Roche and Aileron to develop stapled peptide drugs

September 1, 2010: Aileron Therapeutics and Roche have entered into a collaboration to discover, develop and commercialise a new class of drugs called stapled peptide therapeutics. As part of this agreement, Roche will work with Aileron to develop drug candidates against up to five undisclosed targets selected from Roche’s key therapeutic areas, which include oncology, virology, inflammation, metabolism and CNS. Stapled peptide therapeutics are a result of Aileron’s breakthrough peptide stabilisation technology, and are a potential solution to drug as-yet intractable disease targets, including those originating from long sought-after intracellular protein-protein interactions.

Under the terms of the agreement, Roche will provide Aileron guaranteed funding of at least $25 million in technology access fees and R&D support. Aileron is eligible to receive up to $1.1 billion in payments upon the achievement of discovery, development, regulatory and commercialisation milestones if drug candidates are developed against all five targets. In addition, Aileron will receive royalties on future sales for any marketed products that result from the collaboration. Aileron will have substantial responsibility in collaboration with Roche to develop drug candidates against the selected targets up to clinical development.

Aileron’s proprietary stapled peptide technology platform ‘locks’ peptides into their biologically active shape, mimicking the structures found in nature. This process captures the best features of both small molecules and therapeutic proteins, ultimately endowing the peptide with beneficial drug-like properties, including efficient cell penetration, improved pharmacokinetics, high-affinity binding to large target protein surfaces and excellent stability within the body. This combination of features could greatly expand the number of ‘druggable’ therapeutic targets by providing an opportunity to address the thousands of intracellular protein-protein interactions that remain a challenge for functional modulation by current therapeutics.

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