'Absorption Enhancer' Technology Shows Promise in Converting Injectable to Oral Drugs

Based on technology licensed several years ago from Elan, Merrion Pharma (Wilmington, NC) has been developing a variety of drug formulations that convert an injectable or infusible drug into a pill. One of these, the bisphosphonate zoledronate (sold by Novartis as Zometa), used for strengthening bone for, among others, bone cancer patients, has undergone a multi-center, Phase II trial, showing that the oral version is as effective therapeutically as the injected version, which is usually dispensed as a monthly infusion. The oral version, which Merrion is calling Orazol, would be dispensed as a weekly tablet.

“We are very pleased with these results,” said John Lynch, CEO, at this year’s Am. Soc. of Clinical Oncology annual meeting, “and we will now work on identifying a licensing partner to complete Phase III development and market the product.”

Coating and absorption

Merrion’s technology, called GIPET (Gastrointestinal Permeation Enhancement Technology) uses an enteric coating to get a drug past the mouth, and then “absorption enhancers” that assist in getting the drug across the duodenal cell membrane in the intestines. The advantages are avoiding the inconvenience and risk of infusion/injection, potentially better patient acceptance, and potentially lower administration costs. Merrion has at least three other formulations in preclinical-to-Phase II status, for osteoporosis, thrombosis and oncology, and several other development projects in its pipeline. It also has a variation of GIPET, called GIRES, to enhance retention of a drug in the intestine. PC