ribociclib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
cyclin dependant kinase inhibitors 5218 1211441-98-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ribociclib
  • ribociclib succinate
  • LEE011
  • LEE 011
  • kisqali
  • LEE011-BBA
  • LEE011A
Ribociclib is an inhibitor of cyclin-dependent kinase (CDK) 4 and 6. These kinases are activated upon binding to D-cyclins and play a crucial role in signaling pathways which lead to cell cycle progression and cellular proliferation. The cyclin D-CDK4/6 complex regulates cell cycle progression through phosphorylation of the retinoblastoma protein (pRb). In vitro, ribociclib decreased pRb phosphorylation leading to arrest in the G1 phase of the cell cycle and reduced cell proliferation in breast cancer cell lines. In vivo, treatment with single agent ribociclib in a rat xenograft model with human tumor cells led to decreased tumor volumes, which correlated with inhibition of pRb phosphorylation. In studies using patient-derived estrogen receptor positive breast cancer xenograft models, combination of ribociclib and antiestrogen (e.g. letrozole) resulted in increased tumor growth inhibition compared to each drug alone.
  • Molecular weight: 434.55
  • Formula: C23H30N8O
  • CLOGP: 2.06
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 2
  • TPSA: 91.21
  • ALOGS: -3.28
  • ROTB: 5

  • Status: ONP

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

Drug dosage:

DoseUnitRoute
0.45 g O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Aug. 22, 2017 EMA Novartis Europharm Ltd
March 13, 2017 FDA NOVARTIS PHARMS CORP

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
Neutropenia 2334.22 20.12 1314 29207 146651 50427952
Leukopenia 1087.08 20.12 610 29911 66918 50507685
Malignant neoplasm progression 1084.79 20.12 611 29910 67513 50507090
Metastases to bone 678.20 20.12 291 30230 17704 50556899
Electrocardiogram QT prolonged 532.90 20.12 352 30169 51534 50523069
Metastases to liver 462.70 20.12 231 30290 19873 50554730
Hepatotoxicity 287.23 20.12 188 30333 27038 50547565
Aspartate aminotransferase increased 262.03 20.12 277 30244 77721 50496882
Alanine aminotransferase increased 257.21 20.12 291 30230 88068 50486535
Metastases to lung 251.60 20.12 126 30395 10894 50563709
Thrombocytopenia 249.08 20.12 344 30177 127329 50447274
General physical health deterioration 245.86 20.12 362 30159 142072 50432531
Drug ineffective 245.15 20.12 95 30426 819238 49755365
White blood cell count decreased 242.07 20.12 324 30197 116398 50458205
Gamma-glutamyltransferase increased 240.32 20.12 174 30347 29449 50545154
Skin hypopigmentation 239.01 20.12 59 30462 572 50574031
Neutrophil count decreased 225.18 20.12 201 30320 45825 50528778
Carbohydrate antigen 15-3 increased 218.29 20.12 62 30459 1070 50573533
Anaemia 192.46 20.12 451 30070 252005 50322598
Bone lesion 169.91 20.12 76 30445 5094 50569509
Bone pain 160.72 20.12 169 30352 47060 50527543
Polyneuropathy 158.57 20.12 96 30425 12035 50562568
Nausea 156.98 20.12 836 29685 704562 49870041
Pleural effusion 153.45 20.12 216 30305 81238 50493365
