AIKO-150, an experimental drug to treat to treat constipation associated with opoid use, has completed the second phase-I human clinical, Aiko Bio announced.
AIKO-150 does not interfere with pain relief in healthy subjects at doses which prevent the gastro-intestinal slowing (i.e. constipation) associated with opioid use in trial.
AIKO-150 is a neutral opioid antagonist targeted for the treatment of opioid-induced side effects including opioid-induced bowel dysfunction and addiction.
AIKO-150 is Aiko’s lead compound in its portfolio of naltrexone/naloxone analogs, such as naltrexol, naltrexamine, naloxol and their derivatives, shown to be neutral at the mu opioid receptor (patent 6713488).
Aiko’s second exploratory phase-I trial was designed to demonstrate that AIKO-150 does not interfere with pain relief in healthy subjects, is safe, and peripherally selective.
Four increasing doses of AIKO-150 were administered to healthy subjects who were also administered morphine.
Over 200 million prescriptions for opioids are written annually in the US, and up to 90% of patients experience constipation, nausea and vomiting, and other bowel dysfunction.
The total worldwide market in 2007 was over $7.5 billion in opioid sales. Coincident with market growth, opioid abuse has tripled in the last decade.
“This second trial has confirmed the high potency of AIKO-150 in selectively improving bowel motility while not interfering with pain relief,” said trial the lead compound in its portfolio of opioid antagonists designed to improve pain therapy, according to Wolfgang Sadee, chief scientific officer.
Confirming findings from the first phase-I trial, these results, combined with high tolerability and safety, support development of AIKO-150 as a drug meeting an urgent clinical need, with outstanding commercial potential, he said.
Results showed extremely high potency in blocking opioid GI effects with no interference of opioid-induced pain relief. No significant adverse effects. Dose-proportional pharmacokinetics.
The second trial completed under the US FDA’s Exploratory IND mechanism confirmed the prediction that AIKO-150 does not interfere with pain relief while preventing GI slowing.
Support for this trial was provided, in part, by a Development Award from the Maine Technology Institute.
Aiko Biotechnology, Inc is a start-up biotechnology company located in Portland, Maine, focused on the discovery and validation of novel compounds for the treatment of pain and the side effects associated with prescription pain reliever (opioid) use, such as GI dysfunction, addiction and abuse.