Naloxone derivative launched for opioid-induced constipation

Naloxegol (Moventig) provides a new option for the treatment of opioid-induced constipation in patients who have had an inadequate response to laxatives.

Naloxegol (Moventig) reduces the constipating effects of opioids without lessening their analgesic benefits.
Naloxegol (Moventig) reduces the constipating effects of opioids without lessening their analgesic benefits.

Further information
View Moventig drug record
Summary of Product Characteristics
Manufacturer: AstraZeneca

Naloxegol is a PEGylated derivative of the μ-opioid receptor antagonist naloxone. PEGylation (attachment to a molecule of polyethylene glycol, or PEG) prevents naloxegol from penetrating the CNS, allowing the drug to lessen the peripheral constipating effects of opioids without antagonising their central analgesic effects.

Spontaneous bowel movements

Two identical studies (KODIAC-04, n=652; KODIAC-05, n=700) were carried out in patients with non-cancer pain. Participants were randomised to receive a daily dose of either naloxegol (12.5mg or 25mg) or placebo to treat their opioid-induced constipation.

At 12 weeks, response rates (defined as 3 or more spontaneous bowel movements [SBMs] per week and a change from baseline of at least 1 SBM per week for at least 9 of the 12 study weeks and 3 of the last 4 weeks) were significantly higher than placebo with naloxegol 25mg in both studies (KODIAC-04, p=0.001; KODIAC-05, p=0.02) and with naloxegol 12.5mg in KODIAC-04 (p=0.02).

In KODIAC-04, the response rate was increased by 11.4 percentage points (95% CI 2.4−20.4) with the 12.5mg dose and by 15.0 percentage points (95% CI 5.9–24.0) with the 25mg dose compared with placebo.

In KODIAC-05, the differences in the response rate between active treatment and placebo were 5.6 percentage points (95% CI −2.9 to 14.1) with the 12.5mg dose and 10.3 percentage points (95% CI 1.7−18.9) with the 25mg dose.

Naloxegol use did not interfere with opioid-mediated analgesia.

Gastrointestinal effects

A third study, KODIAC-08 (n=804), demonstrated the long-term safety and tolerability of naloxegol. The most common adverse effects were abdominal pain and diarrhoea, which generally occurred early, resolved during or after naloxegol discontinuation, and were mild to moderate in severity. 

NICE approval

NICE recommends naloxegol as an option for treating opioid-induced constipation in adults who have not responded adequately to laxatives.

MIMS Clinics

Prescribing news and resources for key therapeutic areas, collated by the MIMS editors.

Register or Subscribe to MIMS

GPs can get MIMS print & online and GPonline for free when they register online – take 2 minutes, and make sure you get your free MIMS access! If you're not a GP, you can subscribe to MIMS for full access.

Register or subscribe

MIMS bulletins

News and updates straight to your inbox.

Prescribing Update: Fortnightly news bulletin
Urgent prescribing updates
Spotlight: Disease-themed monthly round-up

Sign me up

MIMS Dermatology

Read the latest issue online exclusively on MIMS Learning.

Read MIMS Dermatology

Mobile apps

MIMS: access the full drug database and quick-reference tables on the go

MIMS Diagnosis and Management: concise information on signs and symptoms, investigations and diseases

Promo Image

Clinical calculators

Handy calculators and conversions for primary care.