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

Stem definition	Drug id	CAS RN
cyclin dependant kinase inhibitors	5259	1231929-97-7

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.30	g	O

ADMET properties:

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Property	Value	Reference
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

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Approvals:

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

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FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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

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FDA Adverse Event Reporting System (Male)

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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

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FDA Adverse Event Reporting System (Pediatric)

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Pharmacologic Action:

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Source	Code	Description
ATC	L01EF03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Cyclin-dependent kinase (CDK) inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000175082	Kinase Inhibitors

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Hormone receptor positive malignant neoplasm of breast	indication	417181009
Human epidermal growth factor 2 negative carcinoma of breast	indication	431396003

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🐶 Veterinary Drug Use

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🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.14	Basic
pKa2	6.26	Basic
pKa3	5.0	Basic
pKa4	3.88	Basic
pKa5	2.67	Basic

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Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Cyclin-dependent kinase 6	Kinase	Q00534	CDK6_HUMAN	INHIBITOR	Ki	8.62	SCIENTIFIC LITERATURE	DRUG LABEL
Cyclin-dependent kinase 4	Kinase	P11802	CDK4_HUMAN	INHIBITOR	Ki	9.22	SCIENTIFIC LITERATURE	DRUG LABEL
Cyclin-dependent kinase 2	Kinase	P24941	CDK2_HUMAN		Kd	4.98	CHEMBL
Serine/threonine-protein kinase pim-1	Kinase	P11309	PIM1_HUMAN		Kd	8.15	CHEMBL
Mitogen-activated protein kinase 8	Kinase	P45983	MK08_HUMAN		Kd	5.42	CHEMBL
Protein kinase C beta type	Kinase	P05771	KPCB_HUMAN		Kd	5.79	CHEMBL
Protein kinase C delta type	Kinase	Q05655	KPCD_HUMAN		Kd	6.10	CHEMBL
Protein kinase C alpha type	Kinase	P17252	KPCA_HUMAN		Kd	6.28	CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta	Kinase	Q13557	KCC2D_HUMAN		Kd	7.72	CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit gamma	Kinase	Q13555	KCC2G_HUMAN		Kd	7.75	CHEMBL

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External reference:

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ID	Source
6ZV	PDB_CHEM_ID
017349	NDDF
10036	INN_ID
1946825	RXNORM
262389	MMSL
33135	MMSL
4036932	VANDF
46220502	PUBCHEM_CID
60UAB198HK	UNII
7382	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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

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