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

Stem definitionDrug idCAS RN
cyclin dependant kinase inhibitors 4941 571190-30-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • palbociclib
  • palbociclib isethionate
  • ibrance
  • PD-0332991
  • PD-0332991-0054
  • PF-00080665-73
  • PD 0332991
Palbociclib is an inhibitor of cyclin-dependent kinases (CDK) 4 and 6. Cyclin D1 and CDK4/6 are downstream of signaling pathways which lead to cellular proliferation. In vitro, palbociclib reduced cellular proliferation of estrogen receptor (ER)-positive breast cancer cell lines by blocking progression of the cell from G1 into S phase of the cell cycle. Treatment of breast cancer cell lines with the combination of palbociclib and antiestrogens leads to decreased retinoblastoma (Rb) protein phosphorylation resulting in reduced E2F expression and signaling, and increased growth arrest compared to treatment with each drug alone. In vitro treatment of ER-positive breast cancer cell lines with the combination of palbociclib and antiestrogens led to increased cell senescence compared to each drug alone, which was sustained for up to 6 days following palbociclib removal and was greater if antiestrogen treatment was continued. In vivo studies using a patient-derived ER-positive breast cancer xenograft model demonstrated that the combination of palbociclib and letrozole increased the inhibition of Rb phosphorylation, downstream signaling, and tumor growth compared to each drug alone.
  • Molecular weight: 447.54
  • Formula: C24H29N7O2
  • CLOGP: 2.20
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 2
  • TPSA: 103.35
  • ALOGS: -4.41
  • ROTB: 5

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 27, 2017 PMDA Pfizer Japan Inc
Nov. 9, 2016 EMA Pfizer Limited
Feb. 3, 2015 FDA PFIZER INC

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
Neoplasm progression 9130.36 17.24 2963 87538 23720 46571841
White blood cell count decreased 5933.15 17.24 3296 87205 108935 46486626
Neutropenia 3302.07 17.24 2501 88000 140703 46454858
Fatigue 3116.00 17.24 4749 85752 603948 45991613
Alopecia 1813.41 17.24 1883 88618 160531 46435030
Blood count abnormal 1110.29 17.24 587 89914 17291 46578270
Disease progression 1071.26 17.24 1089 89412 90211 46505350
Stomatitis 1020.83 17.24 931 89570 67366 46528195
Full blood count decreased 923.75 17.24 561 89940 21650 46573911
Neutrophil count decreased 810.03 17.24 672 89829 42754 46552807
Breast cancer metastatic 701.94 17.24 396 90105 13282 46582279
Hot flush 629.74 17.24 583 89918 42934 46552627
Nausea 583.96 17.24 2747 87754 684707 45910854
Bone marrow failure 582.12 17.24 473 90028 29196 46566365
Tumour marker increased 570.82 17.24 226 90275 3315 46592246
Drug ineffective 554.67 17.24 315 90186 677523 45918038
Decreased appetite 538.18 17.24 1170 89331 192666 46402895
Malignant neoplasm progression 481.50 17.24 611 89890 64315 46531246
Red blood cell count decreased 479.50 17.24 441 90060 32182 46563379
Death 464.14 17.24 1565 88936 333983 46261578
Rheumatoid arthritis 414.60 17.24 11 90490 240204 46355357
Therapy cessation 412.90 17.24 371 90130 26258 46569303
Metastases to bone 401.74 17.24 306 90195 17170 46578391
