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

PropertyValueReference
S (Water solubility) 0.80 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class AAK1,ABL1,ABL2,ACVR2A,ACVR2B,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK9,CHEK1,CHEK2,CLK1,CLK2,CLK4,CSF1R,DDR1,DYRK1A,DYRK1B,DYRK2,DYRK3,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB4,ERBB2,ERBB4,FGFR1,FLT1,FLT3,FYN,GAK,GRK2,GSK3B,HASPIN,HIPK2,IGF1R,INSR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK15,MAPK7,MAPK9,MARK1,MARK4,MELK,MET,MINK1,MKNK1,MKNK2,MST1R,NTRK1,NTRK2,NUAK1,PAK2,PAK4,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CD,PIK3CG,PIM1,PIM2,PIM3,PLK1,PLK2,PLK3,PLK4,PRKAA1,PRKAA2,PRKCD,PRKDC,PTK2,RET,RIPK3,RPS6KA1,SIK2,SIK3,SRC,STK17A,STK33,STK4,SYK,TBK1,TEK,TNIK,TNK1,TTK,TYRO3,ULK1,ULK2,YES1 140
kinase-selectivity-class ACVR2B,ALK,AURKB,AXL,CAMK2A,CAMK2B,CAMK2D,CDK16,CDK4,CDK6,CHEK1,CLK2,CLK4,CSF1R,DDR1,DYRK1B,EGFR,FLT3,GAK,IRAK1,IRAK3,JAK1,LRRK2,MAP3K11,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK7,MARK4,MELK,NTRK1,PDK1,PRKAA2,SIK2,SIK3,STK33,SYK,TNK1,TTK,ULK1,ULK2 42
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 11.482 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
rat-kpuu-brain Rat brain Kpuu 0.015 % High 1

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 6019.00 19.41 3101 68155 221803 90335388
Malignant neoplasm progression 2964.96 19.41 1515 69741 105355 90451836
Leukopenia 2196.64 19.41 1217 70039 99493 90457698
Metastases to bone 1979.18 19.41 747 70509 24758 90532433
Metastases to liver 1463.75 19.41 622 70634 28185 90529006
Electrocardiogram QT prolonged 1460.08 19.41 832 70424 71624 90485567
Hepatotoxicity 908.31 19.41 521 70735 45321 90511870
Alanine aminotransferase increased 855.25 19.41 723 70533 117615 90439576
Aspartate aminotransferase increased 833.77 19.41 672 70584 102265 90454926
Neutrophil count decreased 718.98 19.41 531 70725 71001 90486190
Metastases to lung 658.48 19.41 298 70958 15693 90541498
Carbohydrate antigen 15-3 increased 650.80 19.41 175 71081 1832 90555359
White blood cell count decreased 618.21 19.41 708 70548 166401 90390790
Anaemia 502.56 19.41 952 70304 351850 90205341
Gamma-glutamyltransferase increased 491.14 19.41 329 70927 37623 90519568
Thrombocytopenia 458.38 19.41 684 70572 208041 90349150
Drug ineffective 420.71 19.41 289 70967 1384009 89173182
Transaminases increased 407.36 19.41 291 70965 36901 90520290
Blood creatinine increased 406.07 19.41 448 70808 100938 90456253
Polyneuropathy 367.35 19.41 214 71042 19127 90538064
Bone pain 358.18 19.41 334 70922 61649 90495542
Metastases to lymph nodes 355.95 19.41 177 71079 11512 90545679
Pleural effusion 332.87 19.41 425 70831 111566 90445625
Hepatic cytolysis 325.06 19.41 236 71020 30680 90526511
Liver function test increased 322.64 19.41 365 70891 84490 90472701
Tumour marker increased 313.40 19.41 131 71125 5676 90551515
Infusion related reaction 311.35 19.41 3 71253 416777 90140414
Carcinoembryonic antigen increased 309.05 19.41 102 71154 2248 90554943
Nausea 284.87 19.41 1661 69595 1108655 89448536
Bone lesion 284.22 19.41 126 71130 6311 90550880
Hot flush 261.07 19.41 276 70980 59212 90497979
Blood alkaline phosphatase increased 254.74 19.41 247 71009 47832 90509359
Osteonecrosis of jaw 253.85 19.41 225 71031 38878 90518313
Joint swelling 249.44 19.41 47 71209 503253 90053938
Breast cancer metastatic 242.18 19.41 150 71106 14982 90542209
Rheumatoid arthritis 242.13 19.41 10 71246 362604 90194587
Arthropathy 238.36 19.41 12 71244 366230 90190961
Drug hypersensitivity 236.86 19.41 40 71216 463569 90093622
Blood bilirubin increased 235.34 19.41 226 71030 43244 90513947
Eastern Cooperative Oncology Group performance status worsened 230.50 19.41 78 71178 1861 90555330
Ascites 230.21 19.41 233 71023 47507 90509684
Glossodynia 228.81 19.41 5 71251 321774 90235417
Condition aggravated 210.22 19.41 103 71153 595442 89961749
General physical health deterioration 203.85 19.41 678 70578 354437 90202754
Haematotoxicity 202.48 19.41 125 71131 12410 90544781
Therapeutic product effect decreased 194.68 19.41 5 71251 277566 90279625
Metastases to pleura 192.06 19.41 69 71187 1975 90555216
Skin hypopigmentation 187.00 19.41 59 71197 1120 90556071
Treatment failure 185.60 19.41 14 71242 303914 90253277
Hepatic lesion 184.92 19.41 90 71166 5583 90551608
Fatigue 180.60 19.41 1532 69724 1152491 89404700
Sinusitis 176.48 19.41 29 71227 343059 90214132
PIK3CA-activated mutation 173.46 19.41 56 71200 1148 90556043
Product use issue 171.69 19.41 27 71229 329892 90227299
Wound 171.51 19.41 19 71237 302961 90254230
Spinal pain 164.89 19.41 120 71136 15647 90541544
Metastasis 163.72 19.41 85 71171 6052 90551139
Vitiligo 160.57 19.41 61 71195 2049 90555142
Death 159.73 19.41 746 70510 455805 90101386
Swelling 159.47 19.41 65 71191 418993 90138198
Glomerular filtration rate decreased 157.25 19.41 120 71136 16812 90540379
Pneumonitis 156.02 19.41 183 71073 43987 90513204
Intentional product use issue 155.61 19.41 3 71253 216889 90340302
Irritable bowel syndrome 148.30 19.41 3 71253 207445 90349746
Fibromyalgia 147.39 19.41 3 71253 206266 90350925
