A Phase I, open-label, randomized, crossover study in healthy subjects to evaluate the bioavailability of, and the food effect on, a pomalidomide oral liquid suspension. 2018

Yan Li, and Liangang Liu, and Lian Huang, and Xiaomin Wang, and Matthew Hoffmann, and Josephine Reyes, and Maria Palmisano, and Simon Zhou
Translational Development and Clinical Pharmacology, szhou@celgene.com.

OBJECTIVE The aim of this study was to evaluate the bioavailability of a pomalidomide oral liquid suspension relative to the commercial capsule formulation and to assess the food effect on the pomalidomide oral liquid suspension when administered as a single 4 mg dose. METHODS This was an open-label, randomized, three-period, two-sequence crossover study in healthy subjects consisting of a screening phase, a baseline assessment phase, a treatment phase with three periods, and a follow-up phone call phase. Blood samples for pharmacokinetics (PK) assessment were collected up to 48 h postdose during each treatment period. Safety was evaluated throughout the study. RESULTS Pomalidomide exposures were comparable in healthy subjects administered with a single oral 4 mg dose as the reference capsule or as the test liquid suspension formulations, demonstrated as the 90% confidence intervals of the geometric mean ratios for area under the plasma concentration-time curve calculated from time 0 to the last measurable concentration at time t (AUC0-t), area under the plasma concentration-time curve from time 0 to infinity (AUC0-∞), and peak (maximum) plasma drug concentration (Cmax) were completely contained within the bioequivalence range of 80-125%. Administration of the pomalidomide liquid suspension with a high fat meal resulted in a 3.0 h delay in pomalidomide time to Cmax (tmax) and an ~ 34.5% reduction in Cmax. However, the AUCs were comparable after dose administration with and without food. CONCLUSIONS A single oral dose of 4 mg of liquid suspension was bioequivalent to a single oral dose of 4 mg of capsule formulation. There was no clinically relevant impact of food on pomalidomide liquid suspension. Single oral doses of 4 mg pomalidomide were safe and well tolerated when administered as a liquid suspension under fed and fasted conditions or as a capsule under fasted conditions.

UI MeSH Term Description Entries

Related Publications

Yan Li, and Liangang Liu, and Lian Huang, and Xiaomin Wang, and Matthew Hoffmann, and Josephine Reyes, and Maria Palmisano, and Simon Zhou
September 2021, Clinical therapeutics,
Yan Li, and Liangang Liu, and Lian Huang, and Xiaomin Wang, and Matthew Hoffmann, and Josephine Reyes, and Maria Palmisano, and Simon Zhou
August 2011, Clinical therapeutics,
Yan Li, and Liangang Liu, and Lian Huang, and Xiaomin Wang, and Matthew Hoffmann, and Josephine Reyes, and Maria Palmisano, and Simon Zhou
January 1998, European journal of drug metabolism and pharmacokinetics,
Yan Li, and Liangang Liu, and Lian Huang, and Xiaomin Wang, and Matthew Hoffmann, and Josephine Reyes, and Maria Palmisano, and Simon Zhou
January 2023, Drug design, development and therapy,
Yan Li, and Liangang Liu, and Lian Huang, and Xiaomin Wang, and Matthew Hoffmann, and Josephine Reyes, and Maria Palmisano, and Simon Zhou
September 2015, Clinical pharmacology in drug development,
Yan Li, and Liangang Liu, and Lian Huang, and Xiaomin Wang, and Matthew Hoffmann, and Josephine Reyes, and Maria Palmisano, and Simon Zhou
February 2019, Clinical therapeutics,
Yan Li, and Liangang Liu, and Lian Huang, and Xiaomin Wang, and Matthew Hoffmann, and Josephine Reyes, and Maria Palmisano, and Simon Zhou
May 2018, Clinical pharmacology in drug development,
Yan Li, and Liangang Liu, and Lian Huang, and Xiaomin Wang, and Matthew Hoffmann, and Josephine Reyes, and Maria Palmisano, and Simon Zhou
May 2007, Clinical therapeutics,
Yan Li, and Liangang Liu, and Lian Huang, and Xiaomin Wang, and Matthew Hoffmann, and Josephine Reyes, and Maria Palmisano, and Simon Zhou
February 2023, Epilepsia,
Yan Li, and Liangang Liu, and Lian Huang, and Xiaomin Wang, and Matthew Hoffmann, and Josephine Reyes, and Maria Palmisano, and Simon Zhou
July 2019, Advances in therapy,
Copied contents to your clipboard!