OX382 – oral formulation of buprenorphine

Orexo is developing a swallowable formulation of buprenorphine (OX382). The aim is to be first-to-market in this new product class and to offer clear benefits over today’s treatment options for certain patient categories and treatment settings.

For most treatments without need for immediate absorption of the active ingredient, a swallowable formulation is preferred and generally recognized as the standard formulation. Buprenorphine has poor and unreliable absorption in the gastrointestinal (GI) tract which has so far been the major hurdle to develop a swallowable formulation. Orexo has developed, and filed a patent application for an innovative technology that could address these hurdles and deliver buprenorphine in a controlled and reliable manor in the GI tract.

This new formulation is expected to have several convincing advantages over currently available buprenorphine formulations. Swallowable pharmaceuticals are generally preferred by patients over sublingual or buccal products as they do not have issues with bad taste or local irritation in the mouth. In addition, OX382 would offer specific benefits wherever patients receive their opioid dependence treatment under supervision of a health care professional or a pharmacist. Unlike today, there will be no need to wait for a sublingual or buccal formulation to dissolve in the mouth, allowing for much more efficient processes in the respective clinics. Supervised (opioid dependence) treatment is common in the US, e.g., for patients who receive treatment in methadone clinics, and is particularly common in Europe where about half of opioid dependent patients receive treatment in a monitored setting.

The new unique product could be used in both opioid dependence and pain treatment. The development program is in phase I (first clinical study in humans) with results expected in Q2, 2018. With a positive result of the phase I study Orexo will outline the development plan and priority of potential indications, which will enable more firm guidance on the commercial potential and development risks.

OX-MPI – inflammation

The lead candidate drug in the OX-MPI program, BI1029539, has been identified as a highly selective anti-inflammatory compound targeting microsomal prostaglandin E synthase (mPGES-1).

The OX-MPI program was acquired by Gesynta Pharma AB on September 29 2017. Gesynta Pharma AB is a recently formed research company located in Stockholm, Sweden, and among the founders are highly reputed executives from the biotech industry and experienced researchers at the Karolinska Institute within the field of arachidonic acid pathways and inflammatory diseases. At the time of the acquisition, the project was in the preclinical phase and Gesynta Pharma AB will progress the candidate drug into proof-of-concept clinical trials.

Under the terms of the agreement Orexo will receive a tiered double-digit share of the future revenues that Gesynta Pharma AB generates from the OX-MPI project.

OX51 – acute pain episodes

OX51 is a new sublingual tablet formulation containing alfentanil. The project has been developed to meet the rapidly growing demand for effective pain relief during short surgical and diagnostic procedures.

A placebo-controlled dose-finding study in patients undergoing prostate biopsy was completed in 2013. The results supported a continuation of the development of OX51 to the next phase in development towards a new product. Orexo has decided to discontinue the dialog with the potential partner for OX51 due to disagreement of the key terms reducing the financial attractiveness of a potential agreement. Orexo will have a meeting with FDA during Q1 to assess the required development program and continue the search for a development partner.

New formulation technologies

Novel oral formulation technology

See development project, OX382, above.

 

2nd generation sublingual formulation technology

Orexo is currently developing its second-generation sublingual formulation technology. The aim is to perfect the sublingual delivery of drugs, thereby unlocking new active ingredients that can not currently be administered sublingually. The project is in the exploratory phase, and several active ingredients have been identified as promising candidates for this new technology.

In addition, Orexo has two non-disclosed projects, both of which will also fall into the addiction category and with the aim of providing clear clinical differentiation versus currently available treatment alternatives. Orexo will disclose more details once the final feasibility tests are completed and have shown positive results.