Some cancers with a poor prognosis have had no new treatments in decades. Advances in the genetic characterization of these tumors now offer a range of possibilities for the development of new therapies that could completely change the quality of life and survival of these patients. Read More
Researchers from Revolution Medicines Inc. presented the discovery and preclinical characterization of RMC-5127, a novel noncovalent, tri-complex inhibitor of GTPase KRAS (G12V mutant), or KRAS G12V(ON). Read More
NaPi2b is a sodium-dependent phosphate transporter that is mainly responsible for phosphate homeostasis in humans. Overexpression of NaPi2b has been associated with several types of cancers such as lung, ovarian, thyroid or breast carcinomas and thus is considered a therapeutic target to exploit in these conditions. Read More
Researchers from Eradivir Inc. and affiliated organizations presented the discovery and preclinical evaluation of EV-21, a dual mechanism antiviral immunotherapy for the treatment of influenza infections. EV-21 was designed as a ligand-targeted drug conjugate, developed by linking the neuraminidase inhibitor zanamivir to two distinct haptens that bind to two different naturally occurring antibodies in humans. As a result, the candidate acts though a dual mechanism of action, which consists of potent recruitment of the human immune system to recognize and destroy free viruses and virus-infected cells. Read More
Escient Pharmaceuticals Inc. has patented quinoline derivatives acting as Mas-related G protein-coupled receptor member X2 (MRGPRX2) antagonists and thus reported to be useful for the treatment of pain, psoriasis, inflammatory disorders, atopic dermatitis, eczema, pruritus, urticaria and autoimmune disease, among others. Read More
The checkpoint kinase WEE1 catalyzes the inhibition of cell cycle progression and CDK1 phosphorylation. WEE1 inhibitors have demonstrated clinical benefits in gynecological malignancies, yet limited antitumor activity and a multifaceted toxicity profile of small-molecule inhibitors mean new approaches to target WEE1 are needed. Read More
Epoxysqualene-lanosterol cyclase (lanosterol synthase, OSLC) inhibitors have been reported in a University of Texas System patent as potentially useful for the treatment of amyotrophic lateral sclerosis, glioblastoma, multiple sclerosis, neurodegeneration, Parkinson’s, Alzheimer’s and Huntington’s diseases. Read More
Research at the University of Florida has led to the identification of compounds acting as dual dopamine transporter (DAT) and sigma receptor (sigma nonopioid intracellular receptor 1 [σ1, SIGMAR1] and sigma intracellular receptor 2 [σ2, TMEM97]) antagonists reported to be useful for the treatment of methamphetamine dependence and cocaine dependency. Read More
Data regarding an innovative bispecific antibody – CPL-976 (CPBT-0976) – were recently reported by Celon Pharma SA. Bispecific antibodies targeting more than one antigen on cancer cells improve the specificity and effectiveness of the therapy, and could be utilized for targeting the defense mechanisms of cancer cells, such PD-L1 or EGFR, VEGFR and AXL. Read More
Morphinan derivatives acting as κ-opioid receptor agonists have been discovered by Toray Industries Inc. They are reported to be useful for the treatment of pain, hepatobiliary and hematologic diseases, cardiovascular and respiratory disorders. Read More
Takeda Pharmaceutical Co. Ltd. has identified N-(pyrrolidin-3-yl or piperidin-4-yl)acetamide derivatives acting as somatostatin SST4 receptor agonists and thus reported to be useful for the treatment of Alzheimer’s disease, depression, schizophrenia, autism, epilepsy, pain, bipolar and anxiety disorder. Read More
The glucagon-like peptide-1 receptor (GLP-1R) agonists semaglutide and liraglutide are used for type 2 diabetes and have proven clinically successful in regulating blood glucose levels, but adverse drug reactions (ADRs) have ranged from nausea and diarrhea to pancreatitis. Read More
