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

Stem definitionDrug idCAS RN
cyclin dependant kinase inhibitors 5259 1231929-97-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • abemaciclib
  • LY2835219
  • verzenio
Abemaciclib is an inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6). These kinases are activated upon binding to D-cyclins. In estrogen receptor-positive (ER+) breast cancer cell lines, cyclin D1 and CDK4/6 promote phosphorylation of the retinoblastoma protein (Rb), cell cycle progression, and cell proliferation. In vitro, continuous exposure to abemaciclib inhibited Rb phosphorylation and blocked progression from G1 into S phase of the cell cycle, resulting in senescence and apoptosis. In breast cancer xenograft models, abemaciclib dosed daily without interruption as a single agent or in combination with antiestrogens resulted in reduction of tumor size.
  • Molecular weight: 506.61
  • Formula: C27H32F2N8
  • CLOGP: 4.76
  • LIPINSKI: 1
  • HAC: 8
  • HDO: 1
  • TPSA: 75
  • ALOGS: -4.50
  • ROTB: 7
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.30 g O

ADMET properties:

PropertyValueReference
S (Water solubility) 1.58 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
azlogd74 LogD at pH 7.4 3.323 Moderate 0.72
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.563 Moderate 0.72
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 14.289 10^-6 cm/s Moderate 0.72
dh-clint Dog hepatocyte intrinsic clearance 8.610 uL/min/10^6 cells Moderate 0.72
dppb Dog plasma protein binding (% unbound) 12.180 % Moderate 0.72
fcs-ppb Fetal calf serum protein binding (% unbound) 32.370 % Moderate 0.72
herg hERG pIC50 4.807 pIC50 Moderate 0.72
hh-clint Human hepatocyte intrinsic clearance 4.989 uL/min/10^6 cells Moderate 0.72
hlm-clint Human liver microsomal intrinsic clearance 135.519 uL/min/mg protein Moderate 0.72
hppb Human plasma protein binding (% unbound) 9.020 % Moderate 0.72
kinase-safety-class AAK1,ABL1,ABL2,ACVR2A,ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK8,CDK9,CHEK1,CHUK,CLK1,CLK2,CLK4,CSF1R,CSNK1A1,CSNK1A1L,CSNK1D,CSNK1E,CSNK1G1,CSNK1G2,CSNK1G3,CSNK2A1,CSNK2A2,CSNK2A3,DDR1,DYRK1A,DYRK1B,DYRK2,DYRK3,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GRK1,GRK2,GSK3A,GSK3B,HASPIN,HIPK2,IGF1R,IKBKB,INSR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP3K8,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK11,MAPK12,MAPK15,MAPK3,MAPK7,MAPK8,MAPK9,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK1,MKNK2,MST1R,MTOR,NTRK1,NTRK2,NUAK1,PAK1,PAK4,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PIM3,PLK2,PLK3,PLK4,PRKAA1,PRKAA2,PRKACA,PRKCD,PRKD1,PRKDC,PTK2,RET,ROCK1,ROCK2,RPS6KA1,SGK1,SIK2,SIK3,SRC,STK16,STK17A,STK33,STK4,SYK,TEK,TNIK,TTK,TYRO3,UHMK1,ULK1,ULK2,YES1,ZAP70 164
kinase-selectivity-class AAK1,ABL2,ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2A,CAMK2B,CAMK2D,CDK1,CDK16,CDK2,CDK3,CDK4,CDK6,CDK7,CDK8,CDK9,CHEK1,CHUK,CLK2,CLK4,CSF1R,DDR1,DYRK1A,DYRK1B,DYRK2,DYRK3,EGFR,EIF2AK3,EPHB4,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GRK2,GSK3A,GSK3B,HIPK2,IGF1R,IRAK1,IRAK3,IRAK4,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,MAP2K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K3,MAP4K5,MAPK1,MAPK7,MAPK8,MARK1,MARK2,MARK4,MELK,MET,NTRK1,NUAK1,PAK4,PDK1,PIK3CA,PIM3,PRKAA1,PRKAA2,PRKCD,PTK2,RET,ROCK1,ROCK2,SIK2,SIK3,SRC,STK16,STK17A,STK33,STK4,SYK,TGFBR1,TTK,TYRO3,ULK1,ULK2 101
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 16.672 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 16.032 Moderate 0.72
mh-clint Mouse hepatocyte intrinsic clearance 20.184 Moderate 0.72
mppb Mouse plasma protein binding (% unbound) 4.340 Moderate 0.72
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 34.594 Moderate 0.72
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 12.030 % Moderate 0.72
rat-kpuu-brain Rat brain Kpuu 0.024 % High 1
rh-clint Rat hepatocyte intrinsic clearance 11.967 uL/min/10^6 cells Moderate 0.72
rh-fuinc Rat hepatocyte fraction unbound in incubation 25.790 % Moderate 0.72
rppb Rat plasma protein binding (% unbound) 5.050 % Moderate 0.72
solubility-dd Solubility at pH 7.4 in DMSO 18.450 uM Moderate 0.72

