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

Stem definition	Drug id	CAS RN
isocitrate dehydrogenase inhibitors	5251	1446502-11-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: enasidenib enasidenib mesylate AG-221 CC-90007 Free Base CC-90007 AG-221 mesylate	Enasidenib is a small molecule inhibitor of the isocitrate dehydrogenase 2 (IDH2) enzyme. Enasidenib targets the mutant IDH2 variants R140Q, R172S, and R172K at approximately 40-fold lower concentrations than the wild-type enzyme in vitro. Inhibition of the mutant IDH2 enzyme by enasidenib led to decreased 2-hydroxyglutarate (2-HG) levels and induced myeloid differentiation in vitro and in vivo in mouse xenograft models of IDH2 mutated AML. In blood samples from patients with AML with mutated IDH2, enasidenib decreased 2-HG levels, reduced blast counts and increased percentages of mature myeloid cells. Molecular weight: 473.38 Formula: C19H17F6N7O CLOGP: 3.76 LIPINSKI: 0 HAC: 8 HDO: 3 TPSA: 108.74 ALOGS: -4.11 ROTB: 8 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

enasidenib
enasidenib mesylate
AG-221
CC-90007 Free Base
CC-90007
AG-221 mesylate

Enasidenib is a small molecule inhibitor of the isocitrate dehydrogenase 2 (IDH2) enzyme. Enasidenib targets the mutant IDH2 variants R140Q, R172S, and R172K at approximately 40-fold lower concentrations than the wild-type enzyme in vitro. Inhibition of the mutant IDH2 enzyme by enasidenib led to decreased 2-hydroxyglutarate (2-HG) levels and induced myeloid differentiation in vitro and in vivo in mouse xenograft models of IDH2 mutated AML. In blood samples from patients with AML with mutated IDH2, enasidenib decreased 2-HG levels, reduced blast counts and increased percentages of mature myeloid cells.

Molecular weight: 473.38
Formula: C19H17F6N7O
CLOGP: 3.76
LIPINSKI: 0
HAC: 8
HDO: 3
TPSA: 108.74
ALOGS: -4.11
ROTB: 8

Status: ONP

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

Drug dosage:

None

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
Aug. 1, 2017	FDA	CELGENE CORP

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
Differentiation syndrome	351.07	37.27	53	1465	1050	63486454
Death	279.87	37.27	147	1371	374234	63113270
Platelet count decreased	46.84	37.27	31	1487	116091	63371413
Acute myeloid leukaemia recurrent	40.08	37.27	9	1509	1614	63485890

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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	357.66	39.02	233	1643	397816	34557239
Differentiation syndrome	313.80	39.02	56	1820	1382	34953673
Full blood count decreased	74.12	39.02	30	1846	18058	34936997
Fatigue	49.39	39.02	78	1798	370575	34584480
Platelet count decreased	47.46	39.02	44	1832	119673	34835382
Haemoglobin abnormal	45.17	39.02	14	1862	3866	34951189
Decreased appetite	43.78	39.02	49	1827	166343	34788712
Neutrophil count abnormal	40.61	39.02	11	1865	1891	34953164

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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
Differentiation syndrome	564.34	40.94	90	1935	2434	79739929
Death	507.52	40.94	255	1770	566259	79176104
Febrile neutropenia	72.32	40.94	54	1971	230945	79511418
Sepsis	67.06	40.94	55	1970	269373	79472990
Eastern Cooperative Oncology Group performance status worsened	64.32	40.94	14	2011	2051	79740312
Haemoglobin abnormal	56.12	40.94	16	2009	7038	79735325
Platelet count decreased	53.15	40.94	42	1983	194622	79547741

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01XX59	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:145410	IDP1 inhibitors
FDA EPC	N0000193615	Isocitrate Dehydrogenase 2 Inhibitor
FDA MoA	N0000193614	Isocitrate Dehydrogenase 2 Inhibitors

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

Disease	Relation	SNOMED_ID	DOID
Acute myeloid leukemia, disease	indication	91861009

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.77	Basic
pKa2	2.61	Basic
pKa3	0.4	Basic

