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

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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5390	1513857-77-6

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: pemigatinib pemazyre INCB054828

Pemigatinib inhibited FGFR1-3 phosphorylation and signaling and decreased cell viability in cancer cell lines with activating FGFR amplifications and fusions that resulted in constitutive activation of FGFR signaling. Molecular weight: 487.51 Formula: C24H27F2N5O4 CLOGP: 2.93 LIPINSKI: 0 HAC: 9 HDO: 1 TPSA: 83.16 ALOGS: -3.53 ROTB: 6 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

Dose	Unit	Route
9	mg	O

ADMET properties:

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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ABL1,ABL2,ACVR2B,ALK,AURKA,AXL,BLK,BMX,BRAF,CAMK2D,CDK19,CDK9,CSF1R,CSK,DDR1,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB4,ERBB2,FGFR1,FLT3,FYN,GAK,GRK2,GSK3B,INSR,ITK,KDR,KIT,LCK,LYN,MAP2K1,MAP3K11,MAP3K21,MAP4K1,MAP4K3,MAP4K5,MAPK10,MAPK14,MAPK7,MAPK9,MARK4,MET,NTRK1,PDGFRB,PDK1,PDK2,PDK4,PIK3CA,PIK3CD,PIK3CG,PRKDC,SIK2,SIK3,SRC,STK33,SYK,TTK,YES1	61
kinase-selectivity-class	ACVR2B,AXL,BRAF,CDK9,CSF1R,DDR1,EPHB4,FLT3,LYN,MAP3K21,MAP4K1,MAPK7,MARK4,SIK2,SIK3	15
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

Date	Agency	Company	Orphan
March 26, 2021	EMA	Incyte Biosciences Distribution B.V.
March 23, 2021	PMDA	Incyte Biosciences Japan GK
April 17, 2020	FDA	INCYTE CORP

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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
Disease progression	142.26	68.46	48	397	243986	110344868
Hyperphosphataemia	72.23	68.46	16	429	16365	110572489

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EN02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors
FDA MoA	N0000175082	Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000187061	Organic Cation Transporter 2 Inhibitors
FDA MoA	N0000191423	Multidrug and Toxin Extrusion Transporter 1 Inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agent

Related Drugs by ATC class:

L01EN Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors 3 drugs

erdafitinibfutibatinibinfigratinib

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

Disease	Relation	SNOMED_ID	DOID
Malignant neoplasm of common bile duct (& [carcinoma])	indication	187785004
Biliary tract cancer	indication	363415003	DOID:4607
FGFR1 fusion genepositive myeloid/lymphoid neoplasm	indication	721301004

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.44	Basic

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
13.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	10131667	April 17, 2034	FOR THE TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) FUSION OR OTHER REARRANGEMENT
4.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	10131667	April 17, 2034	FOR THE TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) FUSION OR OTHER REARRANGEMENT
9MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	10131667	April 17, 2034	FOR THE TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) FUSION OR OTHER REARRANGEMENT
13.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11466004	May 3, 2039	TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING ONCE DAILY A TABLET CONTAINING ABOUT 0.5 MG TO ABOUT 10 MG OF PEMIGATINIB
13.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11466004	May 3, 2039	TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB IN A DAILY DOSE OF ABOUT 5 MG TO ABOUT 20 MG
13.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11466004	May 3, 2039	TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB QD FOR 14 DAYS THEN NOT ADMINISTERING PEMIGATINIB FOR 7 DAYS IN A 21-DAY CYCLE
4.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11466004	May 3, 2039	TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING ONCE DAILY A TABLET CONTAINING ABOUT 0.5 MG TO ABOUT 10 MG OF PEMIGATINIB
4.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11466004	May 3, 2039	TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB IN A DAILY DOSE OF ABOUT 5 MG TO ABOUT 20 MG
4.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11466004	May 3, 2039	TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB QD FOR 14 DAYS THEN NOT ADMINISTERING PEMIGATINIB FOR 7 DAYS IN A 21-DAY CYCLE
9MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11466004	May 3, 2039	TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING ONCE DAILY A TABLET CONTAINING ABOUT 0.5 MG TO ABOUT 10 MG OF PEMIGATINIB
9MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11466004	May 3, 2039	TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB IN A DAILY DOSE OF ABOUT 5 MG TO ABOUT 20 MG
9MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11466004	May 3, 2039	TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB QD FOR 14 DAYS THEN NOT ADMINISTERING PEMIGATINIB FOR 7 DAYS IN A 21-DAY CYCLE
13.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11628162	Aug. 30, 2040	TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INDUCERS
13.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11628162	Aug. 30, 2040	TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INHIBITORS
13.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11628162	Aug. 30, 2040	TREATMENT OF RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS WITH FGFR1 REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INDUCERS
13.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11628162	Aug. 30, 2040	TREATMENT OF RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS WITH FGFR1 REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INHIBITORS
4.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11628162	Aug. 30, 2040	TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INDUCERS
4.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11628162	Aug. 30, 2040	TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INHIBITORS
4.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11628162	Aug. 30, 2040	TREATMENT OF RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS WITH FGFR1 REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INDUCERS
4.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11628162	Aug. 30, 2040	TREATMENT OF RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS WITH FGFR1 REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INHIBITORS
9MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11628162	Aug. 30, 2040	TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INDUCERS
9MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11628162	Aug. 30, 2040	TREATMENT OF PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FGFR2 FUSION OR OTHER REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INHIBITORS
9MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11628162	Aug. 30, 2040	TREATMENT OF RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS WITH FGFR1 REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INDUCERS
9MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	11628162	Aug. 30, 2040	TREATMENT OF RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS WITH FGFR1 REARRANGEMENT BY ADMINISTERING PEMIGATINIB WHILE AVOIDING THE CONCOMITANT USE OF STRONG AND MODERATE CYP3A INHIBITORS