Therapy partial responder 145.36 19.41 128 71128 21915 90535276
Metastases to spine 142.25 19.41 66 71190 3677 90553514
Skin toxicity 142.06 19.41 80 71176 6699 90550492
Second primary malignancy 141.52 19.41 93 71163 10285 90546906
Erysipelas 135.46 19.41 86 71170 8966 90548225
Helicobacter infection 134.17 19.41 12 71244 226838 90330353
Wheezing 132.04 19.41 16 71240 238064 90319127
Breast cancer recurrent 132.01 19.41 71 71185 5432 90551759
Weight increased 127.73 19.41 86 71170 417841 90139350
Jaundice 125.42 19.41 141 71115 32376 90524815
Lower respiratory tract infection 124.89 19.41 23 71233 250636 90306555
Haemoglobin decreased 122.56 19.41 341 70915 161615 90395576
Asthma 121.12 19.41 22 71234 242138 90315053
Injury 120.69 19.41 9 71247 197340 90359851
Musculoskeletal stiffness 119.42 19.41 42 71214 296490 90260701
Bone marrow infiltration 116.57 19.41 38 71218 804 90556387
Metastases to central nervous system 115.94 19.41 102 71154 17440 90539751
Lymphoedema 115.83 19.41 92 71164 13661 90543530
Disease progression 115.80 19.41 327 70929 156288 90400903
Dry skin 115.52 19.41 230 71026 87843 90469348
Hepatic failure 112.01 19.41 147 71109 39581 90517610
Type 2 diabetes mellitus 109.46 19.41 15 71241 203229 90353962
Urticaria 107.29 19.41 56 71200 312678 90244513
Decreased immune responsiveness 106.34 19.41 73 71183 8675 90548516
Renal failure 106.26 19.41 283 70973 130724 90426467
Discomfort 105.19 19.41 42 71214 274293 90282898
Abdominal discomfort 102.67 19.41 135 71121 477193 90079998
Off label use 101.73 19.41 484 70772 1101768 89455423
Blood cholesterol increased 101.67 19.41 20 71236 207992 90349199
Hypersensitivity 100.47 19.41 126 71130 454551 90102640
Myelosuppression 98.40 19.41 162 71094 53429 90503762
Confusional state 97.41 19.41 96 71160 386109 90171082
Therapeutic product effect incomplete 94.01 19.41 19 71237 193877 90363314
Neoplasm 93.63 19.41 68 71188 8835 90548356
Blister 91.46 19.41 43 71213 254955 90302236
Impaired healing 91.18 19.41 35 71221 234164 90323027
Onychoclasis 90.55 19.41 62 71194 7337 90549854
Loss of personal independence in daily activities 89.94 19.41 4 71252 136101 90421090
Lacrimation increased 88.78 19.41 108 71148 26954 90530237
Hypotension 87.82 19.41 76 71180 325321 90231870
Constipation 84.17 19.41 439 70817 279956 90277235
Concomitant disease aggravated 82.24 19.41 70 71186 11448 90545743
Arthritis 81.94 19.41 16 71240 167299 90389892
Electrocardiogram QT interval abnormal 81.82 19.41 22 71234 230 90556961
Blood lactate dehydrogenase increased 81.05 19.41 101 71155 25831 90531360
Hydrothorax 79.10 19.41 30 71226 1003 90556188
Adverse event 79.10 19.41 3 71253 117415 90439776
Coronavirus infection 79.06 19.41 51 71205 5464 90551727
Drug intolerance 77.77 19.41 146 71110 447445 90109746
Hypertensive crisis 77.07 19.41 82 71174 17702 90539489
Gait inability 76.09 19.41 12 71244 146444 90410747
Decreased appetite 75.67 19.41 531 70725 376009 90181182
Psoriasis 74.77 19.41 13 71243 147741 90409450
C-reactive protein abnormal 74.62 19.41 7 71249 127422 90429769
Renal impairment 73.90 19.41 216 71040 105205 90451986
Hypoaesthesia 73.70 19.41 83 71173 314127 90243064
Metastases to peritoneum 73.70 19.41 44 71212 4111 90553080
Atrial fibrillation 72.82 19.41 251 71005 133360 90423831
Anisocytosis 71.37 19.41 26 71230 775 90556416
Ill-defined disorder 71.35 19.41 28 71228 184863 90372328
Mobility decreased 70.80 19.41 56 71200 250678 90306513
Product dose omission issue 70.68 19.41 75 71181 291612 90265579
COVID-19 70.32 19.41 291 70965 168552 90388639
Product use in unapproved indication 70.31 19.41 97 71159 336139 90221052
Contusion 69.82 19.41 57 71199 251159 90306032
Basophil count increased 69.01 19.41 28 71228 1123 90556068
Metastases to pelvis 67.79 19.41 23 71233 553 90556638
Elliptocytosis 67.18 19.41 15 71241 65 90557126
Metastases to skin 66.90 19.41 33 71223 2107 90555084
Mean cell volume increased 66.05 19.41 44 71212 4977 90552214
Injection site pain 65.89 19.41 27 71229 173672 90383519
Back pain 65.88 19.41 451 70805 316724 90240467
Lymphadenopathy 64.20 19.41 123 71133 45652 90511539
Invasive breast carcinoma 63.80 19.41 25 71231 914 90556277
Pyelitis 62.61 19.41 18 71238 245 90556946
Breast mass 62.56 19.41 55 71201 9392 90547799
Dyspnoea exertional 62.51 19.41 160 71096 72128 90485063
Injection site erythema 61.63 19.41 4 71252 98498 90458693
Intentional overdose 61.20 19.41 3 71253 93831 90463360
Migraine 61.07 19.41 37 71219 190355 90366836
Metastases to the mediastinum 61.06 19.41 22 71234 635 90556556
Arrhythmia 60.92 19.41 115 71141 42217 90514974
Mean cell haemoglobin increased 60.68 19.41 38 71218 3867 90553324
Overdose 60.66 19.41 24 71232 157685 90399506
Hypertransaminasaemia 58.26 19.41 67 71189 15758 90541433
Night sweats 57.65 19.41 15 71241 128751 90428440
Therapy non-responder 57.37 19.41 18 71238 136686 90420505
Osteosclerosis 57.17 19.41 38 71218 4282 90552909
Platelet count decreased 56.96 19.41 236 71020 136733 90420458
Wound infection 56.92 19.41 8 71248 106394 90450797
Lymphocyte count decreased 56.48 19.41 100 71156 34950 90522241
Red blood cell count decreased 55.96 19.41 117 71139 46234 90510957
