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
Fatigue 10137.74 46.63 3647 15340 81226 2257872
White blood cell count decreased 9541 46.63 2461 16526 15747 2323351
Neoplasm progression 8266.83 46.63 1706 17281 2962 2336136
Neutropenia 5709.38 46.63 1714 17273 19834 2319264
Alopecia 4455.24 46.63 1427 17560 20574 2318524
Nausea 3955.99 46.63 2063 16924 110126 2228972
Disease progression 2515.63 46.63 875 18112 16220 2322878
Stomatitis 2240.61 46.63 699 18288 9011 2330087
Diarrhoea 2212.88 46.63 1281 17706 82283 2256815
Full blood count decreased 2121.97 46.63 540 18447 3053 2336045
Decreased appetite 2068.99 46.63 875 18112 28016 2311082
Constipation 1618.96 46.63 677 18310 20952 2318146
Asthenia 1550.07 46.63 835 18152 46091 2293007
Neutrophil count decreased 1434.29 46.63 454 18533 6113 2332985
Bone marrow failure 1404.70 46.63 432 18555 5254 2333844
Death 1363.34 46.63 937 18050 80531 2258567
Platelet count decreased 1256.03 46.63 517 18470 15296 2323802
Hot flush 1224.65 46.63 412 18575 6787 2332311
Red blood cell count decreased 1112.21 46.63 338 18649 3928 2335170
Leukopenia 1030.55 46.63 397 18590 9799 2329299
Vomiting 1015.72 46.63 746 18241 70856 2268242
Epistaxis 921.61 46.63 362 18625 9417 2329681
Product dose omission 894.99 46.63 545 18442 37712 2301386
Thrombocytopenia 886.06 46.63 429 18558 18702 2320396
Arthralgia 884.37 46.63 616 18371 53669 2285429
Dry skin 850.82 46.63 308 18679 6344 2332754
Pain 845.64 46.63 631 18356 61226 2277872
Blood count abnormal 833.51 46.63 235 18752 2047 2337051
Anaemia 822.05 46.63 499 18488 34293 2304805
Dizziness 811.84 46.63 603 18384 58062 2281036
Back pain 807.33 46.63 477 18510 31182 2307916
Rash 805.94 46.63 604 18383 58954 2280144
Cough 805.59 46.63 484 18503 32633 2306465
Breast cancer metastatic 793.08 46.63 223 18764 1921 2337177
Therapy cessation 791.66 46.63 274 18713 4919 2334179
Neuropathy peripheral 776.96 46.63 335 18652 11097 2328001
Dyspnoea 768.40 46.63 659 18328 78074 2261024
Bone pain 760.40 46.63 308 18679 8688 2330410
Tumour marker increased 678.84 46.63 159 18828 585 2338513
Headache 652.51 46.63 606 18381 79573 2259525
Haemoglobin decreased 643.59 46.63 340 18647 17811 2321287
Weight decreased 603.53 46.63 381 18606 27990 2311108
Oral pain 598.97 46.63 200 18787 3197 2335901
Product use issue 581.13 46.63 279 18708 11890 2327208
Malaise 568.93 46.63 479 18508 55106 2283992
Product use in unapproved indication 565.98 46.63 267 18720 10933 2328165
Pruritus 561.56 46.63 429 18558 42911 2296187
Pain in extremity 537.74 46.63 415 18572 42125 2296973
Nasopharyngitis 534.44 46.63 322 18665 21734 2317364
Dysgeusia 506.68 46.63 227 18760 8232 2330866
Abdominal discomfort 491.62 46.63 281 18706 17175 2321923
Malignant neoplasm progression 457.50 46.63 237 18750 11891 2327207
Insomnia 442.50 46.63 303 18684 25484 2313614
Pyrexia 437.56 46.63 407 18580 53301 2285797
Peripheral swelling 415.94 46.63 253 18734 17344 2321754
Hypoaesthesia 415.71 46.63 266 18721 19949 2319149
Pancytopenia 415.34 46.63 218 18769 11234 2327864
Cytopenia 382.26 46.63 107 18880 902 2338196
Condition aggravated 375.46 46.63 299 18688 31680 2307418
Pneumonia 375.34 46.63 360 18627 48936 2290162
Urinary tract infection 351.53 46.63 280 18707 29662 2309436
Oropharyngeal pain 341.77 46.63 192 18795 11326 2327772
Dyspepsia 341.60 46.63 182 18805 9662 2329436
Metastases to bone 338.79 46.63 118 18869 2151 2336947
Therapy change 326.81 46.63 96 18891 977 2338121
Depression 325.75 46.63 261 18726 27871 2311227
Muscle spasms 317.70 46.63 231 18756 21335 2317763
