Climbazole

Climbazole has shown a high in vitro and in vivo efficacy against Pityrosporum ovale that appears to play an important role in the pathogenesis of dandruff. Its chemical structure and properties are similar to other fungicides such as ketoconazole and miconazole. For climbazole, the range of MICs is between < 0.06 and 1 μg/mL with an empirical median of 0.06 μg/mL. ^[1]

Climbazole is not mutagenic in the Salmonella typhimurium or Escherichia coli Ames assay and does not induce micronuclei in human lymphocytes. An in vivo mouse micronucleus test also shows it is non-mutagenic up to a maximum tolerated dose (MTD) of 150 mg/kg administered orally. In the in vivo/in vitro unscheduled DNA synthesis assay, climbazole shows no evidence of DNA damage in the livers of rats at doses up to the MTD of 200 mg/kg orally. A toxicokinetic study is performed in mice with oral administration of [¹⁴C]-climbazole (150 mg/kg). Radioactivity (20.42 μg-equiv./g plasma) is detected 15 min after oral administration of [¹⁴C]-climbazole, and the peak concentration is 62.96 μg-equiv./g plasma at 8 h after dosing. ^[2]