ixazomib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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:

None

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

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 798.24 20.83 1051 18615 587425 49998033
Neuropathy peripheral 521.04 20.83 372 19294 96385 50489073
Death 488.80 20.83 614 19052 324765 50260693
Adverse event 267.11 20.83 182 19484 43581 50541877
Thrombocytopenia 264.27 20.83 285 19381 127388 50458070
Platelet count decreased 248.26 20.83 247 19419 100479 50484979
Pneumonia 216.49 20.83 462 19204 377939 50207519
Plasma cell myeloma recurrent 176.74 20.83 58 19608 2600 50582858
Plasma cell myeloma 167.07 20.83 120 19546 31202 50554256
Off label use 160.11 20.83 474 19192 473952 50111506
Product physical issue 138.51 20.83 55 19611 4277 50581181
Nausea 134.30 20.83 584 19082 704814 49880644
Constipation 129.85 20.83 247 19419 185461 50399997
White blood cell count decreased 123.75 20.83 187 19479 116535 50468923
No adverse event 120.99 20.83 102 19564 33476 50551982
Full blood count decreased 106.46 20.83 80 19586 22266 50563192
Cytopenia 101.41 20.83 55 19611 8720 50576738
Product dose omission issue 91.64 20.83 213 19453 183625 50401833
Laboratory test abnormal 90.88 20.83 74 19592 23134 50562324
Neutrophil count decreased 86.74 20.83 98 19568 45928 50539530
Vomiting 83.00 20.83 376 19290 460382 50125076
Adverse drug reaction 70.93 20.83 97 19569 55125 50530333
Fatigue 68.66 20.83 489 19177 707112 49878346
Influenza 58.64 20.83 116 19550 89422 50496036
Drug ineffective 57.00 20.83 149 19517 819184 49766274
Dehydration 48.80 20.83 150 19516 152299 50433159
Neutropenia 45.89 20.83 144 19522 147821 50437637
Plasmacytoma 45.47 20.83 21 19645 2364 50583094
Muscle spasms 44.40 20.83 128 19538 125425 50460033
Paraesthesia 43.90 20.83 124 19542 120119 50465339
Drug interaction 43.29 20.83 12 19654 199609 50385849
Rash 42.56 20.83 303 19363 437168 50148290
Asthenia 40.87 20.83 237 19429 318805 50266653
Monoclonal immunoglobulin present 40.69 20.83 14 19652 726 50584732
Body dysmorphic disorder 40.49 20.83 11 19655 254 50585204
Toxicity to various agents 40.44 20.83 16 19650 212483 50372975
Product packaging quantity issue 39.07 20.83 15 19651 1065 50584393
Accidental exposure to product 38.24 20.83 46 19620 23011 50562447
Condition aggravated 37.65 20.83 36 19630 297022 50288436
COVID-19 37.46 20.83 66 19600 46596 50538862
Illness 35.95 20.83 46 19620 24494 50560964
Product blister packaging issue 35.90 20.83 9 19657 150 50585308
Light chain analysis increased 35.30 20.83 14 19652 1084 50584374
Treatment failure 34.42 20.83 6 19660 137631 50447827
Arthralgia 34.13 20.83 75 19591 438627 50146831
Glossodynia 33.84 20.83 3 19663 115566 50469892
Infusion related reaction 33.53 20.83 12 19654 169545 50415913
Cardiac amyloidosis 33.21 20.83 12 19654 719 50584739
Peripheral swelling 33.16 20.83 163 19503 205773 50379685
Cataract 33.04 20.83 63 19603 47237 50538221
Pain 32.44 20.83 116 19550 578787 50006671
Injection site pain 32.19 20.83 3 19663 111021 50474437
Therapeutic product effect decreased 31.77 20.83 7 19659 136043 50449415
COVID-19 pneumonia 31.24 20.83 26 19640 8369 50577089
Vitiligo 31.22 20.83 13 19653 1141 50584317
Drug hypersensitivity 31.12 20.83 31 19635 250979 50334479
Hepatic enzyme increased 30.26 20.83 8 19658 137372 50448086
Product packaging issue 29.94 20.83 12 19654 955 50584503
Joint ankylosis 29.04 20.83 11 19655 753 50584705
Monoclonal immunoglobulin increased 28.93 20.83 7 19659 100 50585358
Discomfort 28.74 20.83 4 19662 108376 50477082
Wound 27.83 20.83 4 19662 105790 50479668
Decreased appetite 27.47 20.83 152 19514 200771 50384687
Back pain 27.17 20.83 162 19504 219868 50365590
VIth nerve paresis 25.25 20.83 6 19660 79 50585379
Blood potassium decreased 24.32 20.83 48 19618 36897 50548561
Product use issue 24.22 20.83 14 19652 149461 50435997
Ageusia 24.11 20.83 26 19640 11557 50573901
Musculoskeletal stiffness 23.89 20.83 10 19656 128471 50456987
Hypoglossal nerve paresis 23.60 20.83 6 19660 106 50585352
Blood immunoglobulin G increased 23.12 20.83 11 19655 1324 50584134
Headache 23.03 20.83 110 19556 506425 50079033
Eye swelling 22.32 20.83 33 19633 20111 50565347
Product packaging difficult to open 22.03 20.83 5 19661 53 50585405
Haemorrhoidal haemorrhage 21.74 20.83 15 19651 3652 50581806
Tumour lysis syndrome 21.62 20.83 20 19646 7401 50578057
Tachycardia 21.60 20.83 6 19660 99757 50485701
Product use in unapproved indication 21.56 20.83 9 19657 115810 50469648
Hypertension 20.96 20.83 31 19635 211172 50374286

