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Subcutaneous injection of ATX-101 offers favorable safety, pharmacokinetic profiles

Researchers found subcutaneous injection of ATX-101 for the reduction of submental fat offered favorable safety and pharmacokinetic profiles, with no clinically meaningful changes in deoxycholic acid, lipids and proinflammatory cytokines.

Ten patients were enrolled in a single center, open-label, phase 1 study conducted in two phases. In stage one, the researchers established baseline endogenous levels of deoxycholic acid (DCA), lipids and adipokines. For stage two, the researchers measured the effects of ATX-101 on these levels. Patients were admitted for stage two at least 3 days, but no more than 10 days, after completing stage one.

The patients received a total dose of 100 mg of ATX-101 injected subcutaneously through a 30-gauge needle into abdominal adipose tissue. Using a grid to ensure even distribution, 50 injections of 0.2 mL a piece were placed 1 cm apart across the area being treated.

Pharmacokinetic evaluation of the patients’ baseline endogenous DCA, lipids and adipokines was performed in both stages of the study, with samples collected at 0.25, 0.5, 1, 1.5, 2, 4, 6, 12, 15.5 and 24.5 hours.

ATX-101 resulted in an approximate twofold increase in mean AUC _0-24 and a 3.6-fold increase in C_max compared with endogenous DCA levels, according to the researchers. On average, DCA plasma concentrations returned to endogenous levels by 12 hours post-ATX-101 administration.

The researchers found no clinically significant differences in lipid pharmacodynamics before vs. after ATX-101 injection for total cholesterol, total triglycerides or free fatty acid plasma levels.

Ten of the patients experienced a total of 41 adverse events, which were mild in severity, and none of the patients discontinued the study for any reason. Injection-site pain, injection-site hematoma and injection-site erythema were among the most commonly reported complaints, present in 12, 10 and eight patients, respectively, according to the researchers. - by Abigail Sutton

Disclosure: Funding for editorial support was provided by Kythera Biopharmaceuticals.