erdafitinib
Other Names
Balversa®
Appearance
tablet
Funding Program
Exceptional Access Program
- erdafitinib - For the treatment of locally advanced unresectable or metastatic urothelial carcinoma, according to specific criteria
B - Mechanism of Action and Pharmacokinetics
Erdafitinib is a tyrosine kinase inhibitor of fibroblast growth factor receptor (FGFR) 1, 2, 3 and 4. By inhibiting FGFR phosphorylation and signaling, erdafitinib decreases cell viability in cancer cell lines with activating FGFR genetic alterations, including point mutations, amplifications, and fusions. Erdafitnib exhibited antitumor activity in multiple FGFR-driven cell lines and tumor models.
Absorption
| Peak plasma levels | 2.5 hours (range 2-6 hours) |
| Time to reach steady state | 2 weeks |
| Effects with food | Clinically significant changes in Cmax and AUC were not observed following a high-fat meal, although Tmax was delayed by ~2 hours with food. |
Distribution
| PPB | 99.7%, mainly to α1-acid glycoprotein AGP |
Metabolism
Erdafitinib is primarily metabolized in human by CYP2C9 and CYP3A4 (39% and 20% of total clearance).
| Active metabolites | No |
| Inactive metabolites | Yes |
Elimination
| Half-life | ~59 hours (effective) |
| Feces | 69% (14-21% unchanged) |
| Urine | 19% (13% unchanged) |
C - Indications and Status
Health Canada Approvals:
- Urothelial carcinoma (UC)
Refer to the product monograph for a full list and details of approved indications.
D - Adverse Effects
The following table lists adverse effects that occurred in ≥10 of patients treated with erdafitinib vs chemotherapy (docetaxel or vinflunine) in a phase III study. It also includes severe, life-threatening and post-marketing adverse effects from other sources.
| ORGAN SITE | SIDE EFFECT* (%) | ONSET** | |||
|---|---|---|---|---|---|
| Dermatological | Alopecia (25%) | E | |||
| Dry skin , rash (27%) | E | ||||
| Nail disorder (70%) (12% severe) | E | ||||
| Palmar-plantar erythrodysesthesia syndrome (PPES) (30%) (10% severe) | E | ||||
| Gastrointestinal | Anorexia, weight loss (27%) (3% severe) | E | |||
| Constipation (27%) | E | ||||
| Diarrhea (63%) (3% severe) | E | ||||
| Dry mouth (39%) | E | ||||
| GI obstruction (3%) | E | ||||
| Mucositis (56%) (10% severe) | E | ||||
| Nausea (15%) | E | ||||
| General | Fatigue (29%) | E | |||
| Hematological | Anemia (26%) (7% severe) | E | |||
| Hepatobiliary | ↑ LFTs (27%) (3% severe) | E | |||
| Metabolic / Endocrine | ↑ Ca (6%) | E | |||
| Hyperparathyroidism (3%) | D | ||||
| Hyperphosphatemia (80%) (5% severe) | E D L | ||||
| ↓ Na (12%) (7% severe) | E | ||||
| Musculoskeletal | Musculoskeletal pain (10%) | E | |||
| Nervous System | Dysgeusia (30%) | E | |||
| Ophthalmic | Conjunctivitis (<10%) | E | |||
| Dry eye (25%) (<1% severe) | E | ||||
| Keratitis (<10%) | E | ||||
| Retinopathy (%) (Central serous retinopathy 18%) (2% severe), retinal pigment epithelial detachment (RPED) | E | ||||
| Renal | Acute kidney injury (2%) | E | |||
| Creatinine increased (14%) | E | ||||
| Respiratory | Epistaxis (13%) | E | |||
| Urinary | Hematuria (12%) (2% severe) | E | |||
| Vascular | Other (%) - Vascular calcification (<1%) | D | |||
* "Incidence" may refer to an absolute value or the higher value from a reported range.
"Rare" may refer to events with < 1% incidence, reported in post-marketing, phase 1 studies,
isolated data or anecdotal reports.
** I = immediate (onset in hours to days) E = early (days to weeks)
D = delayed (weeks to months) L = late (months to years)
The most common side effects for erdafitinib include hyperphosphatemia, nail disorder, diarrhea, mucositis, dry mouth, dysgeusia, palmar-plantar erythrodysesthesia syndrome (ppes), fatigue, ↑ LFTs, anorexia/weight loss.
