Comparative Pharmacology
Head-to-head clinical analysis: CRESEMBA versus LAMISIL AT.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CRESEMBA versus LAMISIL AT.
CRESEMBA vs LAMISIL AT
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Isavuconazole, the active moiety of CRESEMBA, inhibits fungal cytochrome P450-dependent 14-alpha-demethylase, thereby blocking the conversion of lanosterol to ergosterol, disrupting fungal cell membrane synthesis and function.
Terbinafine inhibits squalene epoxidase, an enzyme in the fungal ergosterol biosynthesis pathway. This leads to accumulation of squalene and depletion of ergosterol, disrupting fungal cell membrane integrity and causing cell death.
200 mg intravenously every 8 hours for the first 48 hours (6 doses), then 200 mg intravenously once daily; or 200 mg orally three times daily for the first 48 hours (6 doses), then 200 mg orally once daily.
Terbinafine 250 mg orally once daily for 6 weeks for fingernail onychomycosis or 12 weeks for toenail onychomycosis. Topical: 1% cream applied once daily for 1 week for tinea pedis; 1% solution applied once daily for 1 week for tinea corporis/cruris.
None Documented
None Documented
Terminal elimination half-life is approximately 24 hours (range 20-30 hours) after oral administration, supporting once-daily dosing; steady-state achieved by Day 4-5.
The terminal elimination half-life is approximately 11-17 hours in healthy adults; however, it increases to about 200-400 hours in the distribution phase from tissues (e.g., skin, adipose). Steady-state is reached after 10-14 days of oral dosing.
Fecal: ~76% (primarily as unchanged drug); Renal: <1% (unchanged); Biliary: Not a major route; Metabolism via CYP3A4 to inactive metabolites eliminated fecally.
Terbinafine is extensively metabolized in the liver; approximately 80% of a dose is excreted in urine as metabolites, and 20% in feces. Less than 1% is excreted unchanged in urine.
Category C
Category C
Antifungal
Antifungal