Leukopenia 379.28 17.24 559 89942 67784 46527777
Platelet count decreased 354.68 17.24 669 89832 99355 46496206
Dry skin 345.92 17.24 412 90089 40604 46554957
Constipation 303.47 17.24 881 89620 173216 46422345
Bone pain 285.61 17.24 401 90100 46489 46549072
Toxicity to various agents 273.51 17.24 42 90459 211724 46383837
Completed suicide 266.66 17.24 3 90498 145917 46449644
Oral pain 254.74 17.24 276 90225 24521 46571040
Epistaxis 252.90 17.24 450 90051 63855 46531706
Second primary malignancy 232.48 17.24 150 90351 6434 46589127
Metastases to liver 224.30 17.24 231 90270 19354 46576207
Product dose omission issue 212.83 17.24 764 89737 167756 46427805
Drug hypersensitivity 210.44 17.24 105 90396 243720 46351841
Diarrhoea 200.21 17.24 1802 88699 557800 46037761
Asthenia 197.74 17.24 1151 89350 309924 46285637
Thrombocytopenia 193.45 17.24 612 89889 125969 46469592
Hypotension 180.76 17.24 114 90387 232475 46363086
Maternal exposure during pregnancy 175.59 17.24 5 90496 102544 46493017
Therapy change 170.01 17.24 112 90389 4978 46590583
Cytopenia 165.36 17.24 130 90371 7638 46587923
Neuropathy peripheral 161.94 17.24 464 90037 90429 46505132
Acute kidney injury 161.80 17.24 132 90369 235723 46359838
Dysgeusia 145.99 17.24 273 90228 40218 46555343
Drug interaction 132.74 17.24 119 90382 202975 46392586
Overdose 129.77 17.24 21 90480 101958 46493603
Injection site pain 121.79 17.24 29 90472 107123 46488438
Carbohydrate antigen 15-3 increased 121.60 17.24 51 90450 873 46594688
Onychoclasis 118.01 17.24 90 90411 5054 46590507
Therapeutic product effect decreased 112.12 17.24 14 90487 82587 46512974
Madarosis 111.78 17.24 59 90442 1727 46593834
Off label use 111.07 17.24 372 90129 379469 46216092
Treatment failure 110.21 17.24 23 90478 93064 46502497
Breast cancer 109.37 17.24 260 90241 45258 46550303
Tachycardia 109.28 17.24 29 90472 99593 46495968
Lacrimation increased 109.16 17.24 144 90357 15717 46579844
Injection site erythema 107.69 17.24 10 90491 74417 46521144
Systemic lupus erythematosus 102.15 17.24 6 90495 65174 46530387
Asthma 101.65 17.24 26 90475 91516 46504045
Taste disorder 99.25 17.24 86 90415 5792 46589769
Joint swelling 96.23 17.24 108 90393 165965 46429596
Cardiac arrest 96.01 17.24 28 90473 90371 46505190
Psoriasis 93.92 17.24 19 90482 78585 46516976
Fall 91.62 17.24 329 90172 328768 46266793
Suicide attempt 89.61 17.24 4 90497 55032 46540529
Cardio-respiratory arrest 89.47 17.24 7 90494 59862 46535699
White blood cell count abnormal 88.51 17.24 76 90425 5056 46590505
Metastases to lung 86.10 17.24 105 90396 10591 46584970
Bradycardia 85.81 17.24 13 90488 66285 46529276
Seizure 80.45 17.24 72 90429 122982 46472579
Full blood count abnormal 79.89 17.24 45 90456 1502 46594059
Therapeutic product effect incomplete 79.76 17.24 26 90475 78127 46517434
Drug intolerance 79.45 17.24 101 90400 146948 46448613
Swelling 78.86 17.24 75 90426 124436 46471125
Myelosuppression 77.79 17.24 85 90416 7618 46587943
Cancer pain 77.21 17.24 52 90449 2398 46593163
Anaphylactic reaction 77.19 17.24 7 90494 53105 46542456
Hyponatraemia 75.44 17.24 52 90449 101280 46494281
Arthropathy 75.19 17.24 35 90466 84665 46510896
Hypersensitivity 74.42 17.24 110 90391 150211 46445350
