AFC-5128 is a potent CNS-penetrant oral P2X7 antagonist being developed for the treatment of neuropathic pain and multiple sclerosis.
P2X7 is an ATP-gated ion channel which is essential for the maturation and release of the pro-inflammatory cytokines, including interleukin-1beta (IL-1β). P2X7 activation can also lead to cell death in the presence of high levels of ATP.
A key competitive advantage of AFC-5128 is its ability to cross the blood-brain barrier and target P2X7 expressing cells in the central nervous system (CNS). Overexpression and activation of P2X7 in glia cells as well as other neuronal cells has been linked to neurodegenerative processes associated with diseases such as neuropathic pain and multiple sclerosis.