Off label use 148.09 20.12 51 30470 474375 50100228
Metastases to lymph nodes 141.98 20.12 74 30447 6950 50567653
Liver function test increased 135.54 20.12 117 30404 25489 50549114
Blood creatinine increased 133.23 20.12 195 30326 75965 50498638
Transaminases increased 123.28 20.12 115 30406 27709 50546894
Eastern Cooperative Oncology Group performance status worsened 123.27 20.12 35 30486 603 50574000
Hot flush 115.84 20.12 138 30383 44031 50530572
Tumour marker increased 112.15 20.12 52 30469 3788 50570815
Drug hypersensitivity 111.87 20.12 11 30510 250999 50323604
Breast cancer metastatic 105.42 20.12 70 30451 10294 50564309
PIK3CA-activated mutation 102.33 20.12 32 30489 778 50573825
Condition aggravated 99.57 20.12 28 30493 297030 50277573
Erysipelas 93.39 20.12 55 30466 6553 50568050
Fatigue 92.37 20.12 734 29787 706867 49867736
Arthropathy 82.00 20.12 3 30518 157903 50416700
Blood alkaline phosphatase increased 80.42 20.12 106 30415 37420 50537183
Blood bilirubin increased 70.98 20.12 92 30429 31946 50542657
Carcinoembryonic antigen increased 69.50 20.12 28 30493 1446 50573157
Metastases to pleura 69.23 20.12 27 30494 1279 50573324
Metastases to central nervous system 68.88 20.12 56 30465 11226 50563377
Lymphoedema 68.10 20.12 51 30470 9071 50565532
Ascites 65.83 20.12 94 30427 35767 50538836
Hypertensive crisis 65.36 20.12 58 30463 13096 50561507
Pyelitis 63.83 20.12 16 30505 166 50574437
Glomerular filtration rate decreased 63.18 20.12 54 30467 11598 50563005
Taste disorder 63.17 20.12 47 30474 8277 50566326
Bone marrow infiltration 61.27 20.12 19 30502 449 50574154
Joint swelling 61.27 20.12 36 30485 245250 50329353
Metastases to spine 60.59 20.12 31 30490 2800 50571803
Hypotension 59.60 20.12 34 30487 235435 50339168
Dry skin 59.31 20.12 99 30422 43092 50531511
Sinusitis 59.11 20.12 15 30506 170543 50404060
Metastasis 58.13 20.12 35 30486 4340 50570263
Lacrimation increased 58.10 20.12 61 30460 16931 50557672
Osteonecrosis of jaw 57.86 20.12 84 30437 32442 50542161
Hypocalcaemia 56.29 20.12 75 30446 26741 50547862
Treatment failure 54.11 20.12 9 30512 137628 50436975
Product use issue 54.05 20.12 12 30509 149463 50425140
Alopecia 53.61 20.12 290 30231 244757 50329846
Decreased appetite 53.23 20.12 251 30270 200672 50373931
Breast cancer recurrent 51.99 20.12 31 30490 3777 50570826
Calcium deficiency 51.63 20.12 20 30501 930 50573673
Blood lactate dehydrogenase increased 51.06 20.12 61 30460 19501 50555102
Electrocardiogram PR shortened 50.62 20.12 14 30507 218 50574385
Constipation 49.92 20.12 233 30288 185475 50389128
Spinal pain 48.50 20.12 45 30476 10758 50563845
Isosthenuria 45.39 20.12 11 30510 98 50574505
Haemoglobin decreased 45.36 20.12 174 30347 127042 50447561
Toxicity to various agents 45.33 20.12 37 30484 212462 50362141
Vitiligo 44.53 20.12 19 30502 1135 50573468
Urinary tract inflammation 44.10 20.12 9 30512 32 50574571
Swelling 44.07 20.12 34 30487 200838 50373765
Pneumonitis 42.34 20.12 69 30452 29441 50545162
Anisocytosis 41.70 20.12 15 30506 566 50574037
Musculoskeletal stiffness 41.35 20.12 13 30508 128468 50446135
Weight increased 40.81 20.12 37 30484 201854 50372749
