Chiasma presents Octreolin pharmacology data from clinical studies at International Pituitary Congress

Jun 6 2011

Chiasma, Inc., a privately held biopharma company, presented pharmacology results from clinical studies at the 12th International Pituitary Congress showing that Octreolin, a proprietary investigational new oral formulation of octreotide, demonstrated a consistent pharmacokinetic (PK) profile similar to that of subcutaneously injected octreotide acetate. Most important, the data illustrated that Octreolin reduced growth hormone (GH) levels, a clinical endpoint that has been used for approval in other drugs for acromegaly.

Chiasma is developing Octreolin as an oral treatment for acromegaly and anticipates that a Phase 3 trial in patients will begin enrollment later in 2011.

Pharmacodynamic data presented at the Congress demonstrated that a single dose of Octreolin administered to healthy subjects significantly suppressed both basal GH secretion and Growth Hormone Releasing Hormone (GHRH)-stimulated GH secretion by about 80%. Inhibition was recorded in all 18 subjects receiving Octreolin as compared to their GH levels without Octreolin. The mean reductions in both basal and stimulated GH levels were statistically significant (P<0.001).

In addition, the presentation summarized results from three clinical studies with Octreolin. These data showed that:

• 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 Octreolin 20 mg provided similar systemic exposure to octreotide 0.1 mg given via subcutaneous (SC) injection;
• The drug was well tolerated with no significant clinical or preclinical adverse events;
• Side effects of Octreolin were comparable to those of injectable octreotide.

Octreolin utilizes the Company's proprietary Transient Permeability Enhancer (TPE) technology, which enables previously injectable-only drugs to be taken orally.

Sam Teichman, MD, Chiasma's Chief Medical Officer and presenter at the Congress said, "In addition to the GH reducing effect observed in the trial conducted in the United States under an Investigational New Drug (IND), no significant Octreolin or TPE-related adverse findings were reported in two toxicology studies in primates and, therefore, the No Adverse Event Level (NOAEL) was established at the highest Octreolin dose tested. This clean safety profile paves the way for further Octreolin development with chronic therapy in patients and continues the validation of the safety profile of the underlying technology platform.

"If the results of the Phase 3 program are positive, the Company intends to submit a New Dug Application (NDA) using the 505(b)(2) NDA regulatory pathway in the U.S. and its European Medicines Agency (EMA) equivalent, the Hybrid Application, in Europe."