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

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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5680	1448169-71-8

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: futibatinib lytgobi TAS-120

Futibatinib is a small molecule kinase inhibitor of FGFR 1, 2, 3, and 4 with IC50 values of less than 4 nM. Futibatinib covalently binds FGFR. Constitutive FGFR signaling can support the proliferation and survival of malignant cells. Futibatinib inhibited FGFR phosphorylation and downstream signaling and decreased cell viability in cancer cell lines with FGFR alterations including FGFR fusions/rearrangements, amplifications, and mutations. Futibatinib demonstrated anti-tumor activity in mouse and rat xenograft models of human tumors with activating FGFR genetic alterations. Molecular weight: 418.46 Formula: C22H22N6O3 CLOGP: 1.96 LIPINSKI: 0 HAC: 9 HDO: 1 TPSA: 108.39 ALOGS: -4.02 ROTB: 6 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	BLK,BMX,BTK,DDR1,EGFR,EIF2AK3,ERBB2,ERBB4,PDK1,PDK2,PDK4,RIPK3	12
kinase-selectivity-class	ACVRL1,BLK,BMX,BTK,EGFR,ERBB2,ERBB4,PDK4,RIPK3	9
mdck-mdr1-bcrp-efflux	MDCK-MDR1-BCRP efflux ratio	5.495		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
rat-kpuu-brain	Rat brain Kpuu	0.069	%	High	1

Approvals:

Date	Agency	Company	Orphan
Sept. 30, 2022	FDA	TAIHO ONCOLOGY
July 4, 2023	EMA	TAIHO PHARMA NETHERLANDS B.V.
June 26, 2023	PMDA	Taiho Pharmaceutical Co., Ltd.

FDA Adverse Event Reporting System (Female)

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	82.78	80.22	10	18	3701	90624718

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	109.01	77.15	17	61	16364	110572857

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EN04	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors
MeSH PA	D000970	Antineoplastic Agents
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000190113	Breast Cancer Resistance Protein Inhibitors
FDA MoA	N0000194026	Fibroblast Growth Factor Receptor Inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agent

Related Drugs by ATC class:

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

erdafitinibinfigratinibpemigatinib

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

Disease	Relation	SNOMED_ID	DOID
Intrahepatic cholangiocarcinoma	indication	109842005	DOID:4928
Biliary tract cancer	indication	363415003	DOID:4607

🐶 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
16MG	LYTGOBI	TAIHO ONCOLOGY	N214801	July 28, 2025	DISCN	TABLET	ORAL	9108973	Feb. 13, 2033	METHOD OF TREATING INTRAHEPATIC CHOLANGIOCARCINOMA
4MG	LYTGOBI	TAIHO ONCOLOGY	N214801	Sept. 30, 2022	RX	TABLET	ORAL	9108973	Feb. 13, 2033	METHOD OF TREATING INTRAHEPATIC CHOLANGIOCARCINOMA

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
16MG	LYTGOBI	TAIHO ONCOLOGY	N214801	July 28, 2025	DISCN	TABLET	ORAL	Sept. 30, 2027	NEW CHEMICAL ENTITY
4MG	LYTGOBI	TAIHO ONCOLOGY	N214801	Sept. 30, 2022	RX	TABLET	ORAL	Sept. 30, 2027	NEW CHEMICAL ENTITY
16MG	LYTGOBI	TAIHO ONCOLOGY	N214801	July 28, 2025	DISCN	TABLET	ORAL	Sept. 30, 2029	FDA HAS NOT RECOGNIZED ORPHAN-DRUG EXCLUSIVITY (ODE) FOR THIS DRUG, BUT IT CONTAINS THE SAME ACTIVE MOIETY OR MOIETIES AS ANOTHER DRUG(S) THAT WAS ELIGIBLE FOR ODE, AND ALSO SHARES ODE-PROTECTED USE(S) OR INDICATION(S) WITH THAT DRUG(S). AN APPLICATION SEEKING APPROVAL FOR THE SAME ACTIVE MOIETY OR MOIETIES, INCLUDING AN ANDA THAT CITES THIS NDA AS ITS BASIS OF SUBMISSION, MAY NOT BE APPROVED FOR SUCH ODE-PROTECTED USE(S) AND INDICATION(S)
4MG	LYTGOBI	TAIHO ONCOLOGY	N214801	Sept. 30, 2022	RX	TABLET	ORAL	Sept. 30, 2029	TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC INTRAHEPATIC CHOLANGIOCARCINOMA HARBORING FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) GENE FUSIONS OR OTHER REARRANGEMENTS

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	8.79		SCIENTIFIC LITERATURE	DRUG LABEL
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN	INHIBITOR	IC50	8.74		SCIENTIFIC LITERATURE	DRUG LABEL
Fibroblast growth factor receptor 2	Kinase	P21802	FGFR2_HUMAN	INHIBITOR	IC50	8.85		SCIENTIFIC LITERATURE	DRUG LABEL
Fibroblast growth factor receptor 4	Kinase	P22455	FGFR4_HUMAN	INHIBITOR	IC50	8.79		SCIENTIFIC LITERATURE	DRUG LABEL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN		IC50	5.63		CHEMBL
Tyrosine-protein kinase BTK	Kinase	Q06187	BTK_HUMAN		IC50	7.02		CHEMBL

External reference:

ID	Source
CHEBI:755715	CHEBI
TAW	PDB_CHEM_ID
CHEMBL3701238	ChEMBL_ID
C000713257	MESH_SUPPLEMENTAL_RECORD_UI
9786	IUPHAR_LIGAND_ID
DB15149	DRUGBANK_ID
1351548001	SNOMEDCT_US
4041794	VANDF
C5139845	UMLSCUI
10879	INN_ID
D11725	KEGG_DRUG
71621331	PUBCHEM_CID
361969	MMSL
40947	MMSL
d09927	MMSL
019197	NDDF
4B93MGE4AL	UNII
2628190	RXNORM
4B93MGE4AL	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
LYTGOBI	HUMAN PRESCRIPTION DRUG LABEL	1	64842-0120	TABLET	4 mg	ORAL	NDA	28 sections
LYTGOBI	HUMAN PRESCRIPTION DRUG LABEL	1	64842-0127	TABLET	16 mg	ORAL	NDA	28 sections