Haematocrit decreased 55.74 19.41 110 71146 41722 90515469
Chromaturia 55.64 19.41 72 71184 19115 90538076
Monocyte count decreased 55.44 19.41 31 71225 2560 90554631
Lip dry 55.41 19.41 7 71249 100948 90456243
Hypocalcaemia 54.76 19.41 110 71146 42258 90514933
Infection 54.55 19.41 128 71128 361966 90195225
Electrocardiogram PR shortened 53.61 19.41 19 71237 522 90556669
Toxicity to various agents 52.54 19.41 91 71165 287755 90269436
Calcium deficiency 52.20 19.41 24 71232 1309 90555882
Oestradiol decreased 51.68 19.41 13 71243 102 90557089
Hormone receptor positive HER2 negative breast cancer 51.50 19.41 16 71240 288 90556903
Metastases to bone marrow 51.12 19.41 19 71237 600 90556591
Peripheral swelling 51.00 19.41 161 71095 412945 90144246
Urinary tract inflammation 50.50 19.41 12 71244 72 90557119
Hormone receptor positive breast cancer 50.29 19.41 20 71236 761 90556430
Muscular weakness 50.20 19.41 53 71203 206613 90350578
Isosthenuria 50.20 19.41 13 71243 116 90557075
Granulocytopenia 49.82 19.41 41 71215 6400 90550791
Ageusia 49.26 19.41 62 71194 16014 90541177
Pain 49.14 19.41 524 70732 995817 89561374
Neutrophil count abnormal 49.12 19.41 34 71222 4094 90553097
Lower limb fracture 48.90 19.41 5 71251 85008 90472183
Hospitalisation 48.43 19.41 20 71236 128080 90429111
Anxiety 47.86 19.41 108 71148 309664 90247527
Hepatic cyst 47.06 19.41 40 71216 6528 90550663
Spinal cord haematoma 47.01 19.41 14 71242 217 90556974
White blood cell disorder 46.45 19.41 29 71227 2935 90554256
Memory impairment 46.34 19.41 52 71204 197192 90359999
Amnesia 46.05 19.41 14 71242 108491 90448700
Obesity 45.90 19.41 13 71243 105494 90451697
Calcification metastatic 45.42 19.41 13 71243 174 90557017
Resorption bone increased 44.79 19.41 21 71235 1198 90555993
Breast cancer 44.43 19.41 117 71139 53644 90503547
Poikilocytosis 44.36 19.41 13 71243 190 90557001
Gastrointestinal disorder 44.29 19.41 84 71172 256603 90300588
Pleural thickening 44.02 19.41 29 71227 3219 90553972
Headache 43.61 19.41 451 70805 862295 89694896
Seizure 43.18 19.41 34 71222 152595 90404596
Hepatobiliary disease 42.67 19.41 16 71240 518 90556673
Rouleaux formation 42.40 19.41 9 71247 29 90557162
Mucosal inflammation 42.23 19.41 120 71136 57505 90499686
Suicide attempt 41.94 19.41 5 71251 75394 90481797
Lymphopenia 41.76 19.41 69 71187 22812 90534379
Hyperbilirubinaemia 41.51 19.41 53 71203 13883 90543308
QRS axis abnormal 41.43 19.41 20 71236 1218 90555973
Cornea verticillata 41.29 19.41 13 71243 245 90556946
Cough 40.53 19.41 456 70800 368506 90188685
Autoimmune disorder 40.51 19.41 6 71250 76738 90480453
Oxygen saturation decreased 40.28 19.41 17 71239 107466 90449725
Palmar-plantar erythrodysaesthesia syndrome 40.16 19.41 76 71180 27947 90529244
Metastases to thorax 40.15 19.41 13 71243 269 90556922
Bilirubin conjugated increased 40.14 19.41 27 71229 3103 90554088
Depressed level of consciousness 40.06 19.41 5 71251 72779 90484412
Delirium 39.93 19.41 16 71240 104343 90452848
Breast pain 39.86 19.41 45 71211 10373 90546818
Malaise 39.54 19.41 284 70972 585702 89971489
Osteolysis 39.36 19.41 28 71228 3522 90553669
Cytopenia 39.35 19.41 58 71198 17391 90539800
Aspartate aminotransferase abnormal 39.22 19.41 25 71231 2624 90554567
Peripheral venous disease 39.08 19.41 9 71247 83912 90473279
Pulpitis dental 38.54 19.41 18 71238 1018 90556173
Adverse drug reaction 38.37 19.41 22 71234 116679 90440512
Depressed mood 38.19 19.41 106 71150 50116 90507075
Toothache 37.87 19.41 65 71191 22165 90535026
Fall 37.83 19.41 223 71033 481587 90075604
Alanine aminotransferase decreased 37.81 19.41 17 71239 880 90556311
Gastrointestinal haemorrhage 37.66 19.41 12 71244 90236 90466955
Dysphagia 37.30 19.41 181 71075 112097 90445094
Hepatic echinococciasis 36.80 19.41 9 71247 62 90557129
Alanine aminotransferase abnormal 36.75 19.41 32 71224 5394 90551797
Malignant pleural effusion 36.66 19.41 25 71231 2939 90554252
Pancytopenia 36.51 19.41 189 71067 120074 90437117
General physical condition abnormal 36.36 19.41 31 71225 5080 90552111
Hypercholesterolaemia 36.17 19.41 17 71239 100875 90456316
Musculoskeletal chest pain 36.02 19.41 66 71190 23684 90533507
Pulmonary embolism 35.92 19.41 200 71056 130620 90426571
Red cell distribution width increased 35.70 19.41 46 71210 12161 90545030
Febrile infection 34.35 19.41 21 71235 2048 90555143
Musculoskeletal pain 34.18 19.41 51 71205 171200 90385991
Cancer pain 34.05 19.41 27 71229 3998 90553193
Tumour pain 33.51 19.41 20 71236 1867 90555324
Vitamin D deficiency 33.48 19.41 54 71202 17502 90539689
Asthenia 33.31 19.41 597 70659 533154 90024037
Lymphangiosis carcinomatosa 33.06 19.41 19 71237 1653 90555538
Blepharospasm 32.58 19.41 3 71253 55442 90501749
Medication error 32.35 19.41 13 71243 84639 90472552
Suicidal ideation 32.31 19.41 9 71247 73846 90483345
Bladder hypertrophy 32.02 19.41 13 71243 522 90556669
Burn oesophageal 31.81 19.41 12 71244 395 90556796
Cardiac failure 31.81 19.41 170 71086 109326 90447865
Scar pain 31.68 19.41 11 71245 284 90556907
Electrocardiogram QT interval 31.63 19.41 10 71246 191 90557000
