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GEN News Highlights : May 31, 2011

AstraZeneca Pays Heptares $6.25M to Tap GPCR Expertise for Therapeutic Development

Agreement focuses on small molecules and biologics in multiple disease fields.

AstraZeneca is paying Heptares Therapeutics $6.25 million up front as part of a deal to discover and develop GPCR-targeted drugs. The partnership will focus on specific GPCR targets linked to CNS/pain, cardiovascular/metabolic, and inflammatory disorders, which are part of AstraZeneca’s small molecule and biologics portfolio, including that of its biologics unit MedImmune.

AstraZeneca retains full worldwide commercial rights to any resulting product candidates, and will select resulting preclinical, small and large molecule candidates for further development. The firm will be responsible for all preclinical and clinical development activities. Heptares could receive additional milestone payments, along with future royalties on sales of successfully commercialized drugs.

The four-year collaboration will initially exploit Heptares’ GPCR discovery expertise and technologies, including its StaR® platform, to generate stabilized forms of GPCR targets in their natural conformation. The firms will then separately develop and carry out initial screening and lead identification, and pool their results. The best leads will be further optimized collaboratively.

Heptares’ StaR technology is designed to generate stabilized GPCRs containing a small number of point mutations to generate stable, functionally relevant, purified conformations of target GPCRs that retain their expected drug-binding characteristics. Heptares is exploiting the platform both in house and through partnerships, to generate GPCR-targeting drugs that overcome issues such as low selectivity, poor pharmacokinetic profiles, or toxicity.

In April Heptares inked a deal with Takeda Pharmaceutical focused on the discovery and development of drugs against a previously intractable GPCR target involved in CNS disorders.