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Efficacy and safety of disodium ascorbyl phytostanol phosphates in men with moderate dyslipidemia

OBJECTIVE: This study investigated the efficacy, safety, tolerability, and pharmacokinetics of a novel cholesterol absorption inhibitor, FM-VP4, comprising disodium ascorbyl sitostanol phosphate (DASP) and disodium ascorbyl campestanol phosphate (DACP). METHODS: In phase 1, 30 men received a single...

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Autores principales: Vissers, Maud N., Trip, Mieke D., Pritchard, P. Haydn, Tam, Patrick, Lukic, Tatjana, de Sain-van der Velden, Monique G., de Barse, Martina, Kastelein, John J. P.
Formato: Texto
Lenguaje:English
Publicado: Springer-Verlag 2008
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2426926/
https://www.ncbi.nlm.nih.gov/pubmed/18320185
http://dx.doi.org/10.1007/s00228-008-0462-1
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author Vissers, Maud N.
Trip, Mieke D.
Pritchard, P. Haydn
Tam, Patrick
Lukic, Tatjana
de Sain-van der Velden, Monique G.
de Barse, Martina
Kastelein, John J. P.
author_facet Vissers, Maud N.
Trip, Mieke D.
Pritchard, P. Haydn
Tam, Patrick
Lukic, Tatjana
de Sain-van der Velden, Monique G.
de Barse, Martina
Kastelein, John J. P.
author_sort Vissers, Maud N.
collection PubMed
description OBJECTIVE: This study investigated the efficacy, safety, tolerability, and pharmacokinetics of a novel cholesterol absorption inhibitor, FM-VP4, comprising disodium ascorbyl sitostanol phosphate (DASP) and disodium ascorbyl campestanol phosphate (DACP). METHODS: In phase 1, 30 men received a single dose of 100, 200, 400, 800, 1,600, or 2,000 mg FM-VP4 or placebo. In phase 2, 100 men were treated with 100, 200, 400, or 800 mg/day of FM-VP4 or placebo for 4 weeks. RESULTS: The drug was well tolerated at each single or multiple dose level. After 4 weeks of treatment, low-density lipoprotein cholesterol (LDL-C) levels changed by 2.7% in the placebo group and by 2.9%, −4.2%, and −4.6% in the 100, 200, and 800 mg/day groups, respectively, which was not statistically significant. However, 400 mg/day of FM-VP4 significantly decreased LDL-C by 6.5% (p=0.02). Phase 1 showed that DACP and DASP were absorbed into plasma with a median t(max) of 12 h for both components, and clearance was slow with a mean t(1/2λ) of 57 h. During 4 weeks of treatment, steady state was reached by approximately 8 days. CONCLUSION: This study demonstrated that up to 800 mg/day of FM-VP4 is safe and well tolerated for at least 4 weeks. Furthermore, the higher doses significantly reduced LDL-C by 7% compared with baseline or by 10% compared with placebo, with the maximum effect reached at 400 mg/day.
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spelling pubmed-24269262008-06-13 Efficacy and safety of disodium ascorbyl phytostanol phosphates in men with moderate dyslipidemia Vissers, Maud N. Trip, Mieke D. Pritchard, P. Haydn Tam, Patrick Lukic, Tatjana de Sain-van der Velden, Monique G. de Barse, Martina Kastelein, John J. P. Eur J Clin Pharmacol Clinical Trial OBJECTIVE: This study investigated the efficacy, safety, tolerability, and pharmacokinetics of a novel cholesterol absorption inhibitor, FM-VP4, comprising disodium ascorbyl sitostanol phosphate (DASP) and disodium ascorbyl campestanol phosphate (DACP). METHODS: In phase 1, 30 men received a single dose of 100, 200, 400, 800, 1,600, or 2,000 mg FM-VP4 or placebo. In phase 2, 100 men were treated with 100, 200, 400, or 800 mg/day of FM-VP4 or placebo for 4 weeks. RESULTS: The drug was well tolerated at each single or multiple dose level. After 4 weeks of treatment, low-density lipoprotein cholesterol (LDL-C) levels changed by 2.7% in the placebo group and by 2.9%, −4.2%, and −4.6% in the 100, 200, and 800 mg/day groups, respectively, which was not statistically significant. However, 400 mg/day of FM-VP4 significantly decreased LDL-C by 6.5% (p=0.02). Phase 1 showed that DACP and DASP were absorbed into plasma with a median t(max) of 12 h for both components, and clearance was slow with a mean t(1/2λ) of 57 h. During 4 weeks of treatment, steady state was reached by approximately 8 days. CONCLUSION: This study demonstrated that up to 800 mg/day of FM-VP4 is safe and well tolerated for at least 4 weeks. Furthermore, the higher doses significantly reduced LDL-C by 7% compared with baseline or by 10% compared with placebo, with the maximum effect reached at 400 mg/day. Springer-Verlag 2008-03-05 2008-07 /pmc/articles/PMC2426926/ /pubmed/18320185 http://dx.doi.org/10.1007/s00228-008-0462-1 Text en © The Author(s) 2008
spellingShingle Clinical Trial
Vissers, Maud N.
Trip, Mieke D.
Pritchard, P. Haydn
Tam, Patrick
Lukic, Tatjana
de Sain-van der Velden, Monique G.
de Barse, Martina
Kastelein, John J. P.
Efficacy and safety of disodium ascorbyl phytostanol phosphates in men with moderate dyslipidemia
title Efficacy and safety of disodium ascorbyl phytostanol phosphates in men with moderate dyslipidemia
title_full Efficacy and safety of disodium ascorbyl phytostanol phosphates in men with moderate dyslipidemia
title_fullStr Efficacy and safety of disodium ascorbyl phytostanol phosphates in men with moderate dyslipidemia
title_full_unstemmed Efficacy and safety of disodium ascorbyl phytostanol phosphates in men with moderate dyslipidemia
title_short Efficacy and safety of disodium ascorbyl phytostanol phosphates in men with moderate dyslipidemia
title_sort efficacy and safety of disodium ascorbyl phytostanol phosphates in men with moderate dyslipidemia
topic Clinical Trial
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2426926/
https://www.ncbi.nlm.nih.gov/pubmed/18320185
http://dx.doi.org/10.1007/s00228-008-0462-1
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