QBiotics current focus for human health is oncology and wound healing.
Cancer is a leading cause of death worldwide. It is estimated that globally more than 12 million people are diagnosed with cancer and 7.6 million people die of the disease each year. The majority of these cancers are of the solid tumour type.1 There are currently a large range of anticancer treatments available for solid tumours. However, there is considerable interest in the development of new treatments mainly driven by the ongoing need to treat late stages of disease.2
QBiotics' leading anticancer pharmaceutical, tigilanol tiglate (EBC-46), is a novel small molecule diterpene ester in development as a local treatment for solid tumours. Tigilanol tiglate was discovered by applying the EcoLogic™ approach to drug discovery from the tropical rainforests of Queensland Australia. The drug is not syntheticall tractable and is isolated from the Australian native plant Blushwood. Tigilanol tiglate is a protein kinase C (PKC) activator and when injected into solid tumours causes PKC-dependent haemorrhagic necrosis, rapid tumour cell death and ultimate removal of solid tumours as demonstrated in pre-clinical models of cancer.3
QBiotics recently completed proof of concept clinical trials of tigilanol tiglate in patients involving four Australian hospitals. A Phase I/IIA clinical trial conducted in 22 patients with refractory skin and subcutis solid tumours (specifically melanoma, basal cell carcinoma, squamous cell carcinoma, breast adenocarcinoma, lymphangiosarcoma and angiosarcoma) demonstrated good tolerability following intratumoral injection of tigilanol tiglate. Adverse events were generally limited to transient tumour site swelling and associated pain, responses that were expected given the mode of action of the drug*. In addition, encouraging signs of efficacy were demonstrated in all tumour types, with full tumour destruction (Complete Response) observed in patients that received higher doses*. As well, good healing of the injection site was observed and a maximum tolerated dose (MTD) was not reached.
Local treatment with tigilanol tiglate to date has concentrated on cutaneous and subcutaneous tumours and our ongoing strategy is to continue later stage development and bring this promising natural product to market as soon as possible. However, we also seek to determine if tigilanol tiglate has the potential to treat a range of internally situated solid tumours where injection can be guided by imaging.
The intellectual property and commercial production of tigilanol tiglate has been secured. Composition of matter and use patents have been granted in all major regions. The source plant of tigilanol tiglate, Blushwood, is produced in commercial plantations and a mature good manufacturing process (GMP) for active pharmaceutical ingredient and drug product is established. As a result of these processes, the future commercial supply of tigilanol tiglate is assured.
1 National Cancer Institute USA Website www.cancer.gov
2 GBI Research 2011; GBI Research Report "Oncology Therapeutics Market to 2017 - High Unmet Need in the Management and Treatment of Metastatic Cancers to Drive Drug Development" GBIHC125MR; December 2011.
3 Boyle GM, et al. (2014) Intra-Lesional Injection of the Novel PKC Activator EBC-46 Rapidly Ablates Tumors in Mouse Models. PLoS ONE 9(10): e108887. doi:10.1371/journal.pone.0108887
Chronic wounds, such as slow to heal leg ulcers, present a significant health problem due to an aging population and a sharp rise in the incidence of diabetes and obesity. In the USA alone chronic wounds affect 6.5 million patients annually and an excess of US$25 billion a year is spent on support treatments for sufferers.4 Current treatments are not fully addressing the complex problems of wound healing for both humans and animals.
WH-1 (EBC-1013) is a semi-synthetic novel diterpene ester being developed as a wound healing pharmaceutical for treatment of the full spectrum of wound types. The human development program for WH-1 is initially focusing on the treatment of chronic wounds, including the high demand areas of venous leg ulcers and diabetic foot ulcers. Future wound healing indications under evaluation include the treatment of acute wounds, burns, photo-damaged skin and as an anti-scarring treatment.
WH-1 has a novel mechanism of action that addresses all stages of wound healing and has the potential to:
- Accelerate wound closure;
- Minimise scarring;
- Reduce the incidence of infectious complications through antimicrobial activity.
WH-1 is delivered as a topical gel. It is easy to use, simply being applied over the wound area with the dose dependent on the size of the wound being treated.
To date, WH-1 has been used to treat a range difficult to manage wounds in veterinary clinical cases* including:
- Chronic infected wounds;
- Non-healing surgical wounds;
- Acute wounds with extensive local tissue damage and high infection risk;
- Acute hyper-granulating wounds in horses, which have a high scarring risk.
*Data on file QBiotics
WH-1 is currently in preclinical stage of development for the human market (and early clinical for the veterinary market). Intellectual property and commercial production of WH-1 is progressing well. Composition of matter and use patents are currently under examination in all major regions. The GMP production process for the active pharmaceutical ingredient has commenced and the formulation of drug products has been finalised.
4 Sen, C K, et al. (2009) Human Skin Wounds: A Major and Snowballing Threat to Public Health and the Economy. Wound Repair Regen. 17(6): 763-771.