Liarozole, a novel imidazole derivative, inhibits the cytochrome P450-
dependent 4-hydroxylation of retinoic acid, resulting in increased tis
sue levels of retinoic acid. Twelve male patients with ichthyosis were
given oral liarozole, 150 mg twice daily, in an open study for 12 wee
ks, Immunohistochemical parameters of inflammation, epidermal prolifer
ation and differentiation were assessed before and after treatment. Ex
tent and severity of the skin lesions was markedly reduced in all pati
ents. Clinical side-effects were reminiscent of those with synthetic r
etinoids. No relevant changes were found in the haematological, urinar
y and biochemical parameters. Immunohistochemical assessment showed a
statistically significant induction of keratin 4 after liarozole treat
ment in 10 of 12 patients. In two of these patients keratin 13 was ind
uced. This open study showed that oral liarozole treatment was efficac
ious and well tolerated in the treatment of different types of ichthyo
sis. The immunohistochemical results suggest a retinoid mechanism as t
he mode of action.