The efficacy and side effects of pemetinib/pemetinib instructions

Pemigatinib/Pemigatinib received accelerated approval for the treatment of adult patients with unresectable locally advanced or metastatic cholangiocarcinoma who have previously received fibroblast growth factor receptor 2 fusion therapy. The recommended dose of pemetinib is 13.5 mg once daily for 14 days, followed by 7 days off treatment in a 21-day cycle, with treatment continued until disease progression or unacceptable toxicity.

Pemetinib is a small molecule kinase inhibitor that targetsFGFR1, FGFR2, and FGRF3; it also inhibits FGFR4 at concentrations approximately 100-fold higher than those that inhibit FGFR1, 2, and 3. Pemetinib inhibits FGFR1-3 phosphorylation and signaling in cancer cell lines and reduces cell viability by activating FGFR amplification and fusion, resulting in constitutive activation of FGFR signaling.

ConstitutiveFGFR signaling can support the proliferation and survival of malignant cells. Pemetinib demonstrated antitumor activity in mouse xenograft models of human tumors with alterations in FGFR1, FGFR2, or FGFR3 resulting in constitutive FGFR activation, including a cholangiocarcinoma patient-derived xenograft model expressing an oncogenic FGFR2 transformant-2β homolog fusion protein.

The most common adverse events of any grade were hyperphosphatemia, alopecia, diarrhea, nail toxicity, fatigue, dysgeusia, nausea, constipation, stomatitis, dry eyes, and dry mouth; other adverse events included vomiting, arthralgia, abdominal pain, hypophosphatemia, back pain, and dry skin; the most common grade 3 or 4 laboratory abnormalities were decreased phosphate and sodium levels and increased alkaline phosphatase and urate levels.

Pemetinib has warnings about retinal pigment epithelial detachment, hyperphosphatemia and embryotoxicity/Precautions. During the first 6 months of treatment and every 3 months thereafter, patients should undergo an eye examination, including optical coherence tomography, every 2 months before the start of treatment. Additionally, patients should be examined immediately as soon as visual symptoms occur.