Comparative Pharmacology
Head-to-head clinical analysis: FEXINIDAZOLE versus MEPRON.
Peer-Reviewed Evidence
Head-to-head clinical analysis: FEXINIDAZOLE versus MEPRON.
FEXINIDAZOLE vs MEPRON
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Fexinidazole is a nitroimidazole derivative that enters the parasite and inhibits DNA synthesis by forming reactive metabolites, leading to cell death. It is active against Trypanosoma brucei gambiense.
It is a hydroxynaphthoquinone that selectively inhibits mitochondrial electron transport chain in Plasmodium species, specifically at the cytochrome bc1 complex (Complex III), leading to collapse of mitochondrial membrane potential and inhibition of pyrimidine synthesis.
500 mg orally twice daily for 10 days for trichomoniasis; 2 g orally single dose for giardiasis.
750 mg orally twice daily with food for 21 days for treatment of mild-to-moderate Pneumocystis jirovecii pneumonia. For prophylaxis: 1500 mg orally once daily with food.
None Documented
None Documented
Approximately 8-12 hours in adults; prolonged in hepatic impairment.
Mean terminal elimination half-life is 2.2-3.2 days (approximately 53-77 hours) in adults; prolonged in hepatic impairment (up to 22 days) and in elderly (up to 5 days).
Primarily renal (60-70% unchanged), with 20-30% biliary/fecal.
Primarily fecal (87-94%) via bile; renal excretion accounts for <1% as unchanged drug. A minor metabolite, atovaquone glucuronide, is excreted in urine.
Category C
Category C
Antiprotozoal
Antiprotozoal