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The Lipid-lowering Effects of R-bambuterol in Healthy Chinese Volunteers: A Randomized Phase I Clinical Study
- Source :
- EBioMedicine, Vol 2, Iss 4, Pp 356-364 (2015), EBioMedicine
- Publication Year :
- 2015
- Publisher :
- Elsevier BV, 2015.
-
Abstract
- Background Existing treatments are inadequate for patients at high risk of coronary heart disease caused by elevated levels of plasma low-density lipoprotein cholesterol (LDL-C). Bambuterol is a prodrug of β2-agonist commonly used for the treatment of asthma and chronic obstructive pulmonary disease (COPD) with the advantage of once daily dosing and favorable side effect profile. The potential lipid-lowering effects of bambuterol were unclear, possibly due to the racemic bambuterol (rac-bambuterol) that was used in previous studies. Methods The lipid-lowering effects of R-bambuterol were examined in a randomized phase I trial in 48 healthy Chinese volunteers aged 18–45 years. Participants were randomly assigned to five groups to receive a single dose (2.5 mg, 5 mg or 10 mg) or multiple doses (5 mg) of oral medications of R-bambuterol, or a single dose of rac-bambuterol (10 mg). Plasma lipid levels were measured at baseline, time to peak concentration (Tmax) and 24 h after the treatment. Findings Administration of a single-dose of R-bambuterol resulted in dose-dependent reductions in the levels of plasma LDL-C, high-density lipoprotein cholesterol (HDL-C), total cholesterol (TC), apolipoprotein B (ApoB) and apolipoprotein A1 (ApoA1) at Tmax. Levels of LDL-C exhibited the most reductions, which were statistically significant in all three single-dose R-bambuterol groups (all P values<br />Highlights • Oral administration of R-bambuterol, a long-acting bronchodilator, can significantly lower LDL cholesterol in healthy Chinese volunteers. • R-bambuterol was more potent than rac-bambuterol in lowering LDL-C and raising the ratio of ApoA1/ApoB. • It may provide an alternative for treating high cholesterol, especially for those also suffering from COPD.
- Subjects :
- Adult
Male
Side effect
lcsh:Medicine
Pharmacology
General Biochemistry, Genetics and Molecular Biology
Clinical study
Young Adult
chemistry.chemical_compound
Asian People
R-bambuterol
Terbutaline
Humans
Medicine
Bambuterol
Particle Size
β2-Agonist
LDL-C
Apolipoproteins B
Demography
Hypolipidemic Agents
Asthma
COPD
lcsh:R5-920
Dose-Response Relationship, Drug
business.industry
Cholesterol
lcsh:R
General Medicine
Prodrug
medicine.disease
Healthy Volunteers
chemistry
Health
Female
Original Article
lipids (amino acids, peptides, and proteins)
Lipid lowering
Lipoproteins, HDL
business
lcsh:Medicine (General)
medicine.drug
Subjects
Details
- ISSN :
- 23523964
- Volume :
- 2
- Issue :
- 4
- Database :
- OpenAIRE
- Journal :
- EBioMedicine
- Accession number :
- edsair.doi.dedup.....d28349a609676ce5d590f6a9048abec5
- Full Text :
- https://doi.org/10.1016/j.ebiom.2015.02.006