Sosei Heptares could potentially generate more than $1.2 billion through a collaboration with Takeda Pharmaceutical designed to discover, develop and commercialize small molecules and biologics designed to modulate G protein-coupled receptor (GPCR) targets (pictured). [Sosei Heptares]

Takeda Pharmaceutical will partner with Sosei Heptares to discover, develop, and commercialize small molecules and biologics designed to modulate G protein-coupled receptor (GPCR) targets, through a collaboration that could generate more than $1.2 billion for Sosei Heptares.

The companies said they will focus initial efforts on developing treatments against unspecified “high-priority” gastrointestinal GPCR targets to be nominated by Takeda, with the potential to expand into other therapeutic areas.

“The therapeutic approach presented through this collaboration provides an exciting avenue for discovery in gut inflammation and motility disorders,” Gareth Hicks, PhD, head of Takeda’s gastroenterology drug discovery unit, said in a statement. “We’re eager to advance the identified targets through our research pipeline, in partnership with Sosei Heptares, to accelerate the development of new therapies for patients.”

The partnership is intended to combine Sosei Heptares’ GPCR-focused structure-based drug design capabilities with Takeda’s drug discovery and development expertise across a range of therapeutic areas. Gastroenterology is one of Takeda’s three main therapeutic areas of focus, along with oncology and neuroscience, though the pharma’s pipeline also includes plasma-derived therapies, vaccines, and rare disease treatments.

According to Sosei Heptares, GPCRs form the largest human membrane protein family, with around 400 receptors, of which approximately 224 remain yet to be explored, offering broad untapped potential. Yet drug development has been complicated by the challenge of mapping the structure of GPCRs when isolated from the cell membrane, since GPCRs are unstable in isolation, often preventing structure determination.

Structure-based drug design

Sosei Heptares’s StaR® SBDD (structure-based drug design) platform is designed to overcome these hurdles. The company says StaR is the only platform capable of removing the GPCR structure from the cell membrane while retaining its original three-dimensional integrity and enabling co-structure determination with multiple small molecules, including those with low affinity.

“We have succeeded in generating the world’s first x-ray crystal structures of more than 15 receptors, and have also succeeded in elucidating over 200 structures for these receptors bound to drug molecules, a vital step in a viable SBDD process,” Sosei Heptares stated on its website.

Sosei Heptares agreed to give Takeda exclusive global rights to develop and commercialize therapeutic agents for each novel target through pharmacological approaches the company said will be specified in the collaboration.

In return, Takeda agreed to pay Sosei Heptares up to $26 million in upfront and “near-term” payments, plus research funding over the term of the agreement, and potentially more than $1.2 billion in payments tied to achieving development, commercialization, and net sales-based milestones.

Sosei Heptares is also eligible to receive tiered royalties on net sales of any licensed products by Takeda resulting from the collaboration—the second such partnership inked over the past month by Sosei Heptares and a pharma giant. On July 16, Sosei Heptares and Genentech announced the launch of a GPCR-focused drug discovery alliance aimed “across a range of diseases,” with the Roche subsidiary agreeing to pay Sosei Heptares $26 million upfront and near-term, plus potentially more than $1 billion in milestone payments.

In the case of Takeda, the collaboration arises from the companies’ business relationship, in which Takeda’s venture capital arm had been an early investor in Heptares, stated Malcolm Weir, PhD, executive VP and chief R&D officer of Sosei Heptares.

“Today’s newly announced partnership is the culmination of recent discussions to identify new and exciting programs where our combined expertise can be directed towards challenging diseases and targets to deliver new medicines for patients,” Weir added.

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