Approvals:

DateAgencyCompanyOrphan
Sept. 26, 2018 EMA Eli Lilly Nederland B.V.
Sept. 21, 2018 PMDA Eli Lilly Japan KK
Sept. 28, 2017 FDA ELI LILLY AND CO

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Diarrhoea 1936.76 23.70 1500 15568 937690 89673689
Malignant neoplasm progression 871.73 23.70 417 16651 106453 90504926
Therapy cessation 476.06 23.70 198 16870 36163 90575216
Neutropenia 355.53 23.70 312 16756 224592 90386787
Interstitial lung disease 313.01 23.70 189 16879 76216 90535163
Therapy interrupted 261.13 23.70 145 16923 49963 90561416
Disease progression 228.72 23.70 208 16860 156407 90454972
Pneumonitis 214.33 23.70 122 16946 44048 90567331
Metastases to liver 191.28 23.70 98 16970 28709 90582670
Blood creatinine increased 174.66 23.70 148 16920 101238 90510141
Metastases to bone 170.01 23.70 87 16981 25418 90585961
Nausea 161.08 23.70 515 16553 1109801 89501578
Death 152.24 23.70 292 16776 456259 90155120
Therapy change 135.26 23.70 53 17015 8269 90603110
Dehydration 126.59 23.70 169 16899 194278 90417101
Metastases to lung 125.62 23.70 61 17007 15930 90595449
Fatigue 124.60 23.70 486 16582 1153537 89457842
White blood cell count decreased 119.27 23.70 152 16916 166957 90444422
Anaemia 109.34 23.70 219 16849 352583 90258796
Hot flush 108.91 23.70 90 16978 59398 90551981
Decreased appetite 108.74 23.70 227 16841 376313 90235066
Myelosuppression 100.03 23.70 82 16986 53509 90557870
Vomiting 98.97 23.70 349 16719 787944 89823435
Tumour marker increased 80.56 23.70 33 17035 5774 90605605
Hepatic function abnormal 62.61 23.70 59 17009 46229 90565150
Joint swelling 62.51 23.70 10 17058 503290 90108089
PIK3CA-activated mutation 60.97 23.70 18 17050 1186 90610193
Transaminases increased 59.31 23.70 52 17016 37140 90574239
Pseudocirrhosis 56.18 23.70 16 17052 928 90610451
Carbohydrate antigen 15-3 increased 55.82 23.70 19 17049 1988 90609391
Arthropathy 53.71 23.70 4 17064 366238 90245141
Pulmonary embolism 52.67 23.70 91 16977 130729 90480650
Maternal exposure during pregnancy 52.61 23.70 4 17064 360059 90251320
Drug hypersensitivity 51.66 23.70 12 17056 463597 90147782
Metastases to pleura 51.61 23.70 18 17050 2026 90609353
Progressive bulbar palsy 50.70 23.70 9 17059 54 90611325
Hospice care 50.27 23.70 28 17040 9676 90601703
Hepatic echinococciasis 49.62 23.70 9 17059 62 90611317
Neutrophil count decreased 49.28 23.70 64 17004 71468 90539911
Thrombocytopenia 49.01 23.70 116 16952 208609 90402770
Hepatotoxicity 48.27 23.70 51 17017 45791 90565588
Sinusitis 46.92 23.70 5 17063 343083 90268296
Swelling 46.38 23.70 11 17057 419047 90192332
