Lotilaner (Xdemvy)

概览

Lotilaner is an antiparasitic agent used to treat Demodex blepharitis.

作用机制

Lotilaner is a non-competitive antagonist of the gamma-aminobutyric acid (GABA)-gated chloride channel (GABACl) selective for mites. Inhibition of GABACl causes a paralytic action in the target organism, leading to death. Lotilaner is not an inhibitor of mammalian GABA-mediated chloride channels when tested at up to 30 µM (18 µg/mL) in vitro, which is approximately 1100 times the recommended human ophthalmic dose. The target site in GABACl is hypothesized to be localized in a pore between the T9’ to S15’ region, an interstitial subunit region. A study suggested that lotilaner may migrate within the pore of the GABACl to its final location to stabilize the channel in a closed state; however, this hypothesis requires further investigation.

适应症

Lotilaner is indicated for the treatment of Demodex blepharitis.

• Demodex Blepharitis