Heptares Therapeutics, a leading GPCR drug discovery and development company, has achieved all milestones in its collaboration with Takeda Pharmaceutical Company. By achieving these milestones, Heptares will receive a significant payment from Takeda, under the terms of the agreement signed by the two companies in 2011.

The agreement is focused on a single GPCR target nominated by Takeda that, until now, has proved intractable to rational drug discovery efforts due to its instability when removed from the cell membranes and the resulting lack of insight into its structure. Over the course of the collaboration Heptares has leveraged its structure-based drug design (SBDD) approach to GPCRs and proprietary technologies to generate the first-ever stabilised form of the target in a clinically relevant conformation enabling a series of novel lead candidates against the target to be designed.

Tetsuyuki Maruyama, general manager Pharmaceutical Research Division, Takeda said, "We are impressed with the efficiency and results from this partnership with Heptares. In achieving these milestones, the Heptares team has demonstrated its ability to design new, high-quality small molecules to a previously challenging GPCR target. We look forward to continuing our partnership and taking these leads forward into pre-clinical development."

"Our partnership with Takeda provides an excellent validation of our GPCR-focused structure-based drug design approach and capabilities," said Malcolm Weir, CEO of Heptares. "We see similar good progress in our other partnerships where to date we have hit every milestone. This success, in turn, provides us with an important source of capital, which has enabled us to build an impressive proprietary pipeline and provided funds to advance our first-ever selective M1 agonist into first clinical studies later this year."

Under the terms of the agreement, Takeda receives worldwide commercial rights to new drugs emerging from the collaboration. Upon signing, Heptares received an upfront payment of £1.7 million and an investment in an equity stake of approximately £2.8 million purchased by Takeda Ventures Inc., a wholly-owned subsidiary of Takeda. Heptares has also now received £1 million in research-stage milestones and is eligible to receive $96 million in additional later-stage milestones plus royalties on product sales. Further terms of the agreement are not disclosed.

The GPCR superfamily is the largest and single most important family of drug targets in the human body. It plays a central role in many biological processes and is linked to a wide range of disease areas. GPCRs are expressed in every type of cell in the body where their function is to transmit signals from outside the cell across the membrane to signaling pathways within the cell, between cells and between organ systems. There are over 375 GPCRs encoded in the human genome, of which 225 have known ligands and 150 are orphan targets. GPCRs are the site of action of 25-30% of current drugs. Six of the top ten and 60 of the top 200 best-selling drugs in the US in 2010 target GPCRs.

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.