Asivatrep (PAC14028) is a selective and potent antagonist of transient receptor potential vanilloid subtype 1 (TRPV1) for the study of atopic dermatitis.

Asivatrep has demonstrated significant efficacy in several disease models, including visceral pain, inflammatory bowel disease, and inflammatory pain. Asivatrep has potential in the treatment of atopic dermatitis due to its ability to prevent damage to the skin barrier, accelerate barrier recovery, and inhibit itching.Asivatrep also reduces elevated serum levels of IgE, inhibits inflammatory cell infiltration in the epidermis, and degranulation of mast cells in atopic dermatitis.Asivatrep has been shown to be effective in preventing damage to the skin barrier, accelerating barrier recovery, and inhibiting itching. [2]

Pharmacokinetically, Asivatrep has a plasma half-life of 2.1 hours in rats and is slightly prolonged to 3.8 hours in minipigs. In addition, oral bioavailability was 52.7% in rats and 64.2% in minipigs, demonstrating good oral absorption. [1]
Asivatrep was able to inhibit capsaicin-induced calcium influx into keratinocytes at submicromolar concentrations, suggesting a potent TRPV1 antagonism. In vivo, Asivatrep blocked capsaicin-induced increase in blood perfusion and accelerated the recovery of skin barrier damage induced by tape stripping (in hairless mice). [3]