Efinopegdutide

iStock, Sundry Photography Merck has not disclosed which of its peptide therapies it plans to develop oral formulations for. Merck on Tuesday entered into a nonexclusive licensing and option pact with Austrian biotech Cyprumed in a bid to make its peptide drugs orally available. Details of the deal were scant. Merck will pay up to $493 million, a sum inclusive of the upfront fee plus development, regulatory and commercialization milestones of any product that may arise from the partnership. In exchange for its investment, Merck will gain access to Cyprumed’s proprietary platform to develop novel oral formulations of the pharma’s peptide therapies, though Merck is tight-lipped about specifics. The company did not reveal how many and which of its assets it plans to make orally available. The pharma also did not disclose priority indications. According to Tuesday’s news release, Cyprumed’s platform can be used on several types of peptides, including GLP-1 analogs, mini-proteins and macrocycles. Under the terms of the agreement, Merck will also have the exclusive option to license Cyprumed’s technology for individual targets, in which case Cyprumed will be eligible for additional payments. Merck will be responsible for trialing these oral drug formulations and will take charge of their manufacturing and marketing. According to its pipeline page , Merck has two peptide therapies in development: the late-stage enlicitide decanoate, being studied for high cholesterol, and the Phase II efinopegdutide, a dual agonist of GLP-1 and GIP receptors, to treat metabolic dysfunction-associated steatohepatitis ( MASH ). Enlicitide decanoate, which blocks PCSK9, is already orally available. The pharma has five listed studies running for the asset under the CORALreef program. Merck is developing enlicitide decanoate in partnership with UCB Pharmaceuticals. Meanwhile, efinopegdutide is delivered via a subcutaneous injection. Currently, Merck has four listed studies for the asset, including one that directly compares it with Novo Nordisk’s semaglutide, looking at the drugs’ ability to lower liver fat levels in patients with MASH. Both the Cyprumed deal and the decision to study efinopegdutide in an obesity-adjacent indication fits with Merck’s strategy in the weight loss arena. At the 45th Goldman Sachs Healthcare Conference in June 2024, CEO Robert Davis said that the pharma will focus its R&D efforts on orals rather than injectables, and that it will prioritize drugs that deliver cardiometabolic benefits in addition to weight reduction. “I think everything is couched in terms of obesity first,” Davis said at the time, noting that pharma then considers other health outcomes for “supporting the reimbursement within the broader obesity space.”

Opko Health said a planned phase 1 study would mark the first time that an orally administered GLP-1/glucagon agonist would enter human trials.\n Opko Health and Entera Bio have formalized their partnership as the biotechs prepare to take the first orally administered dual agonist glucagonlike-peptide 1 (GLP-1)/glucagon peptide into the clinic.The once-daily pill combines Opko’s long-acting GLP-1/glucagon dual agonist peptide, dubbed OPK-88006, with Entera’s N-Tab oral delivery tech. The companies’ current timetable would involve seeking permission from the FDA “later this year” to enter human trials, according to a March 17 release.The agreement will see Miami-based Opko and Israel-based Entera holding 60% and 40% ownership, respectively, in the program, and sharing the development costs by the same ratio.Opko will also buy 3.6 million shares of Entera at $2.17 a pop, slightly above the $1.88 price at which the shares closed after Friday’s trading. Entera will use the proceeds to help fund its side of the development costs through to the phase 1 trial.Beyond that first human study, Entera will then have the option to continue to fund its side of the development in order to retain its part of the program’s ownership. If the biotech decides at this point to opt out, it will still keep a 15% ownership interest, with Opko accounting for the remaining 85% while taking on the full development and funding burden.The two blockbuster obesity drugs already on the market are Novo Nordisk’s GLP-1 agonist Wegovy and Eli Lilly’s dual GLP-1/GIP agonist Zepbound. However, there are not yet any approved therapies that follow Opko’s modality of simultaneously activating the GLP-1 and glucagon receptors.Big Pharmas have tended to evaluate dual GLP-1/glucagon co-agonists as potential treatments for metabolic dysfunction-associated steatohepatitis (MASH). AstraZeneca has its own candidate, dubbed AZD9550, in phase 1 development for the liver condition, while Merck & Co.’s efinopegdutide beat Wegovy in the related condition of nonalcoholic fatty liver disease in a phase 2 trial.Opko said taking their drug into the clinic this year would mark the first time an orally administered GLP-1/glucagon agonist would enter human trials. The hope is that the med can be used as a once-daily table treatment for patients with obesity as well as metabolic and fibrotic disorders. Opko and Entera have already been collaborating on the obesity drug as well as on an oral GLP-2 peptide tablet they hope will offer an injection-free alternative for patients suffering from rare malabsorption conditions such as short bowel syndrome.“We are pleased to continue working with Entera on this promising program to develop the first oral GLP-1/glucagon dual agonist in addition to our subcutaneous injectable dual agonist GLP-1/glucagon program,” Onko’s CEO Phillip Frost, M.D., said in the release. “Our goal with this franchise is to provide additional options for patients with obesity, metabolic and fibrotic diseases.”