Zileuton, an Oral 5-Lipoxygenase Inhibitor, Directly Reduces Sebum Production

Abstract

Background: Zileuton, a 5-lipoxygenase inhibitor, reduces the number of inflammatory lesions in moderate acne and inhibits the synthesis of sebaceous lipids. Objective: To detect whether zileuton directly reduces sebum synthesis. Methods: A 40-year-old female with mild disseminated sebaceous gland hyperplasia and seborrhea was treated with zileuton 4 × 600 mg/day over 2 weeks, was followed-up for 6 weeks after discontinuation of zileuton and was re-treated with low-dose isotretinoin 10 mg/2nd day over 5 weeks. Casual skin surface lipids and sebum synthesis were determined. Results: Under treatment with zileuton increased casual skin surface lipids were normalized and synthesis of facial sebum was decreased. Six weeks after discontinuation of treatment casual skin surface lipids were increased again and synthesis of sebum returned to baseline. Subsequent low-dose isotretinoin treatment led to similar changes of casual skin surface lipids and sebum synthesis with zileuton already after 2 weeks. Conclusion: Zileuton directly inhibits sebum synthesis in a transient manner with a potency similar to low-dose isotretinoin at least in our patient.

Hiperplasia sebácea cutânea: estudo piloto para a correlação da doença com hormônios androgênios

“…Other procedures that have also been used include excision, electrocauterization, cryotherapy, shaving, curettage and cauterization with chemical agents used topically, although there is a risk of depigmentation or scarring with these latter options. [16][17][18][19][20][21][22][23][24][25] Many laboratory studies have shown the effect of androgens on the sebaceous glands. A review of the literature on several research models confirmed the effect of androgens in triggering the activity of the sebaceous glands and indicated which of these hormones may be implicated in triggering these glands.…”

Zileuton, a new efficient and safe systemic anti-acne drug

“…The following primers and probes were used: PPARα sense Clinical studies. 23, 24 An open-label drug, ethic committeeapproved, industry-independent study in a small cohort of 10 consecutive patients (4 female, 6 male; median age 17 years) inhibitors as a definitive step for modulation of LT effects in acne patients. Our pilot clinical study with systemic administration of Zileuton in 10 patients with inflammatory acne has detected anti-inflammatory and lipid reducing effects of the compound.…”

“…23 Searching for the primary effect, we have observed that Zileuton inhibited the synthesis of sebaceous lipids in a patient with no inflammatory signs. 24 Inhibition of lipid synthesis, especially of pro-inflammatory lipids, is likely to be the major effect of Zileuton on sebaceous glands followed by reduction of inflammatory lesions in acne. 23 The direct effect of Zileuton on the synthesis of sebaceous lipids was confirmed in the in vitro study.…”

“…over 3 weeks) after receiving written consent. 24 Casual skin surface lipids (CSSL) of the central forehead were measured at 4 p.m. using a computerized photometric devise. To determine new sebum synthesis (NSS), defined areas of the central forehead and the left temple were wiped twice with ethanol after measuring CSSL.…”

“…21 We have conducted experimental 22 and clinical studies 23,24 to test mode of function, as well as efficacy and safety of this compound in the treatment of acne vulgaris.…”