Esperion buys rights to a pill that might lower cholesterol like injectables – Boston, Massachusetts

Boston, Massachusetts 2021-01-13 06:30:43 –

TThe most powerful cholesterol drug invented so far has become a drug warning story, the high price of stickers and the inconvenience of needles have prevented them from reaching their commercial potential. Esperion Therapeutics (ESPR), a small Michigan company with a pair of approved cholesterol treatments, believes its effects can be reproduced in the form of pills, making it cheaper to drink where its predecessors can succeed in declining places. We are producing easy medicine.

Esperion said Wednesday that it had purchased the right to oral treatment targeting PCSK9, a protein found in the liver that regulates LDL’s “bad” cholesterol. The transaction, which involves a privately held company called Serometrix, includes a $ 12.5 million down payment followed by private future payments related to development milestones.

Treatment is in the early stages of development. Also, never tested in human trials, Esperion refused to disclose its development timeline. But the company is confident that Serometrix’s innovative approach to chemistry can achieve its long-held goal of avoiding the pharmaceutical industry: blocking PCSK9 with pills.


The charm is clear. Two injectable PCSK9 treatments marketed by Amgen and partners Sanofi and Regeneron Pharmaceuticals reduced LDL by approximately 60%, leading to long-term improvement in heart attack, stroke and mortality. ..

With the approval of the Food and Drug Administration in 2015, each was expected to be a multi-billion dollar blockbuster, but neither could reach its commercial potential. There were two problems. Payers barked at an annual list price of $ 14,000 for treatment, and the prospect of bimonthly injections proved to be a barrier to the minds of many patients and physicians.


“We believe that what was lacking was the focus on patient needs, convenience, and simplification of the drug for patients,” said Tim Mayleben, CEO of Esperion. If all goes well, Esperion will sell the PCSK9 pill alone and in combination with its FDA-approved cholesterol drug, Nexletol.

Oral PCSK9 treatment is not an original idea. Pfizer fully undertook clinical trials before discontinuing the project in 2016. At the time, as Chief Scientist Michael Dorsten said, “I don’t think the profile is competitive” with injectables.

The problem is that the major segment of the PCSK9 protein is nearly flat and does not provide a quarter of the small molecule drugs that can bind to its surface and shut down. Serometrix’s approach targets different parts of PCSK9 using a method called allosteric inhibition that involves taking a back door to regulate a particular protein. A handful of allosteric inhibitors have been approved by the FDA for the treatment of cancer.

Esperion isn’t the only one giving the PCSK9 pill another shot. Last year, AstraZeneca paid a private amount to a company in Cambridge, Massachusetts called Dogma Therapeutics, whose preclinical treatment targets “new binding pockets” on the surface of PCSK9, according to the company.

Both companies are doing a lot of work in the future. Amgen and Regeneron have shown that knocking out PCSK9 has significant benefits, but they did so using antibodies such as biological homing missiles. Small molecule drugs are notorious for their low accuracy, and the safe replication of the effects of PCSK9 antibodies requires delicate chemistry to avoid untargeted side effects. We also need years of clinical trials to prove the benefits of this idea.

“We don’t think it will be easy, but we are not,” Mailben said. “We are doing a lot to make it easy for patients to use.”

Esperion buys rights to a pill that might lower cholesterol like injectables Source link Esperion buys rights to a pill that might lower cholesterol like injectables

Back to top button