Development of Gallstone Dissolution Agents for Gastrointestinal Diseases

With an in-depth understanding of the complex mechanisms of gastrointestinal diseases, Ace Therapeutics is committed to providing effective experimental solutions to help clients advance the development of gallstone dissolution agents as gastrointestinal disease therapy.

Introduction to Gallstone Dissolution Agents

Gallstone-dissolving medications serve as a primary pharmacological intervention for cholesterol-based gallstones, particularly in patients unsuitable for surgical procedures or those selecting conservative management. These agents exert their therapeutic effects through three principal mechanisms: bile acid composition modulation, direct cholesterol stone dissolution, and enhancement of biliary tract motility.

Fig. 1 Influence factors of gallstones. (Sun H, et al., 2022)

Types of Gallstone Dissolution Agents We Can Develop

• Bile Acid Analogs
  Through targeted modulation of hepatic bile acid synthesis pathways, bile acid analogs effectively downregulate cholesterol biosynthesis enzymes to achieve optimal cholesterol solubilization. We offer comprehensive bile acid analog development services tailored to target specific pathways in cholesterol homeostasis and gallstone pathogenesis.
• Exogenous Cholesterol Solubilizing Agents
  Exogenous cholesterol solubilizing agents represent a specialized class of therapeutic compounds that directly interact with cholesterol gallstones to induce dissolution, administered either via oral delivery or direct biliary infusion. We provide end-to-end development services for novel exogenous cholesterol solubilizing agents with optimized pharmacokinetic and safety profiles.

What Can We Do for the Development of Gallstone Dissolution Agents?

In Vitro Studies

• Gallstone Dissolution Experiment
  We employ synthetic gallstone models to systematically evaluate the dissolution efficacy of therapeutic compounds across gallstone subtypes, including cholesterol-dominant and bilirubin-based calculi. This approach enables comprehensive characterization of drug candidates' activity and substrate specificity under physiologically relevant conditions.
• Dissolution Kinetics Studies
  Our platform enables precise quantification of gallstone dissolution kinetics, including rate determination and efficiency profiling, to establish optimal therapeutic parameters such as concentration-response relationships and minimum effective exposure duration. This analytical approach provides critical data for rational dosing regimen design in clinical development.
• Bile Composition Analysis
  Our analytical platform enables systematic evaluation of pharmaceutical compounds' impact on biliary lipid homeostasis, specifically quantifying drug-induced alterations in the critical cholesterol-bile salt-phospholipid equilibrium. This assessment provides fundamental insights into therapeutic agents' ability to favorably modulate bile composition and mitigate lithogenic potential.

In Vivo Studies

• Preclinical Animal Model Studies for Gallstone Therapeutic Development
  Through established high-cholesterol diet induction protocols, we provide robust cholelithiasis models. Coupled with advanced imaging modalities including high-resolution ultrasonography and micro-computed tomography, we perform longitudinal quantification of gallstone burden dynamics (size/number) and precise evaluation of therapeutic dissolution efficacy under physiologically relevant conditions.
• In Vivo Bile Secretion Studies Our research platform enables systematic evaluation of drug impact on biliary physiology, including quantitative analysis of bile flow dynamics and detailed compositional profiling of cholesterol, bile acid, and phospholipid concentrations. These assessments provide critical insights into drug-induced modifications of bile homeostasis and their implications for gallstone formation risk.
• Biliary Function Assessment Our research platform enables detailed evaluation of candidate effects on biliary tract motility, employing advanced functional assessments to characterize potential drug-induced biliary dyskinesia. These studies provide critical safety and efficacy data regarding compounds' influence on bile flow regulation.

By providing comprehensive in vitro and in vivo evaluation services, Ace Therapeutics helps pharmaceutical companies and research organizations develop novel therapies for the treatment of cholesterol-based gallstones. If you are interested in our services, please do not hesitate to contact us.

Reference

1. Sun, H.; et al. Factors Influencing Gallstone Formation: A Review of the Literature. Biomolecules. 2022;12(4): 550.

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