Serlopitant

Neurokinin-1 receptor antagonist that may be used in patients with severe chronic itching that does not respond to antihistamines or topical glucocorticoids.

Serlopitant is a "small molecule" that is highly potent and selectively antagonizes the NK1 receptor. The substance can easily pass the blood-brain barrier and binds > 90% of the NK1 receptors. This signalling pathway is an essential component in the development of itching.

In a larger multicenter study, patients were treated with either serlopitant (0.25, 1 or 5 mg) or placebo. The drug was administered once daily for six weeks as monotherapy or with steroids and emollients of medium potency. This showed a dose-dependent decrease in itching (Yosipovitch G et al. 2018).

Dosage: 1.0 mg - 5.0 mg/day.

1. Frenkl TL et al (2010) A Multicenter, Double-Blind, Randomized, Placebo Controlled Trial of a Neurokinin-1 Receptor Antagonist for Overactive Bladder. The Journal of Urology 184: 616-622.
2. Payton S et al (2010) Urinary Incontinence: Neurokinin Receptor Antagonist Inferior to Tolterodine for OAB. Nature Reviews Urology 7: 418.
3. Yosipovitch G et al (2018) Serlopitant for the treatment of chronic pruritus: Results of a randomized, multicenter, placebo-controlled phase 2 clinical trial. J Am Acad Dermatol 78:882-891.