abemaciclib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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: OFP

  • 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

Approvals:

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

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 1196.98 26.22 917 8568 714449 62765088
Malignant neoplasm progression 485.70 26.22 239 9246 81882 63397655
Therapy cessation 462.45 26.22 173 9312 30284 63449253
Therapy interrupted 273.83 26.22 121 9364 32334 63447203
Disease progression 248.53 26.22 179 9306 122579 63356958
Interstitial lung disease 210.44 26.22 125 9360 61783 63417754
Neutropenia 177.40 26.22 171 9314 174834 63304703
Death 142.84 26.22 223 9262 374158 63105379
Therapy change 131.63 26.22 45 9440 6036 63473501
Pneumonitis 127.14 26.22 74 9411 35148 63444389
Metastases to liver 113.66 26.22 60 9425 23579 63455958
Metastases to bone 102.89 26.22 54 9431 20965 63458572
Dehydration 98.19 26.22 125 9360 173229 63306308
Decreased appetite 86.48 26.22 143 9342 250909 63228628
Vomiting 81.42 26.22 224 9261 559393 62920144
Nausea 78.72 26.22 292 9193 854179 62625358
White blood cell count decreased 76.65 26.22 99 9386 139005 63340532
Blood creatinine increased 72.58 26.22 77 9408 87767 63391770
Metastases to lung 68.85 26.22 35 9450 12715 63466822
Tumour marker increased 67.51 26.22 26 9459 4889 63474648
PIK3CA-activated mutation 62.68 26.22 17 9468 1042 63478495
Hepatic echinococciasis 52.64 26.22 9 9476 55 63479482
Hospice care 52.44 26.22 25 9460 7907 63471630
Myelosuppression 46.50 26.22 34 9451 23669 63455868
Carbohydrate antigen 15-3 increased 44.61 26.22 14 9471 1434 63478103
Metastases to spinal cord 40.01 26.22 8 9477 125 63479412
Hepatic function abnormal 36.92 26.22 36 9449 37106 63442431
Bone marrow infiltration 35.94 26.22 10 9475 674 63478863
Off label use 33.48 26.22 31 9454 674431 62805106
Fatigue 33.17 26.22 236 9249 887792 62591745
Tumour flare 31.48 26.22 8 9477 380 63479157
Joint swelling 30.46 26.22 6 9479 327660 63151877
Selenium deficiency 29.93 26.22 5 9480 26 63479511
Anaemia 29.01 26.22 103 9382 293327 63186210
Full blood count abnormal 28.31 26.22 29 9456 31688 63447849
Hospitalisation 27.24 26.22 47 9438 85034 63394503
Pulmonary embolism 26.87 26.22 56 9429 116628 63362909
Metastases to lymph nodes 26.43 26.22 16 9469 8142 63471395
Drug ineffective 26.28 26.22 254 9231 1044511 62435026

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Diarrhoea 776.53 25.51 601 5828 879888 78858071
Malignant neoplasm progression 268.16 25.51 155 6274 135835 79602124
Interstitial lung disease 171.78 25.51 109 6320 112491 79625468
Disease progression 135.94 25.51 115 6314 184247 79553712
Neutropenia 128.74 25.51 136 6293 287574 79450385
Therapy cessation 119.48 25.51 59 6370 37503 79700456
Metastases to liver 94.58 25.51 46 6383 28268 79709691
Metastases to bone 91.69 25.51 43 6386 24384 79713575
Nausea 74.75 25.51 206 6223 956990 78780969
Pneumonitis 73.48 25.51 51 6378 60809 79677150
Vomiting 67.11 25.51 158 6271 665670 79072289
Decreased appetite 64.70 25.51 106 6323 342312 79395647
Death 58.71 25.51 136 6293 566378 79171581
Hepatic echinococciasis 58.47 25.51 9 6420 53 79737906
Therapy interrupted 51.84 25.51 32 6397 31309 79706650
Tumour marker increased 49.65 25.51 17 6412 4255 79733704
Hospice care 47.65 25.51 21 6408 10303 79727656
Fatigue 47.41 25.51 173 6256 929554 78808405
Dehydration 47.03 25.51 77 6352 248110 79489849
Therapy change 43.95 25.51 18 6411 7381 79730578
Blood creatinine increased 43.67 25.51 58 6371 154999 79582960
Metastases to lung 39.11 25.51 22 6407 18141 79719818
Metastases to breast 32.96 25.51 7 6422 282 79737677
PIK3CA-activated mutation 32.88 25.51 8 6421 595 79737364
Selenium deficiency 31.86 25.51 5 6424 34 79737925
Myelosuppression 29.30 25.51 25 6404 40271 79697688
Mucosal toxicity 27.88 25.51 7 6422 593 79737366
Transaminases increased 27.64 25.51 27 6402 51716 79686243