Decreased immune responsiveness 73.72 17.24 59 90442 3556 46592005
Neoplasm malignant 73.19 17.24 149 90352 23350 46572211
Lymphoedema 70.06 17.24 85 90416 8527 46587034
Coma 69.91 17.24 14 90487 58335 46537226
Nail disorder 69.29 17.24 81 90420 7815 46587746
Syncope 68.88 17.24 61 90440 104742 46490819
Injection site reaction 67.71 17.24 7 90494 47842 46547719
Cough 66.77 17.24 711 89790 229538 46366023
Injury 66.20 17.24 5 90496 44022 46551539
Loss of consciousness 65.31 17.24 68 90433 108170 46487391
Cardiac failure congestive 63.24 17.24 51 90450 91699 46503862
Suicidal ideation 62.60 17.24 16 90485 56366 46539195
Depressed level of consciousness 62.31 17.24 9 90492 47560 46548001
PIK3CA-activated mutation 62.19 17.24 28 90473 573 46594988
Haemoglobin decreased 60.10 17.24 442 90059 128507 46467054
Anaemia 59.95 17.24 758 89743 255021 46340540
Hepatic lesion 59.78 17.24 54 90447 3843 46591718
Metabolic acidosis 59.47 17.24 4 90497 38776 46556785
Injection site pruritus 58.40 17.24 5 90496 39738 46555823
Hypertension 58.13 17.24 191 90310 196165 46399396
Respiratory failure 57.84 17.24 59 90442 94757 46500804
Oxygen saturation decreased 56.29 17.24 32 90469 69132 46526429
Intentional product use issue 54.84 17.24 17 90484 52763 46542798
Lactic acidosis 53.49 17.24 3 90498 33906 46561655
Gastrointestinal haemorrhage 53.33 17.24 43 90458 77330 46518231
Metastases to lymph nodes 53.22 17.24 65 90436 6566 46588995
Osteoarthritis 52.96 17.24 27 90474 61998 46533563
Urticaria 52.93 17.24 92 90409 117800 46477761
Blood test abnormal 52.90 17.24 78 90423 9442 46586119
Oedema peripheral 52.51 17.24 148 90353 159558 46436003
Dysarthria 51.75 17.24 6 90495 37492 46558069
Product use in unapproved indication 50.70 17.24 324 90177 89949 46505612
Hypoglycaemia 50.53 17.24 21 90480 54328 46541233
Tumour marker abnormal 50.37 17.24 17 90484 153 46595408
Osteonecrosis of jaw 50.31 17.24 164 90337 34238 46561323
Coronary artery disease 50.27 17.24 4 90497 33748 46561813
Back pain 50.26 17.24 625 89876 209414 46386147
Blood pressure increased 49.77 17.24 107 90394 126559 46469002
Breast cancer stage IV 49.36 17.24 21 90480 373 46595188
Rhinorrhoea 49.25 17.24 203 90298 47462 46548099
Pulmonary hypertension 49.07 17.24 6 90495 35987 46559574
White blood cell disorder 48.96 17.24 36 90465 1912 46593649
Delirium 48.86 17.24 7 90494 37221 46558340
Lower respiratory tract infection 48.52 17.24 23 90478 55066 46540495
Product quality issue 48.46 17.24 6 90495 35642 46559919
Septic shock 48.24 17.24 26 90475 57867 46537694
Multiple organ dysfunction syndrome 48.04 17.24 20 90481 51690 46543871
Confusional state 47.67 17.24 155 90346 159737 46435824
Atrial fibrillation 47.26 17.24 80 90421 103510 46492051
Pneumonia 47.26 17.24 484 90017 375836 46219725
Metastases to kidney 47.09 17.24 17 90484 190 46595371
Breast pain 46.27 17.24 65 90436 7529 46588032
Adverse event 45.87 17.24 6 90495 34178 46561383
Encephalopathy 44.83 17.24 6 90495 33583 46561978
Pancytopenia 43.95 17.24 299 90202 84759 46510802
International normalised ratio increased 43.77 17.24 18 90483 46865 46548696
Erythema 43.58 17.24 137 90364 142683 46452878
Hyperkalaemia 43.40 17.24 22 90479 50687 46544874
Incorrect dose administered 43.32 17.24 17 90484 45533 46550028
