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Oral delivery of macromolecules: rationale underpinning Gastrointestinal Permeation Enhancement Technology (GIPET).
A summary of some approaches taken to intestinal permeation enhancement is presented and the oral delivery system developed by Merrion Pharmaceuticals, Gastrointestinal Permeation Enhancement Technology (GIPET) is explored.
Oral administration of the GnRH antagonist acyline, in a GIPET®-enhanced tablet form, acutely suppresses serum testosterone in normal men: single-dose pharmacokinetics and pharmacodynamics
Oral administration of GIPET®-enhanced acyline significantly suppresses testosterone and gonadotropins in normal men without untoward side effects and might have utility in the management of prostate cancer.
MER-104 tablets: a dose-ranging study of an oral formulation of a gonadotropin-releasing hormone antagonist, acyline.
Therapeutically-effective levels of a decapeptide GnRH antagonist, acyline, can be achieved using an oral delivery platform, GIPET™, and indicate that MER-104 tablets may have potential in the treatment of prostate and breast cancer, endometriosis, prostate hypertrophy, and as part of a male contraceptive regimen.