The Marinosolv® technology opens up far-reaching possibilities for a wide range of different substances. Marinosolv® is compatible with applications in sensitive tissue such as nose, eyes and lungs. It provides a non-irritating, safe and effective way to deliver hardly soluble active compounds to the nasal and oral mucosa and the respiratory tract. Compound classes tested with Marinosolv® include steroids such as Budesonide or Fluticasone propionate as well as the immunosuppressant Tacrolimus.
Marinosolv® facilitates drug delivery of organic compounds that can currently only be delivered as a suspension, thus unlocking new possibilities in treating a multitude of diseases.
In general, dissolved compounds may have the following advantages towards suspensions:
- Increase of bioavailability in the target tissue.
- Faster onset of action compared to suspensions due to higher bioavailability.
- In currently marketed products, exemplified by intranasal steroids, an excess of compound is applied compared to the dissolved proportion of the active pharmaceutical ingredient (API), thus, a reduction of the total dose may be possible.
- With suspensions, improper dosing may occur because patients often forget to shake the product.
- Aseptic production with filtration may be possible and preservatives may be omitted.
- Combination with other active pharmaceutical ingredients (API) may be easier to achieve.
- Potential for cost of goods (COGS) reduction based on cheaper production processes.
- New formulation of proven APIs may allow for new patent protection.
- New applications for highly insoluble substances in eyes, lungs, other mucosal tissues, or elsewhere are feasible which may result in low systemic availability and high local activity.
The goal of allergic rhinitis therapy is to manage both the acute and chronic manifestations of the disease by minimizing the associated symptoms and improving quality of life. To achieve this, current treatment recommendations include allergen avoidance, immunotherapy and/or pharmacotherapy. Avoidance is difficult to achieve for the most common allergens (e.g. pollen, dust mites).
Intranasal corticosteroids are considered to be the most effective pharmacology treatment for allergic rhinitis (Source: Wallace et al., J Allergy Clin Immunol 122, p1237 ff, 2008.) because their anti-inflammatory properties enable efficacious control of symptoms of allergic rhinitis in the majority of patients treated. However, due to the insolubility of modern corticosteroids existing products have a delayed onset of action and poor bioavailability.
Budesolv is a new formulation of the non-halogenic glucocorticoid budesonide for intranasal use that intents to achieve:
- Faster onset of action
- Immediate relief
- Reduced dose
The Company plans to perform a pivotal phase III clinical study supporting a subsequent application for marketing authorization. The clinical study is planned to be conducted in Q4 2018 and Q1 2019 with data being available in Q2 2019. This study may be used two-fold: Supporting Marinosolv® technology and being used for supporting the registration of Budesolv in Europe and other countries.
Tacrolimus is a macrolide immunosuppressant with proven efficacy with a biological activity approximately 100-fold higher than the currently used Cyclosporine A. This is reflected by different doses used after transplantation in humans (15.8 mg/kg/day Cyclosporine A versus 0.08 mg/kg/day Tacrolimus). Also the concentration in the blood two hours after dosing illustrates this difference with 700-900 ng/ml Cyclosporine A and 5-12 ng/ml Tacrolimus (Tanaka et al., Liver Transplantation 11, pager 1395-1402). Until today, the use of Tacrolimus in ophthalmology was hampered by its insolubility and stability issues. Tacrosolv goes one step beyond: Marinosolv® enables a broader ophthalmological use of Tacrolimus due to a significant increase in solubility and stability.
The Company plans to initiate clinical trials with Tacrosolv. It is currently foreseen that clinical phases II and III trials are required for this particular product in the indication allergic conjunctivitis. Successful phase II and III data with Tacrosolv would allow to apply for marketing authorization in the indication allergic conjunctivitis, where it would be a first in class product in Europe and US. In addition, these data would support further development of the product towards the dry eye indication.