Advertise With UsAdvertise on our extensive network of industry websites and newsletters.
Get the PBR newsletterSign up to our free email to get all the latest PBR
news.Theravance, a biopharmaceutical company, has dosed first patient with opioid-induced constipation (OIC) in a Phase 2 clinical study with TD-1211, an orally-administered peripherally selective mu opioid receptor antagonist (PUMA). The proof of concept study is designed to assess the efficacy, tolerability and safety of TD-1211 in patients with OIC.
Subscribe to our email newsletter
TD-1211 is a potent, multivalent inhibitor of the mu opioid receptor designed to alleviate gastrointestinal side effects of opioid analgesic therapy without affecting analgesia.
TD-1211 has been administered to healthy volunteers in ascending single and repeat dose studies evaluating safety, tolerability and pharmacokinetics. The results of these studies showed that TD-1211 was well tolerated at all doses administered, and had a predictable and linear pharmacokinetic profile supportive of once-daily dosing.
The Phase 2 clinical study is a randomised, double-blind, multiple-ascending dose study that is expected to evaluate the constipation-relieving effects, safety and tolerability of TD-1211 in patients experiencing constipation while receiving chronic opioid therapy.
Theravance said that approximately 50 patients experiencing OIC will be randomised to TD-1211 or placebo in addition to their opioid treatment. Therapy will be administered orally once-daily over 14 days of treatment. The primary efficacy endpoint of the study is the frequency of spontaneous bowel movements (SBMs). The study will compare the frequency of SBMs in patients receiving TD-1211 to those in patients receiving placebo.
Mathai Mammen, senior vice president of research and early clinical development at Theravance, said: “TD-1211 is a multivalent compound that was designed to contact both a primary and secondary binding pocket on the mu opioid receptor. The secondary binding moiety confers excellent selectivity over non-opioid receptors, and limits penetration into the CNS. We are excited that our core technology continues to yield promising differentiated clinical candidates for patients in need.”
Rick Winningham, CEO of Theravance, said: “There is a significant unmet medical need as there are currently no oral drugs approved in the US to treat constipation resulting from the chronic use of opioids in treating and managing pain. We look forward to the results of this proof of concept study later this year.”