The existence of two approved therapies, Lumakras (sotorasib, Amgen Inc.) and Karzati (adagrasib, Mirati Therapeutics Inc.), has been a triumphant success against KRAS, a protein that was once considered undruggable. KRAS is the most frequently mutated oncogene in solid tumors. KRAS driver mutations are found in about 30% of non-small-cell lung cancers (NSCLC), about half of colorectal cancers, and more than 90% of pancreatic cancers. Lumakras and Karzati both target the G12C mutation. Inhibitors that target other mutations, like G12D, are now making their way through preclinical and clinical development, while some companies are developing therapies that would target mutated KRAS more broadly, irrespective of the specific mutation that is activating the protein. Read More
Son of sevenless homolog 1 (SOS1) plays a crucial role in the conversion of KRAS from its GDP- to its GTP-bound form independently of KRAS mutational status, thus being a promising therapeutic target for all tumors driven by KRAS. Haihe Biopharma Co. Ltd. has presented a potent SOS1 inhibitor, HH-100937, that has been found effective as monotherapy or when combined with drugs targeting the KRAS/MAPK pathway. Read More
Proof-of-concept findings had shown that mRNA silencing of striatal Cav1.3 channels prevented and reversed established levodopa-induced dyskinesia in parkinsonian rats, with these effects being maintained in aged rats. Read More
Ochre Bio Ltd. has established a partnership with Boehringer Ingelheim Pharma GmbH & Co. KG focused on the discovery and development of novel first-in-class regenerative treatments for chronic liver diseases, such as late-stage metabolic dysfunction-associated steatohepatitis (MASH) cirrhosis. Read More
Researchers from Adcentrx Therapeutics Inc. recently reported preclinical data for the Nectin-4-targeting antibody-drug conjugate (ADC) ADRX-0706, currently in phase I development for the treatment of solid tumors (NCT06036121). Read More
New York University has disclosed RAGE receptor antagonists reported to be useful for the treatment of cancer, SARS-CoV-2 infection (COVID-19), diabetic complications, ischemia reperfusion injury, neurodegeneration, obesity, and cardiovascular and inflammatory disorders, among others. Read More
Kaken Pharmaceutical Co. Ltd. has synthesized signal transducer and activator of transcription 6 (STAT6) inhibitors reported to be useful for the treatment of asthma, allergic rhinitis, chronic obstructive pulmonary disease, atopic dermatitis, nasal polyps, bullous pemphigoid, prurigo and urticaria, among others. Read More
Researchers from Royal College of Surgeons in Ireland (RCSI) have created a new orthotopic preclinical model of glioblastoma (GBM), designed to recapitulate patient response to standard-of-care and targeted treatments. Read More
IFM Due Inc. has described proteolysis targeting chimera (PROTAC) compounds comprising cereblon (CRBN) ligands covalently linked to a stimulator of interferon genes protein (STING; TMEM173)-targeting moiety through a linker. Read More
Enyo Pharma SA has identified tertiary amine derivatives reported to be useful for the treatment of respiratory syncytial virus (RSV) infections. Read More
