Antibody-drug conjugates (ADCs) with a dual payload, which deliver two distinct cytotoxic agents via a single antibody, are emerging therapeutics developed to address the limitations of classic ADCs. Primelink Biotherapeutics (Shenzhen) Co. Ltd. recently presented data for their dual-payload ADCs, highlighting PLB-015, which carries a TOP1 inhibitor and an ATR inhibitor with an anti-HER2 antibody and is designed to inhibit the DNA damage response activated by cancer cells when harmed.

Researchers at the School of Pharmacy and Biomolecular Sciences from the Royal College of Surgeons in Ireland and collaborating institutions have detailed the design, synthesis and biological evaluation of a new series of triazine-based multitarget inhibitors aimed at dual inhibition of PI3K and HDAC for breast cancer therapy.

Researchers from the Cleveland Clinic identified a new mechanism of AIC involving upregulated TOP2B expression and directly impacting cardiomyocyte function without the formation of TOP2B-anthracycline-DNA complexes in cardiomyocytes.

China’s National Medical Products Administration (NMPA) has granted clinical trial clearance to SYH-2095 tablets, a novel lysine acetyltransferase 6 (KAT6) inhibitor codeveloped by CSPC Pharmaceutical Group Ltd. and Hangzhou Innogate Pharma Co. Ltd. for the treatment of advanced malignant tumors. SYH-2095 received IND clearance in the U.S. last month.

Degron Therapeutics Inc. closed a $40 million series A extension round that will see the company advance its molecular glue degraders targeting previously undruggable or insufficiently drugged proteins.

Transforming acidic coiled-coil-containing protein 3 (TACC3) is a core member of multiprotein complexes that regulate microtubule- and centrosome-related processes. Its aberrant expression is found in several cancer types with poor prognosis, thus highlighting it as a candidate therapeutic target. Researchers from Beijing Konruns Pharmaceutical Co. Ltd. have presented data for KC-1101, a TACC3 inhibitor for treating aggressive cancers with centrosome amplification.

Ubiquitin carboxyl-terminal hydrolase 1 (USP1) is a synthetic lethality target in cancers with high replication stress, such as tumors with BRCA gene mutations or homologous recombