Pemigatinib Cholangiocarcinoma that has metastasized (spread to other parts of the body) or is locally advanced and cannot be treated with surgery

Pemitinib instructions

Product Name: LuciPem         

Manufacturer: Lucius Pharmaceuticals

Chinese name: pemitinib

English Name: Pemigatinib

Drug approval number : 07 L 0997/23

 

 

【Summary】

Pemigatinib is a small molecule kinase inhibitor targeting FGFR1, 2, and 3 with an IC50 value of less than 2nM.

In vitro, concentrations that inhibit FGFR4 are approximately 100-fold higher than those that inhibit FGFR1, 2, and 3. Pemigatinib leads to constitutive FGFR activation by activating FGFR amplification and fusion, thereby inhibiting FGFR1-3 phosphorylation and signaling and reducing cell viability. Constitutive FGFR signaling can support the proliferation and survival of malignant cells. Pemigatinib exhibits antitumor activity in mouse xenograft models of human tumors with FGFR1, FGFR2, or FGFR3 alterations, leading to constitutive FGFR activation, including a cholangiocarcinoma xenograft model expressing a patient's oncogenic FGFR2-Transformer-2 beta homolog (TRA2b) fusion protein. 

 

【Indications】

Cholangiocarcinoma 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 disease that has FGFR2 gene fusions or other changes in the structure of the FGFR2 gene.

 

【Specification】  

4.5 mg/ tablet , 14 tablets / tablet .

 

【Storage】

 Store at 20 ° C to 25 ° C (68 ° C to 77 ° F) ; short-distance transportation is permitted within the temperature range of 15 to 30 ° C (59 – 86 ° F) .

 

【Usage and Dosage】

1. The recommended dose is 13.5 mg orally per day for 14 consecutive days, followed by 7 days of discontinuation within a 21-day cycle. Continue treatment until disease progression or unacceptable toxicity occurs.

2. Swallow the tablet whole, with or without food.

 

【Adverse Reactions】

1. Diarrhea, nausea, and taste changes

2. Vomiting, loss of appetite, weight loss

3. Constipation, stomachache, mouth ulcers

4. Dry mouth and/or skin; decreased urine output; or increased heart rate

5. Nail inflammation, hair loss, headache

6. Fatigue, joint pain, urinary pain, swelling and pain in the limbs or joints

7. Blurred vision, eye floaters, seeing flashes of light, or other changes in vision

8. Muscle cramps, numbness, or dry mouth

 

【 Taboo 】

none

 

【 Notes 】

1. Pemigatinib can cause retinal pigment epithelial detachment. Perform an ophthalmological examination, including optical coherence tomography (OCT), before the start of treatment, every 2 months for the first 6 months of treatment, and every 3 months thereafter, and urgently if visual symptoms occur at any time.

2. Hyperphosphatemia: Increased phosphate levels are a pharmacodynamic effect of Pemigatinib . Monitor and prevent hyperphosphatemia, reduce the dose or

3. Permanently discontinue treatment based on the duration and severity of hyperphosphatemia.

4. Embryo-fetal toxicity: Can cause fetal harm. Inform patients of reproductive potential of the potential risk to the fetus and use effective contraceptive methods.

 

Safety and efficacy

According to data from a study, the targeted drug pemigatinib for intrahepatic cholangiocarcinoma can achieve an objective response rate of 35.5% and a disease control rate of 82% in the treatment of cholangiocarcinoma patients. The median duration of response was 9.1 months, with up to 63% of patients having a response duration of greater than or equal to 6 months, and 18% of patients having a response duration of greater than or equal to 12 months. It is not difficult to see from these data that the targeted drug pemigatinib has a very significant effect on the control of the disease and improvement of the prognosis of intrahepatic cholangiocarcinoma. The advent of the targeted drug pemigatinib is a blessing for many patients with intrahepatic cholangiocarcinoma. The drug has changed the current treatment status of intrahepatic cholangiocarcinoma and provided doctors and patients with a new diagnosis and treatment plan.