Identification
- Summary
Erdafitinib is a fibroblast growth factor receptor tyrosine kinase inhibitor used to treat locally advanced or metastatic urothelial carcinoma.
- Brand Names
- Balversa
- Generic Name
- Erdafitinib
- DrugBank Accession Number
- DB12147
- Background
In early April of 2019, the US FDA approved Janssen Pharmaceutical Companies' brand name Balversa (erdafitinib) as the first-ever fibroblast growth factor receptor (FGFR) kinase inhibitor indicated for patients with locally advanced or metastatic urothelial carcinoma, with susceptible FGFR3 or FGFR2 genetic alterations, that has progressed during or following platinum-containing chemotherapy, including within 12 months of neoadjuvant or adjuvant platinum-containing chemotherapy. 4,5 At the same time, the FDA also approved the therascreen FGFR RGQ RT-PCR Kit (Qiagen) for utilization as a companion diagnostic with erdafitinib for selecting patients for the indicated therapy 4,5.
Erdafitinib is the first personalized treatment targeting susceptible FGFR genetic alterations for patients with metastatic bladder cancer, which demonstrates the development of more personalized and precise medicines tailoring to a patient's specific genetic mutation.4,5 Considering urothelial cancer is statistically the fourth most common kind of cancer in the world, the introduction of erdafitinib offers a much-needed new option in the ever-expanding therapeutic tool kit to treat such a prevalent medical condition.9
Nevertheless, although erdafitinib was granted Breakthrough Therapy designation and Accelerated Approval from the FDA, such designations mean further ongoing clinical trials are necessary to confirm the clinical benefit of erdafitinib going forward.4,5
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Erdafitinib (DB12147)
- Weight
- Average: 446.555
Monoisotopic: 446.24302423 - Chemical Formula
- C25H30N6O2
- Synonyms
- Erdafitinib
- External IDs
- JNJ-42756493
Pharmacology
- Indication
Erdafitinib is a pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor that is indicated for the treatment of adult patients with locally advanced or metastatic urothelial carcinoma that has susceptible FGFR3 or FGFR2 genetic alterations and has progressed during or following at least one line of prior platinum-containing chemotherapy including within 12 months of neoadjuvant or adjuvant platinum-containing chemotherapy.1,2,3,6
The selection of patients for the treatment of locally advanced or metastatic urothelial carcinoma with erdafitinib should be based on the presence of susceptible FGFR genetic alterations in tumor specimens as detected by an FDA-approved companion diagnostic like the FDA-approved therascreen FGFR RGQ RT-PCR Kit as developed by QIAGEN.6
This above indication is approved under accelerated approval by the FDA based on tumor response rate. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trials.6
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- Contraindications & Blackbox Warnings
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Upon administration, it was observed that erdafitinib increased serum phosphate levels as a consequence of FGFR inhibition. Erdafitinib should be increased to the maximum recommended dose to achieve target serum phosphate levels of 5.5– 7.0 mg/dL in early cycles with continuous daily dosing.1,3,6
Subsequently, in erdafitinib clinical trials, the use of drugs that could increase serum phosphate levels, such as potassium phosphate supplements, vitamin D supplements, antacids, phosphate-containing enemas or laxatives, and medications known to have phosphate as an excipient were prohibited unless no alternatives existed.1,3,6 To manage phosphate elevation, phosphate binders were utilized. Additionally, the concomitant use of agents that can alter serum phosphate levels before the initial erdafitinib dose increase period based on serum phosphate levels was also avoided.1,3,6
Furthermore, based on the evaluation of QTc interval in an open-label, dose escalation, and dose expansion study in 187 patients with cancer, erdafitinib had no large effect (i.e., > 20 ms) on the QTc interval.6
- Mechanism of action