Erdafitinib use is associated with hyperphosphatemia, which can lead to soft tissue mineralization, cutaneous calcinosis, non-uremic calciphylaxis, pruritus, hypocalcemia, anemia, secondary hyperparathyroidism, muscle cramps, seizures, QT interval prolongation, arrhythmias and vascular calcification. Restrict phosphate intake to 600 - 800 mg daily for all patients. About 25% of patients received phosphate binders during erdafitinib treatment.
Eye disorders were reported in patients treated with erdafitinib, including central serous retinopathy (CSR)/ retinal pigment epithelial detachment (RPED) that affect vision. Other SCR events included chorioretinopathy, detachment of retinal pigment epithelium (RPE), retinal detachment, retinopathy and subretinal fluid detachment, etc.
E - Dosing
Refer to protocol by which the patient is being treated.
Screen for hepatitis B virus in all cancer patients starting systemic treatment. Refer to the hepatitis B virus screening and management guideline.
A susceptible FGFR3 gene alteration should be confirmed by a validated test prior to starting erdafitinib. Refer to the product monograph for details on specific genetic alterations.
Phosphate intake should be restricted to 600-800 mg daily for all patients.
To prevent and treat drug eyes, use artificial tears, hydrating or lubricating eye gels or ointments frequently, at least q2h during waking hours. Refer patients to an optometrist or ophthalmologist for severe treatment-related dry eyes.
Adults:
Oral: 8 mg Daily
*May increase to 9 mg daily based tolerability and serum phosphate levels (<2.91 mmol/L) and after 14-21 days. (Refer to the Dosage with Toxicity section below if phosphate level >/= 2.91 mmol/L.) Avoid co-administration of serum phosphate level-altering agents with erdafitinib before the initial dose increase period based on serum phosphate levels. After day 21, do not use serum phosphate to guide further dose increases.
Dosage with Toxicity:
| Dose level | Erdafitinib dose (mg daily) | |
| 0 | 9 | 8 |
| -1 | 8 | 6 |
| -2 | 6 | 5 |
| -3 | 5 | 4 |
| -4 | 4 | Discontinue |
| -5 | Discontinue | |
| Toxicity | Severity/ Grade | Action |
| Hyperphosphatemia | 2.25 - 2.90 mmol/L | Continue at same dose. Initiate phosphate binder^ with food.* Reduce dose 1 level ↓ if not improved in 2 months or as clinically indicated. |
| 2.91 - 3.20 mmol/L | Hold and initiate phosphate binder^ with food.* Restart at same dose. |
|
| >3.20 mmol/L | Hold* and manage appropriately. Restart at 1 dose level ↓. |
|
| Significant alteration from baseline renal function or Grade 3 hypocalcemia due to hyperphosphatemia | Discontinue. | |
| Ocular disorders, including central serous retinopathy/retinal pigment epithelial detachment (CSR/RPED) | Grade 1: Asymptomatic or mild symptoms; clinical or diagnostic observations only, or abnormal Amsler grid test. |
Refer for an ophthalmologic examination (OE). Continue† at same dose if no evidence of eye toxicity. Keratitis or retinal abnormality: Consider dose re-escalation if no recurrence. |
| Grade 2: Moderate; limiting age appropriate instrumental activities of daily living (ADL). |
Hold and refer for an OE. Restart† at 1 dose level ↓ once resolved. Keratitis or retinal abnormality: |
|
| Grade 3: Severe or medically significant but not immediate sight-threatening; limiting self-care ADL. |
Hold until resolved. Restart† at 1 dose level ↓ if completely resolved and asymptomatic within 4 weeks. Recurrence: Consider discontinuation. |
|
| Grade 4: Sight-threatening consequences; blindness (20/200 or worse). |
Discontinue. |
|
| Nail Disorder | Grade 2 | Consider holding# until ≤Grade 1 or baseline. If resolution in >2 weeks: Restart at 1 dose level ↓. Recurrence: Restart at 1 dose level ↓. |
| Grade 3 | Hold# until ≤Grade 1 or baseline. |
|
| Grade 4 | Discontinue. | |
| Dry Skin and Skin Toxicity | Grade 3 | Hold until ≤Grade 1 or baseline, for up to 28 days. Reassess weekly. Restart at 1 dose level ↓. |
| Grade 4 | Discontinue | |
| Oral Mucositis | Grade 2 | Consider holding if patient has other drug-related Grade 2 adverse events. Hold# until ≤ grade 1 or baseline, if symptoms persist for >1 week despite clinical management. If resolution in >2 weeks: Restart at 1 dose level ↓. Recurrence: Restart at 1 dose level ↓. |
| Grade 3 | Hold# until ≤Grade 1 or baseline. |
|
| Grade 4 | Discontinue. | |
| Dry Mouth | Grade 3 | Hold until ≤Grade 1 or baseline, for up to 28 days. Reassess weekly. Restart at 1 dose level ↓. |
| Grade 4 | Discontinue. | |
| Other Adverse Reactions | Grade 3 | Hold until ≤Grade 1 or baseline. Restart at 1 dose level ↓. |
| Grade 4 | Discontinue. |
^ Non-calcium containing phosphate binder (e.g., sevelamer carbonate)
* Until phosphate level <2.25 mmol/L.