Agitation 43.17 17.24 27 90474 55388 46540173
Skin exfoliation 42.86 17.24 151 90350 32787 46562774
Tremor 42.73 17.24 101 90400 115538 46480023
Product use issue 42.70 17.24 322 90179 94322 46501239
Neoplasm recurrence 42.67 17.24 36 90465 2337 46593224
Acute myocardial infarction 41.90 17.24 6 90495 31918 46563643
Musculoskeletal stiffness 41.72 17.24 79 90422 97914 46497647
Malignant pleural effusion 41.57 17.24 36 90465 2422 46593139
Mobility decreased 41.35 17.24 34 90467 60560 46535001
Pneumonia aspiration 41.34 17.24 6 90495 31599 46563962
Oral mucosal blistering 41.22 17.24 49 90452 4811 46590750
Fibromyalgia 41.15 17.24 10 90491 36453 46559108
C-reactive protein increased 41.08 17.24 32 90469 58558 46537003
Hypokalaemia 41.06 17.24 67 90434 87957 46507604
Flushing 40.79 17.24 39 90462 64575 46530986
Haematuria 40.52 17.24 3 90498 26855 46568706
COVID-19 40.24 17.24 102 90399 18473 46577088
Unresponsive to stimuli 40.08 17.24 7 90494 32167 46563394
Carbohydrate antigen 27.29 increased 39.53 17.24 11 90490 47 46595514
Palpitations 39.50 17.24 78 90423 95181 46500380
Immune system disorder 39.47 17.24 62 90439 7933 46587628
Metastases to retroperitoneum 39.31 17.24 14 90487 150 46595411
Metastases to pleura 38.76 17.24 25 90476 1071 46594490
Drug withdrawal syndrome 38.76 17.24 4 90497 27380 46568181
Myocardial infarction 38.62 17.24 82 90419 97446 46498115
Injection site swelling 38.43 17.24 15 90486 40312 46555249
Laboratory test abnormal 38.10 17.24 114 90387 22733 46572828
Musculoskeletal chest pain 37.75 17.24 98 90403 18008 46577553
Chronic kidney disease 37.66 17.24 16 90485 40855 46554706
Pancreatitis 37.23 17.24 19 90482 43608 46551953
Sinusitis 37.16 17.24 128 90373 129640 46465921
Angioedema 36.89 17.24 15 90486 39327 46556234
Inappropriate schedule of product administration 36.83 17.24 43 90458 64970 46530591
Hallucination 36.67 17.24 26 90475 49925 46545636
Arrhythmia 36.59 17.24 11 90490 34830 46560731
Memory impairment 36.52 17.24 266 90235 77071 46518490
Blood pressure systolic increased 36.44 17.24 6 90495 28781 46566780
Pleural neoplasm 35.85 17.24 12 90489 105 46595456
Medication error 35.83 17.24 8 90493 30903 46564658
Metastases to skin 35.81 17.24 26 90475 1354 46594207
Product dose omission in error 35.73 17.24 18 90483 477 46595084
Pericarditis 35.18 17.24 3 90498 23924 46571637
Therapeutic response decreased 35.04 17.24 20 90481 43125 46552436
Metastases to spine 34.92 17.24 34 90467 2660 46592901
Ageusia 34.84 17.24 72 90429 11400 46584161
Heart rate increased 34.81 17.24 57 90444 74734 46520827
Flatulence 34.70 17.24 129 90372 28749 46566812
Abdominal pain 34.39 17.24 283 90218 229748 46365813
Leukocytosis 34.22 17.24 3 90498 23395 46572166
Altered state of consciousness 34.13 17.24 3 90498 23345 46572216
Invasive lobular breast carcinoma 34.03 17.24 19 90482 623 46594938
Dyspepsia 33.77 17.24 238 90263 68234 46527327
Inflammation 33.75 17.24 27 90474 48754 46546807
Cardiac failure 33.55 17.24 65 90436 79883 46515678
Sedation 33.34 17.24 3 90498 22907 46572654
Wrong technique in product usage process 33.03 17.24 34 90467 54388 46541173
Injection site bruising 32.75 17.24 14 90487 35622 46559939
Unevaluable event 32.65 17.24 25 90476 46150 46549411
