Xartemis XR receives FDA approval: May reduce opioid abuse

Oxycodone hydrochloride and acetaminophen (Xartemis XR, Mallinckrodt) Extended-Release Tablets (CII) were approved for the management of acute pain requiring opioid treatment. Xartemis XR has been specifically formulated to reduce abuse, according to the drug’s manufacturer.

As the first and only extended-release oral combination of 2 clinically proven pain medications-oxycodone and acetaminophen-its approval comes at a time when prescriptions for pain medication are soaring. Every year, up to 100 million Americans suffer from some form of chronic pain, according to the Institute of Medicine, and national statistics show that 46 million experience acute pain following inpatient procedures. In the past decade sales of opioid pain relieving drugs have quadrupled, but overdoses due to opioid use have also jumped. A large portion of overdose deaths have been linked to prescribed opioids including Percocet (acetaminophen and oxycodone), and Oxycontin (oxycodone).

While all opioids can be abused, Xartemis XR uses technology that requires abusers to exert an additional effort to extract the active ingredient from its large quantity of inactive and deterrent ingredients.

Xartemis XR contains a low amount of oxycodone in each tablet (7.5 mg), and the large tablet size includes inactive ingredients that make abuse by snorting and injection more difficult. An inactive ingredient called polyethylene oxide (PolyOx) makes the tablets more difficult to crush, break or dissolve. When dissolved in liquid, Xartemis XR transforms into an unpalatable, gelatinous mixture, making it far more challenging to draw the substance into a syringe for IV administration. Likewise, the formulation impedes "cooking" it on a spoon, and if snorted, the humidity in the nasal passage turns it into a thick, pasty substance.

A comparison study also showed that when used intact, recreational drug users preferred Percocet over Xartemis XR.

The approval is partly based on a pivotal phase 3 efficacy study, that was conducted in an acute post-surgical pain model. Xartemis XR met the primary end point and demonstrated   statistically significant improvements in pain scores from baseline over a 48-hour period, as compared to placebo.

The approval label does not currently include abuse-deterrent language, but the manufacturer states that they are continuing to work closely with FDA on more data to characterize the abuse-deterrence features of this product.