Aspartate aminotransferase increased 45.95 23.70 75 16993 102862 90508517
Gastrointestinal toxicity 45.48 23.70 26 17042 9441 90601938
Hepatic cytolysis 42.94 23.70 40 17028 30876 90580503
Acute kidney injury 40.93 23.70 143 16925 320244 90291135
Wound 39.97 23.70 5 17063 302975 90308404
Motor neurone disease 39.43 23.70 9 17059 212 90611167
Condition aggravated 38.97 23.70 33 17035 595512 90015867
Constipation 38.30 23.70 128 16940 280267 90331112
Hypersensitivity 38.15 23.70 19 17049 454658 90156721
Treatment failure 37.78 23.70 6 17062 303922 90307457
Selenium deficiency 37.56 23.70 7 17061 57 90611322
Metastases to spinal cord 36.97 23.70 9 17059 282 90611097
Pericarditis 36.77 23.70 4 17064 270147 90341232
Lower respiratory tract infection 36.00 23.70 3 17065 250656 90360723
Alanine aminotransferase increased 35.98 23.70 73 16995 118265 90493114
Nasopharyngitis 35.71 23.70 16 17052 407088 90204291
Lung opacity 35.46 23.70 19 17049 6083 90605296
Pain 34.85 23.70 86 16982 996255 89615124
Wheezing 33.78 23.70 3 17065 238077 90373302
Metastases to central nervous system 33.04 23.70 27 17041 17515 90593864
Leukopenia 32.86 23.70 64 17004 100646 90510733
Product use issue 32.17 23.70 11 17057 329908 90281471
Blister 31.77 23.70 5 17063 254993 90356386
Bone marrow infiltration 31.60 23.70 10 17058 832 90610547
Rhabdoid tumour 31.56 23.70 6 17062 55 90611324
Gamma-glutamyltransferase increased 31.01 23.70 37 17031 37915 90573464
Tumour flare 30.57 23.70 9 17059 587 90610792
Cancer pain 30.54 23.70 15 17053 4010 90607369
Hepatic failure 28.06 23.70 36 17032 39692 90571687
Drug-induced liver injury 27.78 23.70 56 17012 90262 90521117
Platelet count decreased 27.76 23.70 72 16996 136897 90474482
Hospitalisation 27.69 23.70 69 16999 128031 90483348
Weight increased 27.50 23.70 23 17045 417904 90193475
Therapeutic product effect decreased 27.50 23.70 9 17059 277562 90333817
Pseudocellulitis 26.38 23.70 6 17062 139 90611240
Second primary malignancy 26.18 23.70 19 17049 10359 90601020
Eosinophilic pneumonia 26.14 23.70 12 17056 2761 90608618
Deep vein thrombosis 24.90 23.70 54 17014 91566 90519813
Hormone refractory breast cancer 24.77 23.70 4 17064 12 90611367
Hypertension 24.61 23.70 30 17038 457502 90153877
Renal tubular necrosis 24.51 23.70 21 17047 14534 90596845
Metastases to peritoneum 24.32 23.70 13 17055 4142 90607237
Metastases to lymph nodes 24.16 23.70 19 17049 11670 90599709
Blood bilirubin increased 24.06 23.70 35 17033 43435 90567944
Product use in unapproved indication 24.03 23.70 17 17051 336219 90275160
Pleural effusion 23.87 23.70 60 17008 111931 90499448
Vulvovaginal dryness 23.71 23.70 12 17056 3419 90607960

