All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

olutasidenib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
isocitrate dehydrogenase inhibitors	5693	1887014-12-1

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: olutasidenib rezlidhia FT-2102

Olutasidenib is a small-molecule inhibitor of mutated isocitrate dehydrogenase-1 (IDH1). In patients with AML, 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 olutasidenib and/or 2) inhibition of mutant IDH1 enzymatic activity at concentrations of olutasidenib sustainable at the recommended dosage according to validated methods. The most common of such mutations in patients with AML are R132H and R132C substitutions. In vitro, olutasidenib inhibited mutated IDH1 R132H, R132L, R132S, R132G, and R132C proteins; wild-type IDH1 or mutated IDH2 proteins were not inhibited. Olutasidenib inhibition of mutant IDH1 led to decreased 2-HG levels in vitro and in in vivo xenograft models. Molecular weight: 354.79 Formula: C18H15ClN4O2 CLOGP: 1.11 LIPINSKI: 0 HAC: 6 HDO: 2 TPSA: 85.23 ALOGS: -3.79 ROTB: 3 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK10,MAPK7,MET,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CD,PIK3CG,PRKDC,STK33,TEK,TTK	28
kinase-selectivity-class	AXL,CDK9,GRK2,MAPK7,PIK3CB,PIK3CD,TEK,UHMK1	8
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

Date	Agency	Company	Orphan
Dec. 1, 2022	FDA	RIGEL PHARMS INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01XM03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Isocitrate dehydrogenase (IDH) inhibitors
MeSH PA	D004791	Enzyme Inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agent

Related Drugs by ATC class:

L01XM Isocitrate dehydrogenase (IDH) inhibitors 3 drugs

enasidenibivosidenibvorasidenib

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

Disease	Relation	SNOMED_ID	DOID
Acute myeloid leukemia, disease	indication	91861009
Relapsing acute myeloid leukemia with a susceptible IDH1 mutation	indication
Refractory acute myeloid leukemia with a susceptible IDH1 mutation	indication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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
150MG	REZLIDHIA	RIGEL PHARMS	N215814	Dec. 1, 2022	RX	CAPSULE	ORAL	12275715	Sept. 18, 2035	A METHOD OF TREATING AN ADULT PATIENT WITH RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA HAVING A SUSCEPTIBLE IDH1 MUTATION
150MG	REZLIDHIA	RIGEL PHARMS	N215814	Dec. 1, 2022	RX	CAPSULE	ORAL	9834539	Sept. 18, 2035	A METHOD OF TREATING A CANCER WHERE THE CANCER IS ACUTE MYELOID LEUKEMIA (AML)
150MG	REZLIDHIA	RIGEL PHARMS	N215814	Dec. 1, 2022	RX	CAPSULE	ORAL	11013733	May 16, 2039	A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS ACUTE MYELOID LEUKEMIA (AML)
150MG	REZLIDHIA	RIGEL PHARMS	N215814	Dec. 1, 2022	RX	CAPSULE	ORAL	11013734	May 16, 2039	A METHOD OF TREATING ACUTE MYELOID LEUKEMIA (AML) IN PATIENTS WITH AN ISOCITRATE DEHYDROGENASE-1 (IDH1) MUTATION
150MG	REZLIDHIA	RIGEL PHARMS	N215814	Dec. 1, 2022	RX	CAPSULE	ORAL	11376246	May 16, 2039	A METHOD OF TREATING ACUTE MYELOID LEUKEMIA (AML) IN PATIENTS WITH AN ISOCITRATE DEHYDROGENASE-1 (IDH1) MUTATION
150MG	REZLIDHIA	RIGEL PHARMS	N215814	Dec. 1, 2022	RX	CAPSULE	ORAL	11497743	May 16, 2039	A METHOD OF TREATING ACUTE MYELOID LEUKEMIA (AML) IN PATIENTS WITH AN ISOCITRATE DEHYDROGENASE-1 (IDH1) MUTATION
150MG	REZLIDHIA	RIGEL PHARMS	N215814	Dec. 1, 2022	RX	CAPSULE	ORAL	11738018	July 17, 2039	A METHOD OF TREATING AN ADULT PATIENT WITH RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA HAVING A SUSCEPTIBLE IDH1 MUTATION

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
150MG	REZLIDHIA	RIGEL PHARMS	N215814	Dec. 1, 2022	RX	CAPSULE	ORAL	Dec. 1, 2027	NEW CHEMICAL ENTITY
150MG	REZLIDHIA	RIGEL PHARMS	N215814	Dec. 1, 2022	RX	CAPSULE	ORAL	Dec. 1, 2029	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

Bioactivity Summary:

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	7.67		SCIENTIFIC LITERATURE	DRUG LABEL
Isocitrate dehydrogenase [NADP], mitochondrial	Enzyme	P48735	IDHP_HUMAN		IC50	4.56		CHEMBL

External reference:

ID	Source
CHEBI:757082	CHEBI
CHEMBL4297610	ChEMBL_ID
C000710173	MESH_SUPPLEMENTAL_RECORD_UI
10319	IUPHAR_LIGAND_ID
DB16267	DRUGBANK_ID
4041886	VANDF
C5235389	UMLSCUI
PWV	PDB_CHEM_ID
11036	INN_ID
D12483	KEGG_DRUG
118955396	PUBCHEM_CID
364106	MMSL
41136	MMSL
d09955	MMSL
019241	NDDF
0T4IMT8S5Z	UNII
2623641	RXNORM
0T4IMT8S5Z	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
REZLIDHIA	HUMAN PRESCRIPTION DRUG LABEL	1	71332-005	CAPSULE	150 mg	ORAL	NDA	28 sections
REZLIDHIA	HUMAN PRESCRIPTION DRUG LABEL	1	71332-005	CAPSULE	150 mg	ORAL	NDA	28 sections