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
Death 491.83 20.83 802 17375 341282 29215068
Neuropathy peripheral 443.83 20.83 359 17818 70668 29485682
Pneumonia 299.20 20.83 625 17552 319547 29236803
Adverse event 283.83 20.83 153 18024 15138 29541212
Diarrhoea 271.41 20.83 615 17562 332083 29224267
Off label use 234.91 20.83 547 17630 300253 29256097
Platelet count decreased 184.23 20.83 271 17906 104401 29451949
No adverse event 183.09 20.83 121 18056 17357 29538993
Thrombocytopenia 175.37 20.83 304 17873 134519 29421831
Plasma cell myeloma recurrent 162.36 20.83 67 18110 3616 29552734
Plasma cell myeloma 161.47 20.83 153 18024 36962 29519388
Product physical issue 156.82 20.83 56 18121 2032 29554318
Full blood count decreased 153.79 20.83 105 18072 15887 29540463
Laboratory test abnormal 119.67 20.83 95 18082 18090 29538260
Fatigue 109.34 20.83 433 17744 316388 29239962
Constipation 108.01 20.83 225 17952 113935 29442415
Rash 106.73 20.83 306 17871 189513 29366837
Drug interaction 104.05 20.83 4 18173 197381 29358969
Adverse drug reaction 94.95 20.83 94 18083 23926 29532424
White blood cell count decreased 91.62 20.83 175 18002 83187 29473163
Influenza 83.10 20.83 115 18062 41766 29514584
Peripheral swelling 81.63 20.83 143 18034 63596 29492754
Product dose omission issue 80.81 20.83 181 17996 96202 29460148
Light chain analysis increased 80.68 20.83 29 18148 1072 29555278
Toxicity to various agents 66.61 20.83 13 18164 173648 29382702
COVID-19 61.34 20.83 92 18085 35922 29520428
Cytopenia 53.35 20.83 46 18131 9813 29546537
Accidental exposure to product 51.86 20.83 47 18130 10706 29545644
Back pain 50.73 20.83 158 18019 102126 29454224
Thrombosis 41.94 20.83 86 18091 42959 29513391
Monoclonal immunoglobulin present 41.85 20.83 17 18160 880 29555470
Product packaging issue 38.55 20.83 14 18163 533 29555817
Muscle spasms 38.41 20.83 107 18070 64975 29491375
Product blister packaging issue 37.72 20.83 9 18168 73 29556277
Product use in unapproved indication 36.62 20.83 5 18172 86870 29469480
Lower respiratory tract infection 35.89 20.83 61 18116 26441 29529909
Product packaging quantity issue 33.99 20.83 14 18163 751 29555599
Full blood count increased 33.48 20.83 14 18163 780 29555570
Tachycardia 30.91 20.83 4 18173 72406 29483944
Nausea 30.53 20.83 291 17886 288964 29267386
Neutropenia 29.45 20.83 159 18018 131552 29424798
Nasopharyngitis 29.38 20.83 92 18085 59573 29496777
Morganella infection 29.31 20.83 11 18166 460 29555890
Hypertension 27.52 20.83 19 18158 116595 29439755
Cryptosporidiosis infection 26.90 20.83 10 18167 407 29555943
Rhabdomyolysis 26.84 20.83 3 18174 60805 29495545
Asthenia 26.49 20.83 224 17953 215026 29341324
Illness 26.13 20.83 26 18151 6648 29549702
Condition aggravated 26 20.83 31 18146 146264 29410086
Bronchial haemorrhage 25.35 20.83 11 18166 672 29555678
Unevaluable event 24.88 20.83 56 18121 29795 29526555
JC virus CSF test positive 24.66 20.83 7 18170 118 29556232
Light chain disease 24.45 20.83 7 18170 122 29556228
Chillblains 24.36 20.83 5 18172 18 29556332
Laryngeal cancer metastatic 24.11 20.83 6 18171 59 29556291
Insomnia 23.94 20.83 113 18064 88648 29467702
Hypotension 23.51 20.83 53 18124 194301 29362049
Cataract 23.32 20.83 46 18131 22332 29534018
Spinal pain 22.94 20.83 21 18156 4843 29551507
Immunoglobulins decreased 21.84 20.83 10 18167 694 29555656
Plasmacytoma 21.57 20.83 17 18160 3198 29553152
Otitis externa bacterial 21.19 20.83 4 18173 8 29556342
Pneumonia influenzal 21.06 20.83 12 18165 1318 29555032
Seizure 20.89 20.83 16 18161 93107 29463243