Hepatic lesion 40.58 20.12 27 30494 3981 50570622
Tumour pain 40.15 20.12 18 30503 1212 50573391
Hypersensitivity 39.40 20.12 43 30478 215118 50359485
Wound 39.25 20.12 8 30513 105786 50468817
Elliptocytosis 38.66 20.12 8 30513 31 50574572
Decreased immune responsiveness 38.59 20.12 26 30495 3915 50570688
Metastases to peritoneum 38.51 20.12 23 30498 2810 50571793
Disease progression 38.25 20.12 136 30385 95730 50478873
Bladder hypertrophy 37.78 20.12 11 30510 208 50574395
Drug intolerance 37.73 20.12 46 30475 219058 50355545
Breast pain 36.95 20.12 33 30488 7511 50567092
Fall 36.29 20.12 94 30427 334838 50239765
Neutrophil count abnormal 36.15 20.12 21 30500 2438 50572165
Haematotoxicity 35.66 20.12 33 30488 7862 50566741
Hepatobiliary disease 34.96 20.12 11 30510 273 50574330
Cardiac failure congestive 34.33 20.12 5 30516 84377 50490226
Arthritis 33.35 20.12 6 30515 86715 50487888
Injection site pain 32.70 20.12 13 30508 111011 50463592
CYP3A4 polymorphism 32.18 20.12 8 30513 80 50574523
Lymphocyte count decreased 31.79 20.12 57 30464 26250 50548353
Hepatic failure 31.66 20.12 64 30457 32219 50542384
C-reactive protein increased 31.55 20.12 100 30421 66374 50508229
Loss of personal independence in daily activities 31.34 20.12 3 30518 70047 50504556
Seizure 31.28 20.12 16 30505 117858 50456745
Concomitant disease aggravated 31.21 20.12 31 30490 8060 50566543
Neoplasm 31.17 20.12 27 30494 5901 50568702
Loss of consciousness 31.09 20.12 12 30509 104341 50470262
Psoriasis 30.75 20.12 3 30518 68997 50505606
Dry eye 30.73 20.12 63 30458 32032 50542571
Asthma 30.66 20.12 8 30513 89329 50485274
Therapy partial responder 30.64 20.12 28 30493 6563 50568040
Abdominal discomfort 29.96 20.12 59 30462 231582 50343021
Discomfort 29.84 20.12 14 30507 108366 50466237
Urticaria 29.60 20.12 21 30500 129540 50445063
Sinus arrhythmia 29.32 20.12 15 30506 1354 50573249
Dyspnoea exertional 28.97 20.12 82 30439 51151 50523452
Sleep disorder 28.87 20.12 88 30433 57195 50517408
Adjusted calcium decreased 28.84 20.12 8 30513 126 50574477
Mucosal inflammation 28.57 20.12 70 30451 40072 50534531
Hypermetabolism 27.39 20.12 8 30513 153 50574450
Skin toxicity 27.27 20.12 21 30500 3892 50570711
Radiation oesophagitis 27.21 20.12 9 30512 263 50574340
Intentional overdose 27.12 20.12 3 30518 62501 50512102
Hyperchromic anaemia 26.69 20.12 6 30515 37 50574566
Product dose omission issue 26.28 20.12 44 30477 183794 50390809
Blood phosphorus decreased 25.68 20.12 20 30501 3769 50570834
Jaundice 25.45 20.12 52 30469 26377 50548226
Red blood cell count decreased 25.14 20.12 60 30461 33775 50540828
Adjusted calcium increased 24.91 20.12 5 30516 16 50574587
Hydrothorax 24.83 20.12 11 30510 720 50573883
COVID-19 24.76 20.12 73 30448 46589 50528014
Overdose 24.35 20.12 15 30506 99712 50474891
Tumour marker decreased 24.32 20.12 6 30515 58 50574545
Malaise 24.24 20.12 112 30409 335420 50239183
Creatinine renal clearance increased 23.91 20.12 10 30511 568 50574035
Invasive breast carcinoma 23.80 20.12 10 30511 575 50574028
Lower respiratory tract infection 23.69 20.12 14 30507 95187 50479416