Fibroblast growth factor receptor (FGFR) is a transmembrane protein that is expressed ubiquitously in normal tissues and is involved in various endogenous bio-physiological processes including the homeostasis of phosphate and vitamin D, cell proliferation, cell anti-apoptotic signaling, and cell migration in a variety of cell types.1 Concurrently, genetic mutations such as gene amplification, point mutations, and chromosomal translocations of all four FGFR genes (FGFR1, FGFR2, FGFR3, and FGFR4) or deregulation of FGFR pathways have been implicated in the pathogenesis of various cancers, including urothelial cancer, as they promote cell proliferation, migration, angiogenesis, and anti-apoptosis.1,6
Erdafitinib is an oral selective pan-FGFR kinase inhibitor that binds to and inhibits the enzymatic activity of expressed FGFR1, FGFR2, FGFR3, and FGFR4 based on in vitro data.6,1,3 In particular, erdafitinib demonstrates inhibition of FGFR phosphorylation and signaling as well as decreased cell viability in cell lines expressing FGFR genetic alterations.1,3,6 Erdafitinib demonstrated antitumor activity in FGFR-expressing cell lines and xenograft models derived from tumor types, including bladder cancer.1,3,6
Target Actions Organism AFibroblast growth factor receptor 1 inhibitorHumans AFibroblast growth factor receptor 2 inhibitorHumans AFibroblast growth factor receptor 3 inhibitorHumans AFibroblast growth factor receptor 4 inhibitorHumans URET proto-oncogene substrateHumans UMacrophage colony-stimulating factor 1 receptor substrateHumans UPlatelet-derived growth factor receptor alpha substrateHumans UPlatelet-derived growth factor receptor beta substrateHumans UMast/stem cell growth factor receptor Kit substrateHumans UVascular endothelial growth factor receptor 2 substrateHumans - Absorption
Following administration of erdafitinib 8 mg once daily, the mean (coefficient of variation [CV%]) steady-state maximum observed plasma concentration (Cmax), area under the curve (AUCtau), and minimum observed plasma concentration (Cmin) were 1,399 ng/mL (51%), 29,268 ng·h/mL (60%), and 936 ng/mL (65%), respectively.6
Following single and repeated once-daily dosing, erdafitinib exposure (maximum observed plasma concentration [Cmax] and area under the plasma concentration-time curve [AUC]) increased proportionally across the dose range of 0.5 to 12 mg (0.06 to 1.3 times the maximum approved recommended dose).6 Steady-state was achieved after 2 weeks with once-daily dosing and the mean accumulation ratio was 4-fold.6
The median time to achieve peak plasma concentration (tmax) was 2.5 hours (range: 2 to 6 hours).6 No clinically meaningful differences with erdafitinib pharmacokinetics were observed following the administration of a high-fat and high-calorie meal (800 calories to 1,000 calories with approximately 50% of the total caloric content of the meal from fat) in healthy subjects.6
- Volume of distribution
The mean apparent volume of distribution determined for erdafitinib is about 26 to 29 L in patients.3,6
- Protein binding
The protein binding recorded for erdafitinib is approximately 99.8%, and it was determined to be primarily bound to alpha-1-acid glycoprotein.6
- Metabolism
Erdafitinib is primarily metabolized by the cytochrome CYP2C9 and CYP3A4 isoenzymes in humans to form the O-demethylated major metabolite.6,7. The contribution of CYP2C9 and CYP3A4 in the total clearance of erdafitinib is estimated to be 39% and 20% respectively.6 Unchanged erdafitinib was ultimately the predominant drug-related moiety found in the plasma - no circulating metabolites were observed.6
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- Route of elimination
After administering a single oral dose of radiolabeled erdafitinib, about 69% of the dose was recovered in feces (19% as unchanged) and 19% in urine (13% as unchanged).6
- Half-life
The mean effective half-life documented for erdafitinib is 59 hours, although it has also been observed between 50 to 60 hours.6,3
- Clearance
The mean total apparent clearance (CL/F) documented for erdafitinib is about 0.362 L/h, while the oral clearance has been observed to be approximately 0.26 L/h 6,3.
