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Hello, some info, haven't seen Civelamine (Daiichi) on this page. should increase aqueaus layer..... new? and Milcrin (Vista)? New? etc. read!
Dry Eye Drugs in Development: Part II
This column will provide a snapshot of the many potential dry eye therapeutic agents in various stages of clinical testing. There are additional drugs under development, but information about them remains proprietary.
Anti-inflammatory Agents In addition to the already approved cyclosporine product (Restasis®; Allergan), picrolimus (Elidel®; Novartis), an immunosuppressant whose action is similar to that of cyclosporine, is in an advanced stage of clinical testing.
Several topical ophthalmic corticosteroids are considered relatively "safe" (ie, not associated with a high incidence of cataract formation or glaucoma), and these are being used to treat the inflammatory component of dry eye disease. In recent publications loteprednol etabonate (Lotemax®; Bausch & Lomb) has been shown to be useful in managing dry eye disease. Another corticosteroid, rimexolone (Vexol®; Alcon), is under clinical testing for use in dry eye disease.
Mucin Stimulants and Supplements
Diquafasol (Inspire Pharmaceuticals) is a P2Y2 agonist that stimulates production of MUC-5AC, the gelforming mucin secreted by the conjunctival goblet cells. (MUC-5AC is believed to act as a stabilizing and cleansing agent for the tear film.) Diquafasol also increases chloride ion transport across the conjunctival surface; the chloride ions carry water with them, causing an increase in aqueous tear volume. Phase III clinical trials have been completed and submitted with additional studies to the FDA for approval.
15-(S)-HETE (Alcon) is another mucin stimulator, but this one ignites production of MUC 1, a transmembrane mucin thought to contribute to the structure of the epithelial surface and act as a protective coating. 15-(S)- HETE is in late-stage clinical testing. Other mucin stimulators in clinical development include rebamipide (Otsuka), whose mechanism of action is not yet available, and ecabet (ISTA), a mucin stimulator that is currently in phase II testing.
Milcrin (Vista) is a dairy product with mucin-like characteristics that is under clinical development.
Hormonal Agents and Lacrimal Gland Stimulants
Research over the last decade has implicated androgen deficiency in the pathogenesis of dry eye disease. Now in phase III trials, androgen tears (Allergan) are a topical formulation containing a form of testosterone. Estratest (Solvay) is an orally administered agent that contains esterified estrogens and methyltestosterone.
Civelamine (Daiichi) is a muscarinic agonist that is reported to stimulate the aqueous secretion of the lacrimal gland. It is in clinical trials.
Ocular Surface Protectants
At least two products that aim to protect the epithelial surface of the cornea and conjunctiva are under development. Trehalose (Biovision) is a compound found in the integument of desert-dwelling reptiles. There have been several reports of its efficacy in protecting the ocular surface from staining in dry eye patients. Its development status is unknown. D-ß-hydroxybutyrate (Ophtecs Corporation) is a ketone body produced by the degradation of long-chain fatty acids. In animal studies it appears to suppress epithelial apoptosis. It is in early stage development.
Tear Stabilizers
At least one currently marketed artificial tear preparation, Systane® (Alcon), has been shown to stabilize the tear film up to 30 minutes after application. Also in the tear-stabilizer category is the chemical, hyaluronic acid (HA), a naturally occurring polymer that the FDA considers an "active" ingredient and therefore a "therapeutic" agent. It is available (in low concentration) in the US in two over-the-counter contact lens rewetting drops, as well as in viscoelastic preparations for intraocular use. A number of companies have initiated clinical trials with this agent, but the results have not been announced. Formulations containing HA, however, are widely used in Asia, Europe, and Canada; and they are reported to be very useful.
This list represents only a partial look at the landscape of new treatment strategies. It will, however, give a glimpse of what the future may hold for the treatment of dry eye disease.
Dry Eye Drugs in Development: Part II
This column will provide a snapshot of the many potential dry eye therapeutic agents in various stages of clinical testing. There are additional drugs under development, but information about them remains proprietary.
Anti-inflammatory Agents In addition to the already approved cyclosporine product (Restasis®; Allergan), picrolimus (Elidel®; Novartis), an immunosuppressant whose action is similar to that of cyclosporine, is in an advanced stage of clinical testing.
Several topical ophthalmic corticosteroids are considered relatively "safe" (ie, not associated with a high incidence of cataract formation or glaucoma), and these are being used to treat the inflammatory component of dry eye disease. In recent publications loteprednol etabonate (Lotemax®; Bausch & Lomb) has been shown to be useful in managing dry eye disease. Another corticosteroid, rimexolone (Vexol®; Alcon), is under clinical testing for use in dry eye disease.
Mucin Stimulants and Supplements
Diquafasol (Inspire Pharmaceuticals) is a P2Y2 agonist that stimulates production of MUC-5AC, the gelforming mucin secreted by the conjunctival goblet cells. (MUC-5AC is believed to act as a stabilizing and cleansing agent for the tear film.) Diquafasol also increases chloride ion transport across the conjunctival surface; the chloride ions carry water with them, causing an increase in aqueous tear volume. Phase III clinical trials have been completed and submitted with additional studies to the FDA for approval.
15-(S)-HETE (Alcon) is another mucin stimulator, but this one ignites production of MUC 1, a transmembrane mucin thought to contribute to the structure of the epithelial surface and act as a protective coating. 15-(S)- HETE is in late-stage clinical testing. Other mucin stimulators in clinical development include rebamipide (Otsuka), whose mechanism of action is not yet available, and ecabet (ISTA), a mucin stimulator that is currently in phase II testing.
Milcrin (Vista) is a dairy product with mucin-like characteristics that is under clinical development.
Hormonal Agents and Lacrimal Gland Stimulants
Research over the last decade has implicated androgen deficiency in the pathogenesis of dry eye disease. Now in phase III trials, androgen tears (Allergan) are a topical formulation containing a form of testosterone. Estratest (Solvay) is an orally administered agent that contains esterified estrogens and methyltestosterone.
Civelamine (Daiichi) is a muscarinic agonist that is reported to stimulate the aqueous secretion of the lacrimal gland. It is in clinical trials.
Ocular Surface Protectants
At least two products that aim to protect the epithelial surface of the cornea and conjunctiva are under development. Trehalose (Biovision) is a compound found in the integument of desert-dwelling reptiles. There have been several reports of its efficacy in protecting the ocular surface from staining in dry eye patients. Its development status is unknown. D-ß-hydroxybutyrate (Ophtecs Corporation) is a ketone body produced by the degradation of long-chain fatty acids. In animal studies it appears to suppress epithelial apoptosis. It is in early stage development.
Tear Stabilizers
At least one currently marketed artificial tear preparation, Systane® (Alcon), has been shown to stabilize the tear film up to 30 minutes after application. Also in the tear-stabilizer category is the chemical, hyaluronic acid (HA), a naturally occurring polymer that the FDA considers an "active" ingredient and therefore a "therapeutic" agent. It is available (in low concentration) in the US in two over-the-counter contact lens rewetting drops, as well as in viscoelastic preparations for intraocular use. A number of companies have initiated clinical trials with this agent, but the results have not been announced. Formulations containing HA, however, are widely used in Asia, Europe, and Canada; and they are reported to be very useful.
This list represents only a partial look at the landscape of new treatment strategies. It will, however, give a glimpse of what the future may hold for the treatment of dry eye disease.
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