Absence of Food Effect on the Pharmacokinetics of Telbivudine Following Oral Administration in Healthy Subjects

The influence of food on the pharmacokinetics of telbivudine, a candidate antiviral agent against hepatitis B virus (HBV), was investigated in healthy adult subjects following a 600‐mg oral dose administered with and without a high‐fat/high‐calorie meal. Telbivudine was well tolerated under fasting and fed conditions. Oral absorption of telbivudine as measured by maximum plasma concentration (Cmax), time to reach Cmax (Tmax), and area under the plasma concentration‐time curve (AUC0‐t and AUC0‐∞) was not altered by food intake immediately before oral dosing. Values of Cmax, Tmax, and AUC were comparable when telbivudine was administered under fed and fasting conditions. Results from this study indicated that the absorption of telbivudine was not affected by a high‐fat/high‐calorie meal; telbivudine can therefore be administered orally with no regard to the timing of meals.

[1]  M. Yuen,et al.  A dose‐finding study of once‐daily oral telbivudine in HBeAg‐positive patients with chronic hepatitis B virus infection , 2004, Hepatology.

[2]  M. Trautmann,et al.  Decreased and variable systemic availability of zidovudine in patients with AIDS if administered with a meal , 2004, European Journal of Clinical Pharmacology.

[3]  B. Tennant,et al.  Pharmacokinetics of β-L-thymidine and β-L-2′-deoxycytidine in woodchucks and monkeys , 2003 .

[4]  J. Rodríguez-Orengo,et al.  Pharmacology of β-l-Thymidine and β-l-2′-Deoxycytidine in HepG2 Cells and Primary Human Hepatocytes: Relevance to Chemotherapeutic Efficacy against Hepatitis B Virus , 2002, Antimicrobial Agents and Chemotherapy.

[5]  E. O'Mara,et al.  Effect of Food on the Oral Bioavailability of Didanosine from Encapsulated Enteric‐Coated Beads , 2002, Journal of clinical pharmacology.

[6]  Y. Lou,et al.  Abacavir/Lamivudine/Zidovudme As a Combined Formulation Tablet: Bioequivalence Compared with Each Component Administered Concurrently and the Effect of Food on Absorption , 2001, Journal of clinical pharmacology.

[7]  R. Schinazi,et al.  Antiviral l-Nucleosides Specific for Hepatitis B Virus Infection , 2001, Antimicrobial Agents and Chemotherapy.

[8]  W. Prince,et al.  Abacavir: Absolute Bioavailability, Bioequivalence of Three Oral Formulations, and Effect of Food , 1999, Pharmacotherapy.

[9]  G. E. Pakes,et al.  Lamivudine/Zidovudine as a Combined Formulation Tablet: Bioequivalence Compared with Lamivudine and Zidovudine Administered Concurrently and the Effect of Food on Absorption , 1999, Journal of clinical pharmacology.

[10]  S. Kaul,et al.  Effect of Food on the Bioavailability of Stavudine in Subjects with Human Immunodeficiency Virus Infection , 1998, Antimicrobial Agents and Chemotherapy.

[11]  R. Reichman,et al.  Prolonged, But Not Diminished, Zidovudine Absorption Induced by a High‐Fat Breakfast , 1994, Pharmacotherapy.

[12]  M. Trautmann,et al.  Effects of standard breakfast on pharmacokinetics of oral zidovudine in patients with AIDS , 1993, Antimicrobial Agents and Chemotherapy.

[13]  J. Montaner,et al.  Pharmacokinetics of 3TC (GR109714X) Administered With and Without Food to HIV-infected Patients , 1993 .

[14]  R. Barbhaiya,et al.  Effect of Time of Food Administration on the Bioavailability of Didanosine From a Chewable Tablet Formulation , 1993, Journal of clinical pharmacology.

[15]  P. Davey,et al.  Cost Effectiveness of Once‐Daily Oral Antimicrobial Therapy , 1992, Journal of clinical pharmacology.

[16]  G. Garber,et al.  The effect of a protein meal on zidovudine pharmacokinetics in HIV-infected patients. , 1992, British journal of clinical pharmacology.

[17]  K. Pittman,et al.  Food‐induced reduction in bioavailability of didanosine , 1991, Clinical pharmacology and therapeutics.

[18]  A. Collier,et al.  Pharmacokinetics of oral zidovudine (azidothymidine) in patients with AIDS when administered with and without a high‐fat meal , 1990, AIDS.