Abstract
This study aimed to explore pharmacokinetics, pharmacodynamics, and safety/tolerability of MT921, an injectable cholic acid, after a single subcutaneous administration to healthy volunteers. A randomized, double-blinded, placebo-controlled, single dose-ascending phase 1 study enrolled 24 subjects who were assigned to three groups (60 mg, 120 mg, and 150 mg) of MT921. Blood samples were obtained for a 24-h period before and after injecting MT921 to the submental fat area. Plasma concentrations of cholic acid and deoxycholic acid were determined for pharmacokinetic analysis. Levels of free fatty acid, triglyceride, and total cholesterol were measured for pharmacodynamic analysis. Safety and tolerability were assessed until 21 days post-dose. While systemic exposure to cholic acid tended to increase as the MT921 dose increased, pharmacokinetic profiles of deoxycholic acid were similar among dose groups without showing significant changes. Pharmacodynamic profiles were comparable when measured at baseline and post-dose. The most frequent adverse events were injection site pain and edema. All adverse drug reactions resolved without treatment. MT921 appeared to be well-tolerated after an injection to the submental area at a dose up to 150 mg. Systemic exposure to cholic acid increased as the dose increased. Blood lipid profiles and deoxycholic acid levels were not affected by MT921 treatment.
Highlights
The submental line is one of the criteria that determines a youthful neck [1]
Systemic exposure to cholic acid increased as the dose of MT921 increased, while that to deoxycholic acid was similar without showing significant differences among dose groups (Supplementary Figure S1, Table 2)
Data are presented as [Number of subjects] and median of duration as days. This is the first report on a clinical study of MT921 composed of cholic acid to provide the results such as safety, tolerability and pharmacokinetic profiles along with baseline-adjustments as well as information from the metabolic product, deoxycholic acid, in humans
Summary
The submental line is one of the criteria that determines a youthful neck [1]. Due to the aging process, obesity, and genetic factors, undesirable neck contour by submental fat can appear [2]. In the United States, 63,993 procedures of injection lipolysis were conducted in 2018 with a total expenditure of more than USD 67 million, showing a rising trend [5]. Surgical options such as liposuction have been used for submental fat reduction. Deoxycholic acid was approved in 2015 as a pharmacological agent in the United States of Pharmaceuticals 2021, 14, 830. Injectable cholic acid has not been approved for medical use. Provided that cholic acid injection brings adequate clinical efficacy, it might be a drug of choice for reducing submental fat with less cytotoxicity than deoxycholic acid. The aim of this study was to explore pharmacokinetics (PK), pharmacodynamics (PD), and safety/tolerability of MT921 in healthy adults after a single administration to submental fat
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