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
Diarrhoea 600.76 19.91 971 21573 721733 63754455
Neuropathy peripheral 565.84 19.91 405 22139 117120 64359068
Pneumonia 517.85 19.91 791 21753 558785 63917403
Platelet count decreased 376.21 19.91 372 22172 167339 64308849
Off label use 359.00 19.91 722 21822 632084 63844104
Thrombocytopenia 330.01 19.91 398 22146 223403 64252785
Death 284.00 19.91 560 21984 482145 63994043
Plasma cell myeloma recurrent 220.05 19.91 74 22470 3991 64472197
Plasma cell myeloma 219.35 19.91 158 22386 45917 64430271
Product physical issue 160.23 19.91 56 22488 3393 64472795
No adverse event 152.26 19.91 105 22439 28456 64447732
White blood cell count decreased 145.69 19.91 224 22320 157613 64318575
Neutrophil count decreased 122.76 19.91 143 22401 77053 64399135
Product dose omission issue 121.15 19.91 232 22312 194515 64281673
Full blood count decreased 117.96 19.91 82 22462 22500 64453688
Rash 112.92 19.91 384 22160 458165 64018023
Constipation 98.45 19.91 235 22309 229102 64247086
Influenza 95.13 19.91 149 22395 106382 64369806
Drug interaction 84.26 19.91 13 22531 362070 64114118
Toxicity to various agents 74.15 19.91 18 22526 363495 64112693
Fatigue 72.71 19.91 478 22066 748252 63727936
Cytopenia 71.16 19.91 52 22492 15419 64460769
Nausea 71.13 19.91 493 22051 785307 63690881
Laboratory test abnormal 60.54 19.91 57 22487 24006 64452182
COVID-19 59.35 19.91 92 22452 65048 64411140
Product blister packaging issue 52.79 19.91 12 22532 144 64476044
Light chain analysis increased 52.28 19.91 19 22525 1289 64474899
Plasmacytoma 52.22 19.91 26 22518 3844 64472344
Dehydration 51.77 19.91 180 22364 216583 64259605
Product packaging quantity issue 46.08 19.91 16 22528 950 64475238
Drug ineffective 41.36 19.91 153 22391 840094 63636094
Pain 41.36 19.91 82 22462 553429 63922759
Neutropenia 39.39 19.91 177 22367 239447 64236741
Product packaging issue 38.29 19.91 14 22530 966 64475222
Body dysmorphic disorder 37.14 19.91 10 22534 249 64475939
Cardiac amyloidosis 36.68 19.91 15 22529 1400 64474788
Peripheral swelling 36.27 19.91 157 22387 208996 64267192
Accidental exposure to product 35.61 19.91 45 22499 26319 64449869
Vomiting 34.90 19.91 319 22225 550798 63925390
Hypertension 34.83 19.91 24 22520 259237 64216951
Anaemia 33.08 19.91 236 22308 378444 64097744
Adverse drug reaction 33.02 19.91 58 22486 45406 64430782
Drug hypersensitivity 31.96 19.91 22 22522 237793 64238395