Hypoacusis 32.51 17.24 102 90399 20867 46574694
Dyskinesia 32.51 17.24 8 90493 28917 46566644
Hypomagnesaemia 32.07 17.24 3 90498 22207 46573354
Sleep apnoea syndrome 32.06 17.24 3 90498 22198 46573363
Prehypertension 31.90 17.24 7 90494 7 46595554
Heart rate decreased 31.58 17.24 11 90490 31712 46563849
Pulmonary arterial hypertension 31.52 17.24 6 90495 25922 46569639
Hair texture abnormal 31.45 17.24 33 90468 2823 46592738
Oedema 31.32 17.24 51 90450 67020 46528541
Carcinoembryonic antigen increased 30.89 17.24 24 90477 1385 46594176
Chest pain 30.59 17.24 208 90293 176116 46419445
Wheezing 30.57 17.24 35 90466 53351 46542210
Blood creatine phosphokinase increased 30.52 17.24 8 90493 27716 46567845
Aggression 30.50 17.24 4 90497 22740 46572821
Respiratory distress 30.20 17.24 12 90489 31904 46563657
Oropharyngeal pain 29.96 17.24 246 90255 73922 46521639
Gingival pain 29.67 17.24 47 90454 6056 46589505
Injection site haemorrhage 29.37 17.24 3 90498 20706 46574855
Pulmonary thrombosis 29.31 17.24 52 90449 7350 46588211
Stevens-Johnson syndrome 29.17 17.24 5 90496 23292 46572269
Mucosal inflammation 29.14 17.24 151 90350 38825 46556736
Mental status changes 29.06 17.24 19 90482 38069 46557492
Ill-defined disorder 29.04 17.24 8 90493 26819 46568742
Basal cell carcinoma 28.97 17.24 3 90498 20484 46575077
Angina pectoris 28.95 17.24 8 90493 26767 46568794
Dry mouth 28.91 17.24 194 90307 54732 46540829
Anaphylactic shock 28.59 17.24 3 90498 20271 46575290
Liver function test abnormal 28.26 17.24 29 90472 46458 46549103
Hemiparesis 28.22 17.24 3 90498 20066 46575495
Metastasis 27.91 17.24 38 90463 4274 46591287
Bursitis 27.82 17.24 3 90498 19839 46575722
Epilepsy 27.80 17.24 6 90495 23732 46571829
Hypertransaminasaemia 27.68 17.24 34 90467 3454 46592107
Breast cancer recurrent 27.67 17.24 36 90465 3875 46591686
Nasal dryness 27.59 17.24 34 90467 3466 46592095
Multiple sclerosis 27.58 17.24 7 90494 24784 46570777
Hypoxia 27.56 17.24 36 90465 51802 46543759
Wound 26.82 17.24 26 90475 42776 46552785
Spinal pain 26.49 17.24 59 90442 9833 46585728
Sinus tachycardia 26.34 17.24 5 90496 21644 46573917
Chest discomfort 25.86 17.24 89 90412 90180 46505381
Pleural effusion 25.79 17.24 260 90241 82692 46512869
Rash maculo-papular 25.54 17.24 11 90490 27863 46567698
Melaena 25.38 17.24 11 90490 27761 46567800
Loss of personal independence in daily activities 25.31 17.24 45 90456 57138 46538423
Therapy interrupted 25.21 17.24 61 90440 10730 46584831
Swelling face 25.10 17.24 40 90461 53019 46542542
Metastases to adrenals 25.07 17.24 16 90485 673 46594888
Femur fracture 24.94 17.24 21 90480 36976 46558585
Cytomegalovirus infection 24.79 17.24 3 90498 18141 46577420
Fluid overload 24.47 17.24 11 90490 27174 46568387
Nail growth abnormal 24.38 17.24 14 90487 485 46595076
Feeling cold 24.37 17.24 86 90415 18685 46576876
Pneumonitis 24.01 17.24 114 90387 28306 46567255
Arthralgia 23.77 17.24 897 89604 363706 46231855
Hair growth abnormal 23.72 17.24 27 90474 2531 46593030
Hyperglycaemia 23.53 17.24 20 90481 35051 46560510
Adverse drug reaction 23.38 17.24 31 90470 44331 46551230
Hypoaesthesia 23.15 17.24 341 90160 118528 46477033
Coagulopathy 23.09 17.24 4 90497 18495 46577066
