Sertaconazole (nitrate)

Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells^[1][2][3][4]. In Vitro: Sertaconazole nitrate (0.03-40 µg/mL; 24 h) inhibits 150 strains of yeasts which includes six Candida species with arithmetic mean MIC of 0.77 µg/mL^[1].
Sertaconazole nitrate (1 µg/mL; 5, 10, 30, 60 min) activates p38 MAP kinase in a time-dependent manner^[2].
Sertaconazole nitrate (1, 2 µg/mL; 6, 8, or 24 h) increases a twofold release of PGE2 via COX-2 in keratinocytes, which is dependent on p38 activation^[2].
Sertaconazole nitrate (10, 20, 30, 40 µM; 24 h) induces strong mitotic arrest by depolymerizing interphase and spindle microtubules, thereby inducing chromosome aggregation defects and causing anti-proliferation effect^[3].
Sertaconazole nitrate (20, 40 µM; 24 h) induces apoptosis through p53 pathway in HeLa cells^[3].
Sertaconazole nitrate (20, 30 µM; 24, 48, and 72 h) inhibits the migration of HeLa cells in a concentration-dependent manner^[3].
Sertaconazole nitrate (15, 30 µM; 24 h) induces autophagy in A549, H460 cells^[4]. In Vivo: Sertaconazole nitrate (1% (w/v); apply to the left ear, once) suppresses of TPA-induced ear edema CD-1 mice^[2].