Radiation skin injury 31.55 19.41 16 71240 1084 90556107
Underdose 31.53 19.41 3 71253 54014 90503177
Stomatitis 31.17 19.41 111 71145 274587 90282604
Frequent bowel movements 31.12 19.41 4 71252 56931 90500260
Dilatation intrahepatic duct acquired 30.61 19.41 14 71242 754 90556437
Macrocytosis 30.58 19.41 22 71234 2816 90554375
Vertebral lesion 30.55 19.41 14 71242 758 90556433
Sinus arrhythmia 30.09 19.41 17 71239 1432 90555759
CYP3A4 polymorphism 30.07 19.41 8 71248 80 90557111
Gastrooesophageal reflux disease 29.95 19.41 53 71203 166284 90390907
Vomiting 29.90 19.41 821 70435 787472 89769719
Coma 29.70 19.41 10 71246 72622 90484569
Polychromasia 29.65 19.41 10 71246 236 90556955
Metastases to meninges 29.36 19.41 24 71232 3711 90553480
Ear pain 29.35 19.41 5 71251 57697 90499494
Metastases to chest wall 29.19 19.41 13 71243 658 90556533
Wrong technique in product usage process 29.01 19.41 10 71246 71561 90485630
Pelvic pain 28.96 19.41 47 71209 15310 90541881
Tumour marker abnormal 28.85 19.41 11 71245 373 90556818
Gastrointestinal infection 28.42 19.41 39 71217 10951 90546240
Gamma-glutamyltransferase abnormal 28.38 19.41 12 71244 535 90556656
Metastases to spinal cord 28.01 19.41 10 71246 281 90556910
Hypermetabolism 27.68 19.41 10 71246 291 90556900
Hydronephrosis 27.64 19.41 41 71215 12361 90544830
Metastases to uterus 27.62 19.41 8 71248 112 90557079
Selenium deficiency 27.60 19.41 7 71249 57 90557134
Bone sequestrum 27.38 19.41 16 71240 1437 90555754
Electrocardiogram abnormal 27.32 19.41 37 71219 10261 90546930
Osteoarthritis 27.25 19.41 72 71184 195658 90361533
Joint neoplasm 26.98 19.41 7 71249 63 90557128
Tumour marker decreased 26.88 19.41 7 71249 64 90557127
Somnolence 26.82 19.41 80 71176 209004 90348187
Mucosal dryness 26.27 19.41 21 71235 3146 90554045
Hepatic mass 26.07 19.41 18 71238 2159 90555032
Supraventricular extrasystoles 25.95 19.41 26 71230 5231 90551960
Loss of consciousness 25.87 19.41 44 71212 140194 90416997
Dry eye 25.80 19.41 102 71154 57829 90499362
Adjusted calcium increased 25.69 19.41 6 71250 33 90557158
Swollen tongue 25.68 19.41 3 71253 45953 90511238
Metastases to ovary 25.48 19.41 11 71245 516 90556675
Bilirubin conjugated abnormal 25.39 19.41 7 71249 81 90557110
Unevaluable event 25.30 19.41 6 71250 54842 90502349
Pleural disorder 25.28 19.41 12 71244 704 90556487
Red blood cell sedimentation rate increased 25.17 19.41 17 71239 82578 90474613
Acanthosis 25.17 19.41 9 71247 254 90556937
Alanine aminotransferase 25.08 19.41 7 71249 85 90557106
Metastases to breast 24.93 19.41 10 71246 389 90556802
Transaminases abnormal 24.86 19.41 12 71244 731 90556460
Flushing 24.66 19.41 20 71236 88471 90468720
Pathological fracture 24.56 19.41 34 71222 9626 90547565
Nail toxicity 24.48 19.41 10 71246 408 90556783
Nasal congestion 24.33 19.41 18 71238 83396 90473795
Peripheral sensory neuropathy 24.19 19.41 33 71223 9217 90547974
Rectal haemorrhage 23.94 19.41 18 71238 82726 90474465
Inflammation 23.88 19.41 67 71189 178525 90378666
Soft tissue neoplasm 23.84 19.41 7 71249 103 90557088
Tumour invasion 23.78 19.41 9 71247 299 90556892
Tricuspid valve incompetence 23.51 19.41 45 71211 16686 90540505
Colitis ulcerative 23.45 19.41 9 71247 60257 90496934
Nasopharyngitis 23.39 19.41 206 71050 406898 90150293
Lung disorder 23.33 19.41 52 71204 149831 90407360
Alopecia 23.29 19.41 531 70725 494540 90062651
Insomnia 23.24 19.41 160 71096 333314 90223877
Blood phosphorus decreased 23.22 19.41 24 71232 5010 90552181
Dyspnoea 23.09 19.41 878 70378 880077 89677114
Radiation oesophagitis 23.05 19.41 10 71246 475 90556716
Neoplasm progression 22.86 19.41 82 71174 44404 90512787
Orthostatic hypotension 22.71 19.41 3 71253 41824 90515367
Cell death 22.70 19.41 19 71237 3036 90554155
Intraocular pressure test abnormal 22.57 19.41 8 71248 220 90556971
Adjusted calcium decreased 22.57 19.41 8 71248 220 90556971
Laryngitis 22.54 19.41 6 71250 50747 90506444
Spinal fracture 22.52 19.41 52 71204 21964 90535227
Organ failure 22.43 19.41 19 71237 3086 90554105
Hallucination 22.31 19.41 12 71244 65947 90491244
Bile duct stenosis 22.27 19.41 15 71241 1727 90555464
Malignant neoplasm of pleura 22.20 19.41 6 71250 64 90557127
Skin exfoliation 22.20 19.41 109 71147 67804 90489387
Ebola disease 21.83 19.41 4 71252 4 90557187
Interstitial lung disease 21.76 19.41 118 71138 76287 90480904
Lymphocyte count increased 21.76 19.41 21 71235 4038 90553153
Menopausal disorder 21.64 19.41 6 71250 71 90557120
Lymphocyte percentage increased 21.59 19.41 10 71246 555 90556636
Skin reaction 21.43 19.41 46 71210 18507 90538684
Tongue geographic 21.30 19.41 7 71249 152 90557039
Epilepsy 21.19 19.41 20 71236 82186 90475005
Heart rate decreased 20.80 19.41 8 71248 53497 90503694
Neck pain 20.80 19.41 36 71220 113927 90443264
Periodontitis 20.78 19.41 20 71236 3833 90553358
Blood pressure decreased 20.78 19.41 17 71239 74878 90482313
Stress 20.75 19.41 20 71236 81375 90475816
Oedema 20.73 19.41 84 71172 200211 90356980
Sinus bradycardia 20.70 19.41 43 71213 16909 90540282
Rectal cancer 20.69 19.41 16 71240 2285 90554906
Gaze palsy 20.67 19.41 14 71242 1627 90555564
