Statins have known cholesterol-lowering and immunomodulatory properties, which prompted the novel idea of utilising them as a topical ocular therapy. This is the first eye drop to address all the underlying aspects of Blepharitis, which is an inflammation of the eyelids with increased abnormal cholesterol production.
RGN-259 ophthalmic solution is formulated as thymosin beta 4 preservative-free eye drops for the treatment of both dry eye syndrome and neurotrophic keratopathy. Thymosin beta 4 (Tβ4) is a synthetic copy of the naturally-occurring 43-amino acid peptide that is found in all tissues and in all nucleated cells. In the eye, Tβ4 promotes corneal epithelial cell migration, decreases both inflammation and apoptosis, and accelerates both repair and regeneration.
Tavilermide is a small cyclic peptidomimetic of NGF, a naturally occurring protein in the eye responsible for the maintenance of corneal nerves and epithelium. Tavilermide is differentiated from other investigational therapies in dry eye disease because it induces the production of mucin, a naturally occurring component of the tear film, and works upstream prior to inflammation.
SYL1001 is a chemically synthesized small interference RNA (siRNA) inhibitor of the Transient Receptor Potential Vanilloid-1 (TRPV1) formulated as eye drops. This receptor mediates pain sensation in the eye. SYL1001 belongs to a new emerging drug class whose mechanism of action differs from traditional small-molecules.
Lubricin, which is naturally found on the ocular surface, may play an important role in eye health and comfort by preventing friction between the cornea and conjunctiva which reduces shear stress (such as during eye blinking) to prevent eye injury at the corneal and ocular surface. In patients suffering from moderate to severe dry eye, lubricin is diminished and the act of blinking causes significant discomfort. Topical administration of recombinant human lubricin may provide superior reduction in the signs and symptoms of dry eye disease compared to existing treatments by preventing friction and wear on the ocular surface and restoring homeostasis to the tear film.
rhNGF, an investigational molecule of recombinant human Nerve Growth Factor (NGF), currently being evaluated for the treatment of eye diseases such as neurotrophic keratitis and retinitis pigmentosa. Results of an open-label clinical study exploring the compound’s safety and tolerability in patients with dry eye disease have recently become available and Dompé will soon initiate a multicentre Phase II study evaluating the safety and efficacy of rhNGF for the treatment of dry eye disease.
SkQ1 is the lead molecule of Mitotech, a Russian drug-development project based at the Moscow State University. Preclinical tests showed very promising results in several animal models of age-related ophthalmic diseases with inflammatory component.
KPI-121 is a novel nanoparticle formulation of loteprednol etabonate utilizing Kala’s proprietary MPP technology to enhance penetration into target tissues of the eye. KPI-121 has been studied in multiple clinical trials, including 1% and 0.25% formulations for the treatment of post-surgical ocular inflammation and pain and a 0.25% formulation for dry eye and Meibomian gland disease.
Rigel's ophthalmic JAK/SYK inhibitor, R348, is intended to arrest the inflammation and tissue damage to the eye from ocular GvHD.
P-321 Oophthalmic Solution, is a novel inhibitor of ENaC, which blocks the loss of tears through the absorptive pathway. In multiple pre-clinical models of dry eye, ENaC inhibitors have demonstrated the ability to essentially restore and maintain normal tear volume. Parion has completed a phase 1/2a clinical study in 53 patients with dry eye disease and is pursuing the next steps in the clinical development for this program.
Preclinical studies reveal that a single topical dose of Lacritin naturally promotes basal tearing without irritation that lasts for hours. After multiple daily doses, elevated natural basal tearing is sustained one week later. Lacritin is also protective against inflammatory cytokines. Corneal staining is reduced to background and lacrimal gland inflammation is diminished. No other tear protein, nor dry eye drug, displays these properties.
ML7 is a candidate molecule for the treatment of dry eye syndromes. The first in a new class of therapies, the drug may offer a targeted, effective therapeutic response for millions of people suffering from dry eye. In preclinical trials, the return to normal of the tarsal glands shows that ML7 eye drops significantly reduce inflammation of the eye surface and its associated structure.
AVX-012, a small molecule with a novel mechanism of action regulating basal tearing and blinking rate, is entering clinical trials in Spain late in 2016.
