Vertex Pharmaceuticals Inc. has described orexin OX2 receptor agonists reported to be useful for the treatment of amyotrophic lateral sclerosis, obesity, hypertension, retinopathy, multiple sclerosis, narcolepsy, hypersomnia and Parkinson’s disease.
Celgene Corp. has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a MAP kinase-activated protein kinase 2 (MAPKAPK2; MK2)-targeting moiety via a linker.
Pinotbio Inc. has synthesized antibody-drug conjugates comprising an antibody covalently linked to DNA topoisomerase I inhibitors through a cleavable linker reported to be useful for the treatment of cancer.
Genetic or pharmacologic inhibition of casein kinase 1α (CK1α) has proven effective in suppressing the proliferation of acute myeloid leukemia (AML) cell lines with wild-type TP53. Researchers from Bristol Myers Squibb Co. recently presented the discovery and preclinical characterization of BMS-986397, a cereblon E3 ligase modulatory drug (CELMoD) designed as a molecular glue degrader of CK1α.
The valosin-containing protein (VCP) modulator KUS-121 from Kyoto University is in phase II development as an intravitreal treatment for nonarteritic central retinal artery occlusion, but its efficacy in atherosclerosis is unknown.
Researchers from Nankai University reported on [I], a novel EGFR L858R/T790M/C797S inhibitor designed to overcome the most frequent resistances to non-small-cell lung cancer (NSCLC) treatment.
Repolarization abbreviation with the antiarrhythmic drug mexiletine has been found to normalize the QTc interval and reduce the rate of events in long QT syndrome type 3 (LQT3), but it is only partially efficacious in other malignant forms, including LQT2 and LQT8. There are compounds that have not been tested, such as hERG channel agonists, which are capable of shortening repolarization. The potent hERG agonist ICA-105574 was thus tested in a clinically relevant porcine model of LQT8.
Highfield Biopharmaceuticals Inc. has filed an IND application with China’s National Medical Products Administration (NMPA) to conduct a clinical trial of HF-50, an immunoliposome that directs T cells to attack solid tumors and enhances anticancer activity with an immune modulator.
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