Hyperchromic anaemia 20.65 19.41 6 71250 85 90557106
Invasive ductal breast carcinoma 20.61 19.41 28 71228 7790 90549401
Hyperglycaemia 20.53 19.41 87 71169 50883 90506308
Cauda equina syndrome 20.48 19.41 13 71243 1354 90555837
Cholestasis 20.47 19.41 69 71187 36230 90520961
Oesophageal candidiasis 20.39 19.41 26 71230 6803 90550388
Respiratory disorder 20.21 19.41 13 71243 64803 90492388
Microangiopathy 20.11 19.41 14 71242 1701 90555490
Oesophageal adenocarcinoma 20.01 19.41 7 71249 185 90557006
Hepatic necrosis 19.99 19.41 25 71231 6413 90550778
Osteoporosis 19.99 19.41 28 71228 96503 90460688
Breast inflammation 19.76 19.41 7 71249 192 90556999
BRCA2 gene mutation 19.74 19.41 6 71250 100 90557091
Anaphylactic reaction 19.55 19.41 24 71232 87500 90469691
Paraesthesia 19.54 19.41 116 71140 250210 90306981
Sciatica 19.45 19.41 31 71225 101351 90455840
Blood uric acid increased 19.41 19.41 27 71229 7677 90549514

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
Neutropenia 52.59 37.23 32 508 199399 42421396

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 3144.53 18.67 1865 39377 372755 110175302
Malignant neoplasm progression 1516.29 18.67 892 40350 173675 110374382
Metastases to bone 1460.26 18.67 518 40724 30854 110517203
Metastases to liver 993.33 18.67 404 40838 34982 110513075
Electrocardiogram QT prolonged 882.48 18.67 533 40709 108427 110439630
Hepatotoxicity 564.66 18.67 330 40912 63070 110484987
Leukopenia 501.51 18.67 427 40815 148364 110399693
Neutrophil count decreased 500.03 18.67 391 40851 120550 110427507
Carbohydrate antigen 15-3 increased 497.01 18.67 116 41126 1471 110546586
Metastases to lung 492.61 18.67 217 41025 22846 110525211
White blood cell count decreased 437.05 18.67 481 40761 228909 110319148
Alanine aminotransferase increased 370.22 18.67 397 40845 183376 110364681
Aspartate aminotransferase increased 358.79 18.67 366 40876 159570 110388487
Bone lesion 295.48 18.67 108 41134 6979 110541078
Metastases to lymph nodes 290.79 18.67 132 41110 14900 110533157
Breast cancer metastatic 228.39 18.67 102 41140 11079 110536978
Skin hypopigmentation 213.71 18.67 58 41184 1393 110546664
Hepatic cytolysis 203.83 18.67 167 41075 54886 110493171
Bone pain 203.10 18.67 179 41063 64954 110483103
Carcinoembryonic antigen increased 195.86 18.67 63 41179 2761 110545296
Transaminases increased 185.35 18.67 168 41074 63222 110484835
Nausea 169.74 18.67 906 40336 1234784 109313273
Haematotoxicity 164.83 18.67 101 41141 20981 110527076
Blood alkaline phosphatase increased 163.73 18.67 165 41077 70770 110477287
Tumour marker increased 163.46 18.67 64 41178 4996 110543061
Hepatic lesion 162.42 18.67 74 41168 8419 110539638
Therapy partial responder 155.48 18.67 121 41121 36940 110511117
Off label use 154.28 18.67 201 41041 1499984 109048073
Anaemia 154.18 18.67 501 40741 546585 110001472
Pleural effusion 153.96 18.67 254 40988 177455 110370602
Gamma-glutamyltransferase increased 151.47 18.67 148 41094 61161 110486896
Thrombocytopenia 148.56 18.67 371 40871 348514 110199543
Breast cancer recurrent 147.04 18.67 55 41187 3791 110544266
Blood creatinine increased 143.34 18.67 250 40992 182639 110365418
Drug ineffective 139.28 18.67 221 41021 1520319 109027738
Blood bilirubin increased 136.94 18.67 155 41087 75817 110472240
Infusion related reaction 127.81 18.67 3 41239 381159 110166898
Myelosuppression 125.38 18.67 165 41077 94175 110453882
Liver function test increased 119.42 18.67 156 41086 88392 110459665
Vitiligo 118.46 18.67 44 41198 2973 110545084
Decreased immune responsiveness 109.91 18.67 59 41183 9547 110538510
Hot flush 109.38 18.67 129 41113 65907 110482150
Haemoglobin decreased 102.12 18.67 261 40981 248466 110299591
Condition aggravated 101.05 18.67 76 41166 734760 109813297
Metastases to spine 100.42 18.67 46 41196 5297 110542760
Joint swelling 99.05 18.67 22 41220 442823 110105234
Breast mass 98.78 18.67 52 41190 8089 110539968
Fatigue 97.28 18.67 779 40463 1215179 109332878
PIK3CA-activated mutation 94.91 18.67 26 41216 647 110547410
Rheumatoid arthritis 91.34 18.67 5 41237 299608 110248449
Spinal pain 87.69 18.67 65 41177 18450 110529607
Arthropathy 84.05 18.67 6 41236 287516 110260541
Drug hypersensitivity 80.98 18.67 34 41208 454056 110094001
Intentional product use issue 79.26 18.67 3 41239 247903 110300154
Therapeutic product effect decreased 77.97 18.67 3 41239 244313 110303744
Metastases to pleura 77.04 18.67 29 41213 2034 110546023
Eastern Cooperative Oncology Group performance status worsened 76.76 18.67 32 41210 2937 110545120
Sinusitis 76.73 18.67 10 41232 296678 110251379
Hypotension 76.12 18.67 51 41191 523798 110024259
Anisocytosis 76.11 18.67 25 41217 1171 110546886
Metastasis 76.07 18.67 44 41198 8223 110539834
Skin toxicity 76.01 18.67 50 41192 11733 110536324
Elliptocytosis 74.12 18.67 15 41227 91 110547966
Back pain 74.00 18.67 304 40938 370692 110177365
Metastases to central nervous system 71.67 18.67 63 41179 22754 110525303
Second primary malignancy 71.48 18.67 57 41185 18011 110530046
Treatment failure 70.14 18.67 10 41232 277224 110270833
Glossodynia 69.92 18.67 3 41239 222001 110326056
Invasive breast carcinoma 68.77 18.67 21 41221 774 110547283
