Recommended Topic Related To:

Luzu

"Some cryogenic wart removers—which remove warts from the skin by freezing them off—have caught fire during use at home, harming consumers or setting fire to items around the house.

Since 2009, the Food and Drug Administratio"...

Luzu

CLINICAL PHARMACOLOGY

Mechanism of Action

LUZU Cream, 1% is an azole antifungal.

Pharmacodynamics

At therapeutic doses, LUZU Cream, 1% is not expected to prolong QTc to any clinically relevant extent.

Pharmacokinetics

Luliconazole is the R enantiomer of a chiral molecule. The potential for inter-conversion between R and S enantiomers in humans has not been assessed. Information on the pharmacokinetics of luliconazole presented below refers to both R enantiomer and S enantiomer, if any, combined.

Luliconazole is > 99% protein bound in plasma.

In a pharmacokinetic trial, 12 subjects with moderate to severe tinea pedis and 8 subjects with moderate to severe tinea cruris applied a mean daily amount of approximately 3.5 grams of LUZU Cream, 1% to the affected and surrounding areas once daily for 15 days. Plasma concentrations of luliconazole on Day 15 were measurable in all subjects and fluctuated little during the 24 hour interval. In subjects with tinea pedis, the mean ± SD of the maximum concentration (Cmax) was 0.40 ± 0.76 ng/mL after the first dose and 0.93 ± 1.23 ng/mL after the final dose. The mean time to reach Cmax (Tmax) was 16.9 ± 9.39 hours after the first dose and 5.8 ± 7.61 hours after the final dose. Exposure to luliconazole, as expressed by area under the concentration time curve (AUC0-24) was 6.88 ± 14.50 ng*hr/mL after the first dose and 18.74 ± 27.05 ng*hr/mL after the final dose. In subjects with tinea cruris, the mean ± SD Cmax was 4.91 ± 2.51 ng/mL after the first dose and 7.36 ± 2.66 ng/mL after the final dose. The mean Tmax was 21.0 ± 5.55 hours after the first dose and 6.5 ± 8.25 hours after the final dose. Exposure to luliconazole, as expressed by AUC0-24 was 85.1 ± 43.69 ng*hr/mL after the first dose and 121.74 ± 53.36 ng*hr/mL after the final dose.

Microbiology

Mechanism of Action

Luliconazole is an antifungal that belongs to the azole class. Although the exact mechanism of action against dermatophytes is unknown, luliconazole appears to inhibit ergosterol synthesis by inhibiting the enzyme lanosterol demethylase. Inhibition of this enzyme's activity by azoles results in decreased amounts of ergosterol, a constituent of fungal cell membranes, and a corresponding accumulation of lanosterol.

Mechanism of Resistance

To date, a mechanism of resistance to luliconazole has not been described.

LUZU Cream, 1% has been shown to be active against most isolates of the following fungi, both in vitro and in clinical infections as described in the INDICATIONS AND USAGE section:

Trichophyton rubrum
Epidermophyton floccosum

Clinical Studies

Interdigital Tinea Pedis

The safety and efficacy of LUZU (luliconazole) Cream, 1% was evaluated in two randomized, double-blind, vehicle-controlled, multi-center clinical trials in 423 subjects with a clinical and culture-confirmed diagnosis of interdigital tinea pedis. Subjects were randomized to receive LUZU Cream, 1% or vehicle. Subjects applied either LUZU Cream, 1% or vehicle cream to the entire area of the forefeet including all interdigital web spaces and approximately 2.5 cm (1 in) of the surrounding area of the foot once daily for 14 days.

The mean age of the study population was 41 years; 82% were male; 53% were White and 40% were Black or African American. Signs and symptoms of tinea pedis (erythema, scaling, and pruritus), KOH exam and dermatophyte culture were assessed at baseline, end-of-treatment (Day 14), 2 and 4 weeks post-treatment.

Overall treatment success was defined as complete clearance (clinical cure and mycological cure) at 4 weeks post-treatment. LUZU Cream, 1% demonstrated complete clearance in subjects with interdigital tinea pedis. Treatment outcomes at 4 weeks post-treatment are summarized in Table 1.

Table 1: Efficacy Results at 4 Weeks Post-treatment – Interdigital Tinea Pedis

  Study 1 Study 2
LUZU Cream, 1%
N= 106
n (%)
Vehicle Cream
N= 103
n (%)
LUZU Cream, 1%
N= 107
n (%)
Vehicle Cream
N= 107
n (%)
Complete Clearance1 28 (26%) 2 (2%) 15 (14 %) 3 (3%)
Effective Treatment2 51 (48%) 10 (10%) 35 (33%) 16 (15%)
Clinical Cure3 31 (29%) 8 (8%) 16 (15%) 4 (4%)
Mycological Cure4 66 (62%) 18 (18%) 60 (56%) 29 (27%)
1Proportion of subjects who achieved both clinical cure and mycological cure
2Negative KOH and culture and at most mild erythema and/or scaling and no pruritus
3Absence of erythema, scaling and pruritus
4Negative KOH and negative fungal culture

Tinea Cruris

The safety and efficacy of LUZU (luliconazole) Cream, 1% was evaluated in a randomized, double-blind, vehicle-controlled, multi-center clinical trial in 256 subjects with a clinical and culture confirmed diagnosis of tinea cruris. Subjects were randomized to receive LUZU Cream, 1% or vehicle. Subjects applied either LUZU Cream, 1% or vehicle cream to the affected area and approximately 2.5 cm (1 in) of the surrounding area once daily for 7 days.

The mean age of the study population was 40 years; 83% were male; 58% were White and 34% were Black or African American. Signs and symptoms of tinea cruris (erythema, scaling, and pruritus), positive KOH exam and dermatophyte culture were assessed at baseline, end-of-treatment (Day 7), 2 and 3 weeks post-treatment.

Overall treatment success was defined as complete clearance (clinical cure and mycological cure) at 3 weeks post-treatment. LUZU Cream, 1% demonstrated complete clearance in subjects with tinea cruris. Treatment outcomes at 3 weeks post treatment are summarized in Table 2.

Table 2: Efficacy Results at 3 Weeks Post-treatment - Tinea Cruris

  LUZU Cream, 1%
N= 165
n (%)
Vehicle Cream
N= 91
n (%)
Complete Clearance1 35 (21%) 4 (4%)
Effective Treatment2 71 (43%) 17 (19%)
Clinical Cure3 40 (24%) 6 (7%)
Mycological Cure4 129 (78%) 41 (45%)
1Proportion of subjects who achieved both clinical cure and mycological cure
2Negative KOH and culture and at most mild erythema and/or scaling and no pruritus
3Absence of erythema, scaling and pruritus
4Negative KOH and negative fungal culture

Last reviewed on RxList: 11/27/2013
This monograph has been modified to include the generic and brand name in many instances.

A A A

Report Problems to the Food and Drug Administration

 

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.


Women's Health

Find out what women really need.


From WebMD