Memory impairment 316.02 46.63 190 18797 12733 2326365
Paraesthesia 310.50 46.63 230 18757 21858 2317240
Abdominal pain upper 303.66 46.63 227 18760 21873 2317225
Neoplasm malignant 299.43 46.63 135 18852 4958 2334140
Dehydration 293.01 46.63 223 18764 22072 2317026
Rhinorrhoea 289.64 46.63 149 18838 7351 2331747
Dry mouth 279.01 46.63 150 18837 8103 2330995
Lacrimation increased 270.40 46.63 106 18881 2724 2336374
Pleural effusion 268.42 46.63 165 18822 11503 2327595
Breast cancer 262.02 46.63 151 18836 9344 2329754
Febrile neutropenia 250.59 46.63 154 18833 10728 2328370
Chills 243.60 46.63 173 18814 15379 2323719
Onychoclasis 228.70 46.63 69 18918 775 2338323
Myalgia 227.32 46.63 196 18791 23137 2315961
Skin exfoliation 226.32 46.63 116 18871 5674 2333424
Anxiety 218.40 46.63 212 18775 29147 2309951
Pulmonary embolism 213.84 46.63 170 18817 17913 2321185
Lymphoedema 196.06 46.63 66 18921 1079 2338019
Dysphagia 194.85 46.63 140 18847 12665 2326433
Contusion 190.23 46.63 138 18849 12672 2326426
Flatulence 186.57 46.63 94 18893 4431 2334667
Musculoskeletal chest pain 178.84 46.63 75 18912 2301 2336797
Musculoskeletal pain 177.70 46.63 124 18863 10706 2328392
Weight increased 176.84 46.63 167 18820 22170 2316928
Second primary malignancy 176.26 46.63 59 18928 947 2338151
Metastases to liver 176.12 46.63 79 18908 2862 2336236
Influenza 175.15 46.63 132 18855 12846 2326252
Infection 172.58 46.63 150 18837 17879 2321219
Nail disorder 169.23 46.63 59 18928 1077 2338021
Feeling abnormal 167.30 46.63 166 18821 23415 2315683
Renal impairment 166.62 46.63 116 18871 9976 2329122
Thrombosis 164.92 46.63 111 18876 9033 2330065
Abdominal pain 163.53 46.63 196 18791 34178 2304920
Dry eye 162.56 46.63 82 18905 3874 2335224
Night sweats 156.99 46.63 77 18910 3423 2335675
Mucosal inflammation 154.58 46.63 87 18900 5137 2333961
Dysphonia 153.96 46.63 93 18894 6271 2332827
Somnolence 151.40 46.63 157 18830 23328 2315770
Gait disturbance 149.45 46.63 153 18834 22392 2316706
Carbohydrate antigen 15-3 increased 147.99 46.63 33 18954 91 2339007
Glossodynia 141.72 46.63 60 18927 1885 2337213
Full blood count abnormal 140.18 46.63 38 18949 280 2338818
Blood test abnormal 138.78 46.63 53 18934 1265 2337833
Fall 136.32 46.63 211 18776 46888 2292210
Madarosis 135.49 46.63 44 18943 639 2338459
Breast pain 133.21 46.63 52 18935 1319 2337779
Rash pruritic 129.98 46.63 89 18898 7446 2331652
Abdominal distension 129.71 46.63 101 18886 10310 2328788
Productive cough 129.32 46.63 78 18909 5243 2333855
Vision blurred 128.30 46.63 116 18871 14552 2324546
Gastrooesophageal reflux disease 128.24 46.63 95 18892 9000 2330098
Ascites 122.87 46.63 77 18910 5543 2333555
Laboratory test abnormal 122.03 46.63 75 18912 5215 2333883
Oral mucosal blistering 120.90 46.63 43 18944 834 2338264
Ageusia 120.67 46.63 54 18933 1944 2337154
White blood cell count abnormal 117.63 46.63 40 18947 675 2338423
Nasal congestion 114.79 46.63 80 18907 6886 2332212
Aspartate aminotransferase increased 114.76 46.63 102 18885 12510 2326588
Blister 112.13 46.63 78 18909 6693 2332405
Immune system disorder 110.62 46.63 46 18941 1380 2337718
Sepsis 107.41 46.63 117 18870 18371 2320727
Bronchitis 105.53 46.63 101 18886 13613 2325485
Muscular weakness 102.13 46.63 103 18884 14794 2324304
Hepatic enzyme increased 100.75 46.63 85 18902 9717 2329381
Metastases to lung 98.87 46.63 45 18942 1686 2337412
Hypertransaminasaemia 98.67 46.63 34 18953 598 2338500
Pulmonary oedema 97.31 46.63 74 18913 7289 2331809
