Balversa

— THERAPEUTIC CATEGORIES —
  • Bladder, kidney, and other urologic cancers
PAGE CONTENTS
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  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Balversa Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Erdafitinib 3mg, 4mg, 5mg; tabs.

    Pharmacological Class

    Kinase inhibitor.

    How Supplied

    Tabs 3mg—56, 84; 4mg—28, 56; 5mg—28

    Storage

    Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].

    Manufacturer

    Janssen Pharmaceuticals, Inc.

    Generic Availability

    NO

    Mechanism of Action

    Erdafitinib is a kinase inhibitor that binds to and inhibits enzymatic activity of FGFR1, FGFR2, FGFR3 and FGFR4 based on in vitro data. Erdafitinib also binds to RET, CSF1R, PDGFRA, PDGFRB, FLT4, KIT, and VEGFR2. 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.

    Balversa Indications

    Indications

    Locally advanced or metastatic urothelial carcinoma in adults with susceptible FGFR3 genetic alterations whose disease has progressed on or after at least 1 line of prior systemic therapy.

    Limitations of Use

    Not recommended for patients who are eligible for and have not received prior PD-1 or PD-L1 inhibitor therapy.

    Balversa Dosage and Administration

    Adult

    Confirm presence of FGFR3 genetic alterations in tumor specimens. Swallow whole. Initially 8mg once daily; increase to 9mg once daily at 14–21 days if serum phosphate level <9.0mg/dL with no ocular disorders or Grade ≥2 adverse reactions. Continue until disease progression or unacceptable toxicity occurs. Dose modifications for adverse reactions: see full labeling.

    Children

    Not established.

    Balversa Contraindications

    Not Applicable

    Balversa Boxed Warnings

    Not Applicable

    Balversa Warnings/Precautions

    Warnings/Precautions

    Perform ophthalmic exam (include visual acuity, slit lamp, fundoscopy, optical coherence tomography) monthly for the first 4 months then every 3 months thereafter, and as needed. Monitor for hyperphosphatemia. Restrict phosphate intake to 600–800mg daily; if serum phosphate is >7.0mg/dL, consider adding oral phosphate binder until level returns to <7.0mg/dL. Withhold, reduce dose, or permanently discontinue based on duration and severity of hyperphosphatemia. CYP2C9 poor metabolizers: monitor. Embryo-fetal toxicity. Advise females of reproductive potential and males (w. female partners) to use effective contraception during and for 1 month after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 month after the last dose).

    Balversa Pharmacokinetics

    Absorption

    Median time to achieve peak plasma concentration (tmax) was 2.5 hours (range: 2–6 hours).

    Distribution

    Mean apparent volume of distribution: 29 L. Plasma protein bound: 99.7%, primarily to alpha-1-acid glycoprotein.

    Metabolism

    Primarily by CYP2C9, CYP3A4. 

    Elimination

    Following a single oral dose of radiolabeled erdafitinib, ~69% of the dose was recovered in feces (19% as unchanged) and 19% in urine (13% as unchanged). Half-life: 59 hours.

    Balversa Interactions

    Interactions

    Potentiated by moderate CYP2C9 or strong CYP3A4 inhibitors: consider alternatives; if unavoidable, monitor closely and adjust dose accordingly. May be antagonized by strong CYP3A4 inducers: avoid. May be antagonized by moderate CYP3A4 inducers: if use is necessary after initial dose increase period, increase to erdafitinib 9mg. Concomitant other serum phosphate level-altering agents may affect serum phosphate levels: avoid before initial dose increase period. May potentiate P-gp substrates; if use unavoidable, separate dosing by ≥6hrs before or after substrates.

    Balversa Adverse Reactions

    Adverse Reactions

    Phosphate increased, nail disorders, stomatitis, diarrhea, creatinine increased, ALT/AST increased, hemoglobin decreased, sodium decreased, alkaline phosphatase increased, fatigue, dry mouth, dry skin, phosphate decreased, decreased appetite, dysgeusia, constipation, calcium increased, dry eye, palmar-plantar erythrodysesthesia syndrome, potassium increased, alopecia; ocular disorders (eg, central serous retinopathy/retinal pigment epithelial detachment).

    Balversa Clinical Trials

    Clinical Trials

    The efficacy of erdafitinib was supported by data from cohort 1 of the phase 3 THOR study (ClinicalTrials.gov Identifier: NCT03390504), which compared erdafitinib to standard of care chemotherapy (investigator’s choice of docetaxel or vinflunine). Cohort 1 included 266 adults with advanced urothelial cancer harboring selected FGFR3 alterations. 

    All patients had disease progression after 1 or 2 prior treatments, at least 1 of which included a programmed death receptor 1 (PD-1) or programmed death-ligand 1 (PD-L1) inhibitor. The major efficacy endpoints were overall survival (OS), progression free survival (PFS) and objective response rate (ORR).

    Findings showed treatment with erdafitinib reduced the risk of death by 36% compared with chemotherapy (hazard ratio [HR], 0.64 [95% CI, 0.47-0.88]; P =.005). Median OS was 12.1 months in the erdafitinib arm vs 7.8 months in the chemotherapy arm. Median PFS was 5.6 months in the erdafitinib arm vs 2.7 months in the chemotherapy arm (HR, 0.58 [95% CI, 0.44-0.78; P =.0002). ORR was 35.3% (5.1% with complete response and 30.1% with partial response) with erdafitinib vs 8.5% (0.8% with complete response and 7.7% with partial response) with chemotherapy.

    Balversa Note

    Not Applicable

    Balversa Patient Counseling

    See Literature

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