Danish firm Novo Nordisk A/S has begun first in man studies for its experimental insulin pill which pill replace the routine injection for diabetics even as India’s Biocon is completing its version of oral insulin for scheduled launch in next 18 months.
Novo Nordisk intends to study its insulin pills NN1952 in 80 diabetics and healthy volunteers to assess the mechanism of the drug in human body.
The aim of the trial, which is conducted in Germany, is to investigate the safety, tolerance, exposure and effect of NN1952 in healthy volunteers and people with type 1 and type 2 diabetes. Results from the trial are expected to be reported in the first half of 2011.
There are many challenges with the development and production of a reliable insulin formulation for oral use. They include avoiding enzymatic degradation in the gastrointestinal tract, overcoming poor spontaneous insulin permeability over the intestinal wall, limiting variability of absorption (caused, for example, by interaction with food), and producing insulin in sufficient scale cost-effectively.
“We still have many challenges to overcome, and it is far too early to say whether or when oral insulin will become an alternative to insulin injections,” says Peter Kurtzhals, senior vice president and head of diabetes research at Novo Nordisk.
NN1952 has been designed to address some of the key challenges relating to oral insulin delivery. Furthermore, it utilises the GIPET (Gastrointestinal Permeation Enhancement Technology) formulation technology from Merrion Pharmaceuticals to facilitate insulin absorption from the gut.
Merrion entered into a development and licence agreement to develop and commercialise oral formulations of Novo Nordisk’s proprietary insulin analogues, using Merrion’s proprietary GIPET technology in November 2008. This is the first development milestone achieved by Merrion under this agreement.
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.