Novagali's business is based on a platform emulsion technology that can be used to improve the bioavailability of poorly soluble drugs, whether they are delivered orally, parenterally, topically or into the eye. The company has already started two clinical trials of ophthalmological drugs based on the system, and will start a Phase I trial of an oral drug candidate shortly.
Novagali's chief executive, Jerome Martinez, told In-Pharmatechnologist.com that the principle behind the technology is the creation of particles that are positively charged (cationic) rather than negatively charged (anionic).
This has the advantage of creating an attraction between the emulsion and the tissues of the body, which carry a negative charge. The result is that the particles adhere to the target tissue, improving the delivery of the active drug.
And like other emulsion technologies, the particles act as a carrier vehicle for poorly soluble drugs. But other emulsions are anionic, and this creates a repulsion effect that can limit delivery of the active drug. Novagali's technology is based on a proprietary excipient, oleylamine, that will be filed with the US and European regulatory authorities early next year.
There is a pressing need for technologies that can help solubilise small molecules, as it is estimated that 50-60 per cent of drugs coming through the R&D pipeline have solubility problems. This proportion has risen from about 40 per cent a few years ago, according to Novagali, and is thought to be a result of the more diverse range of compound types being screened from combinatorial chemistry and natural sources.
Martinez explained that Novagali has decided to focus its efforts initially in the ophthalmological area, as there have been few product developments in this area and using drugs to treat eye diseases is problematic.
While it is easy to deliver compounds to the surface of the eye, getting them to stay there while they exert their effects is a tougher proposition. Novagali's positively charged emulsions overcome this by adhering to the cornea - even spreading around the eyeball to reach the back of the eye - and forming a reservoir in the conjunctiva.
The company's initial product - Cationorm (NOVA 23006) - is based on the emulsion on its own and is intended as a physiological replacement for tears in people who suffer from mild to moderate dry eye syndrome. This produce behaves more like natural tears than current artificial products, which tend to be based on sodium chloride, said Martinez.
Cationorm should only need to be dosed twice a day, compared to four to eight times for current artificial tear products. It is currently in Phase II trials that should generate data in the first quarter of next year.
It will be registered as a prescription product in the US, but could be sold over-the-counter in Europe as the regulatory regime there is somewhat different. Unlike the US, Europe does not operate a limited, positive list of excipients that can be used in OTC products.
Following behind Cationorm, and due to start a Phase IIa trial in the next two months, is NOVA 22007, an eyedrop formulation of the immunosuppressant drug cyclosporine.
An eyedrop formulation of cyclosporine - Allergan's Restasis - is already approved in the US, but Martinez believes that Novagali's formulation will provide advantages in patient comfort and could potentially improve efficacy.
Following after the dry eye programmes is NOVA 22008, a cationic emulsion formulation of an antisense oligonucleotide designed to inhibitor vascular endothelial growth factor (VEGF). This is still in preclinical development, and is a candidate treatment for age-related macular degeneration, one of the leading causes of blindness.
Oral programme
Novagali's has also started the first clinical trial of an oral application for its technology. The company has developed an emulsion formulation of paclitaxel, a widely used cancer drug, which could be delivered by mouth instead of intravenously.
It would also do away with the need for patient monitoring around the administration of the current formulation of paclitaxel, which is dissolved in Cremophor, a solvent that is associated with significant toxicity.
Other companies have been developing oral forms of paclitaxel, but have encountered problems. For example, one formulation is said to contain so much ethanol that it is the equivalent of drinking two glasses of whiskey a day.
Martinez noted that Novagali's plan is to out-license the oral paclitaxel project once Phase I is completed, although it may retain its ophthalmic programmes for a little longer, perhaps through Phase II. He did not rule out the possibility that the company might in time market the drugs itself.
The €14 million fundraising should enable the company to continue to operate for another three years - based on its current burn rate - providing it starts to generate revenues from licensing and co-development deals.