Low-dose morphine + oxycodone combo MoxDuo to treat severe pain shows promise: QRxPharma

MoxDuo CR, a controlled release dual opoid formulation containing morphine and oxycodone to provide 12 hours of pain relief in patients suffering from moderate to severe chronic pain, by QRxPharma, is currently undergoing clinical studies.

A phase 1 trial for MoxDuo CR has shown that the drug combo can provide 12 hours of pain relief in patients suffering from moderate to severe chronic pain including cancer, lower back, osteoarthritis and neuropathic.

The purpose of the trial was to determine which of the various experimental formulations provided the optimum duration of drug levels in the blood.

“We are now one step closer to addressing the needs of chronic pain patients and entering the multi-billion dollar chronic pain market,” stated Dr. John Holaday, managing director and chief Executive Officer, QRxPharma in a press statement.

QRxPharma remains on track to finalising the MoxDuo CR tablet by the end of this year and to be in a position to initiate Phase 2 trials shortly thereafter, he said.

The Phase 1 trial, a single dose crossover design, was conducted in 14 normal healthy volunteers at one U.S. clinical research site. This study compared the rate at which key components of the CR formulation were absorbed, distributed, metabolised and eliminated by the body to the pharmacokinetic profile of Oxycontin 20 mg (sustained release oxycodone).

Pharmacokinetic results are encouraging, and the profile is consistent with expectations for a twice-daily formulation. Data from this study will significantly aid QRxPharma and its manufacturing partner, Patheon Inc., in finalising the target release profile for the product and finalising the composition of prototype MoxDuo CR tablets.

QRx Pharma’s MoxDuo product portfolio includes both immediate and controlled release, as well as intravenous formulations.

QRxPharma’s dual opioid is based on patented discoveries at the University of Queensland. Scientists at the University postulated that the opioid oxycodone acts through a different set of neural receptors than other opioids like morphine, oxycodone or fentanyl. They also found that sub-analgesic doses of oxycodone have a synergy with sub-analgesic doses of other opioids, and therefore when combined together in low doses produce pain relief with fewer side effects and risks.

The clinical breakthrough of this patented combination is effective pain relief with a reduction in total daily opioid dose consumption. The dose related adverse effects of opioid-containing products limit their effectiveness and reduce quality of life. Side effects include respiratory depression, constipation, sedation and drowsiness, nausea and vomiting, and psychological dependence and tolerance. Fraud and abuse can also be major issues.

While combination analgesic products such as an NSAID plus an opioid (eg, Vicodin or Percocet) are widely used, at present there are no combination opioid products commercially available anywhere in the world.

Dual-Opioid technology refers to the use of two opioids that bind to different opioid receptor subtypes, thus providing improved tolerability and better pain relief.

The specific Dual-Opioid analgesics selected by QRx for development and commercialisation are morphine sulfate and oxycodone hydrochloride. These opioids were selected because they showed marked analgesic synergy in animal studies of acute and chronic pain and because they have a long history of clinical use as individual agents.

The lead product is an immediate release formulation, MoxDuo IR, currently in Phase 3 trials. It is a fixed ratio combination of morphine sulfate and oxycodone HCl and is available in capsule strengths of 3mg/2mg, 6mg/4mg and 12mg/8mg. Under development are controlled release (MoxDuoCR) formulations that provide for 12 hrs release and an injectible formulation for IV use (MoxDuo IV).

QRxPharma’s Dual-Opioid derives from patented discoveries at the University of Queensland.  Scientists at the University postulated that the opioid oxycodone acts through a different set of neural receptors than other opioids.

They also found that sub-analgesic (i.e., below traditional pain relief) doses of oxycodone have a synergy with sub-analgesic doses of other opioids, and therefore combinations of oxycodone with other opioids in lower doses can produce pain relief with fewer side effects and associated risks.

Evidence from the University of Queensland’s discovery has now been observed in both animal and human trials, and published in peer reviewed research papers.