Over the course of the year, and continuing into the latest scientific meetings, an extraordinary breadth of new antibody-drug conjugate (ADC) designs was reported, with innovations spanning targets, linkers, payloads, conjugation chemistries and overall architectures. Once defined by a simple “one target, one payload” model, the field is lately expanding into a more versatile and diverse therapeutic space. Read More
Long noncoding RNAs (lncRNAs) have emerged as potential markers of disease, since they associate with proteins that regulate gene expression, translation or stability, among others, and where hypoxia might play a role in this scenario. In recently published work, researchers analyzed clinical data from patients with lung adenocarcinoma to identify hypoxia-modulated lncRNAs in vivo and in vitro, and which could correlate with prognosis. Read More
CSPC Pharmaceutical Group Ltd. has obtained approval from the National Medical Products Administration (NMPA) in China to conduct clinical trials of SYH-2072 (tablets), a highly selective and potent aldosterone synthase inhibitor. It is being investigated as a potential treatment for uncontrolled hypertension and primary aldosteronism. Read More
Previous work showed that histone ‘readers’, which bind to post-translational modifications on histones, may be upregulated in melanoma and thereby upregulate oncogenes. Given that the histone reader ATAD2 is known to be overexpressed in several types of cancer, researchers at the University of Alabama at Birmingham asked whether the same is true in melanoma. Read More
Guangzhou Institutes of Biomedicine and Health has disclosed bromodomain-containing protein 4 (BD2 domain) (BRD4 BD2) inhibitors reported to be useful for the treatment of diabetes, autoimmune diseases, cardiovascular disorders, male contraception, chronic obstructive pulmonary disease, viral and parasitic infections and cancer. Read More
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Venetoclax has shown good results for adult acute myeloid leukemia (AML) in combination with azacitidine, but there is increasing evidence of inherent and acquired resistance. High expression of nicotinamide phosphoribosyltransferase (NAMPT) has been associated with cancer aggressiveness and poor prognosis due to increased nicotinamide metabolism. Read More
Neurodawn Pharmaceutical Co. Ltd. has synthesized phosphodiesterase PDE3A inhibitors reported to be useful for the treatment of dementia and cerebrovascular disorders. Read More
Insilico Medicine Inc. has identified serine/threonine-protein salt-inducible kinases (SIK) inhibitors reported to be useful for the treatment of rheumatoid arthritis, nonalcoholic or metabolic dysfunction-associated steatohepatitis (NASH/MASH), giant cell arteritis, primary sclerosing cholangitis, inflammatory bowel disease, atherosclerosis, type 2 diabetes and glomerulonephritis, among others. Read More
Multiple sclerosis (MS) is a chronic immune-mediated disease characterized by the destruction of myelin sheaths, neuroaxonal damage, glial cell activation and formation of demyelinated plaques in the CNS. Since MS is considered a prototypic antigen-specific autoimmune disease, restoring immune tolerance to self-antigens is being explored as a therapeutic strategy. Read More
Chengdu Easton Biopharmaceuticals Co. Ltd. has divulged sodium channel protein type 10 subunit α (SCN10A; Nav1.8) blockers reported to be useful for the treatment of pain, arrhythmia, cough, urinary incontinence and multiple sclerosis. Read More
Huayao Jiyuan (Shenzhen) Pharmaceutical Co. Ltd. has described hypoxia inducible factor-2α (HIF-2α; EPAS1) inhibitors reported to be useful for the treatment of cancer, infections, cardiovascular disorders, anemia, chronic kidney disease, disorders of hematopoiesis, inflammatory disorders and acute respiratory distress syndrome (ARDS). Read More
Alagille syndrome (ALGS) is a rare, multisystem genetic disorder most commonly caused by haploinsufficiency of the JAG1 gene, leading to reduced JAG1 protein function and impaired development of intrahepatic bile ducts. Researchers from Arnatar Therapeutics Inc. described the development of antisense oligonucleotides (ASOs) engineered using their proprietary ACT‑UP1 platform to upregulate endogenous JAG1 expression and thereby address the underlying genetic deficiency. Read More