Mouth ulceration 96.75 46.63 58 18929 3854 2335244
Cancer pain 94.65 46.63 28 18959 292 2338806
Sleep disorder 91.95 46.63 68 18919 6421 2332677
Breast cancer female 91.78 46.63 40 18947 1350 2337748
Oral herpes 91.49 46.63 46 18941 2156 2336942
Alanine aminotransferase increased 90.70 46.63 94 18893 13938 2325160
Pneumonitis 89.94 46.63 56 18931 3983 2335115
Upper respiratory tract infection 89.41 46.63 76 18911 8775 2330323
Visual impairment 89.35 46.63 86 18901 11669 2327429
Feeling cold 89.23 46.63 51 18936 3099 2335999
Balance disorder 88.99 46.63 79 18908 9668 2329430
Sinusitis 88.09 46.63 100 18887 16426 2322672
Dyspnoea exertional 88.00 46.63 63 18924 5657 2333441
Osteonecrosis of jaw 87.69 46.63 72 18915 7924 2331174
Liver function test increased 87.29 46.63 50 18937 3051 2336047
Eating disorder 87.07 46.63 45 18942 2236 2336862
Pulmonary thrombosis 86.01 46.63 36 18951 1098 2338000
Cellulitis 84.85 46.63 75 18912 9126 2329972
Skin discolouration 84.08 46.63 60 18927 5360 2333738
Urine odour abnormal 82.97 46.63 31 18956 695 2338403
Hepatic failure 81.47 46.63 60 18927 5629 2333469
Poor quality sleep 81.46 46.63 41 18946 1926 2337172
Chest pain 81.20 46.63 126 18861 28011 2311087
Increased appetite 80.88 46.63 37 18950 1403 2337695
Renal failure 80.86 46.63 98 18889 17251 2321847
Toothache 80.82 46.63 45 18942 2599 2336499
Limb discomfort 80.72 46.63 49 18938 3330 2335768
Skin lesion 80.15 46.63 52 18935 3973 2335125
Hyperhidrosis 79.96 46.63 92 18895 15330 2323768
Blood creatinine increased 78.05 46.63 76 18911 10457 2328641
Pain of skin 77.56 46.63 36 18951 1412 2337686
Hypersomnia 77.09 46.63 42 18945 2324 2336774
Gingival pain 76.38 46.63 33 18954 1090 2338008
Blood potassium decreased 76.08 46.63 56 18931 5249 2333849
Nasal dryness 74.40 46.63 27 18960 556 2338542
Taste disorder 74.00 46.63 25 18962 413 2338685
Dysuria 73.80 46.63 49 18938 3892 2335206
Hypertension 72.71 46.63 118 18869 27243 2311855
Burning sensation 72.56 46.63 64 18923 7764 2331334
Confusional state 71.61 46.63 110 18877 24234 2314864
Breast cancer stage IV 70.90 46.63 18 18969 99 2338999
Cataract 70.72 46.63 56 18931 5852 2333246
Amnesia 68.63 46.63 60 18927 7193 2331905
Hypoacusis 67.58 46.63 44 18943 3381 2335717
Neck pain 67.51 46.63 61 18926 7636 2331462
White blood cell disorder 66.35 46.63 22 18965 342 2338756
General physical health deterioration 66.09 46.63 80 18907 14059 2325039
Nasal discomfort 65.56 46.63 26 18961 688 2338410
Haematocrit decreased 65.13 46.63 47 18940 4271 2334827
Cerebrovascular accident 64.76 46.63 95 18892 20091 2319007
Gastric disorder 62.02 46.63 43 18944 3667 2335431
Retching 61.95 46.63 35 18952 2079 2337019
Spinal pain 61.52 46.63 30 18957 1315 2337783
Viral upper respiratory tract infection 61.31 46.63 28 18959 1057 2338041
Body height decreased 60.76 46.63 29 18958 1212 2337886
Intentional product misuse 60.28 46.63 63 18924 9426 2329672
Arthritis 59.46 46.63 64 18923 9904 2329194
Pollakiuria 59.22 46.63 42 18945 3714 2335384
Blood pressure increased 58.97 46.63 83 18904 16903 2322195
Sinus congestion 58.20 46.63 33 18954 1974 2337124
Appetite disorder 57.80 46.63 23 18964 614 2338484
Sinus disorder 56.78 46.63 36 18951 2642 2336456
Hospitalisation 56.71 46.63 76 18911 14777 2324321
Joint swelling 56.63 46.63 81 18906 16738 2322360
Feeding disorder 56.32 46.63 29 18958 1429 2337669
Herpes zoster 55.49 46.63 61 18926 9664 2329434
Blood glucose increased 54.94 46.63 68 18919 12222 2326876
Skin fissures 54.52 46.63 27 18960 1224 2337874
Metastases to lymph nodes 54.47 46.63 25 18962 955 2338143