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

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 Dec. 15, 2029 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 Dec. 15, 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
100MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Dec. 15, 2029 IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR THE TREATMENT OF POSTMENOPAUSAL WOMEN, AND MEN WITH 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 Dec. 15, 2029 IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR THE TREATMENT OF POSTMENOPAUSAL WOMEN 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 Dec. 15, 2029 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 Dec. 15, 2029 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 AND A KI-67 SCORE >=20%
100MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Dec. 15, 2029 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
100MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Dec. 15, 2029 IN COMBINATION WITH FULVESTRANT FOR THE TREATMENT OF WOMEN WITH HORMONE RECEPTOR (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 Dec. 15, 2029 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 Dec. 15, 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
150MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Dec. 15, 2029 IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR THE TREATMENT OF POSTMENOPAUSAL WOMEN, AND MEN WITH 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 Dec. 15, 2029 IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR THE TREATMENT OF POSTMENOPAUSAL WOMEN 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 Dec. 15, 2029 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 Dec. 15, 2029 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 AND A KI-67 SCORE >=20%
150MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Dec. 15, 2029 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 Dec. 15, 2029 IN COMBINATION WITH FULVESTRANT FOR THE TREATMENT OF WOMEN WITH HORMONE RECEPTOR (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 Dec. 15, 2029 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 Dec. 15, 2029 IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR THE TREATMENT OF POSTMENOPAUSAL WOMEN 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 Dec. 15, 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
200MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Dec. 15, 2029 IN COMBINATION WITH FULVESTRANT FOR THE TREATMENT OF WOMEN WITH HORMONE RECEPTOR (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 Dec. 15, 2029 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 Dec. 15, 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
50MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Dec. 15, 2029 IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR THE TREATMENT OF POSTMENOPAUSAL WOMEN, AND MEN WITH 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 Dec. 15, 2029 IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR THE TREATMENT OF POSTMENOPAUSAL WOMEN 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 Dec. 15, 2029 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 Dec. 15, 2029 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 AND A KI-67 SCORE >=20%
50MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL 7855211 Dec. 15, 2029 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 Dec. 15, 2029 IN COMBINATION WITH FULVESTRANT FOR THE TREATMENT OF WOMEN WITH HORMONE RECEPTOR (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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL Oct. 12, 2024 INDICATION FOR THE USE OF ABEMACICLIB IN COMBINATION WITH ENDOCRINE THERAPY (TAMOXIFEN OR AN AROMATASE INHIBITOR) FOR THE ADJUVANT TREATMENT OF ADULT PATIENTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE, NODE-POSITIVE, EARLY CANCER (EBC) AT HIGH RISK OF RECURRENCE AND A KI-67 SCORE>20% AS DETERMINED BY AN FDA APPROVED TEST
100MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL Oct. 12, 2024 NEW PATIENT POPULATION
150MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL Oct. 12, 2024 INDICATION FOR THE USE OF ABEMACICLIB IN COMBINATION WITH ENDOCRINE THERAPY (TAMOXIFEN OR AN AROMATASE INHIBITOR) FOR THE ADJUVANT TREATMENT OF ADULT PATIENTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE, NODE-POSITIVE, EARLY CANCER (EBC) AT HIGH RISK OF RECURRENCE AND A KI-67 SCORE>20% AS DETERMINED BY AN FDA APPROVED TEST
150MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL Oct. 12, 2024 NEW PATIENT POPULATION
200MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL Oct. 12, 2024 INDICATION FOR THE USE OF ABEMACICLIB IN COMBINATION WITH ENDOCRINE THERAPY (TAMOXIFEN OR AN AROMATASE INHIBITOR) FOR THE ADJUVANT TREATMENT OF ADULT PATIENTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE, NODE-POSITIVE, EARLY CANCER (EBC) AT HIGH RISK OF RECURRENCE AND A KI-67 SCORE>20% AS DETERMINED BY AN FDA APPROVED TEST
200MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL Oct. 12, 2024 NEW PATIENT POPULATION
50MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL Oct. 12, 2024 INDICATION FOR THE USE OF ABEMACICLIB IN COMBINATION WITH ENDOCRINE THERAPY (TAMOXIFEN OR AN AROMATASE INHIBITOR) FOR THE ADJUVANT TREATMENT OF ADULT PATIENTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE, NODE-POSITIVE, EARLY CANCER (EBC) AT HIGH RISK OF RECURRENCE AND A KI-67 SCORE>20% AS DETERMINED BY AN FDA APPROVED TEST
50MG VERZENIO ELI LILLY AND CO N208716 Sept. 28, 2017 RX TABLET ORAL Oct. 12, 2024 NEW PATIENT POPULATION

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
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
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
Serine/threonine-protein kinase 10 Kinase Kd 5.61 CHEMBL
Serine/threonine-protein kinase 16 Kinase Kd 6.30 CHEMBL
BMP-2-inducible protein kinase Kinase Kd 4.25 CHEMBL
Dual specificity protein kinase CLK1 Kinase Kd 8.15 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
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.96 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 Kd 7.72 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
Serine/threonine-protein kinase ICK Kinase Kd 7.28 CHEMBL
Interleukin-1 receptor-associated kinase 1 Kinase Kd 6.90 CHEMBL
Serine/threonine-protein kinase TAO1 Kinase Kd 6.97 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
Calcium/calmodulin-dependent protein kinase kinase 2 Kinase Kd 5.58 CHEMBL
Cyclin-dependent kinase 1 Kinase IC50 5.82 CHEMBL

External reference:

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Verzenio HUMAN PRESCRIPTION DRUG LABEL 1 0002-4483 TABLET 50 mg ORAL NDA 33 sections
Verzenio HUMAN PRESCRIPTION DRUG LABEL 1 0002-4483 TABLET 50 mg ORAL NDA 33 sections
Verzenio HUMAN PRESCRIPTION DRUG LABEL 1 0002-4815 TABLET 100 mg ORAL NDA 33 sections
Verzenio HUMAN PRESCRIPTION DRUG LABEL 1 0002-4815 TABLET 100 mg ORAL NDA 33 sections
Verzenio HUMAN PRESCRIPTION DRUG LABEL 1 0002-5337 TABLET 150 mg ORAL NDA 33 sections
Verzenio HUMAN PRESCRIPTION DRUG LABEL 1 0002-5337 TABLET 150 mg ORAL NDA 33 sections
Verzenio HUMAN PRESCRIPTION DRUG LABEL 1 0002-6216 TABLET 200 mg ORAL NDA 33 sections
Verzenio HUMAN PRESCRIPTION DRUG LABEL 1 0002-6216 TABLET 200 mg ORAL NDA 33 sections