We apply our proprietary oral drug delivery technologies and capabilities to the development of both new chemical entities and differentiated formulations of existing products, in order to provide clinical benefits for patients, to offer additional proprietary protection to innovators, and to support life cycle management.

Our oral drug delivery technologies are used in ten approved products that are currently sold in numerous different countries by many of the world’s leading pharmaceutical companies.

We also have a number of oral products in various stages of development, some of which are available for licensing.

Approved oral products

There are 10 approved oral products that incorporate our drug delivery technologies that are currently sold in more than 80 different countries by many of the world’s leading pharmaceutical companies, as listed in the table below.

Technical Challenge

Our Solution

Benefit

Product Examples

Zero order release

Geomatrix™ 

Once or twice daily dosing 

Paxil CR™
Requip® Once-a-day
Coruno®
Xatral®/Uroxatral®

Biphasic release  

Geomatrix™ 

Rapid onset followed by sustained duration

Diclofenac-ratiopharm® uno
Zyflo CR® 

Controlled release of several drugs in a single tablet

Geomatrix™   

Several drugs that need to be released at different times or different rates can be combined in a single dose form

Madopar® DR

Ascending profile

Geomatrix™   

Absorption of drugs in the lower GI tract

 Sular®

Multiple pulses

Geoclock™

Two or more pulses of drug release separated by periods of no release

Suitable for drugs having undesirable side effects that can be minimised at certain times of the day

 

Timed release

Geoclock™

The drug effect can be achieved at a pre-determined time after administration

RAYOS®/LODOTRA®
SKP-1041 
SKP-1052

Colonic delivery

Geoclock™

Delivery to the colon where absorption of specific drugs is high or for topical effect in the colon

 

Improved bioavailability and food effect

IDD®
DissoCubes™

Improvement of bioavailability of BCS II and BCS IV drugs

Triglide®

Buccal delivery

Medicated chewing gum

Buccal absorption for improved systemic delivery or local effect

 

 

RAYOS®/LODOTRA®

LODOTRA® (RAYOS® in US), the novel programmed-release formulation of low-dose prednisone, utilises our proprietary Geoclock™ technology.

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Partner: Horizon Pharma, Inc.

Technology challenge

Prednisone is a widely used anti-inflammatory drug for the treatment of moderate to severe rheumatoid arthritis in adults, particularly when accompanied by morning stiffness. The challenge was to develop a new formulation of the drug that released prednisone into the bloodstream in the early hours of the morning to suppress proinflammatory cytokine levels when they are at their peak. The objective was to reduce early morning stiffness.

Our solution

We applied our proprietary Geoclock™ oral drug delivery technology in order to delay the release of prednisone from the tablet for four hours after ingestion. This allows the patient to take the drug at bedtime, whilst the active ingredient is released during the early morning hours to suppress pro-inflammatory cytokines at their peak production.

Outcome

We were able to develop a formulation that can be taken by patients at bedtime and rapidly releases the active drug four hours later. This results in anti-inflammatory activity in the early hours of the morning.

The product was launched in its first market, Germany, in 2009 and subsequently in other European and Asian markets and the US. Horizon has licensed its rights to the product in Europe and some other markets to Mundipharma.

 

Madopar DR®

Madopar® DR incorporates our proprietary Geomatrix™ technology. It is approved for sale in Switzerland where it is marketed by Roche.

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Partner: Roche

Technology challenge

Levodopa and benserazide are used in Parkinson’s disease to increase the levels of dopamine in the brain as dopamine is thought to cause the disease's symptoms. A rapid onset of action together with a prolonged duration of action is desired for the treatment of Parkinson’s disease.

Our solution

We applied our proprietary Geomatrix™ oral drug delivery technology to change the way in which levodopa and benserazide were released from a tablet. The three-layered matrix tablet releases a fraction of levodopa and benserazide within an hour, and then further amounts of levodopa continuously over six hours¹. This was designed to have a steadying effect, particularly on the “on-off” phenomenon that is seen in Parkinson’s disease patients.

Outcome

The product has been available since 1997 in Switzerland as a formulation that combines a rapid onset of action with high bioavailability.

