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

Stem definition	Drug id	CAS RN
B-cell lymphoma 2 (Bcl-2) inhibitors, antineoplastics	5133	1257044-40-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: venclyxto venetoclax ABT-199 venclexta GDC-0199	Venetoclax is a selective and orally bioavailable small-molecule inhibitor of BCL-2, an anti-apoptotic protein. Overexpression of BCL-2 has been demonstrated in CLL cells where it mediates tumor cell survival and has been associated with resistance to chemotherapeutics. Venetoclax helps restore the process of apoptosis by binding directly to the BCL-2 protein, displacing pro-apoptotic proteins like BIM, triggering mitochondrial outer membrane permeabilization and the activation of caspases. In nonclinical studies, venetoclax has demonstrated cytotoxic activity in tumor cells that overexpress BCL-2. Molecular weight: 868.45 Formula: C45H50ClN7O7S CLOGP: 10.21 LIPINSKI: 3 HAC: 14 HDO: 3 TPSA: 172.03 ALOGS: -5.97 ROTB: 12 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

venclyxto
venetoclax
ABT-199
venclexta
GDC-0199

Venetoclax is a selective and orally bioavailable small-molecule inhibitor of BCL-2, an anti-apoptotic protein. Overexpression of BCL-2 has been demonstrated in CLL cells where it mediates tumor cell survival and has been associated with resistance to chemotherapeutics. Venetoclax helps restore the process of apoptosis by binding directly to the BCL-2 protein, displacing pro-apoptotic proteins like BIM, triggering mitochondrial outer membrane permeabilization and the activation of caspases. In nonclinical studies, venetoclax has demonstrated cytotoxic activity in tumor cells that overexpress BCL-2.

Molecular weight: 868.45
Formula: C45H50ClN7O7S
CLOGP: 10.21
LIPINSKI: 3
HAC: 14
HDO: 3
TPSA: 172.03
ALOGS: -5.97
ROTB: 12

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company
April 11, 2016	FDA	ABBVIE INC
Dec. 5, 2016	EMA	AbbVie Ltd
Sept. 20, 2019	PMDA	AbbVie GK

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
Death	1596.39	21.42	1113	17615	373268	63097026
Febrile neutropenia	1050.03	21.42	565	18163	117884	63352410
Off label use	975.93	21.42	1085	17643	673377	62796917
Neutropenia	664.98	21.42	488	18240	174517	63295777
Tumour lysis syndrome	591.14	21.42	182	18546	8808	63461486
Hospice care	347.33	21.42	118	18610	7814	63462480
Myelosuppression	317.42	21.42	150	18578	23553	63446741
Cytopenia	307.10	21.42	119	18609	11482	63458812
Acute myeloid leukaemia recurrent	299.63	21.42	74	18654	1549	63468745
Thrombocytopenia	295.44	21.42	288	18440	150869	63319425

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FDA Adverse Event Reporting System (Male)

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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
Death	1745.55	17.51	1974	30447	396075	34528435
Off label use	1329.15	17.51	1769	30652	417755	34506755
Febrile neutropenia	1116.09	17.51	958	31463	135891	34788619
Tumour lysis syndrome	893.97	17.51	395	32026	16664	34907846
Neutropenia	816.56	17.51	857	31564	155921	34768589
Hospice care	494.28	17.51	200	32221	6740	34917770
COVID-19	425.48	17.51	437	31984	77113	34847397
Intentional product use issue	344.13	17.51	346	32075	59470	34865040
Cytopenia	330.93	17.51	183	32238	12540	34911970
Myelosuppression	306.30	17.51	202	32219	19063	34905447

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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
Febrile neutropenia	2260.94	18.05	1438	40410	229561	79472979
Death	1827.24	18.05	1833	40015	564681	79137859
Neutropenia	1337.69	18.05	1145	40703	286565	79415975
Tumour lysis syndrome	1327.85	18.05	492	41356	23447	79679093
Off label use	855.87	18.05	1620	40228	905595	78796945
Myelosuppression	623.92	18.05	339	41509	39957	79662583
Thrombocytopenia	581.76	18.05	705	41143	264554	79437986
Cytopenia	517.90	18.05	240	41608	20143	79682397
Neutrophil count decreased	513.54	18.05	412	41436	93547	79608993
COVID-19	495.16	18.05	506	41342	157168	79545372

