The Phase II trial may start as early as next week and will involve approximately 600 patients, Chief Science Officer Mads Krogsgaard Thomsen said on Thursday.
“It is a milestone because this is not incremental innovation, it’s disruptive innovation,” he told Reuters in an interview during a visit to London.
Results of the study are expected in around a year’s time.
The Danish company is already the world’s biggest supplier of diabetes medicines, which include its popular GLP-1 product Victoza. Like its top-selling insulins, Victoza is currently delivered using a pen injection device.
An oral pill version would mark a step-change in therapy by making treatment far more convenient, opening up a major new market at a time when cases of diabetes are soaring worldwide.
A total of 382 million people are now estimated to be living with the disease. The vast majority have type 2 diabetes, the kind linked to obesity and lack of exercise.
Sales of diabetes drugs were worth $42.4 billion worldwide in 2012, according to healthcare information company IMS Health.
Glucagon-like peptide-1 (GLP-1) drugs work by stimulating the release of insulin when blood sugar levels become too low.
Novo’s Victoza is the market leader, with sales last year of 9.5 billion Danish crowns ($1.7 billion), but it faces increasing competition, including from a potential new rival from Eli Lilly called dulaglutide.
Making an oral form of such drugs is far from simple and a key hurdle is to ensure that the medicine is adequately absorbed in the body.
Thomsen said the technical challenges meant there might be setbacks in the development program but he was increasingly optimistic that producing an effective GLP-1 pill was feasible.
“The data we have so far suggests we can do it,” he said, adding that Novo was well ahead of rivals in the field.
The 600-patient trial will compare the new once-daily GLP-1 pill against a weekly injection of a GLP-1 medicine, known as semaglutide, that Novo currently has in Phase III trials.
If all goes well, Novo believes the GLP-1 pill could hit the market in around five or six years time.
Novo is also working on an oral version of insulin but that is at an earlier stage, with a decision on progressing into Phase II testing still around a year away.
After two decades of outperforming its pharmaceutical industry rivals, shares in Novo have stalled this year following setbacks for a new long-acting insulin and worries over the prices its products can command.