Metastases to skin 23.54 20.12 13 30508 1370 50573233
Lymphadenopathy 23.39 20.12 58 30463 33441 50541162
Electrocardiogram QT interval abnormal 23.13 20.12 7 30514 152 50574451
Osteolysis 22.98 20.12 16 30505 2541 50572062
Gastrointestinal haemorrhage 22.57 20.12 8 30513 73313 50501290
Oxygen saturation decreased 22.53 20.12 8 30513 73240 50501363
Wheezing 22.38 20.12 5 30516 62042 50512561
Monocyte count decreased 22.28 20.12 14 30507 1872 50572731
Skin reaction 22.22 20.12 31 30490 11537 50563066
Malignant pleural effusion 21.93 20.12 15 30506 2315 50572288
Migraine 21.86 20.12 9 30512 75271 50499332
Haematocrit decreased 21.78 20.12 58 30463 34918 50539685
Back pain 21.56 20.12 215 30306 219815 50354788
Aspartate aminotransferase abnormal 21.38 20.12 11 30510 1005 50573598
Pleural disorder 21.07 20.12 9 30512 539 50574064
Irritable bowel syndrome 21.03 20.12 3 30518 51438 50523165
Oedema peripheral 20.97 20.12 165 30356 157796 50416807
Suicidal ideation 20.93 20.12 4 30517 55381 50519222
Bone sequestrum 20.87 20.12 12 30509 1366 50573237
Blood cholesterol increased 20.84 20.12 4 30517 55211 50519392
Metastases to thorax 20.77 20.12 7 30514 217 50574386
Poikilocytosis 20.73 20.12 6 30515 111 50574492
Pruritus 20.49 20.12 261 30260 283307 50291296
Second primary malignancy 20.45 20.12 23 30498 6891 50567712
Hyperbilirubinaemia 20.44 20.12 27 30494 9543 50565060
Basophil count increased 20.43 20.12 10 30511 822 50573781
Trichorrhexis 20.28 20.12 11 30510 1119 50573484
Onychoclasis 20.21 20.12 20 30501 5176 50569427
Mean cell haemoglobin increased 20.20 20.12 14 30507 2206 50572397

FDA Adverse Event Reporting System (Male)

None

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
Neutropenia 1039.52 19.75 686 15932 238938 64243176
Metastases to bone 541.16 19.75 202 16416 20233 64461881
Malignant neoplasm progression 508.30 19.75 332 16286 112539 64369575
Metastases to liver 329.09 19.75 148 16470 23793 64458321
Electrocardiogram QT prolonged 316.97 19.75 217 16401 79231 64402883
Skin hypopigmentation 264.50 19.75 58 16560 813 64481301
Bone lesion 209.24 19.75 70 16548 5067 64477047
Carbohydrate antigen 15-3 increased 193.42 19.75 46 16572 941 64481173
Metastases to lung 192.77 19.75 89 16529 15175 64466939
Leukopenia 169.74 19.75 167 16451 101075 64381039
Hepatotoxicity 168.32 19.75 113 16505 39849 64442265
White blood cell count decreased 145.80 19.75 191 16427 157646 64324468
Neutrophil count decreased 128.69 19.75 127 16491 77069 64405045
Metastases to lymph nodes 126.44 19.75 56 16562 8661 64473453
Tumour marker increased 105.63 19.75 38 16580 3412 64478702
Alanine aminotransferase increased 105.38 19.75 153 16465 138878 64343236
Breast cancer metastatic 103.80 19.75 46 16572 7123 64474991
Nausea 95.65 19.75 427 16191 785373 63696741
Aspartate aminotransferase increased 93.93 19.75 134 16484 119654 64362460
Bone pain 86.26 19.75 82 16536 47490 64434624
Gamma-glutamyltransferase increased 77.45 19.75 78 16540 48432 64433682
Thrombocytopenia 71.85 19.75 170 16448 223631 64258483
Drug ineffective 69.25 19.75 69 16549 840178 63641936
Off label use 68.72 19.75 39 16579 632767 63849347
