Abstract
A randomized double-blind, placebo-controlled study was conducted in 37 asymptomatic HIV-infected individuals (mean CD4 count 707 cells/mm3) to characterize the safety, pharmacokinetics, and effect on blood thiols of three dosage levels of a cysteine prodrug, L-2-oxothiazolidine-4-carboxylic acid (OTC; Procysteine; Clintec Technologies, Deerfield, IL). Single-dose administration of OTC resulted in measurable plasma levels at all dosages, with a mean peak plasma concentration of 734 +/- 234 nmol/mL at the highest dosage studied. After 4 weeks of administration three times daily, a statistically significant increase was seen in whole blood glutathione in the 1,500 mg and 3,000 mg dose groups compared with the placebo group. A significant increase in whole blood cysteine and peripheral blood mononuclear cell (PBMC) glutathione was not seen during the study period.
Publication types
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Clinical Trial
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Clinical Trial, Phase I
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Clinical Trial, Phase II
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Randomized Controlled Trial
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Adult
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Anti-HIV Agents / adverse effects
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Anti-HIV Agents / pharmacokinetics
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Anti-HIV Agents / pharmacology*
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Anti-HIV Agents / therapeutic use
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Cysteine / blood
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Dose-Response Relationship, Drug
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Double-Blind Method
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Glutathione / blood
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HIV Infections / blood*
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HIV Infections / drug therapy
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Humans
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Leukocytes, Mononuclear / metabolism
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Middle Aged
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Prodrugs / adverse effects
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Prodrugs / pharmacokinetics
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Prodrugs / pharmacology*
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Prodrugs / therapeutic use
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Pyrrolidonecarboxylic Acid
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Thiazoles / adverse effects
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Thiazoles / pharmacokinetics
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Thiazoles / pharmacology*
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Thiazoles / therapeutic use
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Thiazolidines
Substances
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Anti-HIV Agents
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Prodrugs
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Thiazoles
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Thiazolidines
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Glutathione
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Cysteine
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Pyrrolidonecarboxylic Acid
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2-oxothiazolidine-4-carboxylic acid