Hypertransaminasaemia 68.36 18.67 63 41179 24192 110523865
Disease progression 68.08 18.67 223 41019 243811 110304246
Osteosclerosis 66.89 18.67 33 41209 4482 110543575
Oestradiol decreased 66.03 18.67 13 41229 67 110547990
Hydrothorax 64.44 18.67 24 41218 1634 110546423
Glomerular filtration rate decreased 64.31 18.67 66 41176 28890 110519167
Metastases to pelvis 63.17 18.67 20 41222 832 110547225
Pneumonitis 63.02 18.67 107 41135 76424 110471633
Mean cell volume increased 62.80 18.67 39 41203 8291 110539766
Confusional state 61.15 18.67 51 41191 468629 110079428
Metastases to the mediastinum 60.39 18.67 19 41223 774 110547283
Breast cancer 60.05 18.67 73 41169 38469 110509588
Isosthenuria 59.54 18.67 13 41229 119 110547938
Dry skin 59.50 18.67 127 41115 107526 110440531
Electrocardiogram PR shortened 59.36 18.67 16 41226 374 110547683
Lymphadenopathy 58.96 18.67 94 41148 63741 110484316
Wheezing 58.42 18.67 12 41230 255218 110292839
Product use issue 57.73 18.67 22 41220 311673 110236384
Hormone receptor positive breast cancer 57.50 18.67 17 41225 560 110547497
Swelling 56.84 18.67 30 41212 351011 110197046
Asthma 56.81 18.67 12 41230 250279 110297778
Wound 55.82 18.67 10 41232 234427 110313630
Helicobacter infection 55.52 18.67 3 41239 181874 110366183
Mean cell haemoglobin increased 54.64 18.67 31 41211 5586 110542471
Hormone receptor positive HER2 negative breast cancer 51.49 18.67 13 41229 233 110547824
Hepatic cyst 50.13 18.67 33 41209 7750 110540307
Impaired healing 49.97 18.67 7 41235 196710 110351347
Irritable bowel syndrome 49.23 18.67 3 41239 164212 110383845
Rouleaux formation 49.10 18.67 9 41233 29 110548028
Jaundice 49.00 18.67 83 41159 59153 110488904
Fall 48.33 18.67 95 41147 603387 109944670
Injury 48.24 18.67 5 41237 177260 110370797
White blood cell disorder 47.82 18.67 25 41217 3834 110544223
Haematocrit decreased 47.40 18.67 87 41155 66030 110482027
Lymphocyte count decreased 47.08 18.67 80 41162 57163 110490894
Weight increased 46.24 18.67 53 41189 419591 110128466
Depressed mood 46.12 18.67 82 41160 60727 110487330
Toxicity to various agents 45.47 18.67 68 41174 480487 110067570
Poikilocytosis 45.17 18.67 13 41229 389 110547668
Concomitant disease aggravated 45.13 18.67 42 41200 16322 110531735
Red blood cell count decreased 45.07 18.67 85 41157 65838 110482219
Resorption bone increased 44.66 18.67 18 41224 1516 110546541
Osteolysis 44.55 18.67 27 41215 5496 110542561
Pyelitis 44.36 18.67 13 41229 415 110547642
Neutrophil count abnormal 43.75 18.67 26 41216 5106 110542951
Lower respiratory tract infection 43.62 18.67 18 41224 243088 110304969
Hepatic echinococciasis 42.76 18.67 9 41233 68 110547989
Pruritus 42.68 18.67 366 40876 581194 109966863
Macrocytosis 42.63 18.67 22 41220 3285 110544772
Lymphoedema 42.50 18.67 39 41203 14890 110533167
Monocyte count decreased 42.23 18.67 23 41219 3828 110544229
Pleural thickening 42.06 18.67 22 41220 3377 110544680
Ascites 41.83 18.67 101 41141 92707 110455350
Metastases to peritoneum 41.62 18.67 26 41216 5584 110542473
Calcification metastatic 41.59 18.67 10 41232 145 110547912
Loss of personal independence in daily activities 41.43 18.67 4 41238 150016 110398041
Neoplasm 39.69 18.67 33 41209 11054 110537003
Burn oesophageal 39.25 18.67 12 41230 444 110547613
Cornea verticillata 38.88 18.67 11 41231 309 110547748
Urticaria 38.80 18.67 37 41205 318820 110229237
Overdose 37.80 18.67 20 41222 233774 110314283
Electrocardiogram QT interval abnormal 37.72 18.67 11 41231 345 110547712
Bursitis 37.13 18.67 3 41239 129915 110418142
Urinary tract inflammation 36.51 18.67 11 41231 387 110547670
Therapeutic product effect incomplete 36.39 18.67 19 41223 223786 110324271
Asthenia 36.04 18.67 404 40838 688595 109859462
Blister 35.96 18.67 20 41222 227356 110320701
Dilatation intrahepatic duct acquired 35.70 18.67 13 41229 830 110547227
Invasive ductal breast carcinoma 35.27 18.67 25 41217 6621 110541436
Red cell distribution width increased 33.56 18.67 37 41205 17565 110530492
Gastrointestinal haemorrhage 33.56 18.67 10 41232 165508 110382549
QRS axis abnormal 33.50 18.67 17 41225 2451 110545606
Tumour marker decreased 33.24 18.67 7 41235 53 110548004
Seizure 32.80 18.67 21 41221 221164 110326893
Arthritis 32.42 18.67 11 41231 167575 110380482
Joint neoplasm 32.17 18.67 7 41235 63 110547994
Bladder hypertrophy 32.07 18.67 13 41229 1111 110546946
Metastases to spinal cord 32.05 18.67 9 41233 246 110547811
Type 2 diabetes mellitus 31.99 18.67 13 41229 177219 110370838
Arrhythmia 31.65 18.67 76 41166 69499 110478558
CYP3A4 polymorphism 31.50 18.67 7 41235 70 110547987
Vomiting 31.40 18.67 495 40747 910180 109637877
Selenium deficiency 31.32 18.67 7 41235 72 110547985
Electrocardiogram QT interval 31.06 18.67 9 41233 276 110547781
Depressed level of consciousness 30.98 18.67 3 41239 112275 110435782
Muscular weakness 30.02 18.67 29 41213 248439 110299618
Hospitalisation 30.02 18.67 8 41234 142485 110405572
Decreased appetite 29.55 18.67 289 40953 475557 110072500
Death 29.25 18.67 393 40849 698476 109849581
Ovarian cancer 29.20 18.67 19 41223 4377 110543680