- Adverse Effects
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Based on the mechanism of action and findings in animal reproduction studies, erdafitinib can cause fetal harm when administered to a pregnant woman Label. There are no available data on erdafitinib use in pregnant women to inform a drug-associated risk Label. Oral administration of erdafitinib to pregnant rats during organogenesis caused malformations and embryo- fetal death at maternal exposures that were less than the human exposures at the maximum recommended human dose based on AUC Label. Advise pregnant women and females of reproductive potential of the potential risk to the fetus Label.
There are no data on the presence of erdafitinib in human milk, or the effects of erdafitinib on the breastfed child, or on milk production Label. Because of the potential for serious adverse reactions from erdafitinib in a breastfed child, advise lactating women not to breastfeed during treatment with erdafitinib and for one month following the last dose Label.
Pregnancy testing is recommended for females of reproductive potential prior to initiating treatment with erdafitinib Label.
Erdafitinib can cause fetal harm when administered to a pregnant woman Label. Advise females of reproductive potential to use effective contraception during treatment with erdafitinib and for one month after the last dose Label.
Advise male patients with female partners of reproductive potential to use effective contraception during treatment with erdafitinib and for one month after the last dose Label.
Based on findings from animal studies, erdafitinib may impair fertility in females of reproductive potential Label.
Safety and effectiveness of erdafitinib in pediatric patients have not been established Label.
No overall differences in safety or effectiveness were observed between these patients and younger patients in the use of erdafitinib Label.
Erdafitinib plasma concentrations were predicted to be higher in patients with the CYP2C93/3 genotype Label. Monitor for increased adverse reactions in patients who are known or suspected to have CYP2C93/3 genotype Label.
Carcinogenicity studies have not been conducted with erdafitinib Label.
Erdafitinib was not mutagenic in a bacterial reverse mutation (Ames) assay and was not clastogenic in an in vitro micronucleus or an in vivo rat bone marrow micronucleus assay Label.
Fertility studies in animals have not been conducted with erdafitinib. In the 3-month repeat-dose toxicity study, erdafitinib showed effects on female reproductive organs (necrosis of the ovarian corpora lutea) in rats at an exposure less than the human exposure (AUC) at maximum recommended human dose Label.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Erdafitinib can be increased when it is combined with Abametapir. Abatacept The metabolism of Erdafitinib can be increased when combined with Abatacept. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Erdafitinib. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Erdafitinib. Acalabrutinib The serum concentration of Acalabrutinib can be increased when it is combined with Erdafitinib. Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Erdafitinib. Acetaminophen The metabolism of Erdafitinib can be increased when combined with Acetaminophen. Acetazolamide The serum concentration of Erdafitinib can be increased when it is combined with Acetazolamide. Acetohexamide The metabolism of Erdafitinib can be decreased when combined with Acetohexamide. Acetyl sulfisoxazole The metabolism of Erdafitinib can be decreased when combined with Acetyl sulfisoxazole. 
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- Exercise caution with grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of erdafitinib.
- Exercise caution with St. John's Wort. This herb induces the CYP3A metabolism of erdafitinib and may reduce its serum concentration.
