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The aim of this first\u2010in\u2010human study was (a) to evaluate safety and tolerability, (b) to evaluate pharmacokinetics and (c) to assess indications of receptor engagement of single ascending doses of KBP\u2010042, a dual amylin and calcitonin receptor agonist (DACRA) that has shown promising preclinical data, with superior activity in terms of typical amylin\u2010induced responses including reduction of food intake, weight loss and gluco\u2010regulatory capacities. A randomised double\u2010blind placebo\u2010controlled single ascending dose study was performed with six dose levels of KBP\u2010042 (5, 7.5, 10, 20, 20 (evening), 40 ug) in healthy male adults. KBP\u2010042 or placebo was administered as a single dose after an overnight fast, followed by a standardized lunch after 4\u2009hours. KBP\u2010042 was associated with dose\u2010dependent complaints of nausea and vomiting, with a lack of tolerability at doses of 20\u2009\u03bcg and above. 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