Lexacalcitol

Lexacalcitol (KH1060) is a vitamin D analog that demonstrates significantly higher activity than 1alpha,25-dihydroxyvitamin D3 (calcitriol) in in vitro antiproliferative and cell differentiating assays. It undergoes rapid metabolism in vivo and in vitro through various cytochrome P450-mediated enzyme systems, yielding hydroxylated metabolites, such as 24-, 24a-, 26-, and 26a-hydroxylated derivatives, as well as side-chain truncated forms. Notably, many of these metabolites retain substantial biological activity in vitamin D-dependent assay systems. Studies have shown that topical application of Lexacalcitol can cause mild irritation, characterized by vasodilation and increased cutaneous blood flow, but it does not lead to corrosion or increased transepidermal water loss. It is being investigated for its potential in hyperproliferative disorders.

Other names

lexacalcitol20-epi-vitamin D3 analog