BIGBEAR PEMIDX Pemigatinib Tablets 4.5mg

I. Drug Name

Generic Name: Pemigatinib Tablets

English Name: Pemigatinib Tablets

Brand Names: PEMAZYRE, Dabotan, PEMIDX

Dosage Form: Oral Tablets

Specification: 4.5 mg per tablet; 28 tablets per box

Target: FGFR1/2/3 kinase inhibitor (IC50 < 2 nM), with weaker inhibition of FGFR4

Manufacturer: BigBear Pharmaceutical Co., Ltd. (Laos)

Approval Number (Laos National Drug Administration): 10 L 1023/23

II. Indications and Usage

This product is a selective fibroblast growth factor receptor (FGFR) inhibitor indicated for the treatment of:

1.  Cholangiocarcinoma: For the treatment of adults with previously treated, unresectable locally advanced or metastatic cholangiocarcinoma harboring an FGFR2 fusion or rearrangement.

2.  Myeloid/Lymphoid Neoplasms: For the treatment of adults with relapsed or refractory myeloid/lymphoid neoplasms with FGFR1 rearrangement.

Key Prerequisite: The presence of the corresponding FGFR gene alteration must be confirmed using an approved test method prior to use.

III. Dosage and Administration

Recommended Dosage:

"Two Weeks On, One Week Off" Schedule: 13.5 mg orally once daily on Days 1 through 14 of each 21-day cycle. No drug administration on Days 15 through 21.

Continuous Dosing Schedule (for specific situations or following adjustment): 13.5 mg orally once daily, taken continuously until disease progression or unacceptable toxicity occurs.

Administration Method: May be taken with or without food. Tablets should be swallowed whole; do not crush, chew, or dissolve. If a dose is missed or vomiting occurs, do not take a replacement dose; simply resume the schedule with the next planned dose.

Dosage Adjustment: Detailed dosage adjustment guidelines are provided for hyperphosphatemia, ocular toxicity, and other adverse reactions (involving sequential dose reductions to 9 mg or 4.5 mg, or temporary/permanent discontinuation). IV. Contraindications

Patients with severe hypersensitivity to Pemigatinib tablets or to any of the excipients.

V. Warnings and Precautions

1. Ocular Toxicity: The most common manifestations are central serous retinopathy/retinal pigment epithelial detachment. Patients should undergo a comprehensive ophthalmologic examination, including Optical Coherence Tomography (OCT), prior to treatment, at 1 month after initiating treatment, every 3 months thereafter, and at any time visual symptoms occur. For Grade 2 or higher retinopathy, treatment should be suspended and resumed at a reduced dose upon recovery; for Grade 4 retinopathy, treatment should be permanently discontinued.

2. Hyperphosphatemia and Soft Tissue Mineralization: Hyperphosphatemia is a pharmacodynamic effect with an incidence of >90%. Serum phosphate levels should be monitored regularly. For persistent or recurrent Grade 2 (>5.5–7.0 mg/dL) or higher hyperphosphatemia, phosphate-lowering therapy (e.g., phosphate binders) should be initiated, and dose adjustments should be made based on serum phosphate levels and the severity of mineralization-related adverse reactions.

3. Embryo-Fetal Toxicity: May cause fetal harm. Patients of reproductive potential should use effective contraception.

VI. Adverse Reactions

Based on clinical trial data, common adverse reactions (incidence ≥20%) include:

Hyperphosphatemia (incidence >90%), nail toxicity, alopecia, diarrhea, fatigue, nausea, constipation, stomatitis, abdominal pain, dry mouth, dry skin, decreased appetite, vomiting, arthralgia, dysgeusia, and back pain.

Laboratory Abnormalities: Increased blood creatinine, increased blood phosphate, decreased blood calcium, decreased blood sodium, increased alkaline phosphatase, and lymphopenia.

VII. Drug Interactions

Strong CYP3A4 Inducers (e.g., rifampin, phenytoin, carbamazepine, St. John's wort): These agents significantly decrease the plasma concentration of Pemigatinib tablets, potentially compromising efficacy; therefore, co-administration should be avoided. Potent CYP3A4 Inhibitors (e.g., Itraconazole, Clarithromycin): May increase plasma concentrations of Pemigatinib tablets, thereby increasing the risk of adverse reactions. When co-administered, consider reducing the dosage of Pemigatinib tablets to 9 mg once daily (intermittent regimen).

VIII. Use in Specific Populations

Hepatic Impairment: No dose adjustment is required for mild hepatic impairment. For patients with moderate hepatic impairment, the recommended dosage is 9 mg once daily (intermittent regimen). Use is not recommended for patients with severe hepatic impairment.

Renal Impairment: No dose adjustment is required for mild to moderate renal impairment. For patients with severe renal impairment or End-Stage Renal Disease (CLcr < 30 mL/min), the recommended dosage is 9 mg once daily (intermittent regimen).

Pediatric Use: Safety and efficacy have not been established.

Geriatric Use: No specific adjustment to the starting dose is required.

IX. Pharmacological Actions

Pharmacological Class: Selective FGFR1, 2, and 3 tyrosine kinase inhibitor.

Mechanism of Action: Pemigatinib tablets inhibit the proliferation, survival, and migration of tumor cells harboring FGFR gene alterations by selectively inhibiting the activity of FGFR1-3 and blocking downstream signaling pathways.

X. Storage

Store at room temperature (20°C–25°C); excursions are permitted between 15°C and 30°C during short-term transport.

Keep the medication in its original packaging to protect it from moisture.

Keep out of reach of children.

Important Note:

This package insert does not substitute for professional medical advice. Before using Pemigatinib tablets, patients must undergo a comprehensive assessment by a specialist physician and strictly adhere to the detailed medication instructions provided by their doctor and pharmacist. FGFR gene testing must be performed prior to initiating treatment. During treatment, regular ophthalmological examinations, serum phosphate monitoring, and adverse reaction management are mandatory.