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
Diarrhoea 45.63 41.09 40 475 460809 42160011

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Diarrhoea 1415.69 21.96 1126 12238 1138379 109437556
Malignant neoplasm progression 552.80 21.96 312 13052 174255 110401680
Neutropenia 243.26 21.96 261 13103 374359 110201576
Interstitial lung disease 233.85 21.96 167 13197 139167 110436768
Fatigue 159.24 21.96 409 12955 1215549 109360386
Nausea 157.06 21.96 411 12953 1235279 109340656
Metastases to liver 155.88 21.96 79 13285 35307 110540628
Metastases to bone 143.93 21.96 72 13292 31300 110544635
Pneumonitis 140.51 21.96 97 13267 76434 110499501
Therapy cessation 125.02 21.96 74 13290 44783 110531152
Blood creatinine increased 112.35 21.96 124 13240 182765 110393170
Hot flush 103.44 21.96 76 13288 65960 110509975
Disease progression 103.35 21.96 137 13227 243897 110332038
Vomiting 95.48 21.96 283 13081 910392 109665543
Decreased appetite 90.47 21.96 186 13178 475660 110100275
Metastases to lung 88.64 21.96 47 13317 23016 110552919
Anaemia 81.57 21.96 194 13170 546892 110029043
Myelosuppression 72.24 21.96 72 13292 94268 110481667
Tumour marker increased 64.71 21.96 24 13340 5036 110570899
Metastases to pleura 63.60 21.96 19 13345 2044 110573891
Dehydration 61.15 21.96 116 13248 279395 110296540
White blood cell count decreased 58.81 21.96 102 13262 229288 110346647
Death 54.79 21.96 197 13167 698672 109877263
Hepatic echinococciasis 52.88 21.96 9 13355 68 110575867
Transaminases increased 51.53 21.96 50 13314 63340 110512595
Progressive bulbar palsy 50.71 21.96 9 13355 89 110575846
Pseudocirrhosis 48.98 21.96 13 13351 910 110575025
Therapy interrupted 45.65 21.96 42 13322 49780 110526155
Hepatic cytolysis 43.95 21.96 43 13321 55010 110520925
Metastases to central nervous system 42.02 21.96 29 13335 22788 110553147
Constipation 40.93 21.96 115 13249 357671 110218264
Gastrointestinal toxicity 40.81 21.96 22 13342 11126 110564809
Therapy change 40.19 21.96 21 13343 9976 110565959
Selenium deficiency 39.19 21.96 7 13357 72 110575863
Hospice care 38.50 21.96 22 13342 12451 110563484
Carbohydrate antigen 15-3 increased 37.83 21.96 12 13352 1575 110574360
Thrombocytopenia 36.86 21.96 109 13255 348776 110227159
Neutrophil count decreased 36.63 21.96 58 13306 120883 110455052
Hepatic function abnormal 35.99 21.96 49 13315 89246 110486689
Aspartate aminotransferase increased 34.47 21.96 66 13298 159870 110416065
PIK3CA-activated mutation 33.44 21.96 9 13355 664 110575271
Motor neurone disease 32.79 21.96 9 13355 715 110575220
Joint swelling 32.36 21.96 7 13357 442838 110133097
Lung opacity 31.86 21.96 19 13345 11633 110564302
Pulmonary embolism 31.77 21.96 76 13288 214398 110361537
Alanine aminotransferase increased 31.51 21.96 69 13295 183704 110392231
Vulvovaginal dryness 31.39 21.96 12 13352 2735 110573200
Drug-induced liver injury 30.23 21.96 53 13311 120014 110455921
Osteonecrosis of jaw 30.19 21.96 33 13331 47984 110527951
Mucosal toxicity 28.41 21.96 8 13356 698 110575237
Metastases to breast 28.33 21.96 7 13357 368 110575567
Drug hypersensitivity 27.93 21.96 10 13354 454080 110121855
Condition aggravated 27.48 21.96 29 13335 734807 109841128
Taste disorder 26.52 21.96 36 13328 65351 110510584
Metastases to peritoneum 26.08 21.96 13 13351 5597 110570338
Hepatotoxicity 25.86 21.96 35 13329 63365 110512570
Sinusitis 25.45 21.96 3 13361 296685 110279250
Acute kidney injury 25.43 21.96 147 13217 635283 109940652
Gamma-glutamyltransferase increased 25.24 21.96 34 13330 61275 110514660
Cancer pain 23.77 21.96 13 13351 6759 110569176
Amyotrophic lateral sclerosis 23.41 21.96 9 13355 2082 110573853
Swelling 22.86 21.96 7 13357 351034 110224901
Pseudocellulitis 22.34 21.96 6 13358 439 110575496
Leukopenia 22.32 21.96 53 13311 148738 110427197

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EF03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Cyclin-dependent kinase (CDK) inhibitors
FDA MoA N0000175082 Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
CHEBI has role CHEBI:35610 antineoplastic agent

Related Drugs by ATC class:

