Robust laboratory testing, preclinical studies and the company’s phase 1/2a clinical study results to date support Luliconazole’s promise to become the first highly effective and safe topical therapy for onychomycosis.
Preclinical In Vitro Studies
In numerous preclinical studies, Topica’s 10% Luliconazole formulation has demonstrated the in vitro ability to:
- Penetrates full-thickness healthy human toenails (up to 1mm in thickness) at fungicidal levels by day 7 and beyond.
- Completely eradicates fungal infections in a toenail model by day 21 – based on MIC 90 studies of Luliconazole against dermatophytes commonly associated with onychomycosis, the drug has been shown to be one of the most potent antifungals1.
Phase 1/2a Maximal Use PK Trial
A rigorous phase 1/2a maximal use PK trial evaluating the safety, tolerability and pharmacokinetics of 10% Luliconazole solution in adults with moderate-to-severe onychomycosis (toenails up to 3mm in thickness) has demonstrated the following outcomes:
- Topica’s Luliconazole formulation is extremely well tolerated.
- Blood plasma levels of Luliconazole are safe and at very low levels, with no serious adverse events reported.
- Based on in vitro testing with CYP isoforms and the blood plasma levels of Luliconazole seen in phase 1/2a testing, the probability of drug-drug interactions is extremely low.
- Luliconazole is detected in blood plasma up to 7 days post- treatment, demonstrating that the drug crosses highly infected nails – and suggesting that the nail acts a reservoir, continuing to release drug into the nail bed.
Phase 2B/3 Clinical Trial
Based on encouraging preclinical data and phase 1/2a results, Topica will conduct a robust, well- controlled, multi-center phase 2B/3 human trial to evaluate the efficacy and safety of two different dosing regimens of Topica’s 10% Luliconazole formulation. With this 2B/3 trial, Topica intends to demonstrate Luliconazole’s ability to achieve positive measures of complete cure, highlighting the potential for the product to meet the clinical requirements for FDA approval.
1 Hiroyasu Koga, Yasuko Nanjoh, Kazuyoshi Inoue, et al. Luliconazole, a novel topical imidazole: results of the preclinical studies. ISHAM June
2006 P-0090.
2 Hiroyasu Koga, Yasuko Nanjoh, Koichi Makimura, et al. In vitro antifungal activities of luliconazole, a new topical imidazole. Medical
Mycology. 29 December 2008.
