711 110358569
Type 2 diabetes mellitus 40.11 19.33 4 34015 177228 110378052
Folliculitis 40.07 19.33 3 34016 167650 110387630
Vomiting 39.63 19.33 441 33578 910234 109645046
Hypersensitivity 37.91 19.33 41 33978 403957 110151323
N-terminal prohormone brain natriuretic peptide decreased 37.42 19.33 7 34012 33 110555247
Discomfort 37.22 19.33 10 34009 214697 110340583
Ill-defined disorder 36.95 19.33 3 34016 156850 110398430
Irritable bowel syndrome 36.40 19.33 4 34015 164211 110391069
Migraine 36.05 19.33 5 34014 171647 110383633
Asthma 35.91 19.33 16 34003 250275 110305005
Keratopathy 35.44 19.33 14 34005 1359 110553921
Blood cholesterol increased 35.22 19.33 7 34012 184778 110370502
Haemorrhoidal haemorrhage 35.17 19.33 25 33994 8068 110547212
Cardiac amyloidosis 34.36 19.33 17 34002 2820 110552460
Mobility decreased 34.34 19.33 15 34004 237407 110317873
Hypokalaemia 33.73 19.33 128 33891 182320 110372960
Platelet count abnormal 33.45 19.33 22 33997 6260 110549020
Body dysmorphic disorder 33.27 19.33 10 34009 425 110554855
Liver injury 32.50 19.33 4 34015 150409 110404871
Wound 32.07 19.33 16 34003 234421 110320859
Hypotension 32.07 19.33 71 33948 523778 110031502
Renal failure 31.74 19.33 146 33873 226428 110328852
Arthralgia 31.02 19.33 129 33890 779503 109775777
Haemoglobin abnormal 30.52 19.33 24 33995 9014 110546266
Tachycardia 30.21 19.33 16 34003 226629 110328651
Monoclonal immunoglobulin present 30.11 19.33 15 34004 2525 110552755
Psoriasis 29.58 19.33 4 34015 139989 110415291
Upper respiratory tract infection 29.29 19.33 98 33921 131230 110424050
Burning sensation 28.87 19.33 65 33954 69147 110486133
Hypogammaglobulinaemia 28.49 19.33 33 33986 20043 110535237
Pericarditis 28.43 19.33 16 34003 219098 110336182
Light chain disease 28.09 19.33 8 34011 281 110554999
Full blood count increased 27.92 19.33 10 34009 740 110554540
Intentional product misuse 27.61 19.33 4 34015 132900 110422380
Swelling 27.35 19.33 41 33978 351000 110204280
Osteoarthritis 27.27 19.33 11 34008 182612 110372668
Bursitis 26.78 19.33 4 34015 129914 110425366
Hypercalcaemia 26.78 19.33 50 33969 46607 110508673
Inflammation 26.71 19.33 13 34006 193225 110362055
Bone lesion 26.51 19.33 20 33999 7067 110548213
Drug-induced liver injury 26.42 19.33 3 34016 120064 110435216
Fall 26.07 19.33 292 33727 603190 109952090
Injury 25.95 19.33 11 34008 177254 110378026
JC virus CSF test positive 25.83 19.33 7 34012 204 110555076
Overdose 25.11 19.33 21 33998 233773 110321507
Drug ineffective 25.09 19.33 324 33695 1520216 109035064
Hypoproteinaemia 24.99 19.33 18 34001 5927 110549353
Upper respiratory tract inflammation 24.97 19.33 16 34003 4355 110550925
Vitiligo 24.92 19.33 14 34005 3003 110552277
Depression 24.78 19.33 37 33982 317298 110237982
Sepsis 24.76 19.33 179 33840 327167 110228113
Vitamin B12 decreased 24.61 19.33 17 34002 5240 110550040
Muscle spasms 24.55 19.33 158 33861 277999 110277281
Hypoglossal nerve paresis 24.48 19.33 6 34013 116 110555164
Pneumonia influenzal 24.43 19.33 15 34004 3790 110551490
Vulvovaginal mycotic infection 24.27 19.33 17 34002 5360 110549920
Cryptosporidiosis infection 23.83 19.33 10 34009 1133 110554147
Night sweats 23.67 19.33 6 34013 133977 110421303
Laryngeal cancer metastatic 23.46 19.33 5 34014 50 110555230
Anxiety 23.46 19.33 44 33975 345034 110210246
VIth nerve paresis 23.18 19.33 6 34013 146 110555134
Asthenia 23.13 19.33 318 33701 688681 109866599
Peripheral sensory neuropathy 22.97 19.33 27 33992 16653 110538627
Hypoaesthesia 22.72 19.33 170 33849 314053 110241227
Blood calcium abnormal 22.62 19.33 11 34008 1758 110553522
Stomatitis 22.60 19.33 30 33989 270212 110285068
Renal disorder 22.37 19.33 48 33971 49431 110505849
Immunoglobulins decreased 22.21 19.33 12 34007 2387 110552893
Morganella infection 22.03 19.33 10 34009 1369 110553911
Bronchial haemorrhage 21.97 19.33 10 34009 1377 110553903
C-reactive protein increased 21.69 19.33 21 33998 217898 110337382
Musculoskeletal pain 21.49 19.33 15 34004 183008 110372272
Squamous cell carcinoma of skin 20.69 19.33 26 33993 17177 110538103
Light chain analysis abnormal 20.56 19.33 6 34013 230 110555050
Musculoskeletal chest pain 20.55 19.33 34 33985 28813 110526467
Renal impairment 20.44 19.33 113 33906 188332 110366948
Pneumonia bacterial 20.14 19.33 32 33987 26229 110529051
Stress 20.05 19.33 4 34015 105344 110449936
Disease progression 19.94 19.33 136 33883 243898 110311382
Wound infection 19.81 19.33 3 34016 96462 110458818
Arnold-Chiari malformation 19.79 19.33 6 34013 263 110555017
SARS-CoV-2 test positive 19.43 19.33 25 33994 16910 110538370
Paraproteinaemia 19.34 19.33 7 34012 534 110554746

