Safety, tolerability, pharmacokinetics and pharmacodynamics of multiple ascending doses of the novel long-acting glucagon analogue HM15136 in overweight and obese patients with co-morbidities

Diabetes Obes Metab. 2023 Sep;25(9):2723-2733. doi: 10.1111/dom.15162. Epub 2023 Jun 13.

Abstract

Aim: To evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of multiple ascending doses of the novel long-acting glucagon analogue HM15136 in overweight/obese patients with co-morbidities, with and without type 2 diabetes (T2D).

Materials and methods: This was a phase 1, double-blind, randomized, placebo-controlled, two-part trial with a 12-week treatment period of once-weekly subcutaneous HM15136 (0.02/0.04/0.06 mg/kg). Part 1 included patients with dyslipidaemia and/or hypertension and no T2D. Part 2 included patients with dyslipidaemia and/or hypertension plus T2D.

Results: In part 1, 23/27 (85.2%) patients receiving HM15136 and all patients receiving placebo (9/9 [100%]) experienced a treatment-emergent adverse event (TEAE). Five of 27 (18.5%) patients receiving HM15136 developed anti-HM15136 antibodies. Dose-dependent increases in mean HM15136 serum concentration and fasting plasma glucose (FPG) were observed, as were dose-dependent weight reductions of 0.5%/2.3%/2.6% at doses of 0.02/0.04/0.06 mg/kg, respectively. In part 2, 8/12 (66.7%) patients receiving HM15136 and all patients receiving placebo (4/4 [100.0%]) reported a TEAE. Two (16.7%) patients developed anti-HM15136 antibodies. Dose-dependent increases in mean HM15136 serum concentration were observed. FPG of more than 200 mg/dL was reported in 4/9 (44.4%) and 2/3 (66.7%) patients receiving 0.02 and 0.06 mg/kg, respectively. The 0.06 mg/kg dose was not tolerated in part 2 because of hyperglycaemia. Patients receiving 0.02 mg/kg showed a 0.9% weight reduction. No serious TEAEs leading to discontinuation were reported in either study part.

Conclusions: This study of HM15136 provides a preliminary safety and tolerability profile with initial insights into its efficacy profile.

Keywords: glucagon; hypoglycaemia; pharmacodynamics; pharmacokinetics.

Publication types

  • Randomized Controlled Trial
  • Clinical Trial, Phase I
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Blood Glucose
  • Diabetes Mellitus, Type 2* / complications
  • Diabetes Mellitus, Type 2* / drug therapy
  • Dose-Response Relationship, Drug
  • Double-Blind Method
  • Glucagon / therapeutic use
  • Humans
  • Hypertension* / chemically induced
  • Hypertension* / drug therapy
  • Hypoglycemic Agents
  • Morbidity
  • Obesity / chemically induced
  • Obesity / complications
  • Obesity / drug therapy
  • Overweight / chemically induced
  • Overweight / complications
  • Overweight / drug therapy
  • Weight Loss

Substances

  • Glucagon
  • Hypoglycemic Agents
  • Blood Glucose