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Common name: pemigatinib
Trade name: pemazyre
Domestic trade name: dabotan
Full names: pemetinib tablets, pemetinib, pemetinib, pemigatinib, pemazyre, dabotan
Indications:
Cholecarcinoma that has metastasized (spread to other parts of the body) or is locally advanced and cannot be treated with surgery.
For the treatment of adults with diseases involving FGFR2 gene fusions or other changes in the structure of the FGFR2 gene.
Usage and Dosage:
The recommended dose is 13.5mg orally administered daily for 14 days, followed by 7 days off within a 21-day cycle. Continue treatment until disease progression or unacceptable toxicity.
Swallow the tablets whole, with or without food.
Adverse reactions:
Diarrhea, nausea, change in taste, vomiting, loss of appetite, weight loss, constipation, stomach pain, aphtha, dry mouth and/or dry skin; decreased urine output; or rapid heartbeat.
Nail inflammation, hair loss, headache, fatigue, joint pain, painful urination, swelling and pain of limbs or joints.
Blurred vision, floaters in the eye, seeing flashes of light or other vision changes, muscle spasms, numbness, or dry mouth.
Contraindications:
None
Notes:
1.PEMAZYRE can cause retinal pigment epithelial detachment. Ophthalmological examinations, including optical coherence tomography (OCT), were performed before the start of treatment, every 2 months for the first 6 months of treatment and every 3 months thereafter, and at any time visual symptoms emerged urgently.
2. Hyperphosphatemia: Increased phosphate levels are the pharmacodynamic effect of PEMAZYRE. Monitor and prevent hyperphosphatemia, reduce dose, or permanently discontinue treatment based on duration and severity of hyperphosphatemia.
4. Embryo-fetal toxicity: Can cause fetal harm. Inform patients of the potential risk to the fetus of reproductive potential and to use effective contraception.
Storage:
Stored in a sealed container at room temperature, placed in a dry, cool place, out of reach of children.
Mechanism of action:
1. Pemigatinib is a small molecule kinase inhibitor targeting FGFR1, 2 and 3, with an IC50 value of less than 2nM.
2.Pemigatinib also inhibits FGFR4 in vitro at a concentration that is approximately 100 times higher than that of FGFR1, 2, and 3.
3.Pemigatinib leads to constitutive activation of FGFR by activating FGFR amplification and fusion, thereby inhibiting FGFR1-3 phosphorylation and signaling and reducing cell viability.
4. Constitutive FGFR signaling can support the proliferation and survival of malignant cells. Pemetinib exhibits antitumor activity in mouse xenograft models of human tumors with alterations in FGFR1, FGFR2, or FGFR3, resulting in constitutive FGFR activation, including cholangiocarcinoma xenograft models in patients expressing oncogenic FGFR2-Transformer-2 beta homolog (TRA2b) fusion proteins.