Heptares starts dosing in Phase I trial of Alzheimer’s drug


UK-based Heptares Therapeutics has started dosing subjects in a Phase I clinical trial of HTL0016878 being developed for the treatment of neurobehavioural symptoms in Alzheimer’s disease patients.

HTL0016878 is an oral, small molecule agonist of muscarinic M4 receptor currently being developed by the firm in collaboration with Allergan.

Designed using Heptares’ structure-based drug design platform, the drug candidate selectively triggers the M4 receptor activity in the brain to potentially provide an improved safety profile.

The double-blind, randomised Phase I trial will evaluate the safety, tolerability and pharmacokinetics of single and multiple doses of oral HTL0016878 in approximately 106 healthy volunteers.

Preliminary results from the trial are expected to be available in the first half of next year.

"The target selectivity we can build into molecules increasingly highlights the potential of our approach to create new medicines with significantly improved clinical profiles for addressing a range of diseases."

Heptares Therapeutics chief medical officer Tim Tasker said: “The start of this new clinical trial marks the progression of the fourth compound designed by Heptares into clinical studies and follows the advancing clinical studies with selective M1 agonists under our partnership with Allergan.

“The target selectivity we can build into molecules increasingly highlights the potential of our approach to create new medicines with significantly improved clinical profiles for addressing a range of diseases.”

Allergan holds exclusive rights to Heptares’ range of new subtype-selective muscarinic receptor agonists, under a global research and development (R&D) and commercialisation alliance formed last year.

The portfolio of muscarinic receptor agonists is being developed to treat major neurological disorders.

Aside from HTL0016878, the firms are planning to assess selective M1 agonists for treatment of symptomatic cognitive deficits due to Alzheimer’s, and dual M1 / M4 agonists to treat cognitive and neurobehavioural symptoms.