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Analgesics can produce pain relief by acting centrally in the brain where they mimic the actions of neuromodulators called endogenous opioids (endorphins, dynorphins, enkephalins) and "block" the sensation of pain. Using a novel approach, Dr. James Zadina and his coworkers at Tulane University identified a new class of agents, the endomorphins (EMs), as the natural ligands for the mu-opioid receptor - the receptor considered by many to be the most important for the control of pain and the target for many effective drugs, including opioids. The high affinity and selectivity of EMs for the mu-opiod receptor support the position that drugs possessing the novel structural features of this class of natural molecules have desirable therapeutic properties and advantages over currently available opioid analgesics.

Dr. Zadina's Tulane group was awarded two comprehensive patents including composition of matter claims to the most effective naturally occurring molecule - EM1. Through subsequent structure-function studies, Dr. Zadina and colleagues identified the critical structural elements of the EM molecule responsible for its activities and generated a family of molecules based on the core structure of EM1 that possessed enhanced affinity for the mu-opiod receptor and additional advantageous pharmacologic properties. This family of novel molecules was specifically protected in one of the issued Tulane patents. One of these new molecules with a particulary desirable pharmacologic profile, designated Cyt-1010, has been selected by Cytogel as its primary product candidate.

Cytogel acquired from Tulane the exclusive, worldwide license for their patents relating to the endomorhins and related species. The Company is pursuing strategic opportunities to expand its intellectual property pertaining to Cyt-1010 and its variants as the scientific development of Cyt-1010 progresses.


Primary Product Candidate: Cyt-1010

Cyt-1010 has demonstrated robust analgesic activity in a number of animal pain models, including acute and neuropathic pain, by several routes of administration.

 

The potency of Cyt-1010 in animal studies correlates well with the high affinity of the molecule for the mu-opiod receptor in binding studies and supports the development of the molecule for human testing. In animal studies of abuse potential, Cyt-1010 lacked significant activity that was demonstrated with morphine at similar effective dose levels, providing a compelling rationale for the development of this molecule.