Levofloxacin drop introduced for corneal ulcers

November 11, 2007

Levofloxacin ophthalmic solution 1.5% (Iquix) has been introduced for the treatment of corneal ulcers. It is the only newer-generation fluoroquinolone approved by the FDA for this indication, according to the Vistakon Pharmaceuticals LLC. Vistakon is marketing the drop through a co-marketing agreement with Santen Inc. The drug is manufactured by Santen Oy, Tampere, Finland. The brand name is a licensed trademark of Daiichi-Sankyo Co. Ltd., Tokyo.

Levofloxacin ophthalmic solution 1.5% (Iquix) has been introduced for the treatment of cornealulcers. It is the only newer-generation fluoroquinolone approved by the FDA for this indication,according to the Vistakon Pharmaceuticals LLC.

Vistakon is marketing the drop through a co-marketing agreement with Santen Inc. The drug ismanufactured by Santen Oy, Tampere, Finland. The brand name is a licensed trademark of Daiichi-SankyoCo. Ltd., Tokyo.

The sterile, preservative-free, topical formulation is designed to penetrate corneal tissue rapidlyand provide broad coverage of the most sight-threatening gram-negative and the most prevalentgram-positive pathogens, including Corynebacterium species, Staphylococcus aureus, S.epidermis, Streptococcus pneumoniae, Viridans group streptococci, Pseudomonas aeruginosa,and Serratia marcescens.

Levofloxacin ophthalmic solution is designed to eradicate targeted pathogens by inhibiting bothtopoisomerase IV and DNA gyrase, a dual mechanism of action similar to newer fluoroquinolones.Resistance to levofloxacin due to spontaneous mutation in vitro is a rare occurrence, according tothe company. Also, when Skelnik and colleagues tested it in human cell cultures, the solutiondemonstrated less cytotoxicity than other marketed fluoroquinolones.

"Compared [with] existing ophthalmic fluoroquinolones, [levofloxacin] offers a higher sustainedconcentration option," said Penny A. Asbell, MD, professor of ophthalmology and director of corneaservices, external disease, and refractive surgery at Mount Sinai School of Medicine, New York."This, paired with its dual mechanism of action, provides a new and important option for doctors'corneal ulcer treatment."

The drop is contraindicated in patients with histories of hypersensitivity to levafloxacin, to otherquinolones, or to any of the components in the medication. The formulation was well-tolerated inclinical trials, according to the company. Ocular adverse events occurring in 1% to 2% of patientsincluded decreased/blurred vision, instillation site irritation/discomfort, ocular infection, andocular pain/discomfort. Non-ocular adverse events, occurring in approximately 8% to 10% of patients,were headache and taste disturbance.