Asivatrep is an effective and selective transient receptor potential vanilloid type I antagonist.

Asivatrep displays efficacies against diverse disease models including visceral pain, inflammatory bowel disease, and inflammatory pain. Asivatrep could prevent barrier damages, accelerate skin barrier recovery, and inhibit pruritus, displaying a potential for the treatment of atopic dermatitis. It could inhibit serum IgE increase, epidermal infiltration of inflammatory cells, and mast cell degranulation associated with atopic dermatitis[1][2].

Asivatrep displays a plasma half-life of 2.1 h in rats while it is extended slightly to 3.8 h in minipigs. Asivatrep could inhibit capsaicin-evoked calcium influx in keratinocytes at sub-micromolar concentrations. This potent TRPV1 antagonistic activity in keratinocytes is manifested in vivo as the blockade of capsaicin-induced blood perfusion increases, and the accelerated barrier recovery from tape-stripping-induced barrier damages in hairless mice. Oral bioavailability at 10 mg/kg dose is determined to be 52.7% and 64.2% in rats and minipigs, respectively showing that Asivatrep is relatively well-absorbed through oral route[1][3].