- Take with or without food. No clinically meaningful differences with erdafitinib pharmacokinetics were observed following administration of a high-fat and high-calorie meal (800 calories to 1,000 calories with approximately 50% of total caloric content of the meal from fat) in healthy subjects.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Balversa Tablet, film coated 5 mg/1 Oral Janssen Products LP 2019-04-12 Not applicable US 
Balversa Tablet 3 mg Oral Janssen Pharmaceuticals 2019-12-09 Not applicable Canada 
Balversa Tablet, film coated 4 mg/1 Oral Janssen Products LP 2019-04-12 Not applicable US Balversa Tablet 4 mg Oral Janssen Pharmaceuticals Not applicable Not applicable Canada Balversa Tablet 5 mg Oral Janssen Pharmaceuticals 2019-12-09 Not applicable Canada Balversa Tablet, film coated 3 mg/1 Oral Janssen Products LP 2019-04-12 Not applicable US Balversa Tablet 4 mg Oral Janssen Pharmaceuticals 2019-12-09 Not applicable Canada
Categories
- ATC Codes
- L01EN01 — Erdafitinib
- Drug Categories
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP2C9 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors
- Heterocyclic Compounds, Fused-Ring
- Kinase Inhibitor
- Narrow Therapeutic Index Drugs
- OCT2 Inhibitors
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- P-glycoprotein substrates with a Narrow Therapeutic Index
- Protein Kinase Inhibitors
- Receptors, Fibroblast Growth Factor, antagonists & inhibitors
- Tumor Suppressor Proteins
- Tyrosine Kinase Inhibitors
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as alkyldiarylamines. These are tertiary alkylarylamines having two aryl and one alkyl groups attached to the amino group.
- Kingdom
- Organic compounds
- Super Class
- Organic nitrogen compounds
- Class
- Organonitrogen compounds
- Sub Class
- Amines
- Direct Parent
- Alkyldiarylamines
- Alternative Parents
- Quinoxalines / Dimethoxybenzenes / Methoxyanilines / Aminophenyl ethers / Phenoxy compounds / Anisoles / Alkyl aryl ethers / Pyrazines / Pyrazoles / Heteroaromatic compounds show 4 more
- Substituents
- Alkyl aryl ether / Alkyldiarylamine / Aminophenyl ether / Aniline or substituted anilines / Anisole / Aromatic heteropolycyclic compound / Azacycle / Azole / Benzenoid / Diazanaphthalene show 19 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 890E37NHMV
- CAS number
- 1346242-81-6
- InChI Key
- OLAHOMJCDNXHFI-UHFFFAOYSA-N
- InChI
- InChI=1S/C25H30N6O2/c1-17(2)26-8-9-31(20-10-21(32-4)13-22(11-20)33-5)19-6-7-23-24(12-19)29-25(15-27-23)18-14-28-30(3)16-18/h6-7,10-17,26H,8-9H2,1-5H3
- IUPAC Name
- N-(3,5-dimethoxyphenyl)-3-(1-methyl-1H-pyrazol-4-yl)-N-{2-[(propan-2-yl)amino]ethyl}quinoxalin-6-amine
- SMILES
- COC1=CC(=CC(OC)=C1)N(CCNC(C)C)C1=CC=C2N=CC(=NC2=C1)C1=CN(C)N=C1
References
- General References
- Nishina T, Takahashi S, Iwasawa R, Noguchi H, Aoki M, Doi T: Safety, pharmacokinetic, and pharmacodynamics of erdafitinib, a pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor, in patients with advanced or refractory solid tumors. Invest New Drugs. 2018 Jun;36(3):424-434. doi: 10.1007/s10637-017-0514-4. Epub 2017 Sep 30. [Article]
- Perera TPS, Jovcheva E, Mevellec L, Vialard J, De Lange D, Verhulst T, Paulussen C, Van De Ven K, King P, Freyne E, Rees DC, Squires M, Saxty G, Page M, Murray CW, Gilissen R, Ward G, Thompson NT, Newell DR, Cheng N, Xie L, Yang J, Platero SJ, Karkera JD, Moy C, Angibaud P, Laquerre S, Lorenzi MV: Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor. Mol Cancer Ther. 2017 Jun;16(6):1010-1020. doi: 10.1158/1535-7163.MCT-16-0589. Epub 2017 Mar 24. [Article]
- Tabernero J, Bahleda R, Dienstmann R, Infante JR, Mita A, Italiano A, Calvo E, Moreno V, Adamo B, Gazzah A, Zhong B, Platero SJ, Smit JW, Stuyckens K, Chatterjee-Kishore M, Rodon J, Peddareddigari V, Luo FR, Soria JC: Phase I Dose-Escalation Study of JNJ-42756493, an Oral Pan-Fibroblast Growth Factor Receptor Inhibitor, in Patients With Advanced Solid Tumors. J Clin Oncol. 2015 Oct 20;33(30):3401-8. doi: 10.1200/JCO.2014.60.7341. Epub 2015 Aug 31. [Article]
