The invention pertains to novel hybrid peptidomimetics, pharmaceutical composition comprising thereof and use thereof in the treatment of neuropathic pain. The hybrid peptidomimetics according to the invention are comprised of two components: an opioid receptor agonist (OP) and a MC4 receptor antagonist, connected by a linker. The compounds of such a structure will allow to activate opioid receptors with simultaneous blocking of melanocortin type 4 receptors (MC4), which results in enhancing efficiency of the opioid therapy in neuropathic pain.