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- W4387637127 abstract "Encorafenib is a potent and selective ATP competitive inhibitor of BRAF V600-mutant kinase approved for patients with BRAF-mutant melanoma and colorectal cancer. Encorafenib is mainly metabolized by cytochrome P450 (CYP) 3A4 in vitro and may be susceptible to drug-drug interactions when coadministered with CYP3A inhibitors or inducers. The primary objective was to assess the impact of the strong CYP3A inhibitor posaconazole (Part 1) and the moderate CYP3A and P-gp inhibitor diltiazem (Part 2) on encorafenib pharmacokinetics in healthy volunteers following a single 50-mg dose. A total of 32 participants were enrolled (n=16 each in Parts 1 and 2). The AUCinf and Cmax geometric mean for encorafenib increased by 183% and 68.4%, respectively, when coadministered with posaconazole. Apparent encorafenib clearance decreased from 26.0 to 9.2 L/h when coadministered with posaconazole, and plasma t½ of encorafenib increased from 4.3 to 7.3 hours. The AUCinf and Cmax geometric mean for encorafenib increased by 83.0% and 44.7%, respectively, when coadministered with diltiazem. Similarly, the apparent encorafenib clearance decreased from 29.0 to 16.0 L/h when coadministered with diltiazem, and plasma t½ of encorafenib increased from 6.6 to 7.9 hours. There were no deaths, serious adverse events (AEs), or patient discontinuations due to AEs in Part 1 or 2. The most frequently reported treatment-related AEs were erythema (n=14; 88%) and headache (n=11; 69%) in Part 1 and headache (n=7; 44%) in Part 2. The results of this study indicate that coadministration of encorafenib with strong or moderate CYP3A4 inhibitors should be avoided." @default.
- W4387637127 created "2023-10-15" @default.
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- W4387637127 date "2023-10-13" @default.
- W4387637127 modified "2023-10-15" @default.
- W4387637127 title "Impact of Posaconazole and Diltiazem on Pharmacokinetics of Encorafenib, a BRAF V600 Kinase Inhibitor for Melanoma and Colorectal Cancer with BRAF Mutations" @default.
- W4387637127 doi "https://doi.org/10.1111/cts.13662" @default.
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- W4387637127 hasPublicationYear "2023" @default.
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