Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.3.16 (calcineurin)
 17,112 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Calcineurin inhibitors (CNIs) are potent immunosuppressants that reversibly inhibit T-cell proliferation and prevent the release of pro-inflammatory cytokines by blocking the activity of calcineurin, a ubiquitous enzyme that is found in cell cytoplasm. CNIs can be highly effective in immune-mediated ophthalmic diseases such as uveitis, dry eye syndrome and inflammatory blepharitis, as well as for the prevention of rejection in corneal transplants. ISA-247/LX-211 is a novel CNI that is in Phase III clinical development for the treatment of various forms of non-infectious uveitis. ISA-247/LX-211 is a rationally designed analog of ciclosporin A that exhibits more predictable pharmacokinetic and pharmacodynamic properties and a 4-fold greater calcineurin inhibition than its parent compound, ciclosporin A. ISA-247/LX-211 has been observed to be effective, well-tolerated, and safe in early clinical trials, exhibiting a much wider therapeutic window compared with classic CNIs, such as ciclosporin A and tacrolimus. An alternative approach to widening the therapeutic window for the therapy of ophthalmic disorders lies in local delivery of CNIs through polymeric implants that release the drug over long periods of time. The silicone matrix episcleral implant LX-201 is in Phase III development at present for the prevention of rejection in high-risk cornea transplantation.
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PMID:Next-generation calcineurin inhibitors for ophthalmic indications. 1792 18

Atopic keratoconjunctivitis is a chronic noninfectious inflammatory condition and is one of the most severe ophthalmic complications associated with atopic dermatitis. It requires prompt and effective treatment to prevent permanent vision loss. Complications of atopic keratoconjunctivitis include cataracts, keratoconus, infectious keratitis, blepharitis, tear dysfunction, and steroid-induced glaucoma. All treatment for atopic keratoconjunctivitis should be managed in conjunction with an ophthalmologist, and immediate referral is indicated when there is moderate to severe irritation, increased redness, discharge, or any visual symptoms. Treatment options include a combination of mast cell inhibitors, antihistamines, corticosteroids, and calcineurin inhibitors.
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PMID:Atopic keratoconjunctivitis: A review. 2434 54