TOP1630 has been designed to act locally at surface of the eye, where the inflammation occurs, following topical delivery using eye drops. The drug is taken up and retained by the target inflammatory cells but otherwise has low bioavailability which, together with the natural physiology of the eye, means that the rest of the body is unlikely to have a significant exposure to the drug.
DED occurs when there is either insufficient tear production to maintain the aqueous layer or the lipid layer is deficient allowing the eye to dry due to increased evaporation. The latter is the more common cause of DED. The lipid layer thus is crucial to good vision and corneal integrity. It consists of a complex mixture of lipids which are generated form the lacrimal (tear) gland and the Meibomian glands in the eyelids (Tear and Meibum Lipidomes). Importantly, all of these lipids are present in Lamelleye (CXB/1-14).
Coversin™ complement inhibitor, is a second-generation complement inhibitor, acts on complement component-C5, preventing release of C5a and formation of C5b–9 (also known as the membrane attack complex or MAC), and independently also inhibits LTB4 activity.
Cis-urocanic acid (cis-UCA) has been demonstrated to suppress the inflammatory response in ocular epithelial cells. Cis-UCA also has shown a strong cytoprotective effect on the ocular epithelial cells, reversing the loss of cell viability in response to the UVB stress. This observation has important implications in the treatment of inflammatory eye conditions since chronic stress (e.g., inflammation at the ocular surface) is directly linked to cytotoxicity in epithelial cells. Preclinical studies in relevant animal models of eye inflammation also demonstrate strong proof-of-concept for the cis-UCA eye drops.
BL-1230 is a potent and selective cannabinoid receptor type 2 (CB2R) agonist intended as a novel treatment for Dry Eye Syndrome (DES).
TSG-6 attacks inflammation through novel mechanisms of action. The protein has been shown to block early mediators of inflammation. If inflammation remains untreated, over-reaction of host defense paradoxically can worsen tissue repair.
ADP355 is a peptide that mimics the action of adiponection by binding to the same receptors as the native protein. Activation of these receptors leads to a broad anti-inflammatory response, resulting in down-regulation of both pro-inflammatory cytokines and inflammatory cellular activity in a number of organ systems.
SI-614 is a modified hyaluronate that is produced using the Company’s proprietary technology. Ocular instillation of SI-614 in patients with dry eye is expected to protect
the ocular surface and promote corneal wound healing.
Nanomerics is developing NM133, a nano-enabled form of cyclosporine A for the treatment of dry eye syndrome. NM133 is an aqueous MET formulation able to deliver up to 8 times the amount of drug into the ocular tissues on topical application when compared to current licensed products.
RP101 is based on a naturally occurring, endogenous molecule found in the body. In prior clinical trials, the molecule, when used as an active pharmaceutical ingredient, was found to be associated with the mechanism of tear film production.
KPI-190 is a part of the ShK family and is being developed as an eye drop for use in several eye diseases including uveitis and Dry Eye Syndrome (DES).
Pathogenic T cells have been shown to play a role in autoimmune eye disease as T cell infiltration and cytokine and chemokine production lead to tissue damage in the eye. Kv1.3-HIGH autoreactive TEM cells have been identified in uveitis and DES making these conditions a good option for development of KPI-190.
Protearin™ is based on the glycoprotein clusterin, a natural, protective component of fluid-tissue interfaces throughout the body. Protearin™ targets the final common end point for all forms of dry eye, i.e., damage at the ocular surface and disruption of the ocular surface barrier.
The purpose of this study is to evaluate the tolerability and preliminary efficacy of DNase eye drops in patients with Sjogren's and Non-Sjogren Dry Eye Disease.
XG-102, a TAT-coupled dextrogyre peptide inhibiting the c-Jun N-terminal kinase, was shown efficient in the treatment of experimental uveitis.
DMT220, which is currently being formulated, will be our novel ophthalmic formulation. We plan to develop DMT220 for the treatment of ocular rosacea, because it can be treated by dermatologists.
Oculis plans to complete pre-clinical studies for its dry-eye candidate, OC301, before year-end 2015, with phase I and phase II pilot studies conducted in 1H 2016.
Aviara will be developing the topical form of AVA3486 for use in the treatment of DES with the help of a corporate partner specializing in diseases of the eye.
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