Navigation Links
Heptares Initiates Clinical Study With First Selective Muscarinic M1 Receptor Agonist for Improving Cognition in Patients With Alzheimer's Disease
Date:12/9/2013

LONDON and BOSTON, December 9, 2013 /PRNewswire/ --

First Human Trial of Novel Small Molecule Drug Derived From Heptares GPCR-Focused Structure-Based Drug Design Platform

Heptares Therapeutics, the leading GPCR structure-guided drug discovery and development company, announces that it has initiated a Phase 1 clinical study of HTL9936, the first fully selective muscarinic M1 receptor agonist to enter clinical development. HTL9936 is an orally available, small molecule drug candidate discovered using the Heptares GPCR structure-based drug design (SBDD) platform. Heptares plans to develop HTL9936 as a novel treatment for improving cognitive function (memory and thinking abilities) in patients with Alzheimer's disease and other diseases associated with dementia and cognitive impairment.

"We are excited to initiate clinical development of HTL9936, a first-in-class agent with the potential to become an important new medicine for improving cognitive function in patients with Alzheimer's disease and other potential indications including schizophrenia and Lewy body dementia," said Malcolm Weir, CEO of Heptares. "In addition, the initiation of this clinical trial with HTL9936 marks an important milestone for Heptares, as we evolve into a clinical-stage business with a rich portfolio of novel GPCR-targeted agents advancing through Phase 1 and 2a clinical trials in the near-term."

M1 receptor agonism is a well-validated mechanism of action for treating cognitive impairment and a valuable pharmacological profile that the pharmaceutical industry has endeavored to create for decades. The principal challenge has been to engineer selective compounds that activate the M1 receptor subtype without also activating the M2 or M3 receptors, which are associated with undesirable side effects. All previous compounds have been discontinued due to inadequate selectivity. Using a new structure-guided approach, Heptares scientists determined the x-ray crystal structure of the M1 receptor for the first time and leveraged unique insights into the receptor to identify new chemistries with fully selective M1 agonist profiles.

The Phase 1 study will evaluate the safety, tolerability and pharmacokinetics of HTL9936. In addition, the clinical pharmacodynamics of the drug will be investigated in a series of studies over the next year. This study aims to recruit more than 100 healthy volunteers including elderly people at a single clinical centre in the UK. Initial results are expected in mid-2014

About Alzheimer's Disease and Other Disorders of Cognitive Impairment

Today there is significant unmet medical need and heavy economic burden across multiple diseases characterised by cognitive impairment and dementia. In Alzheimer's disease, currently available drugs provide limited and transient effects on cognition. Healthcare costs associated with the epidemic of AD, including nursing home care, continue to grow dramatically and new therapies with better and more durable efficacy are urgently needed. In addition, an estimated 80% of schizophrenics suffer from cognitive impairment and 1.3 million patients in the US suffer from Lewy body dementia. Currently there are no approved therapies for treating cognitive impairment in schizophrenia or for treating Lewy body dementia.

About Heptares Therapeutics

Heptares creates new medicines targeting clinically important, yet historically challenging, GPCRs (G protein-coupled receptors), a superfamily of drug receptors linked to a wide range of human diseases. Leveraging our proprietary structure-based drug design technology platform, we have built an exciting pipeline of novel drug candidates with the potential to transform the treatment of serious diseases, including Alzheimer's disease, ADHD, diabetes, schizophrenia, and migraine. Our pharmaceutical partners include Cubist, MorphoSys, Takeda, AstraZeneca and MedImmune, and we are backed by Clarus Ventures, MVM Life Science Partners, Novartis Venture Fund, the Stanley Family Foundation and Takeda Ventures. To learn more about Heptares, please visit http://www.heptares.com

HEPTARES is a registered trademark in the EU, Switzerland, US and Japan;

StaR is a registered trademark in the EU and Japan.

 


'/>"/>
SOURCE Heptares Therapeutics
Copyright©2012 PR Newswire.
All rights reserved

Related medicine technology :

1. Heptares Achieves First Research Milestone in Research Collaboration with Cubist
2. Heptares Augments Business Development Capabilities in Japan and Other Asian Territories
3. Heptares to Present at Boston Biotech BD and Future Leaders in the Biotech Industry Conferences
4. Heptares to Present at the 6th Annual European Life Sciences CEO Forum (5-6 March)
5. Heptares to Present at 5th CNS Partnering and Deal-Making Conference (13-14 SEPTEMBER)
6. Heptares and UK Medical Research Council Extend GPCR Collaboration
7. Catabasis Initiates Phase 2 Trial of CAT-2003 in Patients with Severe Hypertriglyceridemia
8. Isis Pharmaceuticals Initiates Phase 1 Study of ISIS-GSK3 Rx and Earns $3 Million Milestone Payment From GSK
9. ARMO BioSciences Initiates Phase 1 Clinical Trial of First-In-Class Cancer Immunotherapy
10. Revalesio Initiates Phase IIa Study of RNS60 in Multiple Sclerosis at University Hospital Zurich
11. Perrigo Initiates Nationwide Voluntary Product Recall Of Acetaminophen Infant Suspension Liquid, 160 mg/5 mL, Due To A Potential Defect With The Co-Packaged Oral Syringe
Post Your Comments:
*Name:
*Comment:
*Email:
(Date:4/27/2016)... -- Hologic, Inc. (Nasdaq: HOLX ) announced ... second quarter ended March 26, 2016.  GAAP diluted ... and non-GAAP diluted EPS of $0.47 increased 14.6%.  ... reported basis, and 6.3% on a constant currency ... quarter, highlighted by 14.6% growth in non-GAAP EPS," ...
(Date:4/27/2016)... 27, 2016 Transparency Market Research ... Market - Global Industry Analysis, Size, Share, Growth, Trends, ... the global skincare devices market was valued at US$ ... at a CAGR of 10.1% from 2015 to 2023 ... Browse the full Skincare Devices Market (Treatment Device - LED ...
(Date:4/27/2016)... , April 27, 2016 ... of the  "Global Anesthesia Disposables Market 2016-2020" ... http://photos.prnewswire.com/prnh/20160330/349511LOGO ) ,The global anesthesia disposables ... CAGR of 4.03% during the period 2016-2020.  ... major threat to patients, safety. Organizations like ...
Breaking Medicine Technology:
(Date:4/29/2016)... , ... April 29, 2016 , ... ... healthcare awareness and author of best seller "LOVE, MEDICINE and MIRACLES") addresses touchy ... May 2, 2016 and podcasted thereafter . Dr. Bernie Siegel, author of ...
(Date:4/29/2016)... (PRWEB) , ... April 29, 2016 , ... ... surgeon reveals that infants born with severe congenital diaphragmatic hernia have better survival ... born with congenital diaphragmatic hernia (CDH)—a condition where the diaphragm fails to form ...
(Date:4/29/2016)... (PRWEB) , ... April 29, 2016 , ... ... engineer of patented products, announces the Gyrociser, an exercise invention which aids in ... $2 billion," says Scott Cooper, CEO and Creative Director of World Patent Marketing. ...
(Date:4/29/2016)... New York, NY (PRWEB) , ... April 29, 2016 , ... New York City based ... surgery . This surgery is a very effective way to treat obstructive sleep apnea. Dr. ... , Orthognathic surgery is a procedure that involves one or both jaw bones. This ...
(Date:4/29/2016)... ... April 29, 2016 , ... Innovations with ... in an upcoming episode, airing third quarter 2016 via Discovery Channel. Dates and ... butter, Grassland Dairy Products, located in Greenwood, Wisconsin applies product research and development ...
Breaking Medicine News(10 mins):