PIK3CA-activated mutation 65.32 19.75 17 16601 508 64481606
Breast cancer recurrent 62.73 19.75 24 16594 2559 64479555
Carcinoembryonic antigen increased 62.53 19.75 22 16596 1851 64480263
Anaemia 61.06 19.75 225 16393 378455 64103659
Electrocardiogram PR shortened 60.24 19.75 14 16604 258 64481856
Liver function test increased 59.22 19.75 55 16563 30915 64451199
Pleural effusion 56.54 19.75 110 16508 126449 64355665
Transaminases increased 55.78 19.75 63 16555 44531 64437583
Blood creatinine increased 54.66 19.75 113 16505 135669 64346445
Isosthenuria 54.41 19.75 11 16607 101 64482013
Condition aggravated 49.72 19.75 17 16601 372409 64109705
Anisocytosis 48.40 19.75 15 16603 848 64481266
Metastasis 47.37 19.75 25 16593 5670 64476444
Decreased immune responsiveness 47.14 19.75 23 16595 4425 64477689
Urinary tract inflammation 45.74 19.75 9 16609 71 64482043
Elliptocytosis 45.45 19.75 8 16610 31 64482083
Metastases to spine 45.22 19.75 21 16597 3622 64478492
Hypotension 44.95 19.75 21 16597 380953 64101161
Pyelitis 44.03 19.75 11 16607 278 64481836
Fatigue 42.86 19.75 334 16284 748396 63733718
Metastases to pleura 42.78 19.75 15 16603 1249 64480865
Metastases to central nervous system 41.66 19.75 32 16586 13880 64468234
Haemoglobin decreased 40.24 19.75 126 16492 194937 64287177
Blood alkaline phosphatase increased 39.77 19.75 60 16558 56219 64425895
Hot flush 39.58 19.75 54 16564 46181 64435933
Blood bilirubin increased 38.76 19.75 60 16558 57493 64424621
Hepatic lesion 38.59 19.75 22 16596 5802 64476312
Vitiligo 37.88 19.75 15 16603 1753 64480361
Bladder hypertrophy 36.74 19.75 11 16607 553 64481561
Alopecia 36.00 19.75 109 16509 165581 64316533
Fall 35.62 19.75 33 16585 416793 64065321
Pruritus 35.60 19.75 167 16451 312233 64169881
Eastern Cooperative Oncology Group performance status worsened 35.42 19.75 13 16605 1235 64480879
Trichorrhexis 34.10 19.75 11 16607 709 64481405
CYP3A4 polymorphism 34.08 19.75 7 16611 70 64482044
Adjusted calcium decreased 33.99 19.75 8 16610 156 64481958
Neutrophil count abnormal 33.80 19.75 16 16602 2880 64479234
Blood phosphorus decreased 33.69 19.75 20 16598 5685 64476429
Lymphadenopathy 33.31 19.75 50 16568 46636 64435478
Drug hypersensitivity 33.22 19.75 10 16608 237805 64244309
Haematotoxicity 32.91 19.75 27 16591 12869 64469245
General physical health deterioration 32.45 19.75 121 16497 204304 64277810
Therapy partial responder 31.63 19.75 24 16594 10224 64471890
Tumour marker decreased 30.64 19.75 6 16612 46 64482068
Back pain 30.16 19.75 136 16482 250035 64232079
Lymphocyte count decreased 29.62 19.75 44 16574 40655 64441459
Hypermetabolism 28.86 19.75 8 16610 305 64481809
Dry skin 28.56 19.75 49 16569 51112 64431002
Creatinine renal clearance increased 28.37 19.75 10 16608 846 64481268
Metastases to peritoneum 27.89 19.75 15 16603 3532 64478582
BRCA1 gene mutation 27.54 19.75 5 16613 24 64482090
Glomerular filtration rate decreased 26.79 19.75 29 16589 19543 64462571
Red blood cell count decreased 26.56 19.75 46 16572 48340 64433774
Nail avulsion 26.38 19.75 6 16612 100 64482014
Hypocalcaemia 25.99 19.75 42 16576 41711 64440403
