Simple and convenient dosing is possible with oral tazarotene

Abstract

Background: An oral formulation of tazarotene is currently in development for the treatment of moderate to very severe plaque psoriasis and severe nodulocystic acne. Objectives: To assess the effects of food and body weight on the pharmacokinetics (PK) of oral tazarotene and its primary active metabolite, tazarotenic acid. Methods: A clinical study in healthy volunteers investigated the effects of food and body weight on the PK profile of oral tazarotene (single dose or seven consecutive daily doses ranging from 3 mg to 12 mg). Results: Taking 6 mg oral tazarotene with a high-fat meal did not affect the absorption of tazarotene—plasma tazarotenic acid AUC ratios in subjects who had taken tazarotene with a high-fat meal were completely within the 80–125% boundary (90% confidence interval) of those in fasted subjects. Cmax ratios were partially outside the 80–125% boundary but this divergence was most likely due to data variability and a small sample size. Comparisons of plasma tazarotenic acid Cmax and AUC values among subjects of differing body weights showed virtually no effect of body weight on systemic tazarotenic acid exposure (p > 0.05). Specifically, while there was a significant correlation of AUC with body weight on Day 0, there was no such correlation with Cmax and there was no correlation between Cmax or AUC and body weight on Day 9. Conclusion: The lack of influence of food and body weight on the PK profile of oral tazarotene should help facilitate simple and convenient dosing.