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pemigatinib

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Pemigatinib is the first selective FGFR receptor tyrosine kinase inhibitor approved in China

1. Drug name

1. Generic name:Pemigatinib

2. Product Name: PEMAZYRE™

3. Specifications and properties

4.5mg tablets.

IV. Main ingredients

1. Active ingredient: Pemetinib (chemical name: 3-(2,6-difluoro-3,5-dimethoxyphenyl )-1-ethyl-8-(morpholin-4-ylmethyl)-1,3,4,7-tetrahydro-2H-pyrrolo[3',2':5,6]pyrido[4,3-d]pyrimidin-2-one).

2. Excipients: Magnesium stearate, microcrystalline cellulose, sodium starch glycolate.

V. Usage and Dosage

1. Conventional dosage of : 13.5 mg orally, once a day, taken continuously for 14 days and then stopped for 7 days, forming a 21-day cycle, until disease progression or intolerable toxicity occurs.

2. How to take : Swallow the whole tablet with food or on an empty stomach.

3. Treatment of missed dose or vomiting : If you miss a dose for more than 4 hours or vomit after taking the medicine, skip the dose and take the next dose as originally planned.

6. Dose adjustment

1. Adverse reaction adjustment :

Reduce the dose to 9mg/day for the first time and to 4.5mg/day for the second time. If it is still intolerable, discontinue the drug permanently.

Serum phosphate >7 mg/dL requires suspension of medication and initiation of phosphorus-lowering therapy; retinopathy requires dose adjustment or discontinuation of medication based on symptoms.

2. Drug interaction :

When used in combination with strong/moderate CYP3A inhibitors, the dose needs to be reduced from 13.5mg to 9mg or from 9mg to 4.5mg.

7. Medication Precautions

1. Ocular toxicity : Eye examination (including OCT) is required before treatment, every 2 months during treatment (first 6 months), and every 3 months thereafter. If symptoms such as blurred vision and floaters occur, seek medical attention immediately.

2. Hyperphosphatemia : Monitor blood phosphorus levels. A low-phosphorus diet is required when >5.5 mg/dL, and drug intervention is required when >7 mg/dL.

3. Embryotoxicity :Patients of childbearing age need to take effective contraceptive measures (during treatment and 1 week after stopping the drug).

4. Lactation : Breastfeeding is prohibited during treatment and within 1 week after stopping the drug.

8. Medication for special groups

1. Hepatic/renal insufficiency : No dose adjustment is required for mild to moderate patients, and the safety of medication for severe patients has not been established.

2. Elderly patients : There is no need to adjust the dose for people over 65 years old.

3. Children : The safety and effectiveness have not been established.

9. Adverse reactions

1. Common (≥20%): Including hyperphosphatemia, alopecia, diarrhea, nail toxicity, fatigue, dysgeusia, nausea, constipation, stomatitis, dry eyes, dry mouth, decreased appetite, etc.;

2. Serious adverse reactions: Including retinopathy, hyperphosphatemia-related complications and embryotoxicity.

10. Contraindications

No clear contraindications.

11. Drug interactions

1. CYP3A inducer (such as rifampicin): Avoid combined use, which may reduce drug efficacy.

2. CYP3A inhibitor (such as itraconazole): The dose of pemetinib needs to be reduced.

3. Avoid grapefruit product : May increase drug exposure.

12. Storage method

Stored at room temperature of 20°C-25°C, allowed to fluctuate between 15°C and 30°C for a short period of time, protected from light and moisture.