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01XX52	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:68495	Type I cell-death inducers
CHEBI has role	CHEBI:133022	B-cell lymphoma 2 inhibitors
FDA EPC	N0000192515	BCL-2 Inhibitor
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA PE	N0000009176	Increased Cellular Death
MeSH PA	D000970	Antineoplastic Agents

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

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Disease	Relation	SNOMED_ID
Acute myeloid leukemia, disease	indication	91861009
Chronic lymphoid leukemia, disease	indication	92814006
Malignant lymphoma - small lymphocytic	indication	302841002

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🐶 Veterinary Drug Use

None

🐶 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	2.0	acidic
pKa2	13.01	acidic
pKa3	7.73	Basic
pKa4	4.24	Basic
pKa5	3.47	Basic
pKa6	0.56	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	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	9174982	May 26, 2030	TREATMENT IN COMBINATION WITH AZACITIDINE OR DECITABINE OR LOW-DOSE CYTARABINE OF NEWLY-DIAGNOSED ACUTE MYELOID LEUKEMIA (AML) IN ADULTS WHO ARE AGE 75 YEARS OR OLDER, OR WHO HAVE COMORBIDITIES THAT PRECLUDE USE OF INTENSIVE INDUCTION CHEMOTHERAPY
100MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	9174982	May 26, 2030	TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL)
100MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	9174982	May 26, 2030	TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL), WITH OR WITHOUT 17P DELETION, WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
100MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	9174982	May 26, 2030	TREATMENT OF PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL), WITH OR WITHOUT 17P DELETION, WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
100MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	10993942	Sept. 6, 2033	TREATMENT OF CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL) BY ORALLY ADMINISTERING VENETOCLAX TO AN ADULT ACCORDING TO A DOSE RAMP-UP THAT INCLUDES A DOSE OF 50 MG PER DAY FOR 1 WEEK FOLLOWED BY 100 MG PER DAY FOR 1 WEEK
100MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	11110087	Sept. 6, 2033	TREATMENT OF ACUTE MYELOID LEUKEMIA (AML) BY ORALLY ADMINISTERING VENETOCLAX WITH AZACITIDINE OR DECITABINE OR LOW-DOSE CYTARABINE IN ADULTS 75 YEARS OR OLDER OR HAVING CERTAIN COMORBIDITIES ACCORDING TO A DOSE RAMP-UP INCLUDING A 100 MG PER DAY DOSE
100MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	11110087	Sept. 6, 2033	TREATMENT OF CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL) BY ORALLY ADMINISTERING VENETOCLAX TO AN ADULT ACCORDING TO A DOSE RAMP-UP INCLUDING A 100 MG PER DAY DOSE
100MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	11413282	Sept. 6, 2033	TREATMENT OF ADULTS WITH RELAPSED, REFRACTORY OR PREVIOUSLY UNTREATED CHRONIC LYMPHOCYTIC LEUKEMIA INCLUDING A DOSE RAMP-UP AND IN COMBINATION WITH OBINUTUZUMAB IN MULTIPLE 28-DAY DOSING CYCLES FOLLOWED BY ADMINISTRATION IN ABSENCE OF OBINUTUZUMAB
100MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	11590128	Sept. 6, 2033	TREATMENT OF AML BY ORALLY ADMINISTERING VENETOCLAX WITH AZACITIDINE OR DECITABINE OR LOW-DOSE CYTARABINE TO ADULTS 75 YEARS OR OLDER OR HAVING CERTAIN COMORBIDITIES PER A DOSE RAMP-UP INCLUDING AN INITIAL 100 MG OR A FINAL 400 MG PER DAY DOSE
100MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	9539251	Sept. 6, 2033	TREATMENT OF ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LEUKEMIA (SLL) IN COMBINATION WITH A GA101 ANTIBODY SUCH AS OBINUTUZUMAB FOR ONE OR MORE DOSING PERIODS, WHEREIN THE CLL OR SLL IS A CD20-EXPRESSING 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	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	April 11, 2023	TREATMENT OF PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) WITH 17P DELETION, AS DETECTED BY AN FDA APPROVED TEST, WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
100MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	Oct. 16, 2023	REVISIONS TO THE LABELING TO INCLUDE RESULTS FROM CLINICAL STUDY M15-656 (VIALE-A) AND M16-043 (VIALE-C) TO SUPPORT PMR 3545-1 AND PMR 3545-2
100MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	June 8, 2025	INDICATED FOR THE TREATMENT OF PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL), WITH OR WITHOUT 17P DELETION, WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
100MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	Nov. 21, 2025	INDICATED IN COMBO WITH AZACITIDINE, OR DECITABINE, OR LOW-DOSE CYTARABINE FOR THE TX OF NEWLY-DIAGNOSED ACUTE MYELOID LEUKEMIA IN ADULTS WHO ARE AGE 75 YEARS OR OLDER, OR WHO HAVE COMORBIDITIES THAT PRECLUDE USE OF INTENSIVE INDUCTION CHEMOTHERAPY
100MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	May 15, 2026	TREATMENT OF PREVIOUSLY UNTREATED ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL)
10MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	April 11, 2023	TREATMENT OF PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) WITH 17P DELETION, AS DETECTED BY AN FDA APPROVED TEST, WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
10MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	Oct. 16, 2023	REVISIONS TO THE LABELING TO INCLUDE RESULTS FROM CLINICAL STUDY M15-656 (VIALE-A) AND M16-043 (VIALE-C) TO SUPPORT PMR 3545-1 AND PMR 3545-2
10MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	June 8, 2025	INDICATED FOR THE TREATMENT OF PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL), WITH OR WITHOUT 17P DELETION, WHO HAVE RECEIVED AT LEAST ONE PRIOR THERAPY
10MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	Nov. 21, 2025	INDICATED IN COMBO WITH AZACITIDINE, OR DECITABINE, OR LOW-DOSE CYTARABINE FOR THE TX OF NEWLY-DIAGNOSED ACUTE MYELOID LEUKEMIA IN ADULTS WHO ARE AGE 75 YEARS OR OLDER, OR WHO HAVE COMORBIDITIES THAT PRECLUDE USE OF INTENSIVE INDUCTION CHEMOTHERAPY
10MG	VENCLEXTA	ABBVIE	N208573	April 11, 2016	RX	TABLET	ORAL	May 15, 2026	TREATMENT OF PREVIOUSLY UNTREATED ADULT PATIENTS WITH CHRONIC LYMPHOCYTIC LEUKEMIA (CLL) OR SMALL LYMPHOCYTIC LYMPHOMA (SLL)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Apoptosis regulator Bcl-2	Cytosolic other	P10415	BCL2_HUMAN	INHIBITOR	Ki	11	SCIENTIFIC LITERATURE	DRUG LABEL
Aspartyl/asparaginyl beta-hydroxylase	Enzyme	Q12797	ASPH_HUMAN		IC50	5.89	CHEMBL
Bcl2-associated agonist of cell death	Unclassified	Q92934	BAD_HUMAN		Ki	4.80	CHEMBL
Bcl-2-like protein 1	Cytosolic other	Q07817	B2CL1_HUMAN	INHIBITOR	Ki	7.32	SCIENTIFIC LITERATURE
Apoptosis regulator Bcl-W	Cytosolic other	Q92843	B2CL2_HUMAN	INHIBITOR	Ki	6.61	SCIENTIFIC LITERATURE

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External reference:

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ID	Source
016803	NDDF
1747556	RXNORM
240227	MMSL
31601	MMSL
4035629	VANDF
49846579	PUBCHEM_CID
720491001	SNOMEDCT_US
763511000	SNOMEDCT_US
8318	IUPHAR_LIGAND_ID
9925	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Venclexta	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0561	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Venclexta	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0561	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Venclexta	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0561	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Venclexta	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0566	TABLET, FILM COATED	50 mg	ORAL	NDA	32 sections
Venclexta	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0566	TABLET, FILM COATED	50 mg	ORAL	NDA	32 sections
Venclexta	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0566	TABLET, FILM COATED	50 mg	ORAL	NDA	32 sections
Venclexta	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0576	TABLET, FILM COATED	100 mg	ORAL	NDA	32 sections
Venclexta	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0576	TABLET, FILM COATED	100 mg	ORAL	NDA	32 sections
Venclexta	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0576	TABLET, FILM COATED	100 mg	ORAL	NDA	32 sections

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