Pharmacologic class: Peripherally acting mu-opioid receptor antagonist (PAMORA)
Active ingredient(s): Naloxegol 12.5mg, 25mg; tablets
Company: AstraZeneca Pharmaceuticals
Indication(s): Opioid-induced constipation in adults with chronic non-cancer pain.
Pharmacology: Naloxegol is an antagonist of opioid binding at the mu-opioid receptor. When administered at the recommended dose levels, naloxegol functions as a peripherally acting mu-opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids.
The safety and efficacy of Movantik was evaluated in two replicate, randomized, double-blind, placebo-controlled trials (Study 1 and Study 2) in patients with opioid-induced constipation (OIC) and non-cancer related pain. Patients in Study 1 (n=652) and Study 2 (n=700) were randomized to receive Movantik 12.5mg, Movantik 25mg, or placebo once daily for 12 weeks. The primary endpoint was response defined as: ≥3 spontaneous bowel movements per week and a change from baseline of ≥1 spontaneous bowel movement per week for at least 9 of the 12 study weeks and 3 of the last 4 weeks.
In Study 1, there was a statistically significant difference for the Movantik 12.5 mg and 25 mg treatment groups vs. placebo for the primary endpoint. In the Movantik 12.5 mg group, 41% showed response (difference 11.4%; [95% CI: 2.4, 20.4]; P = .015), and 44% showed response (difference 15%; [95% CI: 5.9, 24.0]; P = .001) in the Movantik 25 mg group, as compared to 29% in the placebo group. In Study 2, there was a statistically significant difference for the Movantik 25-mg treatment group vs. placebo, but not for the Movantik 12.5-mg treatment group. In the Movantik 12.5-mg group, 35% of patients had a response (difference 5.6%; [95% CI: −2.9, 14.1]; P = .202), and 40% had a response in the Movantik 25-mg treatment group (difference 10.3%; [95% CI: 1.7, 18.9]; P = 0.021), as compared to 29% in the placebo group.
For more clinical trial data, see full labeling.
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