Takeda, Heptares probe GPCR’s role in CNS disorders

OSAKA, Japan—Takeda Pharmaceutical Co. and HeptaresTherapeutics on April 11 announced the formation of a two-year drug discoverycollaboration focused on a single G-protein coupled receptor (GPCR) that playsan important role in the pathology of central nervous system disorders.

According to the companies, this GPCR has proved intractableusing historical drug discovery efforts, due to its instability when removedfrom cell membranes and the resulting lack of insight into its structure. A newmedicine targeting this GPCR would be first in class.

Heptares will use its stabilized receptor (StaR) technologyto engineer the first-ever thermally stabilized forms of the GPCR, and alsoapply advanced structural biology and rational drug design approaches tocharacterize the GPCR's structure and to generate early leads. Takeda willparticipate in lead generation and then assume responsibility for preclinicaldevelopment and clinical development of new drugs candidates.

"We are excited to be collaborating with Takeda to unlock akey GPCR target for treating CNS disorders, an area of significant unmetmedical need where Takeda has established a leading scientific and commercialposition," said Malcolm Weir, CEO of Heptares Therapeutics, in a statement. "Aswe advance Heptares' internal pipeline of GPCR-targeted medicines, we also planto pursue attractive external opportunities, such as this partnership withTakeda, to extend our technology broadly across the GPCR universe."

"The Heptares StaR technology is a powerful new capabilityfor discovering GPCR-targeted drugs and we look forward to applying it to aspecific GPCR target of interest to Takeda in the area of neuroscience," addedShigenori Ohkawa, chief scientific officer at Takeda. "The Heptares platformapplies broadly to the GPCR target family and delivers stabilized forms thatmost precisely capture the pharmacological conformations of GPCRs as they existin their natural cellular environments."

Underthe terms of the agreement, Takeda receives worldwide commercial rights to newdrugs emerging from the collaboration. Upon signing, Heptares received anupfront payment of $2.8 million and an investment in an equity stake ofapproximately $4.6 million purchased by Takeda Ventures Inc., a wholly ownedsubsidiary of Takeda. Heptares is also eligible to receive future milestonepayments of up to $98.5 million, 3 plus royalties on product sales. Furtherterms of the agreement were not disclosed.