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

Stem definition	Drug id	CAS RN
isocitrate dehydrogenase inhibitors	5292	1448347-49-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ivosidenib tibsovo AG-120	Ivosidenib is a small molecule inhibitor that targets the mutant isocitrate dehydrogenase 1 (IDH1) enzyme. Susceptible IDH1 mutations are defined as those leading to increased levels of 2-hydroxyglutarate(2-HG) in the leukemia cells and where efficacy is predicted by 1) clinically meaningful remissions with the recommended dose of ivosidenib and/or 2) inhibition of mutant IDH1 enzymatic activity at concentrations of ivosidenib sustainable at the recommended dosage according to validated methods. The most common of such mutations are R132H and R132C substitutions. Molecular weight: 582.97 Formula: C28H22ClF3N6O3 CLOGP: 2.11 LIPINSKI: 2 HAC: 9 HDO: 1 TPSA: 119.29 ALOGS: -4.45 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ivosidenib
tibsovo
AG-120

Ivosidenib is a small molecule inhibitor that targets the mutant isocitrate dehydrogenase 1 (IDH1) enzyme. Susceptible IDH1 mutations are defined as those leading to increased levels of 2-hydroxyglutarate(2-HG) in the leukemia cells and where efficacy is predicted by 1) clinically meaningful remissions with the recommended dose of ivosidenib and/or 2) inhibition of mutant IDH1 enzymatic activity at concentrations of ivosidenib sustainable at the recommended dosage according to validated methods. The most common of such mutations are R132H and R132C substitutions.

Molecular weight: 582.97
Formula: C28H22ClF3N6O3
CLOGP: 2.11
LIPINSKI: 2
HAC: 9
HDO: 1
TPSA: 119.29
ALOGS: -4.45
ROTB: 7

Status: OFP

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)	0.04 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
July 20, 2018	FDA	AGIOS PHARMS INC
May 4, 2023	EMA	LES LABORATOIRES SERVIER

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	66.43	64.97	8	38	1095	63487881

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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
Differentiation syndrome	105.49	61.54	14	60	1424	34955433

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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	160.99	77.18	21	104	2503	79741760

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01XX62	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	N0000193987	Isocitrate Dehydrogenase 1 Inhibitor
FDA MoA	N0000185506	Cytochrome P450 3A4 Inducers
FDA MoA	N0000185507	Cytochrome P450 2C9 Inducers
FDA MoA	N0000193988	Isocitrate Dehydrogenase 1 Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme 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
Acute myeloid leukemia, disease	indication	91861009
Biliary tract cancer	indication	312104005

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.43	acidic
pKa2	0.21	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
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	10610125	June 21, 2030	A METHOD FOR TREATING NEWLY DIAGNOSED AML WITH IVOSIDENIB AND AZACITIDINE WHEREIN THE AML HAS AN IDH1 MUTATION CAPABLE OF CONVERTING ALPHA-KETOGLUTARATE TO 2-HYDROXYGLUTARATE (2HG)
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	10610125	June 21, 2030	A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS NEWLY DIAGNOSED ACUTE MYELOID LEUKEMIA (AML) AND WHERE THE MUTANT IDH1 HAS THE ABILITY TO CONVERT ALPHA-KETOGLUTARATE INTO 2-HYDROXYGLUTARATE (2-HG)
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	10610125	June 21, 2030	A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) AND WHERE THE MUTANT IDH1 HAS THE ABILITY TO CONVERT ALPHA-KETOGLUTARATE INTO 2-HYDROXYGLUTARATE (2-HG)
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	10717764	Jan. 18, 2033	A METHOD OF TREATING PREVIOUSLY TREATED, LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA CHARACTERIZED BY AN IDH1 MUTATION
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	9850277	Jan. 18, 2033	A METHOD FOR TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WITH IVOSIDENIB IN COMBINATION WITH AZACITIDINE WHEREIN THE CANCER IS NEWLY DIAGNOSED AML
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	9850277	Jan. 18, 2033	A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHEREIN THE CANCER IS PREVIOUSLY TREATED, LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	9850277	Jan. 18, 2033	A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS ACUTE MYELOGENOUS LEUKEMIA (AML)
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	9850277	Jan. 18, 2033	A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS NEWLY DIAGNOSED ACUTE MYELOID LEUKEMIA (AML)
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	9850277	Jan. 18, 2033	A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML)
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	9474779	Aug. 19, 2033	A METHOD FOR TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WITH IVOSIDENIB IN COMBINATION WITH AZACITIDINE WHEREIN THE CANCER IS NEWLY DIAGNOSED AML

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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
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	July 20, 2023	NEW CHEMICAL ENTITY
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	Aug. 25, 2024	FOR THE TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY TREATED, LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH AN IDH1 MUTATION AS DETECTED BY AN FDA-APPROVED TEST
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	May 25, 2025	IN COMBINATION WITH AZACITIDINE OR AS MONOTHERAPY FOR THE TREATMENT OFNEWLY DIAGNOSED ACUTE MYELOID LEUKEMIA (AML) WITH A SUSCEPTIBLE ISOCITRATE DEHYDROGENASE-1 (IDH1) MUTATION AS DETECTED BY AN FDA-APPROVED TEST IN ADULTS 75 YEARS OR OLDER, OR WHO HAVE COMORBIDITIES THAT PRECLUDE USE OF INTENSIVE INDUCTION CHEMOTHERAPY
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	July 20, 2025	INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) WITH A SUSCEPTIBLE ISOCITRATE DEHYDROGENASE-1 (IDH1) MUTATION AS DETECTED BY AN FDA-APPROVED TEST
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	May 2, 2026	TX OF NEWLY-DIAGNOSED ACUTE MYELOID LEUKEMIA WITH A SUSCEPTIBLE ISOCITRATE DEHYDROGENASE-1 MUTATION AS DETECTED BY AN FDA-APPROVED TEST IN ADULT PTS WHO ARE >=75 YRS OLD OR WHO HAVE COMORBIDITIES THAT PRECLUDE USE OF INTENSIVE INDUCTION CHEMOTHERAPY
250MG	TIBSOVO	SERVIER	N211192	July 20, 2018	RX	TABLET	ORAL	Aug. 25, 2028	TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY TREATED, LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH AN ISOCITRATE DEHYDROGENASE-1 (IDH1) 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] cytoplasmic	Enzyme	O75874	IDHC_HUMAN	INHIBITOR	IC50	7.15		SCIENTIFIC LITERATURE	DRUG LABEL

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External reference:

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ID	Source
017647	NDDF
10225	INN_ID
2049873	RXNORM
285271	MMSL
34590	MMSL
4037715	VANDF
71657455	PUBCHEM_CID
773137008	SNOMEDCT_US
773232006	SNOMEDCT_US
9217	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Tibsovo	HUMAN PRESCRIPTION DRUG LABEL	1	71334-100	TABLET, FILM COATED	250 mg	ORAL	NDA	28 sections
Tibsovo	HUMAN PRESCRIPTION DRUG LABEL	1	71334-100	TABLET, FILM COATED	250 mg	ORAL	NDA	28 sections
TIBSOVO	HUMAN PRESCRIPTION DRUG LABEL	1	72694-617	TABLET, FILM COATED	250 mg	ORAL	NDA	31 sections
TIBSOVO	HUMAN PRESCRIPTION DRUG LABEL	1	72694-617	TABLET, FILM COATED	250 mg	ORAL	NDA	31 sections

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