1354. Novel Formulation SUBA-Itraconazole in Fed and Fasted Healthy Volunteers: Expanding the Clinical Utility of the Established Mold Active Agent
Session: Poster Abstract Session: Novel Agents
Friday, October 5, 2018
Room: S Poster Hall
  • FINAL IDweek 2018 Novel Formulation SUBA-Itraconazole in Fed and Fasted Healthy Volunteers.pdf (1.5 MB)
  • Background: Itraconazole has been established as an effective mold active agent, however wide interpatient variability in bioavailability and poor gastrointestinal tolerability have made using the agent challenging. A novel formulation, SUBA-Itraconazole¨ (SUperBioAvailable) has been developed by Mayne Pharma to alleviate these negative properties. Methods: An open-label, randomized, cross-over study of SUBA-Itraconazole capsules 65 mg (2 X 65 mg BID) in healthy adults under fasting and fed conditions was assessed for steady-state levels. Subjects (n=20) were administered two capsules of SUBA-Itraconazole twice daily on Days 1-14 and once on the morning of Day 15, either on an empty stomach or with a meal. Safety was monitored by vital signs measurements, electrocardiogram measurements, clinical safety laboratory tests (liver and kidney function tests), and physical examination. Results: Overall, SUBA-Itraconazole demonstrated similar concentrations at the end of the dosing interval (trough), with modestly lower total and peak exposure when administered under fed conditions compared to the fasted state (fed/fasted ratios of 78.09% for AUCtau [14183.2 vs 18479.8] 73.05% for Cmax,ss [1519.1 vs 2085.2] and 91.53% for Ctrough[1071.5 vs 1218.5]); See Figure 1 and 2. The administration of SUBA-Itraconazole 65 mg Capsules was well-tolerated by the healthy subjects participating in this study. Conclusion: The results demonstrate a promising clinical utility for SUBA-Itraconazole in practice. Unlike the conventional capsule formulation which requires a high fat meal for absorption, or the oral solution formulation which requires a fasted administration, SUBA-Itraconazole reached a therapeutic steady state in both fasted and fed states.  The similar trough level, however higher peak with fasted state, likely represents a more gradual absorption of drug in the fed state. The slightly higher bioavailability in a fasted state, without gastrointestinal intolerability is particularly promising for the clinical use of SUBA-Itraconazole in patients unable to have a high fat content meal due to chemotherapy or post-surgery such as hematology patients and transplant recipients.       Figure 1: Mean Pre-dose Plasma Itraconazole Concentrations

    Figure 2: Mean Plasma Itraconazole Concentration-Time Profile (Day 15)


    Julian Lindsay, BPharm(Hons), MClinPharm, Royal North Shore Hospital, Sydney, Australia and Stuart Mudge, PhD, Mayne Pharma, Melbourne, Australia


    J. Lindsay, Mayne Pharma: Consultant , Consulting fee .

    S. Mudge, Mayne Pharma: Employee , Salary .

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