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
13.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	April 17, 2027	INDICATED FOR THE TREATMENT OF ADULTS WITH PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) FUSION OR OTHER REARRANGEMENT AS DETECTED BY AN FDA-APPROVED TEST
4.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	April 17, 2027	INDICATED FOR THE TREATMENT OF ADULTS WITH PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) FUSION OR OTHER REARRANGEMENT AS DETECTED BY AN FDA-APPROVED TEST
9MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	April 17, 2027	INDICATED FOR THE TREATMENT OF ADULTS WITH PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) FUSION OR OTHER REARRANGEMENT AS DETECTED BY AN FDA-APPROVED TEST
13.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	Aug. 26, 2029	TREATMENT OF ADULTS WITH RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS (MLNS) WITH FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FGFR1) REARRANGEMENT
4.5MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	Aug. 26, 2029	TREATMENT OF ADULTS WITH RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS (MLNS) WITH FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FGFR1) REARRANGEMENT
9MG	PEMAZYRE	INCYTE CORP	N213736	April 17, 2020	RX	TABLET	ORAL	Aug. 26, 2029	TREATMENT OF ADULTS WITH RELAPSED OR REFRACTORY MYELOID/LYMPHOID NEOPLASMS (MLNS) WITH FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FGFR1) REARRANGEMENT

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Fibroblast growth factor receptor 3	Kinase	P22607	FGFR3_HUMAN	INHIBITOR	IC50	9		SCIENTIFIC LITERATURE	DRUG LABEL
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN	INHIBITOR	IC50	9.40		SCIENTIFIC LITERATURE	DRUG LABEL
Fibroblast growth factor receptor 2	Kinase	P21802	FGFR2_HUMAN	INHIBITOR	IC50	9.30		SCIENTIFIC LITERATURE	DRUG LABEL
Fibroblast growth factor receptor 4	Kinase	P22455	FGFR4_HUMAN	INHIBITOR	IC50	7.52		SCIENTIFIC LITERATURE

External reference:

ID	Source
Y6BX7BL23K	UNII
4039347	VANDF
C4724807	UMLSCUI
CHEBI:757002	CHEBI
8ZF	PDB_CHEM_ID
CHEMBL4297522	ChEMBL_ID
86705695	PUBCHEM_CID
DB15102	DRUGBANK_ID
10712	INN_ID
C000705477	MESH_SUPPLEMENTAL_RECORD_UI
D11417	KEGG_DRUG
9767	IUPHAR_LIGAND_ID
871699001	SNOMEDCT_US
871709004	SNOMEDCT_US
333127	MMSL
38333	MMSL
d09543	MMSL
018334	NDDF
2359268	RXNORM
Y6BX7BL23K	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
PEMAZYRE	HUMAN PRESCRIPTION DRUG LABEL	1	50881-026	TABLET	4.50 mg	ORAL	NDA	29 sections
PEMAZYRE	HUMAN PRESCRIPTION DRUG LABEL	1	50881-027	TABLET	9 mg	ORAL	NDA	29 sections
PEMAZYRE	HUMAN PRESCRIPTION DRUG LABEL	1	50881-028	TABLET	13.50 mg	ORAL	NDA	29 sections