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01XG03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Proteasome inhibitors
FDA MoA N0000175075 Proteasome Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D011480 Protease Inhibitors
FDA EPC N0000175604 Proteasome Inhibitor
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:50266 prodrug
CHEBI has role CHEBI:52726 proteasome inhibitor
CHEBI has role CHEBI:68495 apoptosis inducer
CHEBI has role CHEBI:71031 orphan drug
CHEBI has role CHEBI:49103 drug metabolite
CHEBI has role CHEBI:64946 anti-HIV agent
CHEBI has role CHEBI:67079 anti-inflammatory agent
CHEBI has role CHEBI:75835 anti-anaemic agent

Related Drugs by ATC class:

L01XG Proteasome inhibitors 2 drugs
bortezomibcarfilzomib

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Multiple myeloma indication 109989006 DOID:9538




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.27 acidic
pKa2 12.17 acidic
pKa3 13.45 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 2.3MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL 8003819 Aug. 6, 2027 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 2.3MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL 8530694 Aug. 6, 2027 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 2.3MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL 8871745 Aug. 6, 2027 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 3MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL 8003819 Aug. 6, 2027 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 3MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL 8530694 Aug. 6, 2027 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 3MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL 8871745 Aug. 6, 2027 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 4MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL 8003819 Aug. 6, 2027 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 4MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL 8530694 Aug. 6, 2027 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 4MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL 8871745 Aug. 6, 2027 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 2.3MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL 9175017 June 16, 2029 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 3MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL 9175017 June 16, 2029 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 4MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL 9175017 June 16, 2029 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 2.3MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL 7442830 Nov. 20, 2029 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 3MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL 7442830 Nov. 20, 2029 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
EQ 4MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL 7442830 Nov. 20, 2029 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Proteasome subunit beta type-5 Enzyme INHIBITOR IC50 8.47 SCIENTIFIC LITERATURE DRUG LABEL
Proteasome subunit beta type-1 Enzyme INHIBITOR IC50 7.51 SCIENTIFIC LITERATURE
Proteasome subunit beta type-2 Enzyme INHIBITOR IC50 5.46 SCIENTIFIC LITERATURE
ATP-dependent Clp protease proteolytic subunit Enzyme EC50 5.44 CHEMBL
NACHT, LRR and PYD domains-containing protein 3 Cytosolic other IC50 6.70 CHEMBL

External reference:

IDSource
71050168A2 UNII
D10130 KEGG_DRUG
1239908-20-3 SECONDARY_CAS_RN
4035138 VANDF
C3273711 UMLSCUI
CHEBI:90942 CHEBI
CHEMBL2141296 ChEMBL_ID
25183872 PUBCHEM_CID
DB09570 DRUGBANK_ID
CHEMBL3545432 ChEMBL_ID
9411 INN_ID
C548400 MESH_SUPPLEMENTAL_RECORD_UI
8450 IUPHAR_LIGAND_ID
C000595706 MESH_SUPPLEMENTAL_RECORD_UI
1723734 RXNORM
237159 MMSL
31293 MMSL
d08398 MMSL
016599 NDDF
016600 NDDF
715256005 SNOMEDCT_US
781324002 SNOMEDCT_US
784168005 SNOMEDCT_US
6V8 PDB_CHEM_ID
71050168A2 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
NINLARO HUMAN PRESCRIPTION DRUG LABEL 1 63020-230 CAPSULE 2.30 mg ORAL NDA 34 sections
NINLARO HUMAN PRESCRIPTION DRUG LABEL 1 63020-390 CAPSULE 3 mg ORAL NDA 34 sections
NINLARO HUMAN PRESCRIPTION DRUG LABEL 1 63020-400 CAPSULE 4 mg ORAL NDA 34 sections