Therapeutic Focus

Inflammatory Bowel Disease
Inventa has a major pre-clinical programme focused on the development of a patented pro-drug formulation of Mesalamine, one of two treatments of choice for Ulcerative Colitis and Crohn’s Disease.

Crohn's Disease and Ulcerative Colitis are the two main forms of Inflammatory Bowel Disease (IBD) and are both chronic conditions. The symptoms vary from person to person and will range from mild to severe and may also change over time, with periods of good health with few or no symptoms (remission) alternating with times when symptoms are more active (relapses or ‘flare-ups’). Common symptoms of IBD include: -

• Diarrhoea sometimes mixed with blood, mucus and pus.
• Cramping pains in the abdomen. These can be very severe and often occur before passing a stool.
• Tiredness and fatigue. This can be due to the illness itself, from anaemia (see below) from the side effects of some of the drugs used for IBD or from a lack of sleep due to pain or diarrhoea.
• Feeling generally unwell / feverish.
• Loss of appetite and loss of weight. Weight loss can be due to the body not absorbing nutrients from the food you eat because of the inflammation in the gut.
• Anaemia (a reduced number of red blood cells) as a consequence of losing a lot of blood and are not eating much.
• Mouth ulcers.

This disease most commonly affects teenagers and young adults but can occur in any age group. The highest reported prevalence of UC and Crohn’s have been in Europe (ulcerative colitis 505 per 100 000 in Norway; Crohn's disease 322 per 100 000 in Germany) and North America (ulcerative colitis 286 per 100 000 in the USA; Crohn's disease 319 per 100 000 in Canada)

The first-line treatment for patients with mild-to-moderate UC is Mesalamine (mesalazine) a 5-aminosalicylic acid compound. There are multiple formulations of mesalamine available, primarily differentiated by their means of delivering active mesalamine to the colon.

The goal of mesalamine treatment of UC is to reduce inflammation in the colon. The drug is effective but current formulations are readily and prematurely broken down in transit to the colon. To overcome this and ensure that therapeutic concentrations of mesalamine reach their target in the colon, the drug dosage and or the dose frequency must be increased. The frequency of dosing reduces patient compliance and the high dosage levels can cause serious adverse effects including, gastric ulcers, hepatotoxicity, nephrotoxicity, pancreatitis and bloody diarrhea.

Inventa’s new treatment for UC (CLX-103A) is designed to produce a slow sustained release of active 5-ASA at the target site (intestine/colon) with reduced systemic exposure to 5-aminosalycilic acid whilst enhancing the anti-inflammatory effects of 5-ASA. CLX-103A is expected to be more efficacious and safer than 5-aminosalicylic acid (5-ASA) at a lower oral dosage compared with the currently marketed formulations of 5-ASA (or its associated prodrugs such as sulfasalazine) thereby significantly improving the compliance rate and beneficial clinical outcomes for patients with UC. The Company plans to focus product development on an oral formulation(s) of CLX-103A as this remains the route of administration preferred by GI physicians. There is however a growing clinical consensus amongst GI opinion leaders that a suppository route of administration would provide clinical benefits in certain circumstances for which reason, the company will consider establishing a second suppository development programme.