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

1、 Drug name

1. Common name: Pemigatinib

2. Product Name: PEMAZYRE ™

2、 Indications

Suitable for treating adult patients with unresectable locally advanced or metastatic cholangiocarcinoma who have received previous treatment and require FDA approved testing to confirm the presence of fibroblast growth factor receptor 2 (FGFR2) fusion or other rearrangements.

3、 Specifications and characteristics

4.5mg tablets.

4、 Main components

1. Active ingredient: Pembatinib (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 [4,3d] pyrimidin-2-one).

2. Accessories: magnesium stearate, microcrystalline cellulose, starch sodium hydroxide.

5、 Usage and dosage

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

2. Usage: Swallow the whole tablet, it can be taken with food or on an empty stomach.

3. Omission or vomiting treatment: If the missed dose exceeds 4 hours or vomiting occurs after taking the medication, skip the dose and follow the original plan for the next dose.

6、 Dose adjustment

1. Adverse reaction adjustment:

The first dose is reduced to 9mg/day, and the second dose is reduced to 4.5mg/day. If it is still intolerable, the medication will be permanently discontinued.

If the serum phosphate level is greater than 7mg/dL, medication should be suspended and phosphate lowering therapy should be initiated; Retinopathy requires dosage adjustment or discontinuation based on symptoms.

2. Drug interactions:

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

7、 Medication precautions

1. Eye toxicity: Ophthalmic examination (including OCT) should be performed before treatment, every 2 months during the treatment period (first 6 months), and every 3 months thereafter. If symptoms such as blurred vision and floaters appear, seek medical attention immediately.

2. Hyperphosphatemia: Monitor blood phosphorus levels. A low phosphorus diet is required for levels>5.5mg/dL, and medication intervention is necessary for levels>7mg/dL.

3. Embryotoxicity: Patients of childbearing age should take effective contraceptive measures (during treatment and 1 week after discontinuation).

4. Breastfeeding period: Breastfeeding is prohibited during the treatment period and within one week after discontinuation of medication.

8、 Medication for special populations

1. Liver/kidney dysfunction: No dose adjustment is required for mild to moderate cases, and the safety of medication for severe patients has not been established.

2. Elderly patients: There is no need to adjust the dosage for individuals aged 65 and above.

3. Children: Safety and efficacy have not been established.

9、 Adverse reactions

1. Common (≥ 20%): including hyperphosphatemia, hair loss, diarrhea, nail toxicity, fatigue, taste disorders, nausea, constipation, stomatitis, dry eyes, dry mouth, decreased appetite, etc;

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

10、 Contraindications

There are no clear contraindications.

11、 Drug interactions

1. CYP3A inducers (such as rifampicin): Avoid combination therapy as it may reduce efficacy.

2. CYP3A inhibitors (such as itraconazole): Need to reduce the dose of pemotinib.

3. Avoid grapefruit products: may increase drug exposure.

12、 Storage method

Store at room temperature of 20 ° C-25 ° C, allow short-term fluctuations of 15 ° C-30 ° C, avoid light and moisture.

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