Sequoia Pharmaceuticals Presents Proof of Clinical Concept of SPI-452, a Novel Pharmacokineti...(Sequoia PKE developmentprogram. ...),Health

"In the HIV community and the clinical arena at large, there is a compelling need for novel agents that enhance the pharmacokinetic profiles of existing drugs in order to increase efficacy, reduce pill burden, and decrease frequency of dosing for patients," said Martin Markowitz, MD, clinical director at the Aaron Diamond AIDS Research Center and an Aaron Diamond professor at Rockefeller University. "Sequoia Pharmaceuticals' PKE development program has demonstrated significant progress toward fulfilling the unmet medical need for a safe and well tolerated PKE that potently enhances the pharmacokinetics of target compounds without the risk of promoting the emergence of resistant mutants due to its lack of antiviral activity."

Data on SPI-452 at this conference

Study 0452-002: Proof of Clinical Concept

Study 0452-002 was designed to evaluate the pharmacokinetic profile of multiple doses of SPI-452 and to establish proof of clinical concept of the pharmacokinetic enhancement ability of SPI-452 when combined with either of 2 currently marketed HIV protease inhibitors, darunavir or atazanavir. Sixty- seven healthy volunteers were enrolled in this randomized, placebo-controlled, repeat- and escalating-dose trial. Before administering SPI-452, subjects received a single dose of darunavir (600 mg), atazanavir (300 mg) or placebo in order to establish PI plasma concentration levels. After a 7 day washout period, subjects were randomized to 15 days of SPI-452 (25 mg, 50 mg, or 200 mg) once daily or placebo. On day 15, subjects also received, once again, either darunavir, atazanavir or placebo co-administered with the final dose of SPI-452. On day 16 subjects received darunavir, atazanavir or placebo only.

Pharmacokinetic results of SPI-452 co-administered with darunavir and atazanavir demonstrated that SPI-452 significantly increased the
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