Haematoma 22.86 17.24 17 90484 31855 46563706
Pain of skin 22.82 17.24 48 90453 7694 46587867
Nasal discomfort 22.78 17.24 32 90469 3706 46591855
Bone cancer 22.72 17.24 18 90483 1069 46594492
Ventricular tachycardia 22.71 17.24 3 90498 16964 46578597
Infusion site coldness 22.61 17.24 10 90491 196 46595365
Urine odour abnormal 22.47 17.24 37 90464 4925 46590636
Hip arthroplasty 22.43 17.24 4 90497 18108 46577453
Abnormal behaviour 21.48 17.24 7 90494 21051 46574510
Adnexa uteri mass 21.46 17.24 13 90488 498 46595063
Pallor 21.45 17.24 9 90492 23157 46572404
Breast cancer female 21.22 17.24 40 90461 5923 46589638
Acute respiratory distress syndrome 21.14 17.24 8 90493 21914 46573647
Blood cholesterol increased 21.05 17.24 28 90473 39985 46555576
Body surface area increased 20.99 17.24 4 90497 0 46595561
Foot fracture 20.90 17.24 6 90495 19576 46575985
Pruritus 20.82 17.24 616 89885 241736 46353825
Chronic obstructive pulmonary disease 20.75 17.24 51 90450 57582 46537979
Deep vein thrombosis 20.65 17.24 82 90419 79691 46515870
Abdominal lymphadenopathy 20.58 17.24 13 90488 537 46595024
Upper gastrointestinal haemorrhage 20.08 17.24 4 90497 16734 46578827
Night sweats 19.97 17.24 105 90396 27145 46568416
Metastases to the mediastinum 19.92 17.24 12 90489 455 46595106
Blood pressure fluctuation 19.66 17.24 18 90483 30430 46565131
Shock 19.42 17.24 9 90492 21836 46573725
Gamma-glutamyltransferase decreased 19.32 17.24 10 90491 281 46595280
Haematotoxicity 19.30 17.24 42 90459 6891 46588670
Pulmonary tumour thrombotic microangiopathy 19.22 17.24 6 90495 41 46595520
Mucosal hypertrophy 19.10 17.24 5 90496 16 46595545
Drug level increased 19.04 17.24 6 90495 18435 46577126
Staphylococcal infection 18.85 17.24 25 90476 35746 46559815
Renal failure 18.70 17.24 136 90365 113458 46482103
Nasopharyngitis 18.37 17.24 409 90092 153589 46441972
Bronchospasm 18.33 17.24 4 90497 15703 46579858
Body temperature increased 18.17 17.24 13 90488 24848 46570713
Cardiac disorder 18.10 17.24 36 90465 43822 46551739
Eating disorder 18.05 17.24 66 90435 14588 46580973
Neutrophil count abnormal 18.03 17.24 23 90478 2427 46593134
Pseudocirrhosis 17.94 17.24 13 90488 675 46594886
Granulocyte count decreased 17.90 17.24 14 90487 816 46594745
Artificial menopause 17.85 17.24 5 90496 22 46595539
Weight decreased 17.85 17.24 535 89966 210314 46385247
Dry eye 17.73 17.24 110 90391 30212 46565349
Somnolence 17.70 17.24 206 90295 156315 46439246
Ovarian cyst 17.69 17.24 3 90498 14084 46581477
Illness 17.62 17.24 58 90443 12166 46583395
Circulatory collapse 17.59 17.24 10 90491 21614 46573947
Skin toxicity 17.57 17.24 28 90473 3626 46591935
Cholelithiasis 17.51 17.24 30 90471 38651 46556910
Cardiomegaly 17.51 17.24 6 90495 17476 46578085
Foreign body in throat 17.50 17.24 5 90496 24 46595537
Ataxia 17.41 17.24 3 90498 13927 46581634
Joint range of motion decreased 17.35 17.24 4 90497 15120 46580441
Body surface area decreased 17.34 17.24 4 90497 6 46595555

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
Product use issue 639.93 40.55 193 1604 45823 29904858
Neoplasm progression 302.35 40.55 88 1709 17935 29932746
Product use in unapproved indication 193.85 40.55 92 1705 73601 29877080
Off label use 120.92 40.55 107 1690 249183 29701498
