Impact case study database

Inflammatory bowel disease (IBD) is a very substantial global problem, with approximately 6.8 million cases reported in 2017. The first line of treatment is usually oral, enteric-coated mesalazine tablets. Previous mesalazine products, however, showed sub-optimal therapeutic effects due to the inter- and intra-individual variability of the gastrointestinal tract. Without successful drug delivery, surgical removal of parts of the intestine can be the only remaining option; 25-40% of sufferers currently have all or a part of their colon removed. This can also necessitate the use of stoma bags that negatively impact quality of life.

PHLORAL^TM and OPTICORE^TM, developed by the Basit group, represent the world’s first dual trigger colonic coating technology. The coatings were the subject of patent applications in 2007 and 2012 respectively, which has since been granted worldwide, including publication of the European Patent in November 2017 [S1]. The licence granted to Tillotts Pharma AG in 2007 for treatment of ulcerative colitis (UC) using mesalazine was the next generation of their current product ASACOL^TM, the market-leading product for treatment of this condition. Phase III clinical trials [S2], which commenced in August 2013 and were conducted with 823 patients with active UC, have demonstrated the effectiveness of the novel coating approach and its superiority to currently available pharmaceuticals in terms of consistent and precise colonic drug targeting. In addition, the new product is formulated with the highest dose of any oral product in the world, containing 1.6g of drug in a single dosage form. Specifically, the study “ showed that once-daily ASACOL™ 1600 mg (mesalazine) is effective for the induction and maintenance treatment of mild to moderate UC with 22.4% of the enrolled patients in clinical and endoscopic remission at week 8 when treated with a 3.2 g/day regimen (2 tablets, once-daily). Data from the open label extension study showed that the extended treatment with 1.6 g/day (1 tablet, once-daily) is effective for the maintenance of clinical remission. At week 38, 70% of the patients, in remission after induction, maintained remission” [S3]. In the same press release, the Chief Scientific Officer of Tillotts Pharmaceuticals Johannes Speiss states, “the development of ASACOL™ 1600 mg was made possible due to the incorporation of the new OPTICORE™ technology.” Following the success of the trials, the new generation ASACOL^TM 1600mg product was successfully launched in 2018 as OCTASA 1600^TM in the UK and ASACOL 1600^TM, YALDIGO 1600^TM and ASACOLON 1600^TM worldwide, including 19 EEA countries . While specific sales figures are commercially sensitive, the mesalazine formulations (the existing 400mg and 800mg enteric coated formulations and the novel 1600mg formulation) are together worth USD155,000,000 in annual sales [S4]. Zeria, the company that owns Tillotts Pharmaceuticals, state in their 2020 Business Report that despite a local sales decreases (in Japan), global sales of the ASACOL^TM products increased from 2019 and ascribe that growth to the introduction of ASACOL^TM 1600 [S4].

In 2014, the PHLORAL^TM technology was also licensed to Biokier Inc. for the formulation of the novel treatment for Type II diabetes, BKR-013. The Chief Executive of BioKier Inc. commented: “ The UCL Phloral^TM coating, which allows for targeted delivery of pharmaceutical ingredients to the colon, is essential for the development of this drug” [S5]. The drug formulation, using the PHLORAL^TM technology, has recently undergone a four-week triple blind study indicating significant improvement in insulin sensitivity within the treated patient group [S6].

In addition, the development of PHLORAL^TM and the advancements of treatments targeted for the gastrointestinal tract has led to the genesis of the spin-out company Intract Pharma [S7] following a GBP1,000,000 investment in 2015 from Cycle Pharmaceuticals based in Cambridge. Intract Pharma, founded by Professor Abdul Basit who also sits on the Board of Directors, is now a rapidly growing biotech which employs 9 members of staff as of September 2020, with a turnover of GBP1,000,000 per year. The PHLORAL^TM technology is also currently accessed by 15 pharmaceutical companies by virtue of licensing deals, options or contracts to date. Licence payments to Intract Pharma are connected to fee-for-service contracts performed with external early-stage start-ups through to small/mid-range biotech firms and global large Pharma. Intract performs development studies to create novel products on behalf of these companies with partnerships across USA, Europe, India and Korea.