Pemetinib/Dabotan drug detailed instructions

1. Generic names: Pemigatinib, Pemigatinib

Product name:Pemazyre, Dabotan

Other names: pemetinib, pemetinib

2. Indications:

1. Cholangiocarcinoma (CCA): Pemigatinib is approved for the treatment of unresectable locally advanced or metastatic cholangiocarcinoma. Patients with this cancer type must have received prior treatment and must have FGFR2 fusions or other FDA-approved rearrangements. The establishment of this indication has greatly enriched the treatment options for cholangiocarcinoma.

2. Myeloid/lymphoid neoplasms (MLNs) with FGFR1 rearrangements: In addition, pemetinib is also suitable for adult patients with relapsed or refractory myeloid/lymphoid tumors with FGFR1 rearrangements. This provides new hope for refractory cases.

3. Usage and dosage:

1. Before use: Before using pemetinib, patients need to undergo an FDA-approved test to confirm the presence of FGFR2 fusion or rearrangement. There is currently no FDA-approved test for patients with myeloid/lymphoid tumors with FGFR1 rearrangements.

2. Recommended dosage:

(1) Cholangiocarcinoma (CCA): The recommended dose is 13.5 mg, taken orally once a day for 14 consecutive days, followed by 7 days of discontinuation, in a 21-day cycle, until disease progression or unacceptable toxicity occurs.

(2) Myeloid/lymphoid neoplasms (MLNs) with FGFR1 rearrangement: The recommended dose is also 13.5 mg, once daily, orally until disease progression or unacceptable toxicity occurs.

If the patient fails to take the dose for more than 4 hours, or vomits, the next scheduled dose should be continued.

3. Dose adjustment: For patients who experience adverse reactions, the dose needs to be adjusted in a timely manner. If the dose is reduced to 9 mg daily for the first time and to 4.5 mg daily for the second time; if it is still intolerable, it is recommended to permanently discontinue pemetinib during 14 days of each 21-day cycle.

4. Adverse reactions:

The safety of pemetinib has been fully evaluated in clinical studies. For patients with cholangiocarcinoma, ≥2% of serious adverse reactions include abdominal pain, fever, cholangitis, etc. However, ≥20% of patients with myeloid/lymphoid tumors with FGFR1 rearrangements develop hyperphosphatemia, nail toxicity, alopecia and other reactions. Recognition and management of these adverse effects is critical to ensure successful patient treatment.

5. Storage:

Pemetinib should be stored at room temperature20°C to 25°C (68°F to 77°F), with an allowed temperature deviation of 15°C to 30°C (59°F to 86°F). This storage requirement ensures the stability and effectiveness of the drug.

6. Mechanism of action:

Pemetinib is known as a small molecule kinase, mainly targeting FGFR1, 2 and 3, with an IC50 value of less than 2nM. Its mechanism of action is to reduce the viability of cancer cells by inhibiting the phosphorylation and signaling of FGFR. Pemetinib has shown good anti-tumor activity in various tumor mouse xenograft models, providing a theoretical basis for clinical treatment.

Through these detailed descriptions, we can see the importance and potential application value of pemetinib in the treatment of specific types of tumors. With in-depth research on the mechanism of the FGFR signaling pathway, the application and efficacy of pemetinib will be more recognized and promoted.

Reference materials:https://go.drugbank.com/drugs/DB15102