Pemazyre (pemigatinib) is a targeted therapeutic drug approved for marketing by the U.S. FDA in 2020. It belongs to the class of kinase inhibitors and is mainly used for the treatment of specific types of cholangiocarcinoma.

What is Pemazyre (Pemigatinib)?

Pemigatinib is a selective fibroblast growth factor receptor (FGFR) inhibitor that primarily targets FGFR1, FGFR2, and FGFR3. Its mechanism of action involves inhibiting the phosphorylation and signal transduction of FGFR1-3, thereby suppressing the proliferation and survival of tumor cells.

Dosage Forms, Specifications, and Properties of Pemazyre (Pemigatinib)

Dosage Forms and Specifications

(1) Film-coated tablets, available in three specifications:

(2) 4.5 mg: Round, white to off-white, engraved with "I" and "4.5" on one side.

(3) 9 mg: Oval, white to off-white, engraved with "I" and "9" on one side.

(4) 13.5 mg: Round, white to off-white, engraved with "I" and "13.5" on one side.

Composition

(1) Active ingredient: Pemigatinib (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 (non-animal source), microcrystalline cellulose, sodium starch glycolate.

Storage Conditions

(1) Store at room temperature of 20°C-25°C (68°F-77°F).

(2) Short-term storage at 15°C-30°C (59°F-86°F) is permitted.

Dosage and Administration of Pemazyre (Pemigatinib)

Standard Administration Regimen

(1) Recommended Dosage: 13.5 mg orally, once daily.

(2) Administration Cycle: Take continuously for 14 days, followed by a 7-day drug holiday, forming a complete 21-day treatment cycle.

(3) Administration Method: Swallow the tablet whole; do not chew, crush, or dissolve it.

(4) Administration Time: Take at approximately the same time each day, either with food or on an empty stomach.

Dosage Adjustment for Adverse Reactions

(1) First dose reduction: 9 mg/day (14 days of administration + 7-day drug holiday).

(2) Second dose reduction: 4.5 mg/day (14 days of administration + 7-day drug holiday).

(3) Permanent discontinuation is required if 4.5 mg cannot be tolerated.

Dosage Adjustment for Drug Interactions

(1) Strong or moderate CYP3A inhibitors: Concurrent use should be avoided; if co-administration is necessary, dosage reduction is required.

(2) Reduce the original dose of 13.5 mg to 9 mg.

(3) Reduce the original dose of 9 mg to 4.5 mg.

Important Precautions

(1) The presence of FGFR2 fusion or rearrangement must be confirmed before treatment initiation.

(2) Management of missed doses: If more than 4 hours have passed since the scheduled dose, do not make up for the missed dose; take the next dose as planned the following day.

(3) Management of vomiting: If vomiting occurs after taking the drug, do not make up for the dose.

(4) Regular monitoring of blood phosphorus levels and ophthalmic examinations are required during treatment.