Suzhou Puhe Biopharma Co. Ltd. presented promising preclinical profile data on PH009-1, a novel fourth-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). Besides ex19del (D), L858R (L) and T790M (T) as the more prevalent EGFR mutations, a segment of patients further acquire C797S (C)-resistant mutation. Current therapies address some single, double or triple mutation-expressing cancers. However, multiple-mutant positive cancers where T790M and/or C797S are involved pose a treatment challenge. The development of pan mutant EGFR TKIs is thus a much-desired research goal.
Lead Discovery Center GmbH and Qli5 Therapeutics GmbH have described macrocyclic compounds acting as proteasome subunit β type-5 (PSMB5) inhibitors reported to be useful for the treatment of cancer, infections, inflammatory disorders, myasthenia gravis and transplant rejection.
At the recently concluded AACR meeting, Biocytogen Pharmaceuticals (Beijing) Co. Ltd. discussed BSA-01, a bispecific antibody-drug conjugate (ADC) targeting both epidermal growth factor receptor (EGFR) and mucin-1 (MUC-1), two tumor-associated antigens that are highly co-expressed in several cancers.
Researchers from Oncovalent Therapeutics Inc. recently provided details on the discovery and preclinical evaluation of SB-4826, a first-in-class oral, covalent small-molecule inhibitor of the SUMO activating enzyme (SUMO E1), the initiating enzyme of the sumoylation cascade. Sumoylation is involved in diverse cell processes such as inflammation, DNA damage response, signaling and cell survival/apoptosis, and it has also emerged as a novel target for activating antitumor immunity due to its role in regulating type I interferon (IFN) signaling.
Researchers from Regor Therapeutics Inc. presented data from the company’s discovery campaign of Son of sevenless homolog 1 (SOS1) inhibitors, which show potential for the treatment of mutated KRAS-positive cancers, such as pancreatic cancers (PAC) and non-small-cell lung cancer (NSCLC). SOS1 is an upstream activator of KRAS. Therefore, SOS1 blockage has great potential as an approach for pan mutant KRAS suppression.
Researchers from Therapex Co. Ltd. recently reported the discovery and preclinical evaluation of a novel fourth-generation epidermal growth factor receptor (EGFR) inhibitor for overcoming C797S mutation-mediated acquired resistance in non-small-cell lung cancer (NSCLC), which has been reported as the most common acquired resistance mechanism in NSCLC.
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