Product use in unapproved indication 31.82 19.91 11 22533 176607 64299581
Muscle spasms 31.81 19.91 115 22429 140908 64335280
Headache 31.12 19.91 89 22455 529378 63946810
COVID-19 pneumonia 30.34 19.91 33 22511 16471 64459717
Hypotension 29.66 19.91 55 22489 380919 64095269
Tachycardia 29.31 19.91 8 22536 149571 64326617
Sepsis 29.17 19.91 158 22386 230183 64246005
Monoclonal immunoglobulin present 29.09 19.91 11 22533 834 64475354
Arthralgia 28.50 19.91 71 22473 442189 64033999
Pneumonia influenzal 28.40 19.91 15 22529 2507 64473681
Injection site pain 28.28 19.91 3 22541 111405 64364783
Cryptosporidiosis infection 28.12 19.91 10 22534 637 64475551
Asthenia 27.68 19.91 249 22295 427795 64048393
Musculoskeletal stiffness 27.33 19.91 5 22539 123201 64352987
Full blood count increased 27.31 19.91 9 22535 455 64475733
Vitiligo 27.22 19.91 13 22531 1755 64474433
Condition aggravated 27.06 19.91 56 22488 372370 64103818
Taste disorder 26.95 19.91 24 22520 9409 64466779
Cataract 26.92 19.91 57 22487 51205 64424983
JC virus CSF test positive 26.87 19.91 7 22537 153 64476035
Joint ankylosis 26.44 19.91 10 22534 759 64475429
Back pain 26.08 19.91 163 22381 250008 64226180
Hypercalcaemia 25.35 19.91 42 22502 31374 64444814
Upper respiratory tract inflammation 25.22 19.91 16 22528 3766 64472422
Light chain disease 24.82 19.91 7 22537 208 64475980
Herpes zoster 24.56 19.91 72 22472 79115 64397073
Immunoglobulins decreased 24.37 19.91 11 22533 1307 64474881
Cardiac failure 24.18 19.91 101 22443 132272 64343916
Hypoglossal nerve paresis 24.08 19.91 6 22538 109 64476079
Squamous cell carcinoma of skin 24.05 19.91 25 22519 11851 64464337
Morganella infection 23.83 19.91 10 22534 996 64475192
Nasopharyngitis 23.81 19.91 133 22411 195940 64280248
Treatment failure 23.35 19.91 6 22538 116810 64359378
Therapeutic product effect decreased 22.91 19.91 6 22538 115345 64360843
Laryngeal cancer metastatic 22.83 19.91 5 22539 50 64476138
VIth nerve paresis 22.82 19.91 6 22538 136 64476052
Infusion related reaction 22.37 19.91 15 22529 164452 64311736
Bronchial haemorrhage 21.96 19.91 10 22534 1212 64474976
Blood calcium abnormal 21.72 19.91 10 22534 1244 64474944
Blood immunoglobulin G increased 20.87 19.91 11 22533 1830 64474358
Polyneuropathy 20.82 19.91 30 22514 19864 64456324
Blood pressure increased 20.59 19.91 18 22526 172534 64303654
Hepatic enzyme increased 20.31 19.91 10 22534 129933 64346255

