FGFR2融合或重排的胆管癌服用培米替尼出现不良反应后的剂量调整

On April 18, 2020, the U.S. FDA officially announced the accelerated approval of the FGFR2 inhibitor (pemigatinib) developed by Incyte to treat patients with previously treated advanced cholangiocarcinoma with FGFR2 gene fusion or other rearrangement types. Pemigatinib opened the door to targeted therapy for cholangiocarcinoma and became the first targeted drug in the history of cholangiocarcinoma treatment. It also means that the era of chemotherapy-only treatment for cholangiocarcinoma has come to an end. But even so, pemetinib also has adverse reactions. So, what is the dose adjustment for patients with FGFR2 fusion or rearranged cholangiocarcinoma who experience adverse reactions when taking pemetinib?

Dose adjustment after adverse reactions of pemetinib in patients with FGFR2 fusion or rearranged cholangiocarcinoma

Table 1: Recommended dose reduction of PEMAZYRE for adverse reactions

Dose adjustments for coadministration of pemetinib with strong or moderate CYP3A inhibitors

Avoid coadministration of strong and moderate CYP3A inhibitors with PEMAZYRE. If coadministration with strong or moderate CYP3A inhibitors cannot be avoided:

1. Reduce the dose of PEMAZYRE from 13.5 mg to 9 mg.

2. Reduce the dose of PEMAZYRE from 9 mg to 4.5 mg.

If a concomitant drug that is a strong or moderate CYP3A inhibitor is discontinued, increase the PEMAZYRE dose (after 3 plasma half-lives of the CYP3A inhibitor) to the dose before starting the strong or moderate inhibitor.

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