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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5327	1346242-81-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: erdafitinib balversa JNJ-42756493 G-024	Erdafitinib inhibited FGFR phosphorylation and signaling and decreased cell viability in cell lines expressing FGFR genetic alterations, including point mutations, amplifications, and fusions. Erdafitinib demonstrated antitumor activity in FGFR-expressing cell lines and xenograft models derived from tumor types, including bladder cancer. Molecular weight: 446.56 Formula: C25H30N6O2 CLOGP: 4.34 LIPINSKI: 0 HAC: 8 HDO: 1 TPSA: 77.33 ALOGS: -4.53 ROTB: 9 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

erdafitinib
balversa
JNJ-42756493
G-024

Erdafitinib inhibited FGFR phosphorylation and signaling and decreased cell viability in cell lines expressing FGFR genetic alterations, including point mutations, amplifications, and fusions. Erdafitinib demonstrated antitumor activity in FGFR-expressing cell lines and xenograft models derived from tumor types, including bladder cancer.

Molecular weight: 446.56
Formula: C25H30N6O2
CLOGP: 4.34
LIPINSKI: 0
HAC: 8
HDO: 1
TPSA: 77.33
ALOGS: -4.53
ROTB: 9

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
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
April 12, 2019	FDA	JANSSEN BIOTECH

FDA Adverse Event Reporting System (Female)

None

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
Death	68.15	61.71	36	167	398013	34558715

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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
Onycholysis	70.97	48.79	12	451	2071	79741854

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01EN01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000182141	Cytochrome P450 3A4 Inhibitors
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000185506	Cytochrome P450 3A4 Inducers
FDA MoA	N0000187061	Organic Cation Transporter 2 Inhibitors
FDA MoA	N0000194026	Fibroblast Growth Factor Receptor Inhibitors

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

Disease	Relation	SNOMED_ID	DOID
Metastatic urothelial carcinoma	indication	458321000124102

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.52	Basic
pKa2	2.13	Basic
pKa3	0.47	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
3MG	BALVERSA	JANSSEN BIOTECH	N212018	April 12, 2019	RX	TABLET	ORAL	9464071	April 28, 2031	TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC UROTHELIAL CARCINOMA THAT HAS SUSCEPTIBLE FGFR3 OR FGFR2 GENETIC ALTERATIONS AND PROGRESSED DURING OR FOLLOWING PRIOR PLATINUM-CONTAINING CHEMOTHERAPY
3MG	BALVERSA	JANSSEN BIOTECH	N212018	April 12, 2019	RX	TABLET	ORAL	10898482	Feb. 9, 2036	TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC, SURGICALLY UNRESECTABLE UROTHELIAL CARCINOMA THAT HAS SUSCEPTIBLE FGFR3 OR FGFR2 GENETIC ALTERATIONS AND PROGRESSED DURING OR FOLLOWING PRIOR PLATINUM-CONTAINING CHEMOTHERAPY
3MG	BALVERSA	JANSSEN BIOTECH	N212018	April 12, 2019	RX	TABLET	ORAL	10898482	Feb. 9, 2036	TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC UROTHELIAL CARCINOMA THAT HAS SUSCEPTIBLE FGFR3 GENETIC ALTERATIONS AND PROGRESSED DURING OR FOLLOWING PRIOR PLATINUM-CONTAINING CHEMOTHERAPY
3MG	BALVERSA	JANSSEN BIOTECH	N212018	April 12, 2019	RX	TABLET	ORAL	10898482	Feb. 9, 2036	TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC UROTHELIAL CARCINOMA THAT HAS SUSCEPTIBLE FGFR3 OR FGFR2 GENETIC ALTERATIONS AND PROGRESSED DURING OR FOLLOWING PRIOR PLATINUM-CONTAINING CHEMOTHERAPY
3MG	BALVERSA	JANSSEN BIOTECH	N212018	April 12, 2019	RX	TABLET	ORAL	10898482	Feb. 9, 2036	TREATMENT OF ADULTS WITH METASTATIC UROTHELIAL CARCINOMA THAT HAS SUSCEPTIBLE FGFR3 OR FGFR2 GENETIC ALTERATIONS AND PROGRESSED DURING OR FOLLOWING PRIOR PLATINUM-CONTAINING CHEMOTHERAPY
3MG	BALVERSA	JANSSEN BIOTECH	N212018	April 12, 2019	RX	TABLET	ORAL	11684620	Feb. 9, 2036	TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC, SURGICALLY UNRESECTABLE UROTHELIAL CARCINOMA THAT HAS SUSCEPTIBLE FGFR3 OR FGFR2 GENETIC ALTERATIONS AND PROGRESSED DURING OR FOLLOWING PRIOR PLATINUM-CONTAINING CHEMOTHERAPY
3MG	BALVERSA	JANSSEN BIOTECH	N212018	April 12, 2019	RX	TABLET	ORAL	11684620	Feb. 9, 2036	TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC UROTHELIAL CARCINOMA THAT HAS SUSCEPTIBLE FGFR3 GENETIC ALTERATIONS AND PROGRESSED DURING OR FOLLOWING PRIOR PLATINUM-CONTAINING CHEMOTHERAPY
3MG	BALVERSA	JANSSEN BIOTECH	N212018	April 12, 2019	RX	TABLET	ORAL	11684620	Feb. 9, 2036	TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC UROTHELIAL CARCINOMA THAT HAS SUSCEPTIBLE FGFR3 OR FGFR2 GENETIC ALTERATIONS AND PROGRESSED DURING OR FOLLOWING PRIOR PLATINUM-CONTAINING CHEMOTHERAPY
3MG	BALVERSA	JANSSEN BIOTECH	N212018	April 12, 2019	RX	TABLET	ORAL	11684620	Feb. 9, 2036	TREATMENT OF ADULTS WITH METASTATIC UROTHELIAL CARCINOMA THAT HAS SUSCEPTIBLE FGFR3 OR FGFR2 GENETIC ALTERATIONS AND PROGRESSED DURING OR FOLLOWING PRIOR PLATINUM-CONTAINING CHEMOTHERAPY
3MG	BALVERSA	JANSSEN BIOTECH	N212018	April 12, 2019	RX	TABLET	ORAL	11077106	Feb. 2, 2038	TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC UROTHELIAL CARCINOMA WITH SUSCEPTIBLE FGFR3 OR FGFR2 GENETIC ALTERATIONS, AND PROGRESSED DURING OR FOLLOWING PRIOR PLATINUM-CONTAINING CHEMOTHERAPY, WITH DOSING BASED ON SERUM PHOSPHATE LEVELS