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

Drug Use | Suggest Off label Use Form| |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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.14 Basic
pKa2 6.26 Basic
pKa3 5.0 Basic
pKa4 3.88 Basic
pKa5 2.67 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 2031 AS MONOTHERAPY FOR THE TREATMENT OF ADULT PATIENTS WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTIC BREAST CANCER WITH DISEASE PROGRESSION FOLLOWING ENDOCRINE THERAPY AND PRIOR CHEMOTHERAPY IN THE METASTATIC SETTING
100MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 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
100MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 2031 IN COMBINATION WITH ENDOCRINE THERAPY (TAMOXIFEN OR AN AROMATASE INHIBITOR) FOR THE ADJUVANT TREATMENT OF ADULT PATIENTS WITH HR-POSITIVE, HER2-NEGATIVE, NODE POSITIVE, EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
100MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 2031 IN COMBINATION WITH FULVESTRANT FOR THE TREATMENT OF ADULT PATIENTS WITH HR-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER WITH DISEASE PROGRESSION FOLLOWING ENDOCRINE THERAPY
150MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 2031 AS MONOTHERAPY FOR THE TREATMENT OF ADULT PATIENTS WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTIC BREAST CANCER WITH DISEASE PROGRESSION FOLLOWING ENDOCRINE THERAPY AND PRIOR CHEMOTHERAPY IN THE METASTATIC SETTING
150MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 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
150MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 2031 IN COMBINATION WITH ENDOCRINE THERAPY (TAMOXIFEN OR AN AROMATASE INHIBITOR) FOR THE ADJUVANT TREATMENT OF ADULT PATIENTS WITH HR-POSITIVE, HER2-NEGATIVE, NODE POSITIVE, EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
150MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 2031 IN COMBINATION WITH FULVESTRANT FOR THE TREATMENT OF ADULT PATIENTS WITH HR-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER WITH DISEASE PROGRESSION FOLLOWING ENDOCRINE THERAPY
200MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 2031 AS MONOTHERAPY FOR THE TREATMENT OF ADULT PATIENTS WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTIC BREAST CANCER WITH DISEASE PROGRESSION FOLLOWING ENDOCRINE THERAPY AND PRIOR CHEMOTHERAPY IN THE METASTATIC SETTING
200MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 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
200MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 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
200MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 2031 IN COMBINATION WITH ENDOCRINE THERAPY (TAMOXIFEN OR AN AROMATASE INHIBITOR) FOR THE ADJUVANT TREATMENT OF ADULT PATIENTS WITH HR-POSITIVE, HER2-NEGATIVE, NODE POSITIVE, EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
200MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 2031 IN COMBINATION WITH FULVESTRANT FOR THE TREATMENT OF ADULT PATIENTS WITH HR-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER WITH DISEASE PROGRESSION FOLLOWING ENDOCRINE THERAPY
50MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 2031 AS MONOTHERAPY FOR THE TREATMENT OF ADULT PATIENTS WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTIC BREAST CANCER WITH DISEASE PROGRESSION FOLLOWING ENDOCRINE THERAPY AND PRIOR CHEMOTHERAPY IN THE METASTATIC SETTING
50MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 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
50MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 2031 IN COMBINATION WITH ENDOCRINE THERAPY (TAMOXIFEN OR AN AROMATASE INHIBITOR) FOR THE ADJUVANT TREATMENT OF ADULT PATIENTS WITH HR-POSITIVE, HER2-NEGATIVE, NODE POSITIVE, EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
50MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Sept. 28, 2031 IN COMBINATION WITH FULVESTRANT FOR THE TREATMENT OF ADULT PATIENTS WITH HR-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER WITH DISEASE PROGRESSION FOLLOWING ENDOCRINE THERAPY

