Abstract

Apremilast is a pioneering oral selective phosphodiesterase-4 inhibitor for the treatment of psoriasis. To evaluate and compare the pharmacokinetic properties and bioavailability of apremilast tablets manufactured by Nanjing Haijing Pharmaceutical Company (Nanjing, China) with apremilast tablets certified by Celgene Europe B.V. (Utrecht, The Netherlands), we conducted a randomized, open-label, single-dose, two-period, crossover study in healthy Chinese subjects under fasted and fed conditions. Eligible subjects were randomly assigned to receive reference or test apremilast tablets in the first treatment period and the other formulation in the second period. Serial blood samples were collected for pharmacokinetic analysis. Adverse events were recorded. A total of 28 healthy subjects were enrolled in the fasting cohort and 36 subjects in the fed cohort. The 90% confidence intervals of the geometric mean ratios of the test to reference formulations were 91.56 – 106.18% for C_max, 96.08 – 108.18% for AUC_0–t, and 96.02 – 107.67% for AUC_0–∞ in the fasting cohort, and 95.15 – 107.05% for C_max, 105.13 – 113.45% for AUC_0–t, and 104.80 – 111.91% for AUC_0–∞ in the fed cohort, all of which were within the bioequivalence range of 80.00 – 125.00%. There were no serious adverse events. The results showed that the test and reference apremilast tablets were bioequivalent and well tolerated in healthy Chinese subjects under fasting and fed conditions.

Author Details

Authors

• Pan Lu¹
• Fang Yao¹
• Jie Wang¹
• Yingxia He¹
• Jun Liang¹
• Xuejia Zhai^{2, 3}
• Guan Liu¹

Departments

• ¹ PhaseI Clinical Research Center, Wuhan Pulmonary Hospital,
• ² Department of Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, and
• ³ Hubei Province Clinical Research Center for Precision Medicine for Critical Illness, Union Hospital, Wuhan, China

Address

Guan Liu, MD
Phase | Clinical Research Center
Wuhan Pulmonary Hospital
Wuhan, People’s Republic of China
Email: [email protected]

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