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MC4‐NN2‐0453 is a novel, long‐acting, selective, melanocortin‐4‐receptor agonist developed for treatment of obesity. This first‐human‐dose, randomized, double‐blind, placebo‐controlled trial investigated the safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple doses of MC4‐NN2‐0453 in overweight to obese but otherwise healthy subjects. The trial included a single‐dose part of ascending subcutaneous 0.03–1.50 mg/kg doses in overweight to obese but otherwise healthy men, and a multiple‐dose part of ascending subcutaneous 0.75–3.0 mg/day doses in obese but otherwise healthy men/women. The single‐dose part included 7 cohorts of 8 subjects, randomized 6:2 to active drug/placebo; the multiple‐dose part included 4 cohorts of 20 subjects, randomized 16:4 to active drug/placebo. MC4‐NN2‐0453 was well tolerated and raised no safety concerns except for nonserious skin‐related adverse events, this along with lack of weight loss effect led to premature termination of the trial. Headache, sexual–arousal disturbance, and penile erection were also reported. Single‐dose pharmacokinetics showed dose‐linearity and dose‐proportionality. Maximum plasma concentration was observed after 50–100 hours, which then declined with a  of approximately 250 hours. Plasma concentration reached steady state after 4 weeks for 0.75 and 1.5 mg/day multiple‐dose cohorts, and the  was similar to single dose. There were no significant pharmacodynamic effects, including effect on body weight.

the journal of clinical pharmacology

Investigation of safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple doses of a long‐acting α‐MSH analog in healthy overweight and obese subjects