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Pharm Res. 2019 Jan 7;36(2):36. doi: 10.1007/s11095-018-2556-5.

Ocular Pharmacokinetics of a Topical Ophthalmic Nanomicellar Solution of Cyclosporine (Cequa®) for Dry Eye Disease.

Author information

1
Division of Pharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Missouri, 2464 Charlotte Street, Kansas City, MO, 64108, USA.
2
Sun Pharmaceutical Industries Ltd., Sun Ophthalmics Inc., 2 Independence Way, Princeton, NJ, 08540, USA.
3
Division of Pharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Missouri, 2464 Charlotte Street, Kansas City, MO, 64108, USA. mitraa@umkc.edu.
4
Department of Ophthalmology, School of Medicine, University of Missouri, Kansas City, MO, USA. mitraa@umkc.edu.

Abstract

Cequa®, a unique and first-in-class preservative free cyclosporine-A (CsA) nanomicellar topical formulation was recently approved by US FDA for treatment of dry eye disease or keratoconjuntivitis sicca (KCS). Being highly hydrophobic, CsA is currently available as an oil based emulsion, which has its own shortcomings. Developing an aqueous and clear formulation of CsA is imperative yet a challenging need in the quest for a safe and better drug product. In this regard, a novel, clear, aqueous nanomicellar solution of CsA was developed which has the potential to deliver therapeutic concentrations of CsA with minimal discomfort to patients. Highly promising pre-clinical results of Cequa® (OTX-101), has led to its advancement to the clinical trials. Phase III clinical trials have demonstrated that OTX-101 is highly effective, safe, and has a rapid onset of action in treating KCS. This review presents a comprehensive insight on formulation development, preclinical and clinical pharmacokinetic results of Cequa®. Additionally, the translational development of Cequa® from the laboratory benchtop to patient bedside has been discussed.

KEYWORDS:

OTX-101; formulation; keratoconjunctivits sicca (KCS); micelles; non-ionic; ocular drug delivery; tear

PMID:
30617777
DOI:
10.1007/s11095-018-2556-5
[Indexed for MEDLINE]

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