- Primary endpoints of Phase I Single Ascending Dose pharmacokinetic study achieved
- Bioavailability of Gordagen's MELT3TM formulation confirmed, with good plasma levels obtained
- Dose relationship of MELT3 TM demonstrated, along with significant duration in plasma.
- MELT3 TM tablets confirmed to be easy to take, palatable and well tolerated
MELBOURNE, Australia, Sept. 8, 2015 (GLOBE NEWSWIRE) -- Gordagen Pharmaceuticals, a privately-held company commercializing evidence-based nutraceuticals and pharmaceuticals, today 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 (MELT3TM), 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 program for evidence-based nutraceuticals. Results from this recent trial provide strong support for the benefits of our MELT3TM 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 MELT3TM will be very valuable in helping us to efficiently design and execute our prescription pharmaceuticals program, which targets large market opportunities, such as cardiovascular disease and diabetes."
The results of the study confirmed that the primary endpoints have been met, showing that the MELT3TM (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 MELT3TM trending above that of orally administered tocotrienols (e.g., at the 40mg dose, the mean maximum plasma concentration (Cmax) for the MELT3TM arm was 70.9 ng/mL of delta tocotrienol isomer, compared to 54.5 ng/mL for the oral arm).
A trend was also observed where 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 MELT3TM and oral arms. In this instance, the oral arm achieved a mean Cmax of 254 ng/mL for the delta tocotrienol isomer, compared with 168 ng/mL for MELT3 TM. This is not considered by the Company to be clinically-relevant due 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 MELT3TM being 14.2 ng/mL, and extending in the trial to 27.7ng/mL for the 20mg dose, and 70.9 ng/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 TM 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 program.
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 MELT3TM.
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 MELT3TM product is very promising indeed and lays a solid foundation for both the second part of the Phase I clinic 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 program to gather supporting evidence for its proprietary MELT3TM 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.
Investor and Media Enquiries:
|Dr Glenn Tong||Paris Brooke||David Burke|
|Managing Director & CEO||Bt Novo Pty Ltd||The Ruth Group|
|Tel: +61 (0) 412 193 350||Tel: +61 (0) 407 715 574||O: 646.536.7009|
About Gordagen Pharmaceuticals Pty Ltd
Gordagen Pharmaceuticals is a privately-held Australian company developing and commercializing novel supplements and prescription medicines based on natural tocotrienols, found in vitamin E. The Company has developed a novel approach to delivering highly potent tocotrienols to target tissues using its proprietary and patent-pending "melt-then-swallow" delivery technology (MELT3TM). The Company is focusing on tocotrienols with wide therapeutic potential, initially targeting heart health, muscle soreness and exercise endurance.
Clinical Trial Overview
Name of Trial: Single Ascending Dose Pharmacokinetic study of Gordagen's MELT3 TM (melt-then-swallow) formulation
Design and Method: Phase 1 open-label single-dose PK study. Three (3) dose levels (10, 20 and 40mg). .
The sample collection time-points chosen for the SAD study were standard time-points for phase 1 PK / safety studies (0, 5, 10, 15, 30, 45 min, 1, 1.5, 2, 3, 4, 6, 8, 12, 24h).
Number of subjects: 60 healthy volunteer subjects in total:
- 10mg MELT3TM group (fasted) – 12 subjects
- 20mg MELT3TM group (fasted) – 12 subjects
- 40mg MELT3TM group (fasted) – 12 subjects
- 40mg MELT3TM group (fed) – 12 subjects
- 40mg ORAL group (fasted) – 6 subjects
- 40mg ORAL group (fed) – 6 subjects
All subjects completed the study.
Primary endpoints: Safety, tolerability and evidence bioavailability (concentration in plasma). Changes in vital signs, physical examination, hematology, biochemistry, urinalysis and 12-lead ECG over the course of the study. Pharmacokinetic descriptors including peak plasma concentration (Cmax), time to peak plasma concentration and elimination half-life.
Exploratory endpoints: Time taken for MELT3 TM to disintegrate. Subject's judgement on palatability of tablet.