Allergan’s partner Heptares Therapeutics has dosed the first patient with a GPCR drug to treat major symptoms of Alzheimer’s disease.
A year ago, Allergan signed a massive deal of up to €3Bn with Heptares Therapeutics for the development of drugs that target G-protein-coupled receptors (GPCRs), a protein superfamily that currently comprises the target of around 40% of all marketed drugs. The team has now put a new candidate in the clinic, triggering a €15M milestone payment for Heptares.
The candidate, which goes by the unremarkable name of HTL0016878, is intended to treat neurobehavioral symptoms of Alzheimer’s disease. It is an agonist that selectively binds the M4 muscarinic receptor, and this feature of high selectivity is essential, given that binding muscarinic receptors M2 and M3, structurally very similar to M4, can lead to severe cardiovascular side effects. The drug will be joining two other candidates from the Allergan-Heptares team already in the clinic that selectively target the M1 muscarinic receptor to treat neurological conditions.
Heptares Therapeutics is specialized in designing drug candidates with high selectivity for GPCRs, which are historically very challenging to target despite their big pharmaceutical value. This has attracted major deals with AstraZeneca, Teva and Pfizer. Learn more about it in our interview with Fiona Marshall, co-founder and CSO of the company.
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