Xenome has begun a Phase I/IIa trial of Xen2174, a new class of peptide therapeutic for the treatment of severe intractable pain. The trial is an open-label, single-blind, multicenter, single-dose, dose-escalating, safety and tolerability study of intrathecally administered Xen2174 in cancer patients suffering severe intractable pain. The trial will be conducted at multiple sites in Australia.
Xen2174, a chi conopeptide, is derived from the venom of the cone snail. It has been shown to selectively inhibit the norepinephrine transporter (NET), a drug target in the central nervous system. In the spinal cord, norepinephrine is the dominant neurotransmitter that activates the descending inhibitory pain pathway. Delivery of Xen2174 directly into the space around the spinal cord deposits the drug adjacent to the NET so that in episodes of pain, pain signals are prevented from reaching the brain.