Funds will be used to progress lead S1P1 agonist into Phase I trials against multiple sclerosis.

GPCR drug discovery company Receptos completed a two-tranche, $25 million Series A round of financing. The firm said it will use the funds to carry out Phase I trials with its lead S1P1 (sphingosine-1-phosphate receptor 1) agonist for multiple sclerosis therapy. An IND for the S1P1 candidate is expected to be filed in 2010. The new financing will also be used to develop a second IND candidate, and promote partnering of Receptos’ technology platform for GPCR drug discovery and development.

To help with the prioritization of its clinical drug candidates, Receptos has determined the crystal structures of S1P1 in complex with an antagonist and agonists. The company claims the resulting molecules show low picomolar potency and high selectivity, and are expected to demonstrate improved safety profile over competitor compounds. The company is also looking into the potential applications of S1P1 agonism in additional immune-mediated disorders.

Receptos is initially targeting the Edg family of receptor proteins, including S1P1, for structure-based drug design. The company hopes to expand its GPCR R&D both in-house and through industry partnerships, to encompass other high-value GPCR targets.

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