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Pharmacokinetics and pharmacodynamics of HTD1801 (berberine ursodeoxycholate, BUDCA) in patients with hyperlipidemia
Adrian M Di Bisceglie1,2, Gerald F Watts3, Philip Lavin4
1Department of Internal Medicine, Saint Louis University, St. Louis, USA. adibisceglie@hightidetx.com.
Insights
Berberine ursodeoxycholate (BUDCA) safely lowers LDL cholesterol in hypercholesterolemia patients. This new compound offers a potential alternative for individuals unable to use statins.
Area of Science:
- Cardiovascular disease research
- Pharmacology
- Metabolic disorders
Background:
- Elevated cholesterol is a key risk factor for atherosclerotic cardiovascular disease (ASCVD).
- Statins are common treatments, but many patients have residual risk due to unaddressed comorbidities like diabetes and fatty liver disease.
- A clinical trial (NCT03381287) investigated a novel compound for hypercholesterolemia management.
Purpose of the Study:
- To evaluate the safety and tolerability of berberine ursodeoxycholate (BUDCA).
- To assess the efficacy of BUDCA in reducing serum lipid and lipoprotein concentrations in hypercholesterolemia patients.
Main Methods:
- A double-blind, randomized, placebo-controlled, dose-ranging study.
- 50 subjects with hypercholesterolemia and elevated LDL cholesterol were enrolled.
- BUDCA was administered in two divided daily doses for 28 days, comparing three doses against a placebo.
Main Results:
- BUDCA was well-tolerated up to 2000 mg/day, with no significant adverse effects.
- The highest dose of BUDCA led to significant reductions in total cholesterol (8.2%) and LDL cholesterol (10.4%) by day 28.
- No significant changes were observed in triglyceride or HDL cholesterol levels.
Conclusions:
- BUDCA is a novel single molecular entity with a modest yet significant LDL-cholesterol-lowering effect.
- It presents a potential therapeutic option for hypercholesterolemia, particularly for statin-intolerant patients.
- BUDCA may also serve as an adjunctive therapy with agents like ezetimibe or bempedoic acid.
Background:
Reduction in elevated serum cholesterol concentrations is important in the management of individuals at risk of atherosclerotic cardiovascular disease (ASCVD), such as myocardial infarction and thrombotic stroke. Although HMGCoA reductase inhibitors ("statins") are frequently used for this purpose, a significant proportion of patients remain at increased residual risk of ASCVD as they do not adequately address some of the associated co-morbidities such as diabetes and fatty liver disease.
Methods:
A double-blind, randomized, placebo-controlled, dose ranging study was carried out that compared three doses of berberine ursodeoxycholate (BUDCA) to placebo in a cohort of subjects with a history of hypercholesterolemia and serum LDL cholesterol levels above 2.59 mmol/L (> 99.9 mg/dL). BUDCA was administered in two divided doses each day for 28 days. The primary endpoints of the study were safety and tolerability of this new compound, as well as its effect in lowering serum lipid and lipoprotein concentrations.
Results:
A total of 50 subjects were enrolled into three dose cohorts in this study. BUDCA was generally well tolerated, even at doses of 2000 mg per day (the highest dose group); there were no significant adverse effects reported and this highest dose was associated with significant reductions in LDL cholesterol. By day 28 and with the highest dose of BUDCA, there were significant reductions in the serum concentrations of total cholesterol by 8.2% (P = 0.0004) and LDL cholesterol by 10.4% (P = 0.0006), but no significant changes in triglyceride and HDL cholesterol concentrations.
Conclusions:
BUDCA is a new single molecular entity that has a significant but modest effect in safely lowering serum LDL-cholesterol concentrations in individuals with a history of hypercholesterolemia. It has a potential use for treating hypercholesterolemia in individuals who cannot take statins, and possibly as adjunctive to other agents, such as ezetimibe or bempedoic acid.
Trial Registration:
The study was registered on Clinicaltrials.gov ( NCT03381287 ).
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