CC-408 – A potentially non addictive opiate based analgesic agent
                                    CC-408 is an inactive chemical derivative of oxycodone.  After oral ingestion CC-408 releases oxycodone via a first order process with a 10 hour half life to yield a plasma oxycodone concentration profile that is truly compatible with a twice-a-day dosing regimen.  Moreover, the slow monophasic release of oxycodone from CC-408 in the digestive tract is anticipated to preclude euphoria, minimize addictive reinforcing effects, and lower the incidence of constipation seen with OxyContin® and immediate release oxycodone formulations. In contrast to OxyContin, the rate of release of oxycodone from CC-408 is unaffected by breaking or chewing or dissolving CC-408 tablets.

Potential Market for CC-408

Pain is the most common reason for seeking medical assistance. The American Academy of Pain Medicine estimates that 50 million people in the U.S. suffer from serious chronic pain lasting more than one month, that 45 million Americans seek care for persistent pain at some point in their lives, and that the annual cost of pain in the U.S. (due to the loss of 4 billion work days) is about 79 billion dollars. Low back pain, one of the most common pain complaints, accounts for over 8 million physician visits per year. Although numerous approaches have been used to treat pain, opiates in the morphine class are the cornerstone of pain management. Oxycodone, a semi-synthetic opiate mu receptor agonist in use since 1917, is one of the most frequently used drugs in this category. A controlled-release formulation of oxycodone called OxyContin® became available in 1996 and definitively improved pain management by providing relief from moderate to severe chronic pain with a twice-a-day oral formulation rather than the four-six times a day dosing required for immediate-release oxycodone. OxyContin (containing 10-80 mg of oxycodone) is now the number one brand name controlled pharmaceutical. Retail OxyContin sales for 2008 were $2.5 billion.

Competition 

CC-408 is a new molecular entity designed to overcome the shortcomings of OxyContin®.  Controlled Chemicals Inc., the parent of Samada Research, holds an issued US Patent (US 7,230,005 B2, filing date Mar 15, 2004) claiming CC-408 and related compositions of matter issued on June 12, 2007. Related patents are issued or pending in Mexico, Canada, Japan and EPO contracting states. Samada anticipates that generic sustained-release oxycodone formulations priced below that of OxyContin will become available after 2013.  The generic formulations, however, will have the same shortcomings of OxyContin.  

The oxycodone in each OxyContin tablet is encapsulated in a matrix from which about 62% of the oxycodone is slowly released so as to increase its duration of action. The remaining 38% of the oxycodone is released rapidly as a bolus that produces light headedness and mild euphoria.  The reinforcing effects of this dose related euphoria may well be a determinant of addiction.  In contrast to OxyContin, CC-408 is an inactive prodrug that gradually releases all of its oxycodone via a monophasic first order process.  The gradual release of oxycodone from CC-408 is anticipated to preclude dose related light-headedness and reinforcing addictive effective effects with CC-408.

Simply chewing or otherwise breaking OxyContin tablets compromises its controlled-release action so as to produce a morphine-like high as well as a potentially fatal rise in systemic oxycodone concentration.  Chewing or otherwise breaking or even dissolving CC-408 tablets does not alter the release of oxycodone from CC-408.   A chemical bond must be broken to release oxycodone from CC-408.

OxyContin does not support a twice-a-day dosing regimen in most patients as evidenced by recent surveys of OxyContin dosing that found that more than half of patients using OxyContin need to take the drug more frequently than every 12 hours (usually every 8 hours) to maintain analgesia throughout the dosing interval.  The 10 hour half life for the release of oxycodone from CC-408, however, is truly compatible with twice-a-day dosing.

Thus, Samada Research anticipates that considerations of safety, abuse potential, tolerability, and duration of analgesia will make CC-408 a first line opiate-based analgesic agent.

                       Anticipated Advantages of CC-408