To date, therapies for multiple sclerosis (MS) focus on modifying or suppressing the immune system rather than on remyelination. Recent findings have pointed to the κ-opioid receptor (KOR) as a therapeutic target for remyelination, but several KOR agonists have undesired side effects that limit their use. Researchers from the Victoria University of Wellington have tested KOR agonists derived from U-50488 in the preclinical setting for the management of MS.
Ribometrix Inc. recently discussed the discovery and preclinical evaluation of a novel potent and selective eukaryotic translation initiation factor 4E (eiF4E) inhibitor, RBX-6610, being developed for the treatment of KRAS-mutant non-small-cell lung cancer (NSCLC).
Researchers from the Chinese Academy of Medical Sciences reported the discovery of the 1,2,4-oxadiazole derivative FO-4-15 for the treatment of Alzheimer’s disease (AD).
The increasing resistance to intravenous artemisinin therapy for malaria highlights the urgent need for new treatments that offer better patient compliance and a single-dose cure to address this global health threat. Novartis AG recently presented the discovery, development and evaluation of aminoisoquinolines as fast-acting intravenous therapeutic agents for severe malaria treatment.
The University of Michigan has published details on the discovery and preclinical characterization of a new potent and selective proteolysis targeting chimera (PROTAC) degrader of BRD9, CW-3308. Synthesis and optimization of two different cereblon ligands led to the discovery of a novel series of highly potent BRD9 degraders, with CW-3308 selected as the lead candidate.
A novel gene therapy that leads to cellular rejuvenation could restore vision after non-arteritic anterior ischemic optic neuropathy (NAION) and glaucoma. The technique is based on a reprogramming process that reverses the epigenetic DNA alterations caused by aging. Preclinical studies in glaucoma mice and nonhuman primates (NHP) models for this stroke-like disorder that affects the eye, showed an improvement of vision and restoration of the damaged axons of the optic nerve.
Novartis AG described the identification and activity of TAK-756, a novel, selective and potent TAK1 inhibitor, as a potential intra-articular therapy for the treatment of osteoarthritis. Previous studies demonstrated that TAK1 appears to be a potential target for controlling inflammation and catabolism through NF-κB and MAPK pathways.
At the recently concluded ACS Fall meeting, Bristol Myers Squibb Co. reported the discovery of potent orally bioavailable B-cell lymphoma 6 protein (BCL6) ligand-directed degraders (LDDs).
Human rhinoviruses (hRVs) are associated with upper respiratory tract infections such as the common cold, otitis media or sinusitis. In immunocompromised individuals or older people, hRVs can exacerbate existing pulmonary conditions such as asthma or chronic obstructive pulmonary disease.
Researchers from Merck & Co Inc. have presented preclinical data for the novel Nav1.8 inhibitor MSD-199, being developed for the treatment of inflammatory and neuropathic pain.
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