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1 September, 2017 - 12:46 By Tony Quested

Heptares Therapeutics clinches $15m milestone

Heptares Fiona Marshall

Japanese owned Heptares Therapeutics, which recently announced a move from Welwyn to Cambridge, has earned a $15 million milestone payment from Allergan under a global R & D and commercialisation partnership announced in April 2016.

The wholly-owned subsidiary of Sosei Group Corporation earned the cash as the first healthy subject was dosed with the first-in-class, selective muscarinic M4 receptor agonist HTL0016878 in a Phase 1 clinical study.

Heptares and Allergan are developing HTL0016878, an orally available, small molecule drug candidate with potential to treat certain neurobehavioural symptoms of Alzheimer’s disease.

The compound stimulates M4 receptor activity in the brain with high selectivity, and offers the possibility for an improved safety profile over previous muscarinic receptor agonists, which have been associated with  adverse effects  elsewhere in the body leading to safety and tolerability issues.

HTL0016878 was designed by Heptares using its proprietary structure-based drug design platform and is the first compound, selected from a series of selective M4 agonists, to progress into clinical studies.
The double-blind, randomised first-in-human study is being conducted in the UK by Heptares and will assess safety, tolerability and pharmacokinetics of single and multiple oral doses of HTL0016878 in up to 106 healthy subjects. Preliminary results are expected in the first half of 2018.

Heptares has separately announced the launch of a new research collaboration under its ORBIT initiative with Juntendo University in Tokyo, Japan.

The new collaboration, Heptares’ fourth ORBIT programme, is with the research group of Professor Takehiko Yokomizo, an expert on molecular biology, immunology and cell biology and Professor of the Department of Molecular and Cellular Biochemistry at Juntendo University. 

The collaboration is the first international industrial partnership for this prestigious university. Research activities will focus on the bespoke design and profiling of novel leukotriene receptor modulators with potential therapeutic utility in intractable skin/intestinal ulcers.
Fiona Marshall, chief scientific officer of Heptares, said: “We are delighted to collaborate with Professor Yokomizo and his group at Juntendo University. Their extensive experience and knowledge of leukotriene receptors, combined with our own structure-based design expertise, forms a strong basis from which to generate novel selective, small molecules with the potential to address difficult-to-treat wounds.”

• PHOTOGRAPH SHOWS: Fiona Marshall

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