Constipation, stomach pains, and nausea affect patients with opioid-induced constipation (OIC) to such an extent that they can be forced to discontinue treatment. Conventional laxatives are often insufficient. The new PAMORA drug class can help target the adverse intestinal effects of opioids – without negatively affecting central pain inhibition. Naloxegol (MOVENTIG®) is the first of this new class of drugs on the market which can be taken in tablet form. This was reason enough for the specialist pain therapist group to name MOVENTIG® the most innovative product of 2020.
Moventig® – Doctors’ experience
In the Pharma Trend 2020 survey, 29% of the surveyed pain specialists chose MOVENTIG® for the award of “Most Innovative Product”. The product by Kyowa Kirin was placed ahead of another orally ingested product of the same drug class, the even newer Naldemedine (Rizmoic®, Shionogi/Hexal). Rizmoic took third place with 5% of the votes. The silver medal was shared between Resolor® (Takeda) and Movicol (Norgine), each with 6%. For 69% of specialist physicians questioned, its innovative mechanism of action was the reason they chose MOVENTIG®. The fact that it is almost free of adverse effects (38%) and improved efficacy (34%) were also named as compelling reasons.
OIC: Evident in almost every case of opioid treatment
The same opioid μ-receptors responsible for analgesic effects in the brain are also found in the intestines. The activation of the intestinal receptors by orally ingested opioids slows down normal intestinal movement (peristalsis). The longer the opioid therapy lasts, the more likely it is that the patient will suffer from constipation. “Constipation, which is an opioid drug class effect, develops sooner or later in between 3 and 95% of patients undergoing opioid treatment”, says Thomas Hibbe, Medical Director at Kyowa Kirin. According to Mr Hibbe, the impact of OIC on daily life and quality of life was underestimated for many years by physicians. Constipation is only the tip of the iceberg; there are more accompanying symptoms of intestinal paralysis, such as abdominal pain, nausea, and vomiting, alongside reduced absorption of orally ingested drugs. According to the German Society for Pain Medicine (DGS e.V. in German), these side effects often lead patients to discontinue their necessary course of opioid therapy.
The PAMORA class drug MOVENTIG® causally improves OIC
Like Naldemedine (Rizmoic®), MOVENTIG® (Naloxegol) belongs to the PAMORA (peripherally acting μ-opioid receptor antagonist) class of drugs. In contrast to older types of μ-opioid receptor antagonists, such as Naloxone, the effects of PAMORA drugs are limited to the periphery. Naloxegol achieves this through a combination of Naloxone and polyethylene glycol (PEG). As a “pegylated” derivative of Naloxone, Naloxegol can no longer pass the blood-brain barrier.
Naloxegol is also the substrate of an efflux transporter in the blood-brain barrier (P-glycoprotein), which immediately channels it back into the bloodstream. Overall, Naloxegol is only effective in the periphery. In the intestines, it counteracts the unwanted motility and secretion-inhibiting effects of opioids. This allows for a return to regular intestinal peristaltic activity and normalisation of bowel movements.
MOVENTIG® is indicated for the treatment of opioid-induced constipation (OIC) in adults who have shown an inadequate response to one or more laxative products. In contrast to Methylnaltrexone (Relistor®), which is administered subcutaneously daily or every second day, the patient is only required to take MOVENTIG® once daily as a tablet.
What counts are mechanism of action, lack of adverse effects as well as ease of use
The award of “Most Innovative Product” is in recognition of the innovation and therapeutic benefit of the drug. The most important criteria for pain therapists when choosing their candidate for the most innovative drug was a new mechanism of action (45%), lack of adverse effects (39%), and ease of use (32%), which has been achieved with the oral administration of MOVENTIG® in tablet form.