Long acting oral insulin pill NN9924 in clinical studies: Novo Nordisk

Novo Nordisk has begun the first-in-man studies for its long acting oral diabetic pill NN9924, the company announced.

NN9924 is Glucagon-Like Peptide-1 (GLP-1), a protein which is normally administered into the body through injection.

GLP-1 (Glucagon-Like Peptide-1) is a natural hormone involved in controlling blood sugar levels. It stimulates the release of insulin only when blood sugar levels become too high. In people with type 2 diabetes, GLP-1 secretion is often impaired.

There are many challenges in developing a formulation of GLP-1 for oral use, in particular obtaining adequate bioavailability (absorption of the drug in the body).

NN9924 addresses some of the key challenges, and utilises the Eligen formulation technology from Emisphere to facilitate GLP-1 absorption from the gut.

Novo Nordisk has initiated its first phase 1 clinical trial with a long-acting oral GLP-1 analogue (NN9924).

This milestone releases a 2 million dollar payment to Emisphere Technologies, Inc., whose proprietary Eligen Technology is used in the formulation of NN9924.

Eli Lilly and Amylin Pharmaceuticals have a GLP-1 drug on the market in the United States, while GlaxoSmithKline, Roche are in the process of developing the next generation GLP-1 products to treat diabetes.

The trial, which is conducted in the UK, is to investigate the safety, tolerability and bioavailability of NN9924 in healthy volunteers.

Results from the trial, which is planned to enrol about 155 people, are expected to be reported in 2011.

“We still have a long road with many challenges ahead of us before a GLP-1 pill becomes a reality,” stated Peter Kurtzhals, senior vice president and head of diabetes research at Novo Nordisk.

In June 2008, Novo Nordisk and Emisphere entered into a development and licence agreement to develop and commercialise oral formulations of Novo Nordisk’s proprietary GLP-1 analogues, using Emisphere Eligen Technology. This is the first development milestone achieved by Emisphere under this agreement.

Novo Nordisk has another GLP-1 anaologue liraglutide (Victoza) in markets. Liraglutide is a once-daily human GLP-1 analogue.

Meanwhile, India’s leading biotherapeutics firm Biocon Ltd’s oral insulin pill is currently undergoing late phase human studies.

Biocon plans to begin commercial production within 18 months, stated Biocon’s managing director Kiran Mazumdar- Shaw, in an interview given to a leading newswire.

Insulin pill, IN-105, in  which is in the final phase 3 stage of patient studies.

Insulin pill IN-105, if comes out successful in patient studies, will have huge potential with a certainty to become a multibillion dollar blockbuster.

“This is a product that we see to be a game-changer. It has huge potential and certainly can be a multibillion dollar blockbuster,” stated Mazumdar-Shaw, adding that she is “confident” of the outcome despite mounting skepticism about whether orally formulated insulin hormone would really do the job.

Insulin pills which could actually save millions of diabetics around the world from the wexing daily pricks have been one of the hot pursuits of drugmakers across the globe.

Efforts to produce needle-free delivery of insulin has come to a naught, so far. Exubera, an inhaled insulin product from world’s top drug maker Pfizer Inc was withdrawn in 2007 after it failed in the market.

Biocon presented the phase IIa trial data of its insulin pill IN 105 at the European Association for the Study of Diabetes meeting in Rome in Sept last year, suggesting that for the first time, oral insulin has shown good dose linearity – the effect of the drug is proportional to the units consumed.

Insulin pill IN-105 studies conducted in India showed a near-perfect linear dose response. IN-105 has also shown a significant two-hour post-prandial glucose drop indicating that the insulin pill has potential in demonstrating efficacy in longer-term trials.

Insulin pill IN105 is formulated as a tablet using a proprietary polymer technology, acquired by Biocon from US firm Nobex Corp. Nobex, whose IP assets were later bought by Biocon when it filed for bankruptcy in 2005, technology platform allows modification in the insulin structure so as to enable it suitable for oral delivery.

Insulin pill IN-105 also ensures better patient compliance, because it is not an injection. Further, injectable insulin has a tendency to get deposited under the skin leading to weight gain, oral insulin, gets around this dangerous problem through being either weight-neutral, or weight loss.

Insulin pill IN-105 is rapid acting and so it can cut down the problem of hypoglycemia, a common  complication with injectable insulin.

Except from Biocon, no other insulin in oral form is currently in final stages of commercialization. Oralyn, an insulin spray to be delivered under tongue (buccal) developed by the Toronto, Canada-based Generex Biotechnology Corp is probably the only other product being marketed in some parts of the world including India by Shreya Life Sciences Pvt. Ltd, Mumbai.

Biocon expects to report the results of phase-3 studies in the first quarter of next year.

Global insulin market is expected to grow 15 percent annually through 2010, predicts New York-based MarketResearch.com.

Nearly 246 million people are suffering from diabetes worldwide, according to the International Diabetes Federation. India has the highest number of diabetes patients in the world- nearly 41 million sufferers, followed by China and the U.S.
Novo Nordisk is a healthcare company and a world leader in diabetes care. In addition, Novo Nordisk has a leading position within areas such as haemostasis management, growth hormone therapy and hormone replacement therapy.

Emisphere is a biopharmaceutical company that focuses on the unique and improved delivery of therapeutic molecules or nutritional supplements using its proprietary Eligen® Technology. The Eligen Technology can be applied to the oral route of administration as well as other delivery pathways such as buccal, rectal, inhalation, intra-vaginal or transdermal.

http://www.dancewithshadows.com/pillscribe/biocons-insulin-pill-for-launch-in-18-months-says-kiran-mazumdar-shaw/