Insilico Medicine Inc. recently discussed the generative artificial intelligence (AI)-powered design of ISM-6331, a novel, potent, selective and non-covalent pan-TEAD inhibitor that blocks TEAD palmitoylation to suppress YAP/TAZ-TEAD transcriptional activity and shows strong antitumor activity in a preclinical model of Hippo pathway-dysregulated cancers and other solid cancers were discussed.
DXC-006 (Hangzhou DAC Biotechnology Co. Ltd.) is an antibody-drug conjugate (ADC) that targets CD56, a molecule involved in cell-cell adhesion and cell-matrix adhesion that is overexpressed in neuroblastoma, small-cell lung cancer and multiple myeloma, but less frequently expressed in normal tissues. DXC-006 consists of an anti-CD56 antibody (DXA-006) linked to the topoisomerase 1 (TOP1) inhibitor CPT-116 through a linker.
The discovery of a potent, selective and orally bioavailable serine/threonine-protein kinase PLK4 (STK18) inhibitor with synthetic lethality in TRIM7-amplified cancers was reported by Oric Pharmaceuticals Inc. at the ongoing AACR meeting in San Diego.
Researchers from Puhe Biopharma Co. Ltd. presented the discovery and preclinical evaluation of PH027-1, a novel small-molecule Werner syndrome protein (WRN) inhibitor targeting microsatellite instability high (MSI-H) tumors.
Prior to this year’s Annual Meeting of the American Association for Cancer Research (AACR), it had been 14 years since metastasis had been the subject of a plenary session. So, the Tuesday session on “Evolution of the genome, microenvironment, and host through metastasis” had plenty of new insights to share.
M-9140 (Merck KGaA) is an antibody-drug conjugate (ADC) that carries a DNA topoisomerase 1 (TOP1) inhibitor payload plus an antibody directed against carcinoembryonic antigen-related cell adhesion molecule 5 (CEACAM5). CEACAM5 is a cell surface protein that is overexpressed in colorectal cancer and other solid tumors.
ABM Therapeutics Inc. presented a novel small-molecule, ATP-uncompetitive, phosphorylated MEK (pMEK) inhibitor – ABM-4095 – that potently prevents phosphorylation of MEK by RAF with moderate inhibition of MEK kinase activity; it is being investigated for the potential treatment of pancreatic cancer.
At the AACR meeting, Innovent Biologics Inc. discussed the discovery and preclinical evaluation of a B7-H3/EGFR bispecific antibody-drug conjugate (bsADC).
Pfizer Inc. has presented preclinical data on its first-in-class, selective cyclin-dependent kinase 4 (CDK4) inhibitor compound, PF-07220060, that has shown 20-fold and 4-fold increased selectivity for CDK4 vs. CDK6 compared to palbociclib and abemaciclib/ribociclib, respectively.
It has been previously demonstrated that B7-H3 and EGFR are co-expressed in multiple solid tumors. At the ongoing AACR meeting in San Diego, researchers from Innovent Biologics Inc. presented preclinical data for their bispecific antibody (bsAb), IBI-334, against B7-H3 and EGFR.
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