Single-dose phase 1 studies to evaluate the more predictable pharmacokinetics of itraconazole in a novel capsule formulation (Lozanoc™) relative to conventional itraconazole capsule formulation.

Stuart J. Mudge, David Hayes, David H. Ellis


Background: Itraconazole is a highly-insoluble yet well-established as an antifungal agent. The conventional 100 mg capsule formulation is taken with food to maximise its absorption. Lozanoc™ is a 50 mg itraconazole capsule with a proprietary SUBA™ formulation designed to enhance itraconazole bioavailability. Objectives: The objective of these trials was to compare the pharmacokinetics of Lozanoc™ 50 mg capsules relative to the conventional itraconazole 100 mg capsule formulation, SPORANOX®. Patients/Methods: Trial 1 had a randomised open-label, four-way cross-over design; Trial 2 a randomised, open-label, two-treatment (repeat dose), four-period, two-sequence, crossover design. Subjects received a single 50 mg Lozanoc™ or 100 mg SPORANOX® capsule in a fed or fasted condition in Trial 1 and in a fed condition in Trial 2. The pharmacokinetics of itraconazole and hydroxyitraconazole were evaluated from plasma concentration measurements up to 120 hours after dosing. Results: 35 subjects completed Trial 1 and 48 subjects completed Trial 2. Regardless of food, the differences in the extent of exposure following a single administrations of 50 mg Lozanoc™ and 100 mg Sporanox® was less than 25%, with the inter- and intra-subject variability significantly lower for the 50 mg Lozanoc™ capsules. Adverse events were reported infrequently and were mainly mild. Conclusions: In both fed and fasted conditions, a single Lozanoc™ 50 mg capsule achieved a similar extent of exposure to a single SPORANOX® 100 mg capsule. Of note, the extent of exposure was less variable with Lozanoc™ than with SPORANOX®, and with no significant food effect.


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19th Congress of the International Society for Human and Animal Mycology
    • ISHAM 19th (2015)