PDF
Full
Outline
To assess the tablet effect of a high-fat diet on the pharmacokinetics of oral FM888 tablet in healthy Chinese participants. FM888 tablet is a novel highly selective adenylyl cyclase 1 (AC1) antagonist potentially involved in chronic pain treatment by modulation of central plasticity.
A single-center, open-label, randomized, single-dose, two-period crossover trial was conducted. Subjects were randomized 1∶1 to receive 400 mg FM888 tablet under fasting or high-fat meal conditions, then crossed over after a 7-day washout. Plasma FM888 concentrations were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS) and analyzed by non-compartmental methods using Phoenix WinNonlin 8.3.1.
The Cmax of FM888 tablet in the fasting state and after a highfat meal were (175.57±89.51) and (63.74±38.74) ng·mL-1, respectively; AUC0-last were (645.84±355.50) and (416.28±245.83) h·ng·mL-1, respectively; AUC0-∞ were (698.22±373.46) and (455.36±290.66) h·ng·mL-1, respectively. Exposure to FM888 tablet was lower under fed conditions than under fasting conditions, with Cmax and AUC0-last reduced to approximately 36.00% and 65.00% of the fasting values, respectively. The geometric mean ratios (fed/fasting) for Cmax、AUC0-last and AUC0-∞ were 36.86% [90% confidence interval (CI): 28.94%-46.95%], 66.01% (90% CI: 55.72%-78.20%), and 67.39% (90% CI: 55.70%-81.53%), respectively. Mixed-effects modeling confirmed a significant effect of feeding status on key parameters (P<0.05). FM888 tablet was well tolerated; all adverse events were grade 1, with no serious events.
A high-fat meal significantly reduced FM888 bioavailability, indicating a marked food effect. Despite lower exposure, FM888 tablet demonstrated favorable safety and tolerability.
PDF
195
30
| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
关闭全屏
No. 86 Xueyuan South Road, Haidian District, Beijing
010-62199257
qkjq@cast.org.cn
Copyright © 2025 China Association for Science and Technology. All rights reserved. For all open access content, the relevant licensing terms apply.
Sponsored by the Office of the Leading Group for Cybersecurity and Informatization of CAST, and supported by Science and Technology Review Publishing House
