Early Results Of Development Program in Nano-Formulated NSAIDs Show Potential For Faster Pain Relief At Lower Doses

Data from Study of Indomethacin Presented to American Headache Society

Several Novel NSAIDs Being Developed by Iroko Pharmaceuticals

WASHINGTON, June 3, 2011 — A novel, lower-dose formulation of indomethacin, a widely used pain reliever, is absorbed faster by the body than a standard formulation and maintains comparable maximum concentrations in the blood despite being administered at a lower dose, according to a study to be reported here tomorrow at the annual meeting of the American Headache Society (AHS).1

The presentation of the study marked the first disclosure at a clinical congress of data from a broader research program that is reformulating a large class of marketed analgesics by means of nanotechnology. Nano-formulations reduce drug-particle size to enhance drug dissolution in the body.

In this Phase I pharmacokinetic study, nano-formulated indomethacin in doses of 20 mg or 40 mg demonstrated a faster time to maximum concentration (Tmax) than a 50-mg dose of standard indomethacin.2 Among patients who fasted ahead of drug administration, the maximum concentration (Cmax) was comparable for 40-mg nano-formulated indomethacin and 50-mg standard indomethacin, and lower for all other doses and feeding states in the study.

As anticipated, under both fasting and fed states, total drug exposure (AUC) was reduced by about 25% when the study subjects received 40-mg nano-formulated indomethacin instead of 50-mg standard indomethacin. Half-life (T1/2) was comparable across all doses, formulations, and feeding states, though slightly higher for 50-mg standard indomethacin under fasting conditions.

Indomethacin, which has been used in various indications for decades, is a member of one of the largest classes of pain medicines, called non-steroidal anti-inflammatory drugs (NSAIDs). To lower the potential for adverse events associated with NSAIDs, both the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) have advised that NSAIDs should be used at their lowest effective dose for the shortest duration of time3,4.

“These early data indicate the promise of re-formulating NSAIDs through nanotechnology,” said Stephen Silberstein, M.D., Professor of Neurology and Director of the Jefferson Headache Center at Thomas Jefferson University. “It is important now to progress studies evaluating the clinical benefit of these compounds.”

Dr. Silberstein continued, “NSAIDs are a mainstay in the treatment of pain, and new formulations to speed pain relief would be a welcome advance in analgesia. Lowering doses may also improve the tolerability and safety of this commonly used class of drugs.”

The study was sponsored by Iroko Pharmaceuticals, LLC, a Philadelphia-based company focusing on scientific innovation in analgesia. Iroko is initiating several Phase III trials of nano-formulated NSAIDs manufactured using the proprietary SoluMatrixä nano-technology of Iroko’s partner, iCeutica, Inc.

All the nano-formulated NSAIDs under development by Iroko are designed for administration at lower doses without compromising onset of action and effectiveness, in keeping with the public-health advisories of the FDA and the EMA.


Notes for editors

1The Pharmacokinetic Parameters of a Novel, Proprietary Nano-formulated Oral Indomethacin – Poster # 129.

2Forty healthy volunteers aged 18 or older participated in this single-dose, randomized, five-period, five-treatment, crossover study. Pharmacokinetics were assessed in fed and fasting states.

3Public Health Advisory – FDA Announces Important Changes and Additional Warnings for COX-2 Selective and Non-Selective Non-Steroidal Anti-Inflammatory Drugs (NSAIDS). July 7, 2005.

4Opinion of the Committee for Medicinal Products for Human Use Pursuant to Article 5(3) of Regulation (EC) No 726/2004, for Non-Selective Non-Steroidal Anti-Inflammatory Drugs (NSAIDS). October 18, 2006.

About Iroko Pharmaceuticals, LLC

Iroko is a pharmaceutical company focused on specialty therapeutic areas. The company acquires, develops and maximizes the potential of currently marketed products on a global basis through focused selling and marketing efforts and product-life-cycle management activities including development of new formulations to improve patient treatment.

Lisa Gray, Managing Partner
Phoenix IP Ventures