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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. The endomorphins (EMs) use a novel approach and are considered the natural ligands for the mu-opioid receptor - the receptor thought 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-opioid 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.

Through subsequent mechanism of action studies, Cytogel identified the critical binding and activation mechanism within the mu-opioid receptor for CYT-1010 that is differentiated from the classical opioids, and is thought to be responsible for its preferential profile of potent effectiveness and favorable safety. CYT-1010 binds preferentially to the truncated form of the mu-opioid receptor, while the classical opioids typically bind to the elongated form.

CYT-1010 and a few additional novel molecules are specifically protected in a number of issued and pending patents. Cytogel owns the rights to these patents outright in the U.S. and other major markets in the world.


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.