¹Crevoisier, C et al; European Journal of Pharmaceutics and Biopharmaceutics 55 (2003) 71-76.

 

Paxil CR™

Paxil CR™ is an improved oral formulation of GlaxoSmithKline's Paxil™ (paroxetine), a leading selective serotonin reuptake inhibitor antidepressant. The product uses our proprietary Geomatrix™ technology.

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Partner: GlaxoSmithKline (GSK)

Technology challenge

Paroxetine is a leading selective serotonin reuptake inhibitor antidepressant. The challenge was to develop a new formulation of the active drug to improve patient compliance and reduce side effects.

Our solution

We applied our proprietary Geomatrix™ oral drug delivery technology to paroxetine to sustain the release of the drug from the tablet and to reduce the local concentration in the gastrointestinal tract.

Outcome

We were able to develop a formulation of the product that can be taken by patients once a day. In clinical trials this resulted in a significant reduction in the dropout rate due to adverse events and improved efficacy. Once daily formulations are also known to improve patient compliance.

The product was launched in the US in 2002 and is currently sold in more than 40 markets worldwide by GSK. The product was approved in Japan in 2012 as one of the first once-a-day antidepressant products.

 

Requip Once-a-day®

Requip® Once-a-day is a formulation of ropinirole that uses our Geomatrix™ technology, that was developed in partnership with GlaxoSmithKline. The product is designed to provide smoother delivery of ropinirole over 24 hours without the peaks and troughs that multiple-daily doses invariably deliver¹. In addition, the product offers a convenient, once-daily dosing schedule compared with the immediate-release ropinirole, which is dosed three times a day.

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Partner:GlaxoSmithKline (GSK)

Technology challenge

Ropinirole is a treatment for Parkinson’s disease that is typically taken three times a day. Administration of multiple daily doses of drugs typically leads to peaks and troughs in the amount of drug in the blood stream which can affect symptomatic control. The challenge was to develop a formulation that allowed once-a-day dosing whilst maintaining therapeutic control.

Our solution

We applied our proprietary Geomatrix™ oral drug delivery technology to provide a once-daily formulation that provided smoother delivery of ropinirole over a 24-hour period, whilst avoiding the peaks and troughs that multiple daily doses typically deliver.

Outcome

The product is marketed in more than 40 countries by GSK, including the US where it was the first once-a-day oral non-ergot dopamine agonist indicated for Parkinson’s disease. It was approved in Japan in 2012 as one of the first once a day treatments for Parkinson’s disease.

¹Tompson D et al; Clinical Therapeutics 2007: 29 (12): 2654-2666

 

Xatral®/Uroxatral®

Xatral®/Uroxatral® is a once-daily version of Sanofi's alfuzosin hydrochloride, that incorporates our proprietary Geomatrix™ oral drug delivery technology.

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Partner: Sanofi

Technology challenge

Alfuzosin is a treatment for the signs and symptoms of BPH (benign prostatic hyperplasia), a common condition affecting middle-aged and older men. The challenge was to develop a once-daily formulation to improve patient convenience and adherence.

Our solution

We applied our proprietary Geomatrix™ oral drug delivery technology to alfuzosin to change the way in which the drug was released from the tablet¹.

Outcome

We were able to develop a formulation of alfuzosin that can be taken by patients once a day. Once-daily formulations offer more convenience to patients and generally improve adherence.

The product was first launched in 2000 and is currently sold in more than 60 countries, including the US, Europe, Africa and Asia.

¹De Nunzio, C et al; Clin Drug Invest 2005; 25 (6): 359-365.

 

Sular®

Sular® (nisoldipine) is a calcium channel blocker antihypertensive agent that incorporates Skyepharma’s proprietary Geomatrix™ oral drug delivery technology.

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Partner: Shionogi Pharma Inc

Technology challenge

In 2006 Shionogi Pharma wanted a low-dose version of its the- leading calcium channel blocker for the treatment of hypertension.

Our solution

We applied our proprietary Geomatrix™ oral drug delivery technology to initiate a fast-track development programme to improve bioavailability by optimisation of the target drug release profile.

