Researchers from Neophore Ltd. presented the discovery and preclinical evaluation of NP-1867, a small molecule inhibitor of DNA mismatch repair (MMR) protein PMS2, being developed for the treatment of cancer.
Researchers from Boehringer Ingelheim Pharma GmbH & Co. KG presented the discovery and preclinical characterization of BI-3706674, a potent and orally available small-molecule inhibitor of the KRAS oncogene, targeting both KRAS-mutant and KRAS wild-type amplified (WTamp) cancers.
Opna Bio AG recently provided findings from preclinical studies of novel dual E1A binding protein P300 (EP300) and CREB binding protein (CBP) inhibitors under investigation as potential anticancer agents.
Researchers from Loxo Oncology at Eli Lilly and Co. recently reported the discovery and preclinical evaluation of a new highly potent and selective pan-KRAS inhibitor, LY-4066434, being developed for the treatment of cancer.
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.
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.
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).
Antibody-drug conjugates (ADCs) are effective anti-cancer agents in a wide variety of solid and hematologic cancers. CD30 (TNFRSF8), a member of the TNF receptor superfamily is the target of antibody drug conjugate Adcetris (brentuximab vedotin/BV, Seagen Inc.) approved for use in multiple CD30-expressing lymphomas.
Researchers from Bridge Biotherapeutics Inc. have presented the discovery and preclinical characterization of BBT-4437, a novel brain-penetrable and reversible pan-transcriptional enhancer factor (TEAD) inhibitor, designed to target the Hippo signaling pathway in solid tumors.