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
FDA EPC N0000175604 Proteasome Inhibitor
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D011480 Protease Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:50266 Prodrugs
CHEBI has role CHEBI:52726 proteasome inhibitors
CHEBI has role CHEBI:68495 Type I cell-death inducers
CHEBI has role CHEBI:71031 orphan drugs
CHEBI has role CHEBI:49103 drug metabolites

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 9233115 Aug. 12, 2024 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 9233115 Aug. 12, 2024 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 9233115 Aug. 12, 2024 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 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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 2.3MG BASE NINLARO TAKEDA PHARMS USA N208462 Nov. 20, 2015 RX CAPSULE ORAL Nov. 20, 2022 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 Nov. 20, 2022 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 Nov. 20, 2022 USE IN COMBINATION WITH LENALIDOMIDE AND DEXAMETHASONE FOR THE TREATMENT OF PATIENTS WITH MULTIPLE MYELOMA WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY

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

External reference:

IDSource
71050168A2 UNII
D10130 KEGG_DRUG
1239908-20-3 SECONDARY_CAS_RN
4035138 VANDF
C3273711 UMLSCUI
CHEBI:90942 CHEBI
6V8 PDB_CHEM_ID
CHEMBL2141296 ChEMBL_ID
25183872 PUBCHEM_CID
DB09570 DRUGBANK_ID
CHEMBL3545432 ChEMBL_ID
CHEMBL1813256 ChEMBL_ID
9411 INN_ID
C548400 MESH_SUPPLEMENTAL_RECORD_UI
C000595706 MESH_SUPPLEMENTAL_RECORD_UI
8450 IUPHAR_LIGAND_ID
1723734 RXNORM
237159 MMSL
31293 MMSL
d08398 MMSL
715256005 SNOMEDCT_US
781324002 SNOMEDCT_US
784168005 SNOMEDCT_US
016599 NDDF
016600 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
NINLARO HUMAN PRESCRIPTION DRUG LABEL 1 63020-078 CAPSULE 2.30 mg ORAL NDA 29 sections
NINLARO HUMAN PRESCRIPTION DRUG LABEL 1 63020-079 CAPSULE 3 mg ORAL NDA 29 sections
NINLARO HUMAN PRESCRIPTION DRUG LABEL 1 63020-080 CAPSULE 4 mg ORAL NDA 29 sections
NINLARO HUMAN PRESCRIPTION DRUG LABEL 1 63020-230 CAPSULE 2.30 mg ORAL NDA 33 sections
NINLARO HUMAN PRESCRIPTION DRUG LABEL 1 63020-230 CAPSULE 2.30 mg ORAL NDA 33 sections
NINLARO HUMAN PRESCRIPTION DRUG LABEL 1 63020-390 CAPSULE 3 mg ORAL NDA 33 sections
NINLARO HUMAN PRESCRIPTION DRUG LABEL 1 63020-390 CAPSULE 3 mg ORAL NDA 33 sections
NINLARO HUMAN PRESCRIPTION DRUG LABEL 1 63020-400 CAPSULE 4 mg ORAL NDA 33 sections
NINLARO HUMAN PRESCRIPTION DRUG LABEL 1 63020-400 CAPSULE 4 mg ORAL NDA 33 sections