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Cyclin-dependent kinase 6 Kinase INHIBITOR Ki 8.62 SCIENTIFIC LITERATURE DRUG LABEL
Cyclin-dependent kinase 4 Kinase INHIBITOR Ki 9.22 SCIENTIFIC LITERATURE DRUG LABEL
Receptor-type tyrosine-protein kinase FLT3 Kinase IC50 6.39 CHEMBL
Cyclin-dependent kinase 1 Kinase IC50 5.82 CHEMBL
Cyclin-dependent kinase 2 Kinase Kd 4.98 CHEMBL
Serine/threonine-protein kinase pim-1 Kinase Kd 8.15 CHEMBL
Mitogen-activated protein kinase 8 Kinase Kd 5.42 CHEMBL
Protein kinase C beta type Kinase Kd 5.79 CHEMBL
Mitogen-activated protein kinase 10 Kinase IC50 6.41 CHEMBL
High affinity nerve growth factor receptor Kinase IC50 5.99 CHEMBL
Protein kinase C delta type Kinase Kd 6.10 CHEMBL
Protein kinase C alpha type Kinase Kd 6.28 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta Kinase Kd 7.72 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit gamma Kinase Kd 7.75 CHEMBL
AP2-associated protein kinase 1 Kinase Kd 6.99 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit beta Kinase IC50 8.46 CHEMBL
Cyclin-dependent-like kinase 5 Kinase IC50 7.09 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 5.61 CHEMBL
Serine/threonine-protein kinase 16 Kinase Kd 6.30 CHEMBL
Serine/threonine-protein kinase 17A Kinase IC50 6.18 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 4.25 CHEMBL
Serine/threonine-protein kinase pim-2 Kinase IC50 5.47 CHEMBL
Dual specificity protein kinase CLK1 Kinase Kd 8.15 CHEMBL
Dual specificity protein kinase CLK2 Kinase IC50 6.73 CHEMBL
Dual specificity protein kinase CLK3 Kinase IC50 5.13 CHEMBL
Cyclin-G-associated kinase Kinase Kd 5.66 CHEMBL
Glycogen synthase kinase-3 beta Kinase Kd 7.89 CHEMBL
Cyclin-dependent kinase 16 Kinase Kd 7.30 CHEMBL
Dual specificity protein kinase CLK4 Kinase Kd 7.89 CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2 Kinase Kd 5.58 CHEMBL
Cyclin-dependent kinase 9 Kinase IC50 7.24 CHEMBL
Glycogen synthase kinase-3 alpha Kinase Kd 7.89 CHEMBL
Cyclin-dependent kinase 7 Kinase IC50 6.52 CHEMBL
Casein kinase II subunit alpha Kinase IC50 6.93 CHEMBL
Casein kinase II subunit alpha' Kinase Kd 7.72 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1B Kinase IC50 8.46 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4 Kinase Kd 5.88 CHEMBL
Citron Rho-interacting kinase Kinase Kd 6.10 CHEMBL
Serine/threonine-protein kinase D2 Kinase Kd 5.68 CHEMBL
Serine/threonine-protein kinase D3 Kinase Kd 5.74 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1A Kinase Kd 6.69 CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 2 Kinase IC50 7.59 CHEMBL
Homeodomain-interacting protein kinase 2 Kinase IC50 7.51 CHEMBL
Serine/threonine-protein kinase ICK Kinase Kd 7.28 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 6.90 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.96 CHEMBL
Serine/threonine-protein kinase TAO3 Kinase Kd 5.76 CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 1 Kinase Kd 5.32 CHEMBL
Uncharacterized protein FLJ45252 Unclassified Kd 7.06 CHEMBL
Uncharacterized aarF domain-containing protein kinase 1 Kinase Kd 7.40 CHEMBL
Serine/threonine-protein kinase TAO1 Kinase Kd 6.97 CHEMBL
Serine/threonine-protein kinase B-raf Kinase IC50 5.20 CHEMBL

External reference:

IDSource
60UAB198HK UNII
4036932 VANDF
C3852841 UMLSCUI
CHEBI:233362 CHEBI
6ZV PDB_CHEM_ID
CHEMBL3301610 ChEMBL_ID
46220502 PUBCHEM_CID
DB12001 DRUGBANK_ID
D10688 KEGG_DRUG
10036 INN_ID
C000590451 MESH_SUPPLEMENTAL_RECORD_UI
7382 IUPHAR_LIGAND_ID
761851004 SNOMEDCT_US
763501007 SNOMEDCT_US
262389 MMSL
33135 MMSL
d08665 MMSL
017349 NDDF
1946825 RXNORM
60UAB198HK INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Verzenio HUMAN PRESCRIPTION DRUG LABEL 1 0002-4483 TABLET 50 mg ORAL NDA 32 sections
Verzenio HUMAN PRESCRIPTION DRUG LABEL 1 0002-4815 TABLET 100 mg ORAL NDA 32 sections
Verzenio HUMAN PRESCRIPTION DRUG LABEL 1 0002-5337 TABLET 150 mg ORAL NDA 32 sections
Verzenio HUMAN PRESCRIPTION DRUG LABEL 1 0002-6216 TABLET 200 mg ORAL NDA 32 sections