Injection site pain 29.08 18.67 15 41227 177907 110370150
Soft tissue neoplasm 29.02 18.67 7 41235 103 110547954
Metastases to skin 28.79 18.67 15 41227 2284 110545773
BRCA2 gene mutation 28.65 18.67 7 41235 109 110547948
Metastases to breast 28.62 18.67 9 41233 366 110547691
Alanine aminotransferase decreased 28.57 18.67 14 41228 1874 110546183
Breast pain 28.22 18.67 26 41216 9974 110538083
Product use in unapproved indication 28.13 18.67 80 41162 447297 110100760
Osteonecrosis of jaw 28.09 18.67 58 41184 47959 110500098
Product dose omission issue 28.08 18.67 48 41194 321734 110226323
C-reactive protein abnormal 27.86 18.67 7 41235 129688 110418369
Hypermetabolism 27.86 18.67 10 41232 613 110547444
Blood phosphorus decreased 27.82 18.67 23 41219 7642 110540415
Delirium 27.66 18.67 8 41234 135017 110413040
Adjusted calcium decreased 27.49 18.67 8 41234 249 110547808
Abdominal discomfort 27.37 18.67 67 41175 393791 110154266
Electrocardiogram abnormal 26.83 18.67 34 41208 18675 110529382
Blood cholesterol increased 26.78 18.67 18 41224 184767 110363290
Blood lactate dehydrogenase increased 26.47 18.67 54 41188 44280 110503777
Metastases to bone marrow 26.45 18.67 11 41231 1003 110547054
Blood calcium increased 26.22 18.67 33 41209 18007 110530050
Nail avulsion 26.08 18.67 7 41235 161 110547896
Musculoskeletal stiffness 26.05 18.67 40 41202 279782 110268275
Oxygen saturation decreased 26.01 18.67 13 41229 156969 110391088
Psoriasis 25.70 18.67 10 41232 139983 110408074
Adjusted calcium increased 25.63 18.67 6 41236 77 110547980
Night sweats 25.56 18.67 9 41233 133974 110414083
Hepatic mass 25.54 18.67 15 41227 2883 110545174
Suicide attempt 25.51 18.67 4 41238 103390 110444667
Metastases to uterus 25.35 18.67 6 41236 81 110547976
Mobility decreased 25.05 18.67 31 41211 237391 110310666
Lymphangiosis carcinomatosa 24.96 18.67 14 41228 2468 110545589
Bilirubin conjugated abnormal 24.87 18.67 7 41235 193 110547864
Calcium deficiency 24.83 18.67 11 41231 1171 110546886
Therapy non-responder 24.63 18.67 14 41228 157293 110390764
Carbohydrate antigen 125 increased 24.62 18.67 14 41228 2533 110545524
Gait inability 24.61 18.67 10 41232 136366 110411691
Lip dry 24.40 18.67 4 41238 100079 110447978
Hypersensitivity 24.12 18.67 74 41168 403924 110144133
Coma 24.11 18.67 7 41235 117862 110430195
Chromaturia 24.09 18.67 41 41201 29319 110518738
Metastases to ovary 24.01 18.67 8 41234 392 110547665
Medication error 24 18.67 5 41237 105361 110442696
Erysipelas 23.95 18.67 27 41215 13131 110534926
Polychromasia 23.90 18.67 9 41233 632 110547425
Trichorrhexis 23.81 18.67 10 41232 935 110547122
Vertebral lesion 23.51 18.67 9 41233 661 110547396
Coronavirus infection 23.48 18.67 23 41219 9522 110538535
Infection 23.33 18.67 64 41178 362136 110185921
Dry eye 23.32 18.67 59 41183 55734 110492323
Basophil count increased 23.21 18.67 12 41230 1798 110546259
Hypocalcaemia 23.15 18.67 65 41177 65301 110482756
Constipation 23.03 18.67 219 41023 357567 110190490
Autoimmune hepatitis 22.99 18.67 28 41214 14776 110533281
Hypoaesthesia 22.99 18.67 52 41190 314171 110233886
General physical health deterioration 22.93 18.67 251 40991 425044 110123013
International normalised ratio abnormal 22.92 18.67 19 41223 6338 110541719
Hallucination 22.72 18.67 5 41237 101427 110446630
Pleural disorder 22.71 18.67 10 41232 1049 110547008
Lacrimation increased 22.52 18.67 41 41201 30909 110517148
Injection site erythema 22.44 18.67 4 41238 94172 110453885
Suicidal ideation 22.36 18.67 4 41238 93933 110454124
Contusion 22.06 18.67 33 41209 233328 110314729
Tumour marker abnormal 22.04 18.67 7 41235 294 110547763
Inflammation 21.70 18.67 24 41218 193214 110354843
Discomfort 21.65 18.67 29 41213 214678 110333379
Invasive lobular breast carcinoma 21.60 18.67 9 41233 825 110547232
Lymphocyte percentage increased 21.47 18.67 9 41233 837 110547220
Alopecia 21.40 18.67 219 41023 364534 110183523
Sinus arrhythmia 21.17 18.67 12 41230 2158 110545899
Supraventricular extrasystoles 20.89 18.67 20 41222 8053 110540004
Pulmonary embolism 20.70 18.67 144 41098 214330 110333727
BRCA1 gene mutation 20.52 18.67 5 41237 77 110547980
Ill-defined disorder 20.51 18.67 17 41225 156836 110391221
Memory impairment 20.47 18.67 26 41216 196918 110351139
Dorsal ramus syndrome 20.42 18.67 4 41238 20 110548037
Hepatomegaly 20.41 18.67 32 41210 21382 110526675
Wrong technique in product usage process 20.20 18.67 4 41238 87344 110460713
Granulocytopenia 19.67 18.67 24 41218 12691 110535366
Hepatobiliary disease 19.51 18.67 9 41233 1053 110547004
Septic shock 19.48 18.67 18 41224 157510 110390547
Aphthous ulcer 19.34 18.67 31 41211 21105 110526952
Loss of consciousness 19.30 18.67 27 41215 196279 110351778
Post procedural inflammation 19.30 18.67 6 41236 235 110547822
Mean cell haemoglobin 19.24 18.67 5 41237 101 110547956
Wound infection 19.24 18.67 6 41236 96459 110451598
Musculoskeletal pain 19.19 18.67 24 41218 182999 110365058
Pulpitis dental 19.09 18.67 10 41232 1539 110546518
Mucinous breast carcinoma 19.03 18.67 4 41238 30 110548027
Platelet count decreased 18.98 18.67 149 41093 230294 110317763
Dyspnoea exertional 18.93 18.67 83 41159 103977 110444080
