Octreolin® is being developed first for the treatment of acromegaly, a hormonal disorder that results from an excess of growth hormone. Octreolin is taken as a capsule that contains octreotide acetate as the active peptide ingredient and is formulated using Chiasma's proprietary TPE System, which enables this peptide to be taken orally.
Octreolin successfully completed four clinical studies in healthy volunteers. To date, a total of 74 healthy volunteers received up to 3 separate doses of Octreolin. Studies were conducted in Israel and in the US as an Investigational New Drug (IND). These Phase 1 clinical trials demonstrated that investigational Octreolin has a phrarmacokinetic (PK) profile similar to that of the commercially available subcutaneously injected octreotide acetate and a pharmacodynamic (PD) effect of reducing growth hormone. No serious adverse safety events were reported in any of the studies in which we demonstrated the following:
Octreolin® was absorbed after oral administration within 1 hour;
There was a reproducible linear dose-dependent relationship for the 3 doses studied;
An oral dose of the investigational Octreolin® 20 mg provided similar systemic exposure to the commercially available octreotide 0.1 mg given via subcutaneous (SC) injection;
Study subjects reported no serious adverse events, no other safety concerns and good tolerability of Octreolin®;
Side effects of investigational Octreolin® were comparable to those of the commercially available injectable octreotide;
Octreolin® administered to healthy subjects significantly (P<0.001) suppressed basal GH secretion and Growth Hormone Releasing Hormone (GHRH)-stimulated GH secretion by about 80%.
Chiasma Pivotal studies (Phase 3) enrollment began in Q4 2011.