Toxicity to various agents 25.31 19.75 34 16584 363479 64118635
Osteolysis 25.30 19.75 13 16605 2790 64479324
Disease progression 25.14 19.75 87 16531 141593 64340521
Metastases to the mediastinum 24.64 19.75 8 16610 526 64481588
Taste disorder 24.59 19.75 20 16598 9413 64472701
Adjusted calcium increased 24.17 19.75 5 16613 52 64482062
Blood calcium increased 24.17 19.75 19 16599 8523 64473591
Metastases to uterus 23.75 19.75 5 16613 57 64482057
Spinal pain 23.32 19.75 22 16596 12599 64469515
Hepatobiliary disease 23.05 19.75 8 16610 646 64481468
Breast pain 22.82 19.75 17 16601 7044 64475070
Haematocrit decreased 22.57 19.75 46 16572 54609 64427505
Depressed mood 22.52 19.75 39 16579 40973 64441141
Joint swelling 22.26 19.75 14 16604 215368 64266746
Pleural disorder 22.17 19.75 8 16610 724 64481390
Calcium deficiency 22.11 19.75 8 16610 730 64481384
Rouleaux formation 21.79 19.75 3 16615 0 64482114
Vomiting 21.71 19.75 227 16391 550890 63931224
Hydrothorax 21.25 19.75 9 16609 1248 64480866
Cardiac failure congestive 21.15 19.75 4 16614 130576 64351538
Metastases to ovary 20.99 19.75 6 16612 256 64481858
Mean cell haemoglobin increased 20.96 19.75 12 16606 3190 64478924
Sinus arrhythmia 20.81 19.75 10 16608 1860 64480254
Psychomotor disadaptation syndrome 20.62 19.75 4 16614 29 64482085
Sinusitis 20.62 19.75 6 16612 145922 64336192
Breast cancer 20.48 19.75 31 16587 29117 64452997
Poikilocytosis 20.41 19.75 6 16612 283 64481831
Constipation 20.10 19.75 114 16504 229223 64252891
Pleural thickening 20.03 19.75 11 16607 2699 64479415
Breast mass 19.93 19.75 14 16604 5296 64476818

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EF02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Cyclin-dependent kinase (CDK) inhibitors
FDA MoA N0000175082 Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000190114 Cytochrome P450 3A Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hormone receptor positive malignant neoplasm of breast indication 417181009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.03 Basic
pKa2 6.09 Basic
pKa3 5.48 Basic
pKa4 0.57 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 9416136 Aug. 20, 2029 IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR THE TREATMENT OF ADULT PATIENTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 9416136 Aug. 20, 2029 IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR TREATMENT OF POSTMENOPAUSAL WOMEN WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER-2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 9416136 Aug. 20, 2029 IN COMBINATION WITH AN AROMATASE INHIBITOR FOR THE TREATMENT OF PRE/PERIMENOPAUSAL OR POSTMENOPAUSAL WOMEN WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER, AS INITIAL ENDOCRINE-BASED THERAPY
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 9416136 Aug. 20, 2029 IN COMBINATION WITH FULVESTRANT AS INITIAL ENDOCRINE-BASED THERAPY OR FOLLOWING DISEASE PROGRESSION ON ENDOCRINE THERAPY IN POSTMENOPAUSAL WOMEN OR IN MEN, FOR THE TREATMENT OF HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 9416136 Aug. 20, 2029 IN COMBINATION WITH FULVESTRANT FOR THE TREATMENT OF POSTMENOPAUSAL WOMEN WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER, AS INITIAL ENDOCRINE BASED THERAPY OR FOLLOWING DISEASE PROGRESSION ON ENDOCRINE THERAPY
