SYNTHESIS OF NOVEL OPHTHALMIC DRUG CONJUGATES

Our synthesis team develops novel combinations of drugs for the treatment of ophthalmic conditions such as glaucoma. Therapeutics are combined by applying specific linker chemistry for the conjugation of the drugs. When applied to the eye, the molecular structure of the conjugates is broken down into its original therapeutics, following our pro-drug strategy.

Combination drugs for the treatment of eye diseases have changed and will continue to change the management of ophthalmic conditions. The potential benefits of combination drugs include a reduction in the total number of drops and preservatives instilled per day, higher patient comfort and hence improved compliance and therapeutic efficacy. As an example, 4 out of 10 patients with glaucoma require two or more drugs to control elevated IOP levels.

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INCREASING BIOAVAILABILITY OF KNOWN THERAPEUTICS

CIS Pharma develops novel formulations for ophthalmic drugs. Marketed ophthalmic drug products are based on formulation technologies with relatively low solubility of therapeutics, resulting in poor bioavailability. Some of the formulations also irritate eyes and cause redness, keeping patients from adhering to the prescribed regimen. As a result, some patients may drop out of their therapies.

At CIS Pharma, we increase solubility of hydrophobic drugs compared to older generation formulations. By applying our formulation technology to ophthalmic drugs, the bioavailability and patient comfort of marketed ophthalmic drugs is improved.

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CONTACT LENS COATING TO INCREASE COMFORT

CIS Pharma has developed a contact lens coating for silicone-hydrogel contact lenses. The coating is based on our Cellophil® Smart Polymer platform and is applied to the lens thermally during terminal sterilization of contact lenses. Cellophil® Smart Polymers bind to the lens surface and increase surface wettability and lubricity, as demonstrated in micro-tribiological measurements of coated vs. non-coated contact lenses.

Both lubricity and wettability are essential for good wearing comfort of contact lenses. Functionalized groups in Cellophil® Smart Polymers prevent the deposition of tear film lipids that normally decrease the comfort and vision of contact lenses. The Cellophil® coating technology is suitable for different contact lens materials. Let us know if you are interested in obtaining a customized version for your lens material.

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BIO-INSPIRED CONTACT LENS CARE TECHNOLOGY

CIS Pharma has developed the latest generation bio-inspired lens care solution for cleaning, disinfection and storage of silicone hydrogel contact lenses. The MPS comprises a unique comfort complex that delivers an unsurpassed amount of hyaluronic acid (HA) and a physiological mix of minerals to the contact lens surface. The complex increases the lens wettability, shows uncompromised disinfection power and simultaneously supports the regeneration of corneal cells. The MPS offers good disinfection and cleaning characteristics without rubbing the lens. The solution showed a superior disinfection potential for various bacteria & fungi related to eye infections in the FDA standalone test procedure. The MPS was also highly effective against the active “trophozoite” as well as the stress resistant “cyst” forms of acanthamoeba. These uni-cellular organisms are responsible for severe eye infections that can lead to blindness. Safety was demonstrated by measuring conjunctival redness, conjunctival and corneal stippling. The solution was well tolerated in these tests.

The MPS formulation is patent protected in Europe, Japan and China and patent pending in the USA and Canada. The patent allows any combination between HA and polymeric disinfectants (polymeric quaternary ammonium compounds). This is a clear advantage over common formulations. If you are interested in the product or in a licence to the patent, please contact us.

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