First-in-human data with SPI-256
The primary objective of this Phase 1; randomized, double-blind, placebo-controlled, single- and escalating-dose crossover study was to evaluate the safety, tolerability and pharmacokinetics of single, ascending doses of SPI-256 administered alone or in combination with 100mg ritonavir (RTV) in healthy volunteers.
Data were presented on 59 healthy volunteers who took a single dose of SPI-256 (150mg, 450mg, 600mg, 900mg, or 1200mg) alone in Phase 1 of the study (n=38); in Phase 2 of the study, 37 subjects took either a single dose of SPI-256 (150mg, 450mg, 900mg) in combination with 100mg of RTV or received a single dose of 1200mg of SPI-256 with a high-fat meal.
SPI-256 demonstrated that it was generally safe and well tolerated in this healthy volunteer population. Adverse events (AEs) were reported by approximately half of subjects, although most were judged to be unrelated or unlikely to be related to study drug. In Phase 1 of the study, three subjects reported a total of 8 AEs possibly related to study drug. In Phase 2 of the study, two subjects reported one AE each that was possibly or definitely related to study drug.
Peak exposure to SPI-256 given alone was dose proportional over the range of 150 to 1200mg. In addition, a single dose of SPI-256 achieved sufficient plasma concentration to suggest the potential of once- or twice-daily dosing regimens in treatment-naive or -experienced patients.
When combined with ritonavir, SPI-256 levels were markedly elevated.
This finding suggests that SPI-256 may be amenable to boosting with
Sequoia's own pharmacokinetic enhancer, SPI-452, which is
|SOURCE Sequoia Pharmaceuticals|
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