2.5MG;EQ 200MG BASE KISQALI FEMARA CO-PACK (COPACKAGED) NOVARTIS N209935 May 4, 2017 RX TABLET ORAL 9416136 Aug. 20, 2029 AS INITIAL ENDOCRINE-BASED THERAPY FOR THE TREATMENT OF ADULT PATIENTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
2.5MG;EQ 200MG BASE KISQALI FEMARA CO-PACK (COPACKAGED) NOVARTIS N209935 May 4, 2017 RX TABLET ORAL 9416136 Aug. 20, 2029 TREATMENT OF PRE/PERIMENOPAUSAL WOMEN WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 8962630 Dec. 9, 2029 IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR THE TREATMENT OF ADULT PATIENTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 8962630 Dec. 9, 2029 IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR TREATMENT OF POSTMENOPAUSAL WOMEN WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER-2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 8962630 Dec. 9, 2029 IN COMBINATION WITH AN AROMATASE INHIBITOR FOR THE TREATMENT OF PRE/PERIMENOPAUSAL OR POSTMENOPAUSAL WOMEN WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER, AS INITIAL ENDOCRINE-BASED THERAPY
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 8962630 Dec. 9, 2029 IN COMBINATION WITH FULVESTRANT AS INITIAL ENDOCRINE-BASED THERAPY OR FOLLOWING DISEASE PROGRESSION ON ENDOCRINE THERAPY IN POSTMENOPAUSAL WOMEN OR IN MEN, FOR THE TREATMENT OF HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 8962630 Dec. 9, 2029 IN COMBINATION WITH FULVESTRANT FOR THE TREATMENT OF POSTMENOPAUSAL WOMEN WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER, AS INITIAL ENDOCRINE BASED THERAPY OR FOLLOWING DISEASE PROGRESSION ON ENDOCRINE THERAPY
2.5MG;EQ 200MG BASE KISQALI FEMARA CO-PACK (COPACKAGED) NOVARTIS N209935 May 4, 2017 RX TABLET ORAL 8962630 Dec. 9, 2029 AS INITIAL ENDOCRINE-BASED THERAPY FOR THE TREATMENT OF ADULT PATIENTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
2.5MG;EQ 200MG BASE KISQALI FEMARA CO-PACK (COPACKAGED) NOVARTIS N209935 May 4, 2017 RX TABLET ORAL 8962630 Dec. 9, 2029 TREATMENT OF PRE/PERIMENOPAUSAL WOMEN WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 9868739 Nov. 9, 2031 IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR THE TREATMENT OF ADULT PATIENTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 9868739 Nov. 9, 2031 IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR TREATMENT OF POSTMENOPAUSAL WOMEN WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER-2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 9868739 Nov. 9, 2031 IN COMBINATION WITH AN AROMATASE INHIBITOR FOR THE TREATMENT OF PRE/PERIMENOPAUSAL OR POSTMENOPAUSAL WOMEN WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER, AS INITIAL ENDOCRINE-BASED THERAPY
