Assessment of Food Effect and pH‐Dependent Drug–Drug Interactions of Fruquintinib in Healthy Subjects
ABSTRACT This two‐sequence, three‐period study (NCT04645940) was designed to evaluate the effect of food and concomitant rabeprazole, a proton pump inhibitor, on the pharmacokinetics (PK) and safety of fruquintinib and its metabolite M11 after a single oral dose of fruquintinib 5 mg in healthy subje...
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| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Wiley
2025-03-01
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| Series: | Clinical and Translational Science |
| Subjects: | |
| Online Access: | https://doi.org/10.1111/cts.70168 |
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| Summary: | ABSTRACT This two‐sequence, three‐period study (NCT04645940) was designed to evaluate the effect of food and concomitant rabeprazole, a proton pump inhibitor, on the pharmacokinetics (PK) and safety of fruquintinib and its metabolite M11 after a single oral dose of fruquintinib 5 mg in healthy subjects. In the food effect treatment periods, 14 subjects were randomized in a 1:1 ratio utilizing a two‐sequence (fed/fasted vs. fasted/fed), two‐period, cross‐over design. Fruquintinib was administered on Day 1 (Period 1) and Day 15 (Period 2). In the drug‐interaction period (Period 3), all subjects received rabeprazole 40 mg 1 h prior to fruquintinib under fasted conditions, following a 6‐day lead‐in of rabeprazole 40 mg once daily. PK samples to measure fruquintinib and M11 were collected pre‐dose and over 168 h after fruquintinib dosing. Administration of fruquintinib with a high‐fat meal resulted in similar systemic exposure compared with fasted conditions. In addition, coadministration of fruquintinib with rabeprazole resulted in similar exposure compared with fruquintinib alone. For both evaluations, 90% confidence intervals for the ratio of geometric least square mean of the area under the curve and peak concentration for fruquintinib and M11 were entirely within 80%–125% bounds. The study results showed no effects of food or rabeprazole on fruquintinib PK, and support that fruquintinib can be taken without regard to food or concurrent gastric acid‐reducing agents. |
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| ISSN: | 1752-8054 1752-8062 |