Trial Underway Testing Alzheimer’s-Schizophrenia Drug

(HypnoArt, Pixabay)

1 September 2017. A new clinical trial began in the U.K. in a test of an experimental drug to treat schizophrenia associated with Alzheimer’s disease. The study is sponsored by Heptares Therapeutics Ltd., a biotechnology company in Hertfordshire, U.K., assessing the safety and chemical effects of the drug with healthy volunteers.

The early-stage trial is investigating Heptares’s small-molecule, or low molecular weight, drug code-named HTL0016878, designed to treat behavioral complications from Alzheimer’s disease, including schizophrenia. Alzheimer’s disease is a progressive neurodegenerative condition affecting growing numbers of older people worldwide. In some Alzheimer’s disease cases schizophrenia also occurs, although a causal relationship between the two disorders has not been established.

Heptares Therapeutics develops treatments for diseases that address a family of proteins known as G protein-coupled receptors, or GPCRs, associated with a number of conditions.  GPCRs appear on the surface membranes of cells and act as gateways for other proteins, sugar, lipids, and energy. GPCRs are involved in a wide range of biological signaling functions, with about 1,000 of these receptors in humans, each receiving specific signals.

HTL0016878 is designed to stimulate a specific GPCR called muscarinic M₄ receptor, associated with both Alzheimer’s disease and schizophrenia. While the muscarinic M₄ receptor is in a known collection of targets for drugs treating these disorders, many earlier attempts addressing these receptors resulted in adverse side effects. Heptares says its technology makes it possible to specifically target these receptors, reducing the chance for adverse effects from hitting other receptors.

The clinical trial, the first test of the drug with humans, is enrolling 106 healthy individuals in the U.K., including a sub-set of participants age 65 and older to test effects of the drug on older persons. The study is assessing different dosage levels of HTL0016878 for 14 days following single or multiple doses of the drug, looking primarily at safety and health effects gauged by physical exams showing heart rate and blood pressure, electrocardiogram, and behavioral effects such as thoughts of suicide. The study team is looking as well at concentrations of HTL0016878 in blood and urine to evaluate its chemical activity in the body.

Heptares licensed HTL0016878 to international drug maker Allergan in April 2016, in a deal with a potential total value of more than $US 3 billion. The company says starting this trial makes it eligible for a $15 million milestone payment from Allergan. Initial results of the trial are expected in the first half of 2018.

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