23rd December 2012
Opportunity to out license MMP-9 inhibitor-related patent IP
Compton Group is looking to outlicense patent IP relating to a natural MMP-9 inhibitor derived from botanical sources. Compton Group owns the IP which was generated through research by academics at Cardiff University in Wales, UK in conjunction with our Research Director, Dr Ahmed Ali.
1. Research
The research team, led by Professor Vic Duance and Dr Emma Blain of Cardiff University, tested an extract from Boswellia frereana in an in vitro model of articular cartilage degradation using the pro-inflammatory cytokines interleukin-1 alpha and oncostatin M; the extract reduced collagen degradation and inhibited the production of several key cytokine-induced inflammatory markers, including prostaglandin E2 (PGE2) and nitric oxide (NO); more importantly, the extract significantly inhibited in the model the expression and activation of matrix metalloproteinease-9 (MMP-9). Further work has demonstrated that the active compound in the extract is epi-lupeol. More detail on this research work can be found in the article on B. frereana in the June 2010 edition of Phytotherapy Research.
2. Frankincense
The sap from the Boswellia tree is commonly known as frankincense in the flavour and fragrance industry and as olibanum in the pharmaceutical industry. The US FDA has approved the resin extract as a food additive (i.e. EAFUS status) and classified the essential oil as GRAS.
A fundamental characteristic of the Boswellia species is the presence of boswellic acids, which are well known for their anti-inflammatory properties; however, the striking feature of B. frereana (which is native to northern Somalia) is that it contains no detectable level of boswellic acids; instead 60% of the resin comprises epi-lupeol which is also present in other plants, such as the Mexican Copal Sonora, so that it would not be necessary to rely on the Horn of Africa as a source of supply.
3. The patent application
The reference of the patent application is PCT/GB/2010/001286 [WO2011/010080], now pending in Europe, USA and China.
There is a great deal of prior art on the anti inflammatory properties of lupeol, of which epi-lupeol is an isomer. However, tests have been carried out which show that epi-lupeol is far more effective than lupeol in inhibiting the expression of MMP-9. Using a cell-free MMP-9 colorimetric drug discovery ELISA, epi-lupeol was observed to have between 4 and 7 – fold greater efficacy than lupeol in inhibiting MMP-9 (fold changes dependent on epi-lupeol/lupeol concentrations). Increased MMP-9 inhibition by epi-lupeol, compared with lupeol, was also confirmed in the in vitro inflammatory model of articular cartilage degradation.
4. Applications
The initial research work was confined to arthritis models. However, given that inflammation is implicated in a wide variety of diseases and that epi-lupeol is effective at inhibiting MMP-9, further work has been, and is being, done on other applications. To give just one example, in animal trials involving a murine model of acute Sodium Dextran Sulphate – induced colitis, it was found that the shortening of the colon was reduced by 27% for mice treated with an extract from B. frereana when compared with a saline treated group.
One possibility for the development and commercialisation of the IP could be to concentrate (at least initially) on an application which qualifies for orphan drug status so that regulatory costs and time to market can be minimised.
5. Type of deal (subject to contract)
Compton Group has 100% control of the IP contained in the patent application; we can reach decisions quickly.
We are prepared to outlicense exclusively all of the IP in all of the territories currently covered by the patent application for the nominal sum of 1 US dollar now, in return for which we would look to the licensee to use reasonable endeavours to push forward, at its own cost, with the commercialisation of the IP. We would not expect any financial return until the IP is generating revenue, but, if it is commercialised, we would look for a royalty percentage based on sales, such percentage to escalate according to stepped sales thresholds.
We are looking for this type of deal because we believe that there could be substantial rewards further down the line and we are prepared to forego immediate returns for higher future rewards. Furthermore, we recognise that we will require a partner with far greater resources than our own to take forward the IP.
6. Further enquiries
Should you have any technical queries, please contact our Research Director, Dr Ahmed Ali, by e-mail on alia@cardiff.ac.uk. Otherwise, please feel free to contact me. Clearly, if you wish to go into more detail on the additional research work, a confidentiality agreement will be necessary.
I look forward to hearing from you.
Angela Coyle
Head of Group Marketing, Compton Group
Tel: 01792 315482, Fax: 01792 315513