Pemazyre (pemigatinib) is a targeted therapy 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.

Specifications and Properties of Pemazyre (Pemigatinib)

Dosage Form and Specifications

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

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

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

(4) 13.5mg: 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 between 20°C and 25°C (68°F and 77°F).

(2) Short-term storage between 15°C and 30°C (59°F and 86°F) is allowed.

Dosage and Administration of Pemazyre (Pemigatinib)

Standard Dosing Regimen

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

(2) Dosing cycle: Administer 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: 9mg per day (14 days of administration + 7-day drug holiday).

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

(3) Permanent discontinuation: If the 4.5mg dose is not tolerated, permanent discontinuation of the drug is required.

Dosage Adjustment for Drug Interactions

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

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

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

Important Precautions

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

(2) Management of missed dose: If a dose is missed by more than 4 hours, do not make up the dose; take the next dose as scheduled the next day.

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

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