† Upon restarting erdafitinib, continue to monitor for recurrence every 1-2 weeks for a month.
# With reassessment in 1-2 weeks.
Dosage with Hepatic Impairment:
| Hepatic Impairment | Erdafitinib Dose |
| Mild (Child-Pugh A) |
No dose adjustment recommended. |
| Moderate (Child-Pugh B) |
|
Severe |
Limited data. Use with caution and monitor closely for adverse reactions. |
Dosage with Renal Impairment:
| Creatinine Clearance* | Erdafitinib Dose |
| ≥30 | No dose adjustment recommended. |
| <30 | Limited data. Use with caution and monitor closely for adverse reactions. |
*Reported as eGFR (mL/min/1.73 m2)
Dosage in the elderly:
No dose adjustment is recommended. Patients aged ≥ 65 years old experienced a higher incidence of adverse reactions requiring treatment interruption or discontinuation compared to younger patients. No overall differences in efficacy was observed.
Dosage based on gender:
No clinically meaningful differences in the pharmacokinetics of erdafitinib were observed based on gender.
Dosage based on ethnicity:
No clinically meaningful differences in the pharmacokinetics of erdafitinib were observed based race/ ethnicity (white, Hispanic or Asian patients).
Children:
No data is available for pediatric use. Bone and teeth toxicities were observed in animal studies.
F - Administration Guidelines
- Administer erdafitinib with or without food.
- Swallow tablets whole.
- If a dose is missed, administer the dose as soon as possible. Resume regular daily dose schedule the next day. Do not give extra tablets to make up for the missed dose.
- Do not administer a replacement dose if a dose is vomited. The next regular daily dose should be given on the next day.
- Store at room temperature (15ºC - 30ºC).
G - Special Precautions
Contraindications:
Other Drug Properties:
- Patients who have a hypersensitivity to this drug or any of its components
- Patients enrolled in Study BLC3001 had confirmation of at least one of the following:
- Mutations: FGFR3-S249C, FGFR3-Y373C, FGFR3-R248C, FGFR3-G370C
- Fusions: FGFR3-TACC3, FGFR3-BAIAP2L1
- Erdafitinib exposure may be increased in patients who are CYP2C9 poor metabolizer (CYP2C9 *3/*3 genotype), monitor these patients for increased adverse reactions.
- Eye disorders have been reported with erdafitinib treatment. Patients should not drive or use machinery until the effect subsides.
Other Drug Properties:
- Carcinogenicity: No information available
- Mutagenicity: No
- Genotoxicity: No
- Embryotoxicity: Documented in animals
- Fetotoxicity: Documented in animals
- Teratogenicity: Documented in animals
- Pregnancy:
- Erdafitinib is not recommended for use in pregnancy. Adequate contraception should be used by patients and their partners during treatment, and for 1 month after the last dose.
Patients should not donate or store sperm during treatment and for 1 month after the last dose.
- Breastfeeding:
Breastfeeding is not recommended during treatment and for 1 month after the last dose.
- Fertility effects:
Documented in studies with female animals.
H - Interactions
Erdafitinib is primarily metabolized by CYP2C9 and CYP3A4.
Erdafitinib is an inhibitor and inducer of CYP3A4, and an inhibitor of OCT2 and P-gp in vitro (clinical significance is not established).
