AGV Discovery SAS, in collaboration with scientists from Centre National de la Recherche Scientifique, Inserm and Universite de Montpellier, divulged azaindole derivatives acting as extracellular-regulated kinase (ERK) inhibitors, particularly ERK2, reported to be useful for the treatment of cancer, inflammation, autoimmune disease, substance abuse and dependence, metabolic syndrome, neurodegeneration, HIV infection, and pain, among other disorders.
Researchers from Jiangsu Hansoh Pharmaceutical Group Co. Ltd. and Shanghai Hansoh Biomedical Co. Ltd. have disclosed MAP kinase-activated protein kinase 2 (MK2) inhibitors reported to be useful for the treatment of cancer, inflammatory disorders, atherosclerosis, diabetes and fibrosis, as well as metabolic and autoimmune diseases.
Dong Wha Pharmaceutical Co. Ltd. has defined histone-lysine N-methyltransferase EZH1 and/or EZH2 inhibitors reported to be useful for the treatment of cancer.
The Shanghai Institute of Materia Medica of the Chinese Academy of Sciences has described androgen receptor antagonists and/or androgen receptor degradation inducers reported to be useful for the treatment of gastrointestinal disorders, osteoporosis and SARS-CoV-2 infection (COVID-19), as well as breast and castration-resistant prostate cancer.
Researchers from Tokyo University of Science presented the discovery and preclinical evaluation of a novel KRAS-degrading small molecule candidate being developed for the treatment of cancer.
Mansonone E is a type of plant toxin with various pharmacological properties, including antimicrobial, anti-MRSA and antitumor activities. In the current study, researchers from Sun Yat-Sen University presented the discovery of novel mansonone E analogue, MSN-8C, being developed as a potential anticancer agent.
Biocity Biopharma announced that the U.S. FDA has accepted its investigational new drug (IND) application for BC-3448, a bispecific antibody that targets the T cell marker CD3 and epidermal growth factor receptor (EGFR), bringing antitumor T cells in proximity to EGFR-expressing cells. To reduce the risk of cytokine release syndrome (CRS), a known risk of CD3-targeting antibodies, the bispecific has a higher affinity for EGFR than CD3.
Most lung adenocarcinoma tumors with EGFR mutations respond to tyrosine kinase inhibitors (TKIs, e.g., osimertinib). Accordingly, there are now >50 different FDA-approved TKIs. Still, acquired resistance remains as the major limitation preventing long-term efficacy.
Despite continual investment in research focused on high-grade serous ovarian cancer (HGSOC), the 5-year survival rate of ∼30% for most patients has remained unchanged for decades. While ≤20% of HGSOC patients present with treatment-refractory disease, therapeutic strategies have not changed outcomes for these patients in 40 years.