Adult: In patients with susceptible FGFR2 or FGFR3 genetic alteration that has progressed during or following at least 1 line of platinum-based chemotherapy, including within 12 months of neoadjuvant or adjuvant platinum-containing chemotherapy: 8 mg once daily, may increase to 9 mg once daily based on serum phosphate concentrations and tolerability at 14-21 days. Continued until disease progression or unacceptable toxicity occurs. Dose reduction, dosing interruption, or discontinuation may be required according to individual safety and tolerability (refer to detailed product guidelines).
Special Patient Group
Erdafitinib is metabolised by CYP3A4 and CYP2C9 isoenzymes. Simulation data presented in the prescribing information estimate no clinically meaningful differences in erdafitinib exposure in subjects with CYP2C9*2/*2 and *2/*3 genotypes but predict a 50% higher exposure in subjects with the CYP2C9*3/*3 genotype.
CYP2C9 poor metabolisers (CYP2C9 *3/*3 genotype)
Individuals with reduced CYP2C9 enzyme activity, known as CYP2C9 poor metabolisers, may experience increased erdafitinib exposure and increased risk of adverse reactions. Although no specific dosage adjustment is recommended, individuals with known or suspected CYP2C9*3/*3 genotype should be monitored for adverse reactions.
May be taken with or without food.
Pregnancy and lactation.
CYP2C9 poor metabolisers (with known or suspected CYP2C9*3/*3 genotype).
Significant: Central serous retinopathy, retinal pigment epithelial detachment, dry eye syndrome, hyperphosphataemia. Blood and lymphatic system disorders: Decreased haemoglobin, decreased platelet count, decreased white blood cell count. Gastrointestinal disorders: Stomatitis, diarrhoea, dry mouth, dysgeusia, constipation, abdominal pain, nausea, vomiting. General disorders and administration site conditions: Fatigue. Investigations: Increased creatinine, increased aminotransferase, increased alkaline phosphatase, decreased serum Na, decreased serum albumin, increased aspartate aminotransferase, decreased serum Mg, decreased serum phosphate, increased serum Ca, increased serum K, weight loss. Metabolism and nutrition disorders: Decreased appetite. Musculoskeletal and connective tissue disorders: Musculoskeletal pain, arthralgia. Skin and subcutaneous tissue disorders: Onycholysis, xeroderma, alopecia, palmar-plantar erythrodysesthesia syndrome, paronychia, nail discolouration.
Patient Counseling Information
Females of childbearing potential and males (with non-pregnant partner of childbearing potential) must use effective contraceptive methods during therapy and for at least 1 month after the last dose.
Confirm presence of FGFR mutation and pregnancy status (in females of childbearing potential) prior to initiation of therapy. Perform ophthalmological examination at baseline, monthly for 1st 4 months of treatment, then every 3 months thereafter and as clinically necessary. Monitor serum phosphate level at baseline, at 14-21 days after therapy initiation and then monthly or as clinically necessary. Monitor for increased adverse reactions in patients with known or suspected CYP2C9*3/*3 genotype.
Increased plasma concentration and increased risk of toxicity with potent CYP3A4 and CYP2C9 inhibitors (e.g. fluconazole, itraconazole). Decreased plasma concentration and reduced efficacy with potent CYP3A4 and CYP2C9 inducers (e.g. rifampicin). May increase plasma concentration and increase risk of toxicity of P-gp substrates (e.g. digoxin) and OCT2 substrate (e.g. metformin).
Description: Erdafitinib is a potent tyrosine kinase inhibitor. It binds to and inhibits fibroblast growth factor receptors (FGFR)-1, FGFR-2, FGFR-3, and FGFR-4 enzyme activity. Inhibition results in decreased of FGFR signalling and decreased in cell viability in cell lines expressing FGFR genetic alterations, including point mutations, amplifications, and fusions. Pharmacokinetics: Absorption: Time to peak plasma concentration: 2.5 hours (range: 2-6 hours). Distribution: Volume of distribution: 29 L. Plasma protein binding: 99.8%, primarily to α1-acid glycoproteins. Metabolism: Metabolised in the liver by CYP2C9 and CYP3A4 enzymes. Excretion: Via faeces (Approx 69%, [19%, as unchanged drug]); urine (19%, [13% as unchanged drug]). Elimination half-life: 59 hours.
Store between 20-25°C. Follow applicable procedures for receiving, handling, administration, and disposal.
L01EN01 - erdafitinib ; Belongs to the class of Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors. Used in the treatment of cancer.
Annotation of FDA Label for Erdafitinib and CYP2C9. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org. Accessed 01/07/2021.Annotation of FDA Label for Erdafitinib and FGFR2, FGFR3. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org. Accessed 20/07/2021.Anon. CYP2C9 - Erdafitinib (Pharmacogenomics). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 20/07/2021.Anon. Erdafitinib. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 20/07/2021.Anon. Erdafitinib. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 20/07/2021.Balversa Tablet, Film Coated (Janssen Products, LP). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 30/06/2021.Balversa Tablets, for Oral Use (Janssen Products, LP). U.S. FDA. https://www.fda.gov. Accessed 30/06/2021.Buckingham R (ed). Erdafitinib. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/06/2021.