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:

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

Approvals:

Date	Agency	Company
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 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
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 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
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:

Source	Code	Description
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|

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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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

Orange Book patent data (new drug applications)

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
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 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

Bioactivity Summary:

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
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN		Kd	6.99	CHEMBL
Serine/threonine-protein kinase 10	Kinase	O94804	STK10_HUMAN		Kd	5.61	CHEMBL
Serine/threonine-protein kinase 16	Kinase	O75716	STK16_HUMAN		Kd	6.30	CHEMBL
BMP-2-inducible protein kinase	Kinase	Q9NSY1	BMP2K_HUMAN		Kd	4.25	CHEMBL
Dual specificity protein kinase CLK1	Kinase	P49759	CLK1_HUMAN		Kd	8.15	CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	5.66	CHEMBL
Glycogen synthase kinase-3 beta	Kinase	P49841	GSK3B_HUMAN		Kd	7.89	CHEMBL
Cyclin-dependent kinase 16	Kinase	Q00536	CDK16_HUMAN		Kd	7.30	CHEMBL
Dual specificity protein kinase CLK4	Kinase	Q9HAZ1	CLK4_HUMAN		Kd	7.89	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.96	CHEMBL
Cyclin-dependent kinase 9	Kinase	P50750	CDK9_HUMAN		IC50	7.24	CHEMBL
Glycogen synthase kinase-3 alpha	Kinase	P49840	GSK3A_HUMAN		Kd	7.89	CHEMBL
Cyclin-dependent kinase 7	Kinase	P50613	CDK7_HUMAN		IC50	6.52	CHEMBL
Casein kinase II subunit alpha'	Kinase	P19784	CSK22_HUMAN		Kd	7.72	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4	Kinase	O95819	M4K4_HUMAN		Kd	5.88	CHEMBL
Citron Rho-interacting kinase	Kinase	O14578	CTRO_HUMAN		Kd	6.10	CHEMBL
Serine/threonine-protein kinase D2	Kinase	Q9BZL6	KPCD2_HUMAN		Kd	5.68	CHEMBL
Serine/threonine-protein kinase D3	Kinase	O94806	KPCD3_HUMAN		Kd	5.74	CHEMBL
Dual specificity tyrosine-phosphorylation-regulated kinase 1A	Kinase	Q13627	DYR1A_HUMAN		Kd	6.69	CHEMBL
Serine/threonine-protein kinase ICK	Kinase	Q9UPZ9	ICK_HUMAN		Kd	7.28	CHEMBL
Interleukin-1 receptor-associated kinase 1	Kinase	P51617	IRAK1_HUMAN		Kd	6.90	CHEMBL
Serine/threonine-protein kinase TAO1	Kinase	Q7L7X3	TAOK1_HUMAN		Kd	6.97	CHEMBL
Serine/threonine-protein kinase TAO3	Kinase	Q9H2K8	TAOK3_HUMAN		Kd	5.76	CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 1	Kinase	Q9BQI3	E2AK1_HUMAN		Kd	5.32	CHEMBL
Uncharacterized protein FLJ45252	Unclassified	Q6ZSR9	YJ005_HUMAN		Kd	7.06	CHEMBL
Uncharacterized aarF domain-containing protein kinase 1	Kinase	Q86TW2	ADCK1_HUMAN		Kd	7.40	CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2	Kinase	Q96RR4	KKCC2_HUMAN		Kd	5.58	CHEMBL
Cyclin-dependent kinase 1	Kinase	P06493	CDK1_HUMAN		IC50	5.82	CHEMBL

External reference:

ID	Source
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:

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