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 9868739 Nov. 9, 2031 IN COMBINATION WITH FULVESTRANT AS INITIAL ENDOCRINE-BASED THERAPY OR FOLLOWING DISEASE PROGRESSION ON ENDOCRINE THERAPY IN POSTMENOPAUSAL WOMEN OR IN MEN, FOR THE TREATMENT OF HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 9868739 Nov. 9, 2031 IN COMBINATION WITH FULVESTRANT FOR THE TREATMENT OF POSTMENOPAUSAL WOMEN WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER, AS INITIAL ENDOCRINE BASED THERAPY OR FOLLOWING DISEASE PROGRESSION ON ENDOCRINE THERAPY
2.5MG;EQ 200MG BASE KISQALI FEMARA CO-PACK (COPACKAGED) NOVARTIS N209935 May 4, 2017 RX TABLET ORAL 9868739 Nov. 9, 2031 AS INITIAL ENDOCRINE-BASED THERAPY FOR THE TREATMENT OF ADULT PATIENTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
2.5MG;EQ 200MG BASE KISQALI FEMARA CO-PACK (COPACKAGED) NOVARTIS N209935 May 4, 2017 RX TABLET ORAL 9868739 Nov. 9, 2031 TREATMENT OF PRE/PERIMENOPAUSAL WOMEN WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL March 13, 2022 NEW CHEMICAL ENTITY
2.5MG;EQ 200MG BASE KISQALI FEMARA CO-PACK (COPACKAGED) NOVARTIS N209935 May 4, 2017 RX TABLET ORAL March 13, 2022 NEW CHEMICAL ENTITY
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL Dec. 10, 2024 NEW PATIENT POPULATION
2.5MG;EQ 200MG BASE KISQALI FEMARA CO-PACK (COPACKAGED) NOVARTIS N209935 May 4, 2017 RX TABLET ORAL Dec. 10, 2024 NEW PATIENT POPULATION

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Cyclin-dependent kinase 6 Kinase INHIBITOR IC50 7.41 SCIENTIFIC LITERATURE DRUG LABEL
Cyclin-dependent kinase 4 Kinase INHIBITOR IC50 8 SCIENTIFIC LITERATURE DRUG LABEL
Calcium/calmodulin-dependent protein kinase type II subunit gamma Kinase Kd 6.61 CHEMBL
Cyclin-G-associated kinase Kinase Kd 6.18 CHEMBL
Cyclin-dependent kinase 16 Kinase Kd 5.42 CHEMBL
Cyclin-dependent kinase 9 Kinase Kd 5.43 CHEMBL
Cyclin-dependent kinase 2 Kinase IC50 4.12 CHEMBL
Serine/threonine-protein kinase D2 Kinase Kd 4.60 CHEMBL
Mitogen-activated protein kinase kinase kinase 1 Kinase Kd 4.90 CHEMBL
Ferrochelatase, mitochondrial Enzyme Kd 4.91 CHEMBL
Uncharacterized protein FLJ45252 Unclassified Kd 5.03 CHEMBL
Serine/threonine-protein kinase SIK2 Kinase Kd 5.60 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta Kinase Kd 6.53 CHEMBL

External reference:

IDSource
TK8ERE8P56 UNII
C4045494 UMLSCUI
6ZZ PDB_CHEM_ID
CHEMBL3545110 ChEMBL_ID
44631912 PUBCHEM_CID
DB11730 DRUGBANK_ID
CHEMBL3707266 ChEMBL_ID
D10883 KEGG_DRUG
7383 IUPHAR_LIGAND_ID
1873916 RXNORM
254040 MMSL
32443 MMSL
d08533 MMSL
732257004 SNOMEDCT_US
732258009 SNOMEDCT_US
763537002 SNOMEDCT_US
4036504 VANDF
017131 NDDF
017132 NDDF
C000589651 MESH_SUPPLEMENTAL_RECORD_UI
9968 INN_ID
1374639-75-4 SECONDARY_CAS_RN

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
KISQALI HUMAN PRESCRIPTION DRUG LABEL 1 0078-0860 TABLET, FILM COATED 200 mg ORAL NDA 33 sections
KISQALI HUMAN PRESCRIPTION DRUG LABEL 1 0078-0860 TABLET, FILM COATED 200 mg ORAL NDA 33 sections
KISQALI HUMAN PRESCRIPTION DRUG LABEL 1 0078-0867 TABLET, FILM COATED 200 mg ORAL NDA 33 sections
KISQALI HUMAN PRESCRIPTION DRUG LABEL 1 0078-0867 TABLET, FILM COATED 200 mg ORAL NDA 33 sections
KISQALI HUMAN PRESCRIPTION DRUG LABEL 1 0078-0874 TABLET, FILM COATED 200 mg ORAL NDA 33 sections
KISQALI HUMAN PRESCRIPTION DRUG LABEL 1 0078-0874 TABLET, FILM COATED 200 mg ORAL NDA 33 sections