Bile duct stenosis 18.84 18.67 12 41230 2664 110545393
Aspartate aminotransferase abnormal 18.79 18.67 13 41229 3312 110544745
Cauda equina syndrome 18.74 18.67 11 41231 2111 110545946

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
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:231911 renoprotective agent
CHEBI has role CHEBI:233423 antifibrotic agent

Related Drugs by ATC class:

L01EF Cyclin-dependent kinase (CDK) inhibitors 2 drugs
abemaciclibpalbociclib

Drug Use | Suggest Off label Use Form| |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 ADJUVANT TREATMENT OF ADULTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE STAGE II AND III EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
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, FOR THE TREATMENT OF ADULT PATIENTS WITH 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 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 ADJUVANT TREATMENT OF ADULTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE STAGE II AND III EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
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 ADJUVANT TREATMENT OF ADULTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE STAGE II AND III EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
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, FOR THE TREATMENT OF ADULT PATIENTS WITH 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 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 ADJUVANT TREATMENT OF ADULTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE STAGE II AND III EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
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 ADJUVANT TREATMENT OF ADULTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE STAGE II AND III EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
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, FOR THE TREATMENT OF ADULT PATIENTS WITH 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 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 ADJUVANT TREATMENT OF ADULTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE STAGE II AND III EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
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
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 12544379 Aug. 7, 2034 IN COMBINATION WITH FULVESTRANT AS INITIAL ENDOCRINE-BASED THERAPY OR FOLLOWING DISEASE PROGRESSION ON ENDOCRINE THERAPY, FOR THE TREATMENT OF ADULT PATIENTS WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 12544380 Aug. 7, 2034 IN COMBINATION WITH AN AROMATASE INHIBITOR (LETROZOLE OR ANASTROZOLE) AS INITIAL ENDOCRINE-BASED THERAPY FOR TREATMENT OF ADULTS WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL 12544380 Aug. 7, 2034 IN COMBINATION WITH AN AROMATASE INHIBITOR (LETROZOLE OR ANASTROZOLE) FOR THE ADJUVANT TREATMENT OF ADULTS WITH HR-POSITIVE, HER2-NEGATIVE STAGE II AND III EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
2.5MG;EQ 200MG BASE KISQALI FEMARA CO-PACK (COPACKAGED) NOVARTIS N209935 May 4, 2017 RX TABLET ORAL 12544380 Aug. 7, 2034 ADJUVANT TREATMENT OF ADULTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE STAGE II AND III EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
2.5MG;EQ 200MG BASE KISQALI FEMARA CO-PACK (COPACKAGED) NOVARTIS N209935 May 4, 2017 RX TABLET ORAL 12544380 Aug. 7, 2034 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

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 Sept. 17, 2027 IN COMBINATION WITH AN AROMATASE INHIBITOR FOR THE ADJUVANT TREATMENT OF ADULTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE STAGE II AND III EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
2.5MG;EQ 200MG BASE KISQALI FEMARA CO-PACK (COPACKAGED) NOVARTIS N209935 May 4, 2017 RX TABLET ORAL Sept. 17, 2027 FOR THE ADJUVANT TREATMENT OF ADULTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2(HER2)-NEGATIVE STAGE II AND III EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
EQ 200MG BASE KISQALI NOVARTIS N209092 March 13, 2017 RX TABLET ORAL March 17, 2028 PEDIATRIC EXCLUSIVITY
2.5MG;EQ 200MG BASE KISQALI FEMARA CO-PACK (COPACKAGED) NOVARTIS N209935 May 4, 2017 RX TABLET ORAL March 17, 2028 PEDIATRIC EXCLUSIVITY

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
1374639-75-4 SECONDARY_CAS_RN
4036504 VANDF
C4045494 UMLSCUI
CHEBI:230905 CHEBI
6ZZ PDB_CHEM_ID
CHEMBL3545110 ChEMBL_ID
44631912 PUBCHEM_CID
DB11730 DRUGBANK_ID
CHEMBL3707266 ChEMBL_ID
D10883 KEGG_DRUG
9968 INN_ID
C000589651 MESH_SUPPLEMENTAL_RECORD_UI
7383 IUPHAR_LIGAND_ID
732257004 SNOMEDCT_US
732258009 SNOMEDCT_US
763537002 SNOMEDCT_US
254040 MMSL
32443 MMSL
331981 MMSL
331984 MMSL
331986 MMSL
d08533 MMSL
017131 NDDF
017132 NDDF
1873916 RXNORM
TK8ERE8P56 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
KISQALI HUMAN PRESCRIPTION DRUG LABEL 1 0078-0860 TABLET, FILM COATED 200 mg ORAL NDA 31 sections
KISQALI HUMAN PRESCRIPTION DRUG LABEL 1 0078-0867 TABLET, FILM COATED 200 mg ORAL NDA 31 sections
KISQALI HUMAN PRESCRIPTION DRUG LABEL 1 0078-0874 TABLET, FILM COATED 200 mg ORAL NDA 31 sections