Cystitis 54.03 46.63 47 18940 5595 2333503
Skin disorder 53.57 46.63 39 18948 3592 2335506
Oedema peripheral 51.94 46.63 94 18893 23669 2315429
Decreased immune responsiveness 51.86 46.63 22 18965 694 2338404
Neoplasm recurrence 51.70 46.63 19 18968 406 2338692
Aphthous ulcer 51.33 46.63 27 18960 1391 2337707
Stress 51.27 46.63 50 18937 6888 2332210
Renal disorder 50.43 46.63 41 18946 4447 2334651
Hepatocellular injury 49.74 46.63 39 18948 4016 2335082
Feeling hot 49.47 46.63 49 18938 6879 2332219
Depressed mood 49.17 46.63 43 18944 5155 2333943
Carbohydrate antigen 27.29 increased 48.90 46.63 10 18977 15 2339083
Tumour marker abnormal 47.77 46.63 10 18977 18 2339080
Carcinoembryonic antigen increased 47.66 46.63 16 18971 259 2338839
Localised infection 47.29 46.63 33 18954 2843 2336255
Hair texture abnormal 47.07 46.63 19 18968 527 2338571
Mean cell volume increased 47.07 46.63 17 18970 345 2338753

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 912.08 44.52 178 385 8393 1737825
Neoplasm progression 298.70 44.52 61 502 3206 1743012
Product use in unapproved indication 239.29 44.52 62 501 9360 1736858
Fatigue 169.95 44.52 72 491 50709 1695509
Off label use 132.66 44.52 56 507 38515 1707703
Death 94.40 44.52 58 505 87385 1658833
Disease progression 72.11 44.52 29 534 17234 1728984
Neutropenia 70.53 44.52 29 534 18231 1727987
White blood cell count decreased 68.70 44.52 26 537 13123 1733095
Xerosis 61.47 44.52 10 553 136 1746082

Pharmacologic Action:

SourceCodeDescription
ATC L01XE33 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Protein kinase inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000175082 Kinase Inhibitors
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
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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MG IBRANCE PFIZER INC N207103 Feb. 3, 2015 RX CAPSULE ORAL 7456168 Jan. 16, 2023 PALBOCICLIB FOR HR-POS. HER2-NEG. ADVANCED OR METASTATIC BREAST CANCER IN COMBO WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY IN POSTMENOPAUSAL WOMEN OR MEN, OR WITH FULVESTRANT IN PTS WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY
100MG IBRANCE PFIZER INC N207103 Feb. 3, 2015 RX CAPSULE ORAL 7456168 Jan. 16, 2023 TREATING HR-POS., HER2-NEG. ADVANCED OR METASTATIC BREAST CANCER WITH PALBOCICLIB IN COMBO WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE BASED THERAPY IN POSTMENOPAUSAL WOMEN OR FULVESTRANT IN WOMEN WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY
125MG IBRANCE PFIZER INC N207103 Feb. 3, 2015 RX CAPSULE ORAL 7456168 Jan. 16, 2023 PALBOCICLIB FOR HR-POS. HER2-NEG. ADVANCED OR METASTATIC BREAST CANCER IN COMBO WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY IN POSTMENOPAUSAL WOMEN OR MEN, OR WITH FULVESTRANT IN PTS WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY
125MG IBRANCE PFIZER INC N207103 Feb. 3, 2015 RX CAPSULE ORAL 7456168 Jan. 16, 2023 TREATING HR-POS., HER2-NEG. ADVANCED OR METASTATIC BREAST CANCER WITH PALBOCICLIB IN COMBO WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE BASED THERAPY IN POSTMENOPAUSAL WOMEN OR FULVESTRANT IN WOMEN WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY
75MG IBRANCE PFIZER INC N207103 Feb. 3, 2015 RX CAPSULE ORAL 7456168 Jan. 16, 2023 PALBOCICLIB FOR HR-POS. HER2-NEG. ADVANCED OR METASTATIC BREAST CANCER IN COMBO WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY IN POSTMENOPAUSAL WOMEN OR MEN, OR WITH FULVESTRANT IN PTS WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY
