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

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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5459	872511-34-7

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: infigratinib infigratinib phosphate truseltiq BGJ-398 NVP-BGJ398

Infigratinib is a small molecule kinase inhibitor of FGFR with IC50 values of 1.1, 1, 2, and 61 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. The major human metabolites of infigratinib, BHS697 and CQM157, have similar in vitro binding affinities for FGFR1, FGFR2, and FGFR3 compared to infigratinib. Infigratinib inhibited FGFR signaling and decreased cell proliferation in cancer cell lines with activating FGFR amplifications, mutations, or fusions. Constitutive FGFR signaling can support the proliferation and survival of malignant cells. Infigratinib had anti-tumor activity in mouse and rat xenograft models of human tumors with activating FGFR2 or FGFR3 alterations, including two patient-derived xenograft models of cholangiocarcinoma that expressed FGFR2-TTC28 or FGFR2-TRA2B fusions. Infigratinib demonstrated brain-to-plasma concentration ratios (based on AUC0-inf) of 0.682 in rats after a single oral dose. Molecular weight: 560.48 Formula: C26H31Cl2N7O3 CLOGP: 5.44 LIPINSKI: 1 HAC: 10 HDO: 2 TPSA: 95.09 ALOGS: -4.27 ROTB: 8 Status: OFM 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
June 28, 2019	FDA	QED THERAP

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
Hyperphosphataemia	32.96	23.70	4	3	6372	79738009

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EN03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors
MeSH PA	D000970	Antineoplastic Agents
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:63457	FGFR inhibitors

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

Disease	Relation	SNOMED_ID	DOID
Unresectable locally advanced or metastatic cholangiocarcinoma with FGFR2 fusion	indication	312104005

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
100MG	TRUSELTIQ	HELSINN HLTHCARE	N214622	May 28, 2021	DISCN	CAPSULE	ORAL	May 28, 2026	NEW CHEMICAL ENTITY
25MG	TRUSELTIQ	HELSINN HLTHCARE	N214622	May 28, 2021	DISCN	CAPSULE	ORAL	May 28, 2026	NEW CHEMICAL ENTITY
100MG	TRUSELTIQ	HELSINN HLTHCARE	N214622	May 28, 2021	DISCN	CAPSULE	ORAL	May 28, 2028	FOR 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
25MG	TRUSELTIQ	HELSINN HLTHCARE	N214622	May 28, 2021	DISCN	CAPSULE	ORAL	May 28, 2028	FOR 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

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN	INHIBITOR		8.99		DRUG LABEL	DRUG LABEL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		IC50	5.64		CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN		IC50	6.12		CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN		IC50	5.53		CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		IC50	5.60		CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN		IC50	5.96		CHEMBL
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		IC50	5.72		CHEMBL
Serine/threonine-protein kinase B-raf	Kinase	P15056	BRAF_HUMAN		IC50	5.38		CHEMBL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		IC50	5.49		CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		IC50	5.47		CHEMBL
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN		IC50	5.82		CHEMBL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	INHIBITOR	IC50	6.74		IUPHAR
Vascular endothelial growth factor receptor 3	Kinase	P35916	VGFR3_HUMAN		IC50	5.68		CHEMBL
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN		IC50	5.57		CHEMBL
Insulin receptor	Kinase	P06213	INSR_HUMAN		IC50	5.47		CHEMBL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN		IC50	5.54		CHEMBL
Macrophage-stimulating protein receptor	Kinase	Q04912	RON_HUMAN		IC50	5.54		CHEMBL
Angiopoietin-1 receptor	Kinase	Q02763	TIE2_HUMAN		IC50	5.69		CHEMBL
Hepatocyte growth factor receptor	Kinase	P08581	MET_HUMAN		IC50	5.52		CHEMBL
Tyrosine-protein kinase Lyn	Kinase	P07948	LYN_HUMAN		IC50	6.52		CHEMBL
Cytoplasmic tyrosine-protein kinase BMX	Kinase	P51813	BMX_HUMAN		IC50	5.47		CHEMBL
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN		IC50	5.51		CHEMBL
Ephrin type-B receptor 1	Kinase	P54762	EPHB1_HUMAN		IC50	5.52		CHEMBL
BDNF/NT-3 growth factors receptor	Kinase	Q16620	NTRK2_HUMAN		IC50	5.50		CHEMBL
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN		IC50	5.48		CHEMBL
Proto-oncogene tyrosine-protein kinase ROS	Kinase	P08922	ROS1_HUMAN		IC50	5.49		CHEMBL
Smoothened homolog	GPCR	Q99835	SMO_HUMAN		Ki	7.33		CHEMBL
Fibroblast growth factor receptor 3	Kinase	P22607	FGFR3_HUMAN	INHIBITOR		8.70		DRUG LABEL
Fibroblast growth factor receptor 2	Kinase	P21802	FGFR2_HUMAN	INHIBITOR		9		DRUG LABEL
Fibroblast growth factor receptor 4	Kinase	P22455	FGFR4_HUMAN	INHIBITOR		7.21		DRUG LABEL
Tyrosine-protein kinase SYK	Kinase	P43405	KSYK_HUMAN		IC50	5.27		CHEMBL
Fibroblast growth factor receptor 4, FGFR-4, EC 2.7.10.1	Unclassified		FGFR4_MOUSE		IC50	6.27		CHEMBL

External reference:

ID	Source
D11589	KEGG_DRUG
A4055ME1VK	UNII
1310746-10-1	SECONDARY_CAS_RN
C3254591	UMLSCUI
CHEBI:63451	CHEBI
07J	PDB_CHEM_ID
CHEMBL1852688	ChEMBL_ID
53235510	PUBCHEM_CID
DB11886	DRUGBANK_ID
CHEMBL1834657	ChEMBL_ID
10032	INN_ID
7877	IUPHAR_LIGAND_ID
018743	NDDF
018752	NDDF
1162483003	SNOMEDCT_US
1162514000	SNOMEDCT_US
4040560	VANDF
2550729	RXNORM
347055	MMSL
39550	MMSL
d09752	MMSL
C568950	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
TRUSELTIQ	HUMAN PRESCRIPTION DRUG LABEL	1	72730-101	CAPSULE	125 mg	ORAL	NDA	17 sections
TRUSELTIQ	HUMAN PRESCRIPTION DRUG LABEL	1	72730-111	CAPSULE	100 mg	ORAL	NDA	17 sections
TRUSELTIQ	HUMAN PRESCRIPTION DRUG LABEL	1	72730-202	CAPSULE	75 mg	ORAL	NDA	17 sections
TRUSELTIQ	HUMAN PRESCRIPTION DRUG LABEL	1	72730-506	CAPSULE	50 mg	ORAL	NDA	17 sections