Gordagen confirms bioavailability in phase I study for evidence-based nutraceuticals

Gordagen Pharmaceuticals, a privately held company commercialising evidence-based nutraceuticals and pharmaceuticals, has announced results for the first part of its Phase I clinical trial, a single ascending dose pharmacokinetics (PK) study, with the company preparing results for publication.

The study assessed the company's 'melt-then-swallow' technology (MELT3), which is a formulation based on annatto-derived tocotrienols.

'The successful completion of this first part of the Phase I clinical trial is a major milestone in our product development programme for evidence-based nutraceuticals. Results from this recent trial provide strong support for the benefits of our MELT3 tablets as a new proprietary and patent-pending tocotrienol formulation that is close to commercial launch in the US, and also demonstrate safety and tolerability among healthy volunteers,' said Dr Glenn Tong, Gordagen's Managing Director and Chief Executive Officer.

'Importantly, the data and general learnings we gain from these Phase I studies of MELT3 will be very valuable in helping us to efficiently design and execute our prescription pharmaceuticals programme, which targets large market opportunities, such as cardiovascular disease and diabetes,' he added.

The results of the study confirmed that the primary endpoints have been met, showing that the MELT3 (melt-then-swallow) formulation had good bioavailability, with good plasma levels achieved. While Phase I clinical studies generally comprise insufficient subject numbers to generate statistically meaningful data, this study showed that, as expected, the most clinically relevant arm comprising subjects not fed a high-fat and high-calorie meal, saw the bioavailability of MELT3 trending above that of orally administered tocotrienols (at the 40mg dose, the mean maximum plasma concentration [Cmax] for the MELT3 arm was 70.9ng/mL of delta tocotrienol isomer, compared with 54.5ng/mL for the oral arm).

A trend was also observed wherein feeding subjects with a high-fat and high-calorie diet (approximately 800-1000 calories of which at least 50% was fat) increased the bioavailability of both the MELT3 and oral arms. In this instance, the oral arm achieved a mean Cmax of 254ng/mL for the delta tocotrienol isomer, compared with 168ng/mL for MELT3. This is not considered by the company to be clinically relevant owing to the unlikelihood of healthy, exercise conscious users consistently consuming high amounts of fat while also taking exercise supplements.

A clear dose response relationship was observed with the mean Cmax of the delta tocotrienol isomer for a 10mg dose of MELT3 being 14.2ng/mL, and extending in the trial to 27.7ng/mL for the 20mg dose, and 70.9ng/mL for the 40mg dose. The duration in plasma, about 12 hours, could potentially have a positive impact on dosing. An additional PK study is planned to focus on the elimination phase of the pharmacokinetic profile and whether less frequent dosing may still achieve efficacy.

The safety endpoint was achieved with MELT3 observed as very well tolerated. The tablets were also found to be easy to administer and palatable.

The Phase I study to assess the safety, tolerability and plasma PK for Gordagen's tocotrienol tablet formulation commenced in June 2015. Sixty healthy volunteers were enrolled at a Western Australian trial site and the study was conducted in strict compliance with ICH-GCP (International Conference on Harmonisation Good Clinical Practice) guidelines. Results will form an integral part of Gordagen's international regulatory affairs and market entry programme.

Additional information derived from a more detailed analysis of the elimination phase of the PK profile study will also allow a more accurate analysis of the Area Under the Curve. This will help inform total study exposure of MELT3.

The multiple ascending dose PK study and Phase II efficacy studies planned for late 2015 and 2016 will also provide additional information with regard to an effective dosing regimen.

'The results from this part of Gordagen's Phase I clinical trial indicates that the MELT3 product is very promising indeed and lays a solid foundation for both the second part of the Phase I clinical trial, the multiple ascending dose PK study, and also the Phase II clinical studies for muscle recovery and exercise endurance,' commented Dr Ric DeGaris, the Chief Operating Officer for Gordagen.

Gordagen is on track to progress its clinical development programme to gather supporting evidence for its proprietary MELT3 technology and is pleased with current progress on negotiations to engage with manufacturing, marketing and distribution partners in two of the largest dietary supplement markets, the US and Japan.