Must-read for patients: Overview of basic information in the Chinese instructions for pemetinib/pemetinib

1. Name: pemigatinib, pemigatinib, dabotan, PEMAZYRE, dabotan

Product aliases: pemetinib, pemigatinib, pemetinib, pemetinib

2. Who can take pemetinib? Indications?

1. Cholangiocarcinoma (CCA):Pemetinib/Pemetinib

2. Myeloid/lymphoid neoplasm (MLN) with FGFR1 rearrangement:PemetinibIt is suitable for the treatment of adult patients with relapsed or refractory bone marrow/lymphoid tumors associated with fibroblast growth factor receptor 1 (FGFR1) rearrangement.

3.PemetinibWhat are the side effects?

The most common side effects of pemetinib are high or low phosphate levels in the blood, hair loss, diarrhea, nail problems, fatigue, nausea, dysgeusia, stomatitis (inflammation of the mucous membranes in the mouth), constipation, joint pain, dry mouth, dry eyes and skin, rash and numbness on the palms and soles of the feet, low sodium levels in the blood, and high levels of creatinine in the blood, which may indicate kidney problems.

For patients with cholangiocarcinoma (For patients with CCA), the recommended dose is 13.5 mg orally once daily for 14 days, followed by 7 days off treatment in a 21-day cycle; for patients with FGFR1-rearranged myeloid/lymphoid neoplasms, the recommended dose is 13.5 mg orally once daily, with continued treatment until disease progression or unacceptable toxicity.

Patients shouldtake it at approximately the same time every daypemetinib, swallow the tablet whole with or without food. Do not crush, chew, split or dissolve tablets. If the patient misses a dose of pemaziram by 4 hours or more or experiences vomiting, continue with the next scheduled dose.

5.PemitinibHow to store?

Store at room temperature20°C to 25°C (68°F to 77°F)PemetinibTablet; allowed15°C to 30°C (59°F to 86°F) excursion.

6.How does pemetinib work?

Pemetinib is a small molecule kinase inhibitor targeting FGFR1, 2 and 3 with IC50 value less than 2nM. Pemetinib inhibits FGFR1-3 phosphorylation and signaling in cancer cell lines by activating FGFR amplification and fusion and reduces cell viability, resulting in constitutive activation of FGFR signaling. Constitutive FGFR signaling can support the proliferation and survival of malignant cells.

pemetinibAlternations inFGFR1, 2, and 3 result in mouse xenografts of human tumors with constitutive FGFR activation Antitumor activity was demonstrated in models including a patient-derived cholangiocarcinoma xenograft model expressing oncogenic FGFR2-transformant-2β homolog (TRA2b) fusion protein and a KG1 leukemia model harboring an FGFR1 translocation (FGFR1OP2-FGFR1).