- FDA grants accelerated approval to erdafitinib for metastatic urothelial carcinoma: Press Release [Link]
- First Targeted Therapy for Metastatic Bladder Cancer Receives FDA Approval [Link]
- FDA Approved Drug Products: BALVERSA® (erdafitinib) tablets, for oral use [Link]
- Health Canada Approved Drug Proucts: BALVERSA (Erdafitinib) tablets, for oral use [Link]
- Cayman Chemical Erdafitinib MSDS [File]
- NHS Evidence Briefing On: Erdafitinib capsules for metastatic or surgically unresectable urothelial cancer with FGFR gene aberrations – second line therapy [File]
- External Links
- Human Metabolome Database
- HMDB0251903
- PubChem Compound
- 67462786
- PubChem Substance
- 347828443
- ChemSpider
- 35308353
- BindingDB
- 50525939
- 2123125
- ChEMBL
- CHEMBL3545376
- ZINC
- ZINC000168520308
- PDBe Ligand
- 5SF
- Wikipedia
- Erdafitinib
- PDB Entries
- 5ew8
- FDA label
- Download (558 KB)
- MSDS
- Download (56.5 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 3 mg Tablet Oral 3.000 mg Tablet Oral 4 mg Tablet Oral 5 mg Tablet, film coated Oral 3 mg/1 Tablet, film coated Oral 4 mg/1 Tablet, film coated Oral 5 mg/1 Tablet, film coated Oral 3.00 mg Tablet, film coated Oral 4.00 mg Tablet, film coated Oral 5.00 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US9464071 No 2016-10-11 2031-04-28 US US9902714 No 2018-02-27 2035-03-26 US US8895601 No 2014-11-25 2031-05-22 US US10898482 No 2021-01-26 2036-02-09 US US11077106 No 2021-08-03 2038-02-02 US US11684620 No 2016-02-09 2036-02-09 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility <1 mg/mL MSDS - Predicted Properties
Property Value Source Water Solubility 0.013 mg/mL ALOGPS logP 3.57 ALOGPS logP 3.52 Chemaxon logS -4.5 ALOGPS pKa (Strongest Basic) 9.72 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 7 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 77.33 Å2 Chemaxon Rotatable Bond Count 9 Chemaxon Refractivity 139.32 m3·mol-1 Chemaxon Polarizability 51 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- Curator comments
- Erdafitinib inhibited FGFR phosphorylation and signaling and decreased cell viability in cell lines expressing FGFR genetic alterations, including point mutations, amplifications, and fusions
- General Function
- Protein tyrosine kinase activity
- Specific Function
- Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of embryonic development, cell proliferation, differentiation ...
- Gene Name
- FGFR1
- Uniprot ID
- P11362
- Uniprot Name
- Fibroblast growth factor receptor 1
- Molecular Weight
- 91866.935 Da
References
- Nishina T, Takahashi S, Iwasawa R, Noguchi H, Aoki M, Doi T: Safety, pharmacokinetic, and pharmacodynamics of erdafitinib, a pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor, in patients with advanced or refractory solid tumors. Invest New Drugs. 2018 Jun;36(3):424-434. doi: 10.1007/s10637-017-0514-4. Epub 2017 Sep 30. [Article]
- Tabernero J, Bahleda R, Dienstmann R, Infante JR, Mita A, Italiano A, Calvo E, Moreno V, Adamo B, Gazzah A, Zhong B, Platero SJ, Smit JW, Stuyckens K, Chatterjee-Kishore M, Rodon J, Peddareddigari V, Luo FR, Soria JC: Phase I Dose-Escalation Study of JNJ-42756493, an Oral Pan-Fibroblast Growth Factor Receptor Inhibitor, in Patients With Advanced Solid Tumors. J Clin Oncol. 2015 Oct 20;33(30):3401-8. doi: 10.1200/JCO.2014.60.7341. Epub 2015 Aug 31. [Article]
- Erdafitinib FDA Label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- Curator comments
- Erdafitinib inhibited FGFR phosphorylation and signaling and decreased cell viability in cell lines expressing FGFR genetic alterations, including point mutations, amplifications, and fusions
- General Function
- Protein tyrosine kinase activity
- Specific Function
- Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation, migration and apoptosi...
