The recent first global approval of naldemedine has been reviewed in detail in the First Global Approval report in Adis journal Drugs, based on the development milestones tracked in AdisInsight.
In March 2017, naldemedine (Symproic®), developed by Shiongi & Co, Ltd, received its first global approval in the USA for the treatment of opioid-induced constipation in adult patients with chronic non-cancer pain.1 Naldemedine is an orally active π-opioid receptor antagonist that inhibits peripheral π-opioid receptors such as those present in the gastrointestinal tract, and has minimal or no effect on central opioid activity.
Shortly after the US approval, nalmededine was also approved in Japan for the treatment of opioid-induced constipation in patients with non-cancer and cancer pain.2 Shiongi has recently partnered with Purdue Pharma L.P. to jointly launch and commercialise the drug in the USA.
Due to its similar structure to naloxone, naldemedine is currently a Schedule II controlled substance, however, the manufacturer is seeking removal of this classification.
Constipation is a common side effect of opioid use, yet many patients are not effectively treated. Opioids are the most commonly prescribed pain-relieving medication for non-cancer and cancer pain in the US, with use exponentially growing. In the US, 4% of adults are receiving chronic opioid therapy, largely for non-cancer pain.3 In patients with chronic non-cancer pain, the prevalence of opioid-induced constipation is around 40-50%, and estimated to be up to 95% across all opioid users.4 The underlying cause of opioid-induced constipation is opioid binding to the π-opioid receptors in the enteric system. Opioids are often underprescribed for severe pain due to concerns about such side effects as well as addiction.