OPKO Biologics Ltd., an OPKO Health company (NASDAQ: OPK), today announced that the first participant has been dosed in a first-in-human Phase 1/2a clinical trial of OPK-8801001, an investigational, long acting human growth hormone receptor antagonist being developed for the treatment of acromegaly. The study is designed to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamic activity of OPK-8801001.

OPK-8801001 is being developed using OPKO Biologics’ stabilizer based technology to extend serum half life and reduce injection frequency, with the goal of once weekly administration. In preclinical studies, OPK-8801001 produced robust, dose dependent sustained suppression of insulin-like growth factor-1 (IGF-1), a key marker of disease activity in acromegaly. In vitro studies also demonstrated potent growth hormone receptor antagonism.

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