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Aileron CEO Hails Expanded Roche Deal as a Validation of Stapled-Peptide Drug Technology

Yesterday, Cambridge, MA-based Aileron Therapeutics announced that a collaboration it had formed with European drug giant Roche in 2010 has been expanded. The companies, which have been working together on two programs focused on turning Aileron’s “stapled peptide” technology into cancer treatments, have now added a third program focused on inflammatory diseases. The financial details weren’t disclosed, but the original agreement was already quite lucrative for Aileron: Roche vowed $25 million to the biotech over the first two years of the partnership. And Aileron is eligible for up to $1.1 billion in milestone payments—one of which it said yesterday it recently received.

Stapled peptides are fragments of proteins that are linked in a way that’s designed to stabilize them, so they don’t degrade too quickly in the body. And rather than attaching to targets on the surface of cells—like many drugs do—Aileron’s compounds are designed to penetrate cell’s outer membranes so they can more effectively hit disease targets.

Aileron CEO Joseph Yanchik believes Roche’s support will be vital to advancing the entire field of stapled peptides. “Until a year ago, all discussion about stapled peptides as a drug platform was coming out of the academic world and our presentations,” he says. “People wanted to see a large pharma company, with all its skepticism, believing it could have success with this technology. This is the first validation that stapled peptides are valuable.”

Aileron has taken a deliberately slow approach to proving out the idea of stapled peptides and finding the right partner to take it forward. The company was founded in 2005 on technology developed by a Harvard chemist and two biologists from Harvard Medical School and the Dana-Farber Cancer Institute. The basic concept is to combine the best properties of conventional, small-molecule chemical drugs with large-molecule protein drugs in a way that eliminates the shortcomings of both. “Small molecules can’t occupy the whole surface of cells,” says Steven Kafka, Aileron’s chief operating officer and chief financial officer. “Large molecules can’t actually get inside of cells.” Plus most proteins unravel in the body and are chewed up by enzymes within minutes, rendering them useless as therapies.

So Aileron’s scientists have spent much of the last five years figuring out how to staple peptides—fragments of proteins—together so they’re not only resistant to degradation, but they’re also effective at penetrating cell membranes and binding to disease targets within those cells. “This is a difficult thing to do because you improve one property and end up losing another,” says Tomi Sawyer, Aileron’s chief scientific officer. “We’re able to break through that threshold to get both … Next Page »

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