No clinically meaningful differences in erdafitinib pharmacokinetics were observed in patients taking sevelamer.[
Erdafitinib is a substrate for P-gp, but P-gp inhibitors are not expected to have a clinically meaningful effect on the pharmacokinetics of erdafitinib.
| AGENT | EFFECT | MECHANISM | MANAGEMENT |
|---|---|---|---|
| Medications that increase phosphate levels (i.e. potassium phosphate supplements, vitamin D supplements, antacids, and phosphate-containing enemas and laxatives) | ↑ risk of hyperphosphatemia | Additive effect | Avoid coadministration. |
| Combined CYP2C9 and strong CYP3A4 inducers (i.e. rifampin, carbamazepine) | ↓ erdafitinib concentration and/or efficacy (e.g. carbamazepine ↓ erdafitinib exposure by 45%) | ↑ metabolism of erdafitinib | Avoid coadministration. If must co-administer, consider increasing dose up to 9 mg based on serum phosphate and drug-related toxicities. Dose may be adjusted once inducer is discontinued. |
| CYP2C9 inducers (i.e. aprepitant) | ↓ erdafitinib concentration and/or efficacy | ↑ metabolism of erdafitinib | Avoid coadministration. If must co-administer, consider increasing dose up to 9 mg based on serum phosphate and drug-related toxicities. Dose may be adjusted once inducer is discontinued. |
| CYP3A4 inducers (i.e. phenytoin, dexamethasone) | ↓ erdafitinib concentration and/or efficacy | ↑ metabolism of erdafitinib | Avoid coadministration. If must co-administer, consider increasing dose up to 9 mg based on serum phosphate and drug-related toxicities. Dose may be adjusted once inducer is discontinued. |
| Strong CYP3A4 inhibitors (i.e. fluconazole, ketoconazole, itraconazole clarithromycin, ritonavir) | ↑ erdafitinib concentration and/or toxicity (e.g. itraconazole ↑ erdafitinib exposure by 134%) | ↓ metabolism of erdafitinib | Avoid coadministration. If must co-administer, monitor closely for adverse reactions. If the inhibitor is discontinued, erdafitinib dose may be adjusted in the absence of drug-related toxicity. |
| Moderate CYP2C9 inhibitors (i.e. fluconazole) | ↑ erdafitinib concentration and/or toxicity (e.g. fluconazole ↑ erdafitinib exposure by 148%) | ↓ metabolism of erdafitinib | Avoid coadministration. If must co-administer, monitor closely for adverse reactions. If the inhibitor is discontinued, erdafitinib dose may be adjusted in the absence of drug-related toxicity. |
| P-glycoprotein substrates (i.e. verapamil, digoxin, morphine, ondansetron) | ↑ concentration and/or toxicity of P-gp substrates | Erdafitinib is a substrate and inhibitor of P-gp | P-gp substrates with narrow therapeutic index should be taken at least 6 hours before or after erdafitinib. |
I - Recommended Clinical Monitoring
Treating physicians may decide to monitor more or less frequently for individual patients but should always consider recommendations from the product monograph.
Screen for hepatitis B virus in all cancer patients starting systemic treatment. Refer to the hepatitis B virus screening and management guideline.
Recommended Clinical Monitoring
| Monitor Type | Monitor Frequency |
|---|---|
Liver function tests |
Baseline, at each visit, and as clinically indicated |
Renal function tests |
Baseline, at each visit, and as clinically indicated |
CBC |
Baseline, at each visit, and as clinically indicated |
Serum phosphate |
Baseline, day 14 to 21 after treatment initiation, and monthly thereafter |
Ophthalmological exam* |
Baseline, monthly for the first 4 months, and every 3 months afterwards, and as clinically indicated (Instruct patients to self-administer the Amsler grid test between visits) |
Clinical toxicity assessment for hyperphosphatemia, nail disorder, diarrhea, mucositis, dry mouth, dysgeusia, palmar-plantar erythrodysesthesia syndrome (PPES), fatigue, ↑ LFTs, anorexia/weight loss. |
Baseline and as clinically indicated |
*including an Amsler grid test, fundoscopy, visual acuity and, if available, an optical coherence tomography (OCT)
Grade toxicity using the current NCI-CTCAE (Common Terminology Criteria for Adverse Events) version
J - Supplementary Public Funding
Exceptional Access Program (EAP Website )
- erdafitinib - For the treatment of locally advanced unresectable or metastatic urothelial carcinoma, according to specific criteria
K - References
Loriot Y, Necchi A, Park SH, et al. Erdafitinib in locally advanced or metastatic urothelial carcinoma. N Engl J Med 2019;381(4):338-48. doi: 10.1056/NEJMoa1817323
Prescribing Information: Balversa® (erdafitinib). Janssen Products, LP. October 2024.
Product Monograph: Balversa® (erdafitinib). Janssen Inc. December 18, 2025.
September 2026 new drug monograph
L - Disclaimer
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Last Updated: September 24, 2026
