Targeting the adenosine A2A receptor, a critical mediator of immunosuppression on the tumor microenvironment, has emerged as a strategy to improve cancer immunotherapy, and several A2A receptor antagonists are under clinical evaluation both as monotherapy and in combination with checkpoint inhibitors.
Researchers at Merck & Co. Inc. have presented the discovery of novel selective metabotropic glutamate receptor 2 (mGluR2) negative allosteric modulators (NAMs) as potential PET imaging agents. Synthesis and optimization of a series of analogues of a potent and selective mGluR2 NAM resulted in the identification of compound MK-8056 as a high-affinity mGluR2 NAM (Ki=0.19 nM) with desirable lipophilicity (logD7.0=2.46) and low P-gp susceptibility.
Astex Pharmaceuticals Inc. is getting $35 million up front and up to $500 million per program as it extends its drug discovery collaboration with Merck & Co. Inc. to include small-molecule activators of the p53 tumor suppressor protein. The number of programs was not disclosed, but they will target forms of p53 that have lost their function as a result of cancer-induced mutations in the TP53 gene. The aim will be to override the mutation and restore the ability of the wild-type protein to bind DNA and perform its functions as a transcription factor.
For people living with HIV, the single greatest achievement to date has been the emergence of antiretroviral treatments (ART) that completely block the virus, resulting in reduced mortality and morbidity and improved quality of life. But taking one pill a day for life cannot be the end of this journey, speakers said during the International AIDS Society meeting held July 23 to 26 in Brisbane, Australia.
For people living with HIV, the single greatest achievement to date has been the emergence of antiretroviral treatments (ART) that completely block the virus, resulting in reduced mortality and morbidity and improved quality of life. But taking one pill a day for life cannot be the end of this journey, speakers said during the International AIDS Society meeting held July 23 to 26 in Brisbane, Australia. Even with the success of ART, drug adherence remains a problem due to pill fatigue or depression and other mental health conditions, as well as drug-drug interactions, said Claudia Cortes, associate professor at the University of Chile in Santiago. New drugs that are longer lasting, more convenient, and affordable are desperately needed, she said.
The U.S. SEC is settling insider trading charges against Nirdosh Jagota, former vice president of global regulatory affairs at Merck & Co. Inc., stemming from Merck’s $1.85 billion acquisition of Pandion Therapeutics Inc. in 2021.
SK Bioscience Ltd. and Sanofi Pasteur SA announced June 30 positive results from a phase II study for its 21-valent pneumococcal conjugate vaccine (PCV) candidate called GBP-410, or SP-0202 under Sanofi.
Merck & Co. Inc. has reported the development of a novel monobactam for use in combination with its class A/C β-lactamase inhibitor (BIL) relebactam (MK-7655) in order to achieve the broadest activity against multidrug-resistant (MDR) gram-negative pathogens that express a variety of β-lactamases. The in vitro efficacy of the combination of the monobactam – MSD-045934942 – against a panel of MDR and non-MDR gram-negative bacteria was evaluated using in vitro broth microdilution testing.
The floodgates have opened for challenges to the new U.S. drug price negotiation process laid out in the Inflation Reduction Act (IRA) that was narrowly passed last year.
Bristol Meyers Squibb Co. (BMS) joined the Inflation Reduction Act (IRA) pile-on June 16, filing a third constitutional challenge to the U.S. Medicare drug price negotiations mandated in the law that was narrowly passed last year on a partisan vote.
