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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5347	936091-26-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: fedratinib fedratinib hydrochloride SAR302503 SAR-302503 TG101348 TG-101348 FEDR inrebic	Fedratinib is an oral kinase inhibitor with activity against wild type and mutationally activated Janus Associated Kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3). Fedratinib is a JAK2-selective inhibitor with higher inhibitory activity for JAK2 over family members JAK1, JAK3 and TYK2. Abnormal activation of JAK2 is associated with myeloproliferative neoplasms (MPNs), including myelofibrosis and polycythemia vera. Molecular weight: 524.68 Formula: C27H36N6O3S CLOGP: 6.25 LIPINSKI: 2 HAC: 9 HDO: 3 TPSA: 108.48 ALOGS: -4.74 ROTB: 10 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

fedratinib
fedratinib hydrochloride
SAR302503
SAR-302503
TG101348
TG-101348
FEDR
inrebic

Fedratinib is an oral kinase inhibitor with activity against wild type and mutationally activated Janus Associated Kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3). Fedratinib is a JAK2-selective inhibitor with higher inhibitory activity for JAK2 over family members JAK1, JAK3 and TYK2. Abnormal activation of JAK2 is associated with myeloproliferative neoplasms (MPNs), including myelofibrosis and polycythemia vera.

Molecular weight: 524.68
Formula: C27H36N6O3S
CLOGP: 6.25
LIPINSKI: 2
HAC: 9
HDO: 3
TPSA: 108.48
ALOGS: -4.74
ROTB: 10

Status: ONP

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

Drug dosage:

Dose	Unit	Route
0.40	g	O

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Aug. 16, 2019	FDA	IMPACT
Feb. 8, 2021	EMA	CELGENE EUROPE BV

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
Vitamin B1 decreased	103.24	41.87	13	503	199	63488307
Vitamin B1 deficiency	63.88	41.87	9	507	331	63488175
Diarrhoea	56.59	41.87	46	470	715320	62773186

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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
Vitamin B1 decreased	130.82	43.87	18	469	320	34956124
Vitamin B1 deficiency	122.51	43.87	17	470	322	34956122
Death	60.83	43.87	47	440	398002	34558442

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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
Vitamin B1 decreased	248.43	39.24	31	519	532	79743306
Vitamin B1 deficiency	172.34	39.24	23	527	675	79743163
Death	88.69	39.24	52	498	566462	79177376

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01EJ02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Janus-associated kinase (JAK) 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
Myelofibrosis	indication	52967002	DOID:4971
Primary myelofibrosis	indication	307651005
Post-polycythaemia vera myelofibrosis	indication	871540009
Post-essential thrombocythaemia myelofibrosis	indication	871541008

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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	9.42	acidic
pKa2	8.9	Basic
pKa3	5.69	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	INREBIC	IMPACT	N212327	Aug. 16, 2019	RX	CAPSULE	ORAL	8138199	June 30, 2028	TREATMENT OF ADULT PATIENTS WITH INTERMEDIATE-2 OR HIGH-RISK PRIMARY OR SECONDARY MYELOFIBROSIS
EQ 100MG BASE	INREBIC	IMPACT	N212327	Aug. 16, 2019	RX	CAPSULE	ORAL	10391094	June 4, 2032	TREATMENT OF ADULT PATIENTS WITH INTERMEDIATE-2 OR HIGH-RISK PRIMARY OR SECONDARY MYELOFIBROSIS
EQ 100MG BASE	INREBIC	IMPACT	N212327	Aug. 16, 2019	RX	CAPSULE	ORAL	11400092	Sept. 24, 2039	TREATING ADULT PATIENTS WITH INTERMEDIATE-2 OR HIGH-RISK PRIMARY OR SECONDARY MYELOFIBROSIS, MONITORING THIAMINE LEVELS AND ADMINISTERING THIAMINE OR A THIAMINE EQUIVALENT

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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	INREBIC	IMPACT	N212327	Aug. 16, 2019	RX	CAPSULE	ORAL	Aug. 16, 2024	NEW CHEMICAL ENTITY
EQ 100MG BASE	INREBIC	IMPACT	N212327	Aug. 16, 2019	RX	CAPSULE	ORAL	Aug. 16, 2026	INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH INTERMEDIATE-2 OR HIGH-RISK PRIMARY OR SECONDARY (POST-POLYCYTHEMIA VERA OR POST-ESSENTIAL THROMBOCYTHEMIA) MYELOFIBROSIS (MF)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN	INHIBITOR	IC50	7.82	SCIENTIFIC LITERATURE	DRUG LABEL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN	INHIBITOR	IC50	8.52	SCIENTIFIC LITERATURE	DRUG LABEL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		Kd	7.40	CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN		Kd	7.34	CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		Kd	6.24	CHEMBL
Breakpoint cluster region protein	Kinase	P11274	BCR_HUMAN		Kd	5.76	CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN		Kd	7.12	CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	7.14	CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN		Kd	6.92	CHEMBL
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		Kd	7.42	CHEMBL

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External reference:

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ID	Source
2TA	PDB_CHEM_ID
018090	NDDF
1374744-69-0	SECONDARY_CAS_RN
16722836	PUBCHEM_CID
2197490	RXNORM
321679	MMSL
4038661	VANDF
5716	IUPHAR_LIGAND_ID
6L1XP550I6	UNII
789359000	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Inrebic	HUMAN PRESCRIPTION DRUG LABEL	1	59572-720	CAPSULE	100 mg	ORAL	NDA	31 sections
Inrebic	HUMAN PRESCRIPTION DRUG LABEL	1	59572-720	CAPSULE	100 mg	ORAL	NDA	31 sections
Inrebic	HUMAN PRESCRIPTION DRUG LABEL	1	59572-720	CAPSULE	100 mg	ORAL	NDA	31 sections

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