Celtic Pharma declares Transfersome carrier interest

IDEA's Transfersome technology consists of ultra deformable vesicle carriers designed to deliver drugs non-invasively through the skin barrier. Transfersomes can be applied to target muscles and joints below the application site without being cleared by the local cutaneous blood microcirculation.

This enables the targeted and non-invasive delivery of drugs (including large molecules such as proteins) through the skin, with a particular focus on pain relief and dermatology.

IDEA are applying this technology to one of its proprietary compound, IDEA-033, currently in phase III trials in Europe for the treatment of peripheral pain.

Given the well-publicised side effects of COX-2 pain relievers, IDEA-033's has the potential to be an important product in non-steroidal anti-inflammatory drugs (NSAIDs) markets worldwide.

The resulting targeted drug delivery of IDEA-033 can increase product efficacy (having higher local drug concentration) and improve product safety (having lower systemic drug concentration) in comparison with existing oral and/or topical NSAID formulations.

IDEA-033 is expected to become the first, truly effective, topical analgesic on the market for treating peripheral chronic pain, such as that caused by osteoarthritis.

Worldwide sales of non-steroidal anti-inflammatory drugs (NSAIDs) are estimated to be €14 billion.

Approximately 30 million people worldwide take oral NSAIDs on a daily basis and until recently, COX-2 inhibitors were seen by broad opinion as a relatively safe arthritis treatment option.

"IDEA's clinical data show that the Transfersome technology represents a powerful tool for delivering drugs through the skin and for achieving tissue specific drug action,​ said John Mayo, a managing principal of Celtic Pharma.​

"Our exposure to IDEA-033 represents the fifth late stage development product investment for Celtic Pharma during 2005."​

NSAIDs have become the gold standard for treating the majority of arthritic diseases and chronic pain such as osteoarthritis.

The main disadvantage is that all classic oral NSAIDs carry a risk of upper gastrointestinal (GI) side effects, with up to 30 per cent of long-term NSAID users developing gastric ulcers.

Close to 20,000 osteoarthritis patients and 2,000 rheumatoid arthritis patients in the US alone die each year from GI complications associated with oral NSAID use.

"The fast enrolment, moreover, indicates the unmet medical need for IDEA's product, which avoids the side effects of current analgesic, anti-inflammatory products without compromising on efficacy,"​ said Dr. Matthias Rother, executive head of R&D at IDEA.​

"We believe IDEA will bring the first targeted analgesic, anti-inflammatory topical product for long-term use in osteoarthritis to the market as early as the end of 2007,"​ he added.

Recent worldwide withdrawals of both Vioxx (rofecoxib) and Bextra (valdecoxib), have called into question the safety of the COX-2 inhibitor class. There are now fears that this drug class could lead to serious adverse side effects as well, such as cardiovascular events.

Consequently, the US Food and Drug Agency (FDA) has recently mandated black-box warnings on all prescribed NSAIDs and similar labelling changes for comparable over-the-counter medicines.

Osteoarthritis (OA), the clinical syndrome of joint pain and dysfunction caused by joint degeneration, affects more people than any other joint disease.

It is one of the leading causes of disability, as by the age of 65 an estimated 85 per cent of the population will have some degree of OA.

Oral non-steroidal anti-inflammatory drugs (NSAIDs) are most commonly used to treat OA. Although effective, they cause serious adverse side effects.

Topical NSAIDs, which are marketed in the EU but have never been approved to date in the US, may be seen as generally safer; these formulations were shown, however, to be ineffective for the treatment of chronic pain beyond a two-week treatment duration.