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.

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.

The sterile, preservative-free, topical formulation is designed to penetrate corneal tissue rapidly and provide broad coverage of the most sight-threatening gram-negative and the most prevalent gram-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 both topoisomerase 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 to the company. Also, when Skelnik and colleagues tested it in human cell cultures, the solution demonstrated less cytotoxicity than other marketed fluoroquinolones.

"Compared with existing ophthalmic fluoroquinolones, levofloxacin offers a higher sustained concentration option," said Penny A. Asbell, MD, professor of ophthalmology and director of cornea services, 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 other quinolones, or to any of the components in the medication. The formulation was well-tolerated in clinical trials, according to the company. Ocular adverse events occurring in 1% to 2% of patients included decreased/blurred vision, instillation site irritation/discomfort, ocular infection, and ocular pain/discomfort. Non-ocular adverse events, occurring in approximately 8% to 10% of patients, were headache and taste disturbance.