75MG IBRANCE PFIZER INC N207103 Feb. 3, 2015 RX CAPSULE ORAL 7456168 Jan. 16, 2023 TREATING HR-POS., HER2-NEG. ADVANCED OR METASTATIC BREAST CANCER WITH PALBOCICLIB IN COMBO WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE BASED THERAPY IN POSTMENOPAUSAL WOMEN OR FULVESTRANT IN WOMEN WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY
100MG IBRANCE PFIZER INC N212436 Nov. 1, 2019 RX TABLET ORAL 7456168 Jan. 16, 2023 PALBOCICLIB FOR HR-POS. HER2-NEG. ADVANCED OR METASTATIC BREAST CANCER IN COMBO WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY IN POSTMENOPAUSAL WOMEN OR MEN, OR WITH FULVESTRANT IN PTS WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY
125MG IBRANCE PFIZER INC N212436 Nov. 1, 2019 RX TABLET ORAL 7456168 Jan. 16, 2023 PALBOCICLIB FOR HR-POS. HER2-NEG. ADVANCED OR METASTATIC BREAST CANCER IN COMBO WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY IN POSTMENOPAUSAL WOMEN OR MEN, OR WITH FULVESTRANT IN PTS WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY
75MG IBRANCE PFIZER INC N212436 Nov. 1, 2019 RX TABLET ORAL 7456168 Jan. 16, 2023 PALBOCICLIB FOR HR-POS. HER2-NEG. ADVANCED OR METASTATIC BREAST CANCER IN COMBO WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY IN POSTMENOPAUSAL WOMEN OR MEN, OR WITH FULVESTRANT IN PTS WITH DISEASE PROGRESSION AFTER ENDOCRINE THERAPY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG IBRANCE PFIZER INC N207103 Feb. 3, 2015 RX CAPSULE ORAL Feb. 3, 2020 NEW CHEMICAL ENTITY
125MG IBRANCE PFIZER INC N207103 Feb. 3, 2015 RX CAPSULE ORAL Feb. 3, 2020 NEW CHEMICAL ENTITY
75MG IBRANCE PFIZER INC N207103 Feb. 3, 2015 RX CAPSULE ORAL Feb. 3, 2020 NEW CHEMICAL ENTITY
100MG IBRANCE PFIZER INC N212436 Nov. 1, 2019 RX TABLET ORAL Feb. 3, 2020 NEW CHEMICAL ENTITY
125MG IBRANCE PFIZER INC N212436 Nov. 1, 2019 RX TABLET ORAL Feb. 3, 2020 NEW CHEMICAL ENTITY
75MG IBRANCE PFIZER INC N212436 Nov. 1, 2019 RX TABLET ORAL Feb. 3, 2020 NEW CHEMICAL ENTITY

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
C3853822 UMLSCUI
763549001 SNOMEDCT_US
1601374 RXNORM
30872 MMSL
d08342 MMSL
015881 NDDF
4034136 VANDF
715958001 SNOMEDCT_US
5330286 PUBCHEM_CID
CHEBI:85993 CHEBI
CHEMBL189963 ChEMBL_ID
G9ZF61LE7G UNII
9802 INN_ID
827022-33-3 SECONDARY_CAS_RN
LQQ PDB_CHEM_ID
DB09073 DRUGBANK_ID
C500026 MESH_SUPPLEMENTAL_RECORD_UI
CHEMBL2364621 ChEMBL_ID
7380 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 0069-0187 CAPSULE 75 mg ORAL NDA 19 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 0069-0188 CAPSULE 100 mg ORAL NDA 19 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 0069-0189 CAPSULE 125 mg ORAL NDA 19 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 0069-0284 TABLET, FILM COATED 75 mg ORAL NDA 18 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 0069-0486 TABLET, FILM COATED 100 mg ORAL NDA 18 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 0069-0688 TABLET, FILM COATED 125 mg ORAL NDA 18 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 63539-187 CAPSULE 75 mg ORAL NDA 19 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 63539-188 CAPSULE 100 mg ORAL NDA 19 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 63539-189 CAPSULE 125 mg ORAL NDA 19 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 63539-284 TABLET, FILM COATED 75 mg ORAL NDA 18 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 63539-486 TABLET, FILM COATED 100 mg ORAL NDA 18 sections
Ibrance HUMAN PRESCRIPTION DRUG LABEL 1 63539-688 TABLET, FILM COATED 125 mg ORAL NDA 18 sections