Fatigue 75.95 40.55 94 1703 320579 29630102
Death 50.50 40.55 82 1715 357201 29593480
Xerosis 48.09 40.55 10 1787 493 29950188
White blood cell count decreased 46.19 40.55 39 1758 83908 29866773
Neutropenia 40.71 40.55 44 1753 128496 29822185

Pharmacologic Action:

SourceCodeDescription
ATC L01EF01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Cyclin-dependent kinase (CDK) inhibitors
FDA MoA N0000175082 Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA MoA N0000190114 Cytochrome P450 3A Inhibitors
CHEBI has role CHEBI:35610 cytostatic
CHEBI has role CHEBI:82665 ndk inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hormone receptor positive malignant neoplasm of breast indication 417181009
Human epidermal growth factor 2 negative carcinoma of breast indication 431396003

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.03 Basic
pKa2 7.08 Basic
pKa3 5.81 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Cyclin-dependent kinase 4 Kinase INHIBITOR IC50 7.96 SCIENTIFIC LITERATURE DRUG LABEL
Cyclin-dependent kinase 6 Kinase INHIBITOR IC50 7.82 SCIENTIFIC LITERATURE DRUG LABEL
Dual specificity tyrosine-phosphorylation-regulated kinase 1A Kinase INHIBITOR IC50 5.70 SCIENTIFIC LITERATURE
Ribosomal protein S6 kinase alpha-1 Kinase INHIBITOR IC50 5.10 SCIENTIFIC LITERATURE
Receptor-type tyrosine-protein kinase FLT3 Kinase IC50 5.46 CHEMBL
CDK2/Cyclin A Kinase IC50 6.64 CHEMBL
Tyrosine-protein kinase JAK3 Kinase IC50 7.20 CHEMBL
Cyclin-dependent kinase 9 Kinase IC50 6.10 CHEMBL
Cyclin-dependent kinase 4/cyclin D1 Kinase IC50 8.70 CHEMBL
CDK6/cyclin D1 Kinase IC50 8.42 CHEMBL

External reference:

IDSource
D10372 KEGG_DRUG
4034136 VUID
N0000191426 NUI
827022-33-3 SECONDARY_CAS_RN
4034136 VANDF
C3883373 UMLSCUI
CHEBI:85993 CHEBI
LQQ PDB_CHEM_ID
CHEMBL189963 ChEMBL_ID
CHEMBL2364621 ChEMBL_ID
DB09073 DRUGBANK_ID
C500026 MESH_SUPPLEMENTAL_RECORD_UI
7380 IUPHAR_LIGAND_ID
9802 INN_ID
G9ZF61LE7G UNII
5330286 PUBCHEM_CID
1601374 RXNORM
232484 MMSL
30872 MMSL
d08342 MMSL
015881 NDDF
715958001 SNOMEDCT_US
763549001 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 0069-0187 CAPSULE 75 mg ORAL NDA 29 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 0069-0188 CAPSULE 100 mg ORAL NDA 29 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 0069-0189 CAPSULE 125 mg ORAL NDA 29 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 0069-0284 TABLET, FILM COATED 75 mg ORAL NDA 32 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 0069-0486 TABLET, FILM COATED 100 mg ORAL NDA 32 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 0069-0688 TABLET, FILM COATED 125 mg ORAL NDA 32 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 63539-187 CAPSULE 75 mg ORAL NDA 30 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 63539-188 CAPSULE 100 mg ORAL NDA 30 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 63539-189 CAPSULE 125 mg ORAL NDA 30 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 63539-284 TABLET, FILM COATED 75 mg ORAL NDA 32 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 63539-486 TABLET, FILM COATED 100 mg ORAL NDA 32 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 63539-688 TABLET, FILM COATED 125 mg ORAL NDA 32 sections