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
EQ 100MG BASE	IDHIFA	BRISTOL MYERS SQUIBB	N209606	Aug. 1, 2017	RX	TABLET	ORAL	10610125	June 21, 2030	TREATMENT OF RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) WITH AN ISOCITRATE DEHYDROGENASE-2 (IDH2) MUTATION
EQ 100MG BASE	IDHIFA	BRISTOL MYERS SQUIBB	N209606	Aug. 1, 2017	RX	TABLET	ORAL	10294215	Jan. 7, 2033	TREATMENT OF RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) WITH AN ISOCITRATE DEHYDROGENASE-2 (IDH2) MUTATION
EQ 100MG BASE	IDHIFA	BRISTOL MYERS SQUIBB	N209606	Aug. 1, 2017	RX	TABLET	ORAL	9512107	Jan. 7, 2033	TREATMENT OF RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) WITH AN ISOCITRATE DEHYDROGENASE-2 (IDH2) MUTATION
EQ 100MG BASE	IDHIFA	BRISTOL MYERS SQUIBB	N209606	Aug. 1, 2017	RX	TABLET	ORAL	10093654	Aug. 1, 2034	TREATMENT OF RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) WITH AN ISOCITRATE DEHYDROGENASE-2 (IDH2) MUTATION
EQ 50MG BASE	IDHIFA	BRISTOL MYERS SQUIBB	N209606	Aug. 1, 2017	RX	TABLET	ORAL	10610125	June 21, 2030	TREATMENT OF RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) WITH AN ISOCITRATE DEHYDROGENASE-2 (IDH2) MUTATION
EQ 50MG BASE	IDHIFA	BRISTOL MYERS SQUIBB	N209606	Aug. 1, 2017	RX	TABLET	ORAL	10294215	Jan. 7, 2033	TREATMENT OF RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) WITH AN ISOCITRATE DEHYDROGENASE-2 (IDH2) MUTATION
EQ 50MG BASE	IDHIFA	BRISTOL MYERS SQUIBB	N209606	Aug. 1, 2017	RX	TABLET	ORAL	9512107	Jan. 7, 2033	TREATMENT OF RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) WITH AN ISOCITRATE DEHYDROGENASE-2 (IDH2) MUTATION
EQ 50MG BASE	IDHIFA	BRISTOL MYERS SQUIBB	N209606	Aug. 1, 2017	RX	TABLET	ORAL	10093654	Aug. 1, 2034	TREATMENT OF RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) WITH AN ISOCITRATE DEHYDROGENASE-2 (IDH2) MUTATION

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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
EQ 100MG BASE	IDHIFA	BRISTOL MYERS SQUIBB	N209606	Aug. 1, 2017	RX	TABLET	ORAL	Aug. 1, 2024	TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA WITH AN ISOCITRATE DEHYDROGENASE-2 (IDH2) MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 50MG BASE	IDHIFA	BRISTOL MYERS SQUIBB	N209606	Aug. 1, 2017	RX	TABLET	ORAL	Aug. 1, 2024	TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA WITH AN ISOCITRATE DEHYDROGENASE-2 (IDH2) MUTATION AS DETECTED BY AN FDA-APPROVED TEST

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Isocitrate dehydrogenase [NADP], mitochondrial	Enzyme	P48735	IDHP_HUMAN	INHIBITOR	IC50	7		SCIENTIFIC LITERATURE	DRUG LABEL
Isocitrate dehydrogenase [NADP] cytoplasmic	Enzyme	O75874	IDHC_HUMAN		IC50	5.30		CHEMBL

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External reference:

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ID	Source
69Q	PDB_CHEM_ID
017290	NDDF
017291	NDDF
10162	INN_ID
1650550-25-6	SECONDARY_CAS_RN
1940331	RXNORM
32972	MMSL
3T1SS4E7AG	UNII
4036873	VANDF
763038001	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Idhifa	HUMAN PRESCRIPTION DRUG LABEL	1	59572-705	TABLET, FILM COATED	50 mg	ORAL	NDA	29 sections
Idhifa	HUMAN PRESCRIPTION DRUG LABEL	1	59572-705	TABLET, FILM COATED	50 mg	ORAL	NDA	29 sections
Idhifa	HUMAN PRESCRIPTION DRUG LABEL	1	59572-710	TABLET, FILM COATED	100 mg	ORAL	NDA	29 sections
Idhifa	HUMAN PRESCRIPTION DRUG LABEL	1	59572-710	TABLET, FILM COATED	100 mg	ORAL	NDA	29 sections

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