Poorly permeable drugs remain a significant formulation challenge for achieving therapeutically-effective oral drug delivery. Gastrointestinal Permeation Enhancement Technology (GIPETTM, Merrion Pharmaceuticals PLC) is a platform technology that addresses this challenge by safely delivering drugs across the small intestine in therapeutically-relevant concentrations. This monograph provides an evaluation of GIPET, with particular emphasis on the use of a simple, inexpensive, preclinical feasibility model to advance formulations into clinical testing.