Chemical formula: C₁₂H₁₇NO₂ Molecular mass: 207.269 g/mol PubChem compound: 2749
Ciclopirox is a hydroxypyridone antifungal agent which is active in vitro inhibiting the growth of various fungal species including the yeast Malassezia furfur (formerly known as Pityrosporum ovale or Pityrosporum orbiculare). The latter has been implicated as a causative organism in dandruff and seborrhoeic dermatitis. Ciclopirox also exhibits some anti-inflammatory activity.
Ciclopirox 1.5% shampoo shows in vivo antifungal activity against Malassezia spp. A clinical study has shown that ciclopirox 1.5% shampoo significantly reduced the count of Malassezia furfur spp. in samples obtained from the scalp of subjects with dandruff and/or seborrhoeic dermatitis.
The potential for clinically significant systemic absorption of ciclopirox from a wash-off shampoo containing 1.5% ciclopirox is expected to be low.
Following oral administration of ciclopirox to humans, affinity of ciclopirox to serum proteins was found to be 96±2% in the concentration range of 0.01 to 11.0 µg/mL.
The metabolic patterns after oral and dermal application are similar. Glucuronidation of ciclopirox appears to be the major form of its metabolism.
Following oral administration of ciclopirox to humans, 96% of the administered dose is excreted within 12 hours. Ciclopirox is excreted in urine with approximately 80% of an oral dose excreted as the glucuronide metabolite.
Ciclopirox has been in use for twenty years. It is used in leave-on topical antifungal preparations and vaginal creams. Studies have not demonstrated any prohibitive findings in reproduction toxicology, mutagenicity, carcinogenicity or phototoxicity.
A dermal carcinogenic study in mice at concentrations of 1% and 5% ciclopirox formulated in polyethylene glycol 400 applied to the intact skin, twice a week, for one year, followed by a six-month non-treatment period was conducted. No tumours were observed in any of the mice at the site of application. Overall incidence of neoplasms was similar among the treated and control groups. In addition, there is no evidence that ciclopirox is carcinogenic following oral or subcutaneous administration to a number of animal species.
Ciclopirox did not cause gene mutation or chromosomal damage in severacterial mutagen assays or in two mammalian assays. In a battery of in vitro genotoxicity assays with ciclopirox free acid, one assay was weakly positive. The weight of evidence provided by the in vitro and in vivo assessments suggest that ciclopirox does not present a genotoxic hazard to humans.
Reproductive studies in mice, rats, rabbits and monkeys, at doses of ciclopirox 10 times that of a topical human dose, have revealed no significant evidence of impaired fertility or harm to the foetus. There is evidence that ciclopirox crosses the placental barrier in animals.
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