Outcome

The new product was approved by the US FDA in January 2008, and was launched in the US soon afterwards.

 

Zyflo CR®

Zyflo CR® is an oral anti-inflammatory asthma drug marketed by Cornerstone Therapeutics. The product incorporates Skyepharma’s proprietary Geomatrix™ oral drug delivery technology that allows the dosing to be reduced from four times a day to twice-a-day.

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Partner: Cornerstone Therapeutics, Inc.

Technology challenge

Zileuton is an oral leukotriene synthesis inhibitor drug for asthma that is typically administered four times a day. The challenge was to develop a formulation that allowed twice a day dosing.

Our solution

We applied our proprietary Geomatrix™ oral drug delivery technology to modify the release characteristics of zileuton from the tablet. We formulated the tablets in a way that the drug is released over a period of approximately 10 hours in order that a twice-daily regimen was possible.

Outcome

The product received regulatory approval by the US FDA in 2007 and is available in a twice-daily dose form.

 

Triglide®

Triglide® is an oral treatment for elevated blood lipid disorders, marketed in the US by Shionogi Pharma. It was formulated using our proprietary Insoluble Drug Delivery (IDD®) technology to allow the product to be taken independently of food ingestion.

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Partner: Shionogi Pharma, Inc.

Technology challenge

Fenofibrate is an oral fibrate that markedly reduces elevated plasma concentrations of triglycerides. It also decreases low density lipoprotein (LDL) and total cholesterol. However, fenofibrate is insoluble in water, which may result in a variable uptake from the stomach and so require the tablets to be taken with food. Shionogi wanted to develop a form of the product that could be taken independently of food.

Our solution

We applied our proprietary IDD® technology to fenofibrate, resulting in comparable absorption without regard to food.

Outcome

We were able to develop an improved formulation of fenofibrate that allows patients to take the drug separately from food intake, thereby providing a simpler dosing regimen. The product is marketed by Shionogi Pharma in the US.

The product is available for licensing outside of the US.

 

Coruno®

Coruno® (molsidomine) is an oral treatment for chronic angina pectoris. It incorporates Skyepharma’s proprietary Geomatrix™ oral drug delivery technology in order to offer a once-daily formulation.

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Partner: Therabel

Technology challenge

Molsidomine is an oral treatment for chronic angina pectoris. The challenge was to develop a once-daily formulation to offer a better plasma concentration plateau than the existing twice a day formulation of the product.

Our solution

We applied our proprietary Geomatrix™ oral drug delivery technology to molsidomine to change the way in which the drug was released from the tablet at zero order rate.

Outcome

We were able to develop a formulation that can be taken once a day as an alternative to being taken twice a day. Once-daily formulations offer more convenience to patients and generally improve adherence.

The product is marketed in several countries in Europe by Therabel, a privately owned Belgium-based company.

 

Diclofenac-ratiopharm® uno

Diclofenac-ratiopharm® uno is a product incorporating Skyepharma’s proprietary Geomatrix™ oral drug delivery technology.

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Partner: Ratiopharm (Teva)

Technology challenge

Diclofenac is a non-steroidal anti-inflammatory drug that is used in the symptomatic treatment of pain and inflammation. In the treatment of pain and inflammation it is desirable to have a rapid onset of pain relief that also lasts for a prolonged period of time.

Our solution

We applied our proprietary Geomatrix™ oral drug delivery technology to change the way in which diclofenac was released from the tablet. The tablet was designed to provide a rapid release of diclofenac to manage the immediate pain, whilst slowly releasing further quantities of the drug over the following hours.

Outcome

Following regulatory approval the product has been available in a number of European countries since 1998, where it is marketed by Ratipharm (Teva).

 

Licensing opportunities

 The following licensing opportunities are available for products that include Skyepharma’s proprietary oral drug delivery technologies.

Project/Product

Indication

Project status

Availability for licensing

SKP-1052

Reduction of nocturnal hypoglycaemia

Successful proof of concept in diabetes patients

Worldwide

Triglide®

Treatment of hypertriglyceridemia

Marketed in the US

Worldwide, except US

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