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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
3MG	BALVERSA	JANSSEN BIOTECH	N212018	April 12, 2019	RX	TABLET	ORAL	April 12, 2024	NEW CHEMICAL ENTITY
4MG	BALVERSA	JANSSEN BIOTECH	N212018	April 12, 2019	RX	TABLET	ORAL	April 12, 2024	NEW CHEMICAL ENTITY
5MG	BALVERSA	JANSSEN BIOTECH	N212018	April 12, 2019	RX	TABLET	ORAL	April 12, 2024	NEW CHEMICAL ENTITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	INHIBITOR	IC50	7.43	SCIENTIFIC LITERATURE	DRUG LABEL
Fibroblast growth factor receptor 3	Kinase	P22607	FGFR3_HUMAN	INHIBITOR	IC50	8.52	SCIENTIFIC LITERATURE	DRUG LABEL
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN	INHIBITOR	IC50	8.92	SCIENTIFIC LITERATURE	DRUG LABEL
Fibroblast growth factor receptor 2	Kinase	P21802	FGFR2_HUMAN	INHIBITOR	IC50	8.60	SCIENTIFIC LITERATURE	DRUG LABEL
Fibroblast growth factor receptor 4	Kinase	P22455	FGFR4_HUMAN	INHIBITOR	IC50	8.24	SCIENTIFIC LITERATURE	DRUG LABEL
Vascular endothelial growth factor receptor 2	Kinase		VGFR2_MOUSE		IC50	10	CHEMBL

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External reference:

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ID	Source
017965	NDDF
10147	INN_ID
2123125	RXNORM
314002	MMSL
36736	MMSL
4038332	VANDF
5SF	PDB_CHEM_ID
67462786	PUBCHEM_CID
787731007	SNOMEDCT_US
787742003	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
BALVERSA	HUMAN PRESCRIPTION DRUG LABEL	1	59676-030	TABLET, FILM COATED	3 mg	ORAL	NDA	31 sections
BALVERSA	HUMAN PRESCRIPTION DRUG LABEL	1	59676-030	TABLET, FILM COATED	3 mg	ORAL	NDA	31 sections
BALVERSA	HUMAN PRESCRIPTION DRUG LABEL	1	59676-030	TABLET, FILM COATED	3 mg	ORAL	NDA	31 sections
BALVERSA	HUMAN PRESCRIPTION DRUG LABEL	1	59676-030	TABLET, FILM COATED	3 mg	ORAL	NDA	31 sections
BALVERSA	HUMAN PRESCRIPTION DRUG LABEL	1	59676-040	TABLET, FILM COATED	4 mg	ORAL	NDA	31 sections
BALVERSA	HUMAN PRESCRIPTION DRUG LABEL	1	59676-040	TABLET, FILM COATED	4 mg	ORAL	NDA	31 sections
BALVERSA	HUMAN PRESCRIPTION DRUG LABEL	1	59676-040	TABLET, FILM COATED	4 mg	ORAL	NDA	31 sections
BALVERSA	HUMAN PRESCRIPTION DRUG LABEL	1	59676-040	TABLET, FILM COATED	4 mg	ORAL	NDA	31 sections
BALVERSA	HUMAN PRESCRIPTION DRUG LABEL	1	59676-050	TABLET, FILM COATED	5 mg	ORAL	NDA	31 sections
BALVERSA	HUMAN PRESCRIPTION DRUG LABEL	1	59676-050	TABLET, FILM COATED	5 mg	ORAL	NDA	31 sections

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