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ONO-5788 is a novel, orally administered small molecule that acts as a potent and selective agonist of the human somatostatin receptor type 2 (SST2). It was developed by Ono Pharmaceutical for the treatment of acromegaly and potentially other conditions where somatostatin analogues are indicated. Unlike existing somatostatin analogues, which require parenteral administration, ONO-5788 offers an oral route of delivery. Preclinical studies demonstrated that ONO-5788 and its active metabolite (ONO-ST1-641) significantly attenuate growth hormone (GH) hypersecretion in human GH-secreting pituitary adenoma-derived cells by activating SST2 receptors. Clinical trials showed favorable safety and pharmacokinetic profiles in healthy volunteers, with mild to moderate gastrointestinal adverse events at higher doses. Despite promising early results, development for acromegaly was discontinued after phase 1 trials[1][3][4][5][6].
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