- Gene Name
- FGFR2
- Uniprot ID
- P21802
- Uniprot Name
- Fibroblast growth factor receptor 2
- Molecular Weight
- 92024.29 Da
References
- Nishina T, Takahashi S, Iwasawa R, Noguchi H, Aoki M, Doi T: Safety, pharmacokinetic, and pharmacodynamics of erdafitinib, a pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor, in patients with advanced or refractory solid tumors. Invest New Drugs. 2018 Jun;36(3):424-434. doi: 10.1007/s10637-017-0514-4. Epub 2017 Sep 30. [Article]
- Tabernero J, Bahleda R, Dienstmann R, Infante JR, Mita A, Italiano A, Calvo E, Moreno V, Adamo B, Gazzah A, Zhong B, Platero SJ, Smit JW, Stuyckens K, Chatterjee-Kishore M, Rodon J, Peddareddigari V, Luo FR, Soria JC: Phase I Dose-Escalation Study of JNJ-42756493, an Oral Pan-Fibroblast Growth Factor Receptor Inhibitor, in Patients With Advanced Solid Tumors. J Clin Oncol. 2015 Oct 20;33(30):3401-8. doi: 10.1200/JCO.2014.60.7341. Epub 2015 Aug 31. [Article]
- Erdafitinib FDA Label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- Curator comments
- Erdafitinib inhibited FGFR phosphorylation and signaling and decreased cell viability in cell lines expressing FGFR genetic alterations, including point mutations, amplifications, and fusions
- General Function
- Protein tyrosine kinase activity
- Specific Function
- Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation and apoptosis. Plays an...
- Gene Name
- FGFR3
- Uniprot ID
- P22607
- Uniprot Name
- Fibroblast growth factor receptor 3
- Molecular Weight
- 87708.905 Da
References
- Nishina T, Takahashi S, Iwasawa R, Noguchi H, Aoki M, Doi T: Safety, pharmacokinetic, and pharmacodynamics of erdafitinib, a pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor, in patients with advanced or refractory solid tumors. Invest New Drugs. 2018 Jun;36(3):424-434. doi: 10.1007/s10637-017-0514-4. Epub 2017 Sep 30. [Article]
- Tabernero J, Bahleda R, Dienstmann R, Infante JR, Mita A, Italiano A, Calvo E, Moreno V, Adamo B, Gazzah A, Zhong B, Platero SJ, Smit JW, Stuyckens K, Chatterjee-Kishore M, Rodon J, Peddareddigari V, Luo FR, Soria JC: Phase I Dose-Escalation Study of JNJ-42756493, an Oral Pan-Fibroblast Growth Factor Receptor Inhibitor, in Patients With Advanced Solid Tumors. J Clin Oncol. 2015 Oct 20;33(30):3401-8. doi: 10.1200/JCO.2014.60.7341. Epub 2015 Aug 31. [Article]
- Erdafitinib FDA Label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- Curator comments
- Erdafitinib inhibited FGFR phosphorylation and signaling and decreased cell viability in cell lines expressing FGFR genetic alterations, including point mutations, amplifications, and fusions
- General Function
- Protein tyrosine kinase activity
- Specific Function
- Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays a role in the regulation of cell proliferation, differentiation and migration, and in regulation o...
- Gene Name
- FGFR4
- Uniprot ID
- P22455
- Uniprot Name
- Fibroblast growth factor receptor 4
- Molecular Weight
- 87953.535 Da
References
- Nishina T, Takahashi S, Iwasawa R, Noguchi H, Aoki M, Doi T: Safety, pharmacokinetic, and pharmacodynamics of erdafitinib, a pan-fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor, in patients with advanced or refractory solid tumors. Invest New Drugs. 2018 Jun;36(3):424-434. doi: 10.1007/s10637-017-0514-4. Epub 2017 Sep 30. [Article]
- Tabernero J, Bahleda R, Dienstmann R, Infante JR, Mita A, Italiano A, Calvo E, Moreno V, Adamo B, Gazzah A, Zhong B, Platero SJ, Smit JW, Stuyckens K, Chatterjee-Kishore M, Rodon J, Peddareddigari V, Luo FR, Soria JC: Phase I Dose-Escalation Study of JNJ-42756493, an Oral Pan-Fibroblast Growth Factor Receptor Inhibitor, in Patients With Advanced Solid Tumors. J Clin Oncol. 2015 Oct 20;33(30):3401-8. doi: 10.1200/JCO.2014.60.7341. Epub 2015 Aug 31. [Article]
- Erdafitinib FDA Label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Protein homodimerization activity
- Specific Function
- Tyrosine-protein kinase that acts as cell-surface receptor for CSF1 and IL34 and plays an essential role in the regulation of survival, proliferation and differentiation of hematopoietic precursor ...
- Gene Name
- CSF1R
- Uniprot ID
- P07333
- Uniprot Name
- Macrophage colony-stimulating factor 1 receptor
- Molecular Weight
- 107982.955 Da
References
- Erdafitinib FDA Label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vascular endothelial growth factor-activated receptor activity
- Specific Function
- Tyrosine-protein kinase that acts as a cell-surface receptor for PDGFA, PDGFB and PDGFC and plays an essential role in the regulation of embryonic development, cell proliferation, survival and chem...
- Gene Name
- PDGFRA
- Uniprot ID
- P16234
- Uniprot Name
- Platelet-derived growth factor receptor alpha
- Molecular Weight
- 122668.46 Da
References
- Erdafitinib FDA Label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vascular endothelial growth factor binding
- Specific Function
- Tyrosine-protein kinase that acts as cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic...
- Gene Name
- PDGFRB
- Uniprot ID
- P09619
- Uniprot Name
- Platelet-derived growth factor receptor beta
- Molecular Weight
- 123966.895 Da
References
- Erdafitinib FDA Label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Transmembrane receptor protein tyrosine kinase activity
- Specific Function
- Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell main...
- Gene Name
- KIT
- Uniprot ID
- P10721
- Uniprot Name
- Mast/stem cell growth factor receptor Kit
- Molecular Weight
- 109863.655 Da
References
- Erdafitinib FDA Label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vascular endothelial growth factor-activated receptor activity
- Specific Function
- Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and ...
- Gene Name
- KDR
- Uniprot ID
- P35968
- Uniprot Name
- Vascular endothelial growth factor receptor 2
- Molecular Weight
- 151525.555 Da
References
- Erdafitinib FDA Label [File]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Erdafitinib FDA Label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitorInducer
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
Carriers
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- General Function
- Not Available
- Specific Function
- Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Components:
References
- FDA Approved Drug Products: BALVERSA® (erdafitinib) tablets, for oral use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Erdafitinib FDA Label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Quaternary ammonium group transmembrane transporter activity
- Specific Function
- Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
- Gene Name
- SLC22A2
- Uniprot ID
- O15244
- Uniprot Name
- Solute carrier family 22 member 2
- Molecular Weight
- 62579.99 Da
References
- Erdafitinib FDA Label [File]
Drug created at October 20, 2016 21:28 / Updated at December 03, 2023 06:20