Erdafitinib 5 mg is indicated for the treatment of adult patients with locally advanced or metastatic urothelial carcinoma

Erdafitinib Instructions

Product Name: LuciErda

Manufacturer: Lucius Pharmaceuticals

Chinese name: Erdafitinib

English name: Erdafitinib

Drug approval number: 02 L 1069/24

 

 

【Summary】

Erdafitinib is a kinase inhibitor that binds to and inhibits the 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 inhibits FGFR phosphorylation and signaling and reduces cell viability in cell lines expressing FGFR genetic alterations, including point mutations, amplifications, and fusions. Erdafitinib has demonstrated antitumor activity in cell lines and xenograft models expressing FGFR derived from tumor types, including bladder cancer.

 

【Indications】

Indicated for the treatment of adult patients with locally advanced or metastatic urothelial carcinoma

 

【Specification】

5mg/tablet, 28 tablets/bottle.

 

【Storage】

Store at 20°C to 25°C (68°C to 77°F); short-distance transport is permitted at a temperature range of 15 to 30°C (59–86°F).

 

【Usage and Dosage】

The starting dose is 8 mg once daily, taken orally on an empty stomach or with food. For patients whose serum phosphorus levels are below the target value of 5.5 mg/dL between days 14 and 21, the dose is increased to 9 mg once daily until disease progression or intolerance.

If you vomit after taking the medicine, you cannot make up for it. You should take the next dose according to the original interval. If you miss a dose, you can make up for it on the same day. You should take the next dose according to the original interval.

 

【Adverse Reactions】

1. The most common adverse reactions (≥20%) are:

1) Hyperphosphatemia, stomatitis, fatigue, and elevated creatinine

2) Diarrhea, xerostomia, nail bed detachment, and elevated ALT

3) Increased alkaline phosphatase, hyponatremia, decreased appetite, and decreased albumin

4) Taste disturbance, decreased hemoglobin, dry skin, increased AST

5) Hypomagnesemia, dry eyes, hair loss, hand-foot syndrome

6) Constipation, hypophosphatemia, abdominal pain, hypercalcemia, nausea and skeletal muscle pain.

2. The most common (>1%) grade 3 or above adverse reactions are:

Stomatitis, nail dystrophy, hand-foot syndrome, paronychia, nail diseases, keratitis, onycholysis, and hyperphosphatemia.

 

【 Notes 】

1. Eye diseases: Erdafitinib can cause central serous retinopathy or retinal pigment epithelial detachment, with clinical symptoms of blurred vision, visual floaters or visual fatigue, with an incidence of 25% (3% for grade 3), a median onset of 50 days, 13% of patients were relieved, and 13% of patients still had the disease at the end of the clinical trial. 9% of patients therefore suspended Erdafitinib, 14% of patients reduced the dose, and 3% of patients permanently discontinued Erdafitinib.

2. The incidence of dry eyes is 28% (6% for grade 3). Use eye drops if necessary.

3. Perform an ophthalmological examination, including optical coherence tomography (OCT), before taking Erdafitinib, and check once a month in the first 4 months of medication, and once every 3 months after 4 months. If visual symptoms are found, see a doctor immediately and check every 3 weeks until the symptoms are relieved.

4. Hyperphosphatemia: 76% of patients had serum phosphate levels exceeding the upper limit of normal, with a median onset time of 20 days. 32% of patients required the use of phosphate-lowering drugs. If the patient's blood phosphorus level exceeds 5.5 mg/dL, adjust the drug dosage regimen according to Tables 1 and 2.

5. Embryo-fetal toxicity: Animal studies have shown that Erdafitinib has embryo-fetal toxicity. Patients and their partners should use effective contraceptive measures during medication and within one month of stopping medication.

【Efficacy and safety】

The BLC2001 study is a multicenter, open-label, single-arm phase II clinical trial. 87 patients with urothelial carcinoma were available for evaluation, with a median age of 67 years, 79% male, 74% white, 92% PS score of 0-1, and 66% of patients with metastatic lesions. 97% of patients had received at least 1 platinum-containing chemotherapy, and 3 patients had only received neoadjuvant chemotherapy or adjuvant chemotherapy. 24% of patients had received PD-1/L1 immunotherapy. The complete remission rate was 2.3%, the partial remission rate was 29.9%, the total effective rate was 32.2%, and the median effective duration was 5.4 months.

 

All patients enrolled carried at least one FGFR2/3 mutation or fusion, such as FGFR3 mutation (R248C, S249C, G370C and Y373C), FGFR2 fusion (FGFR2-BICC1 and FGFR2-CASP7) and FGFR3 fusion (FGFR3-TACC3 and FGFR3-BAIAP2L1). For FGFR3 mutation (n=64), the total response rate was 40.6%; for FGFR3 fusion (n=18), the total response rate was 11.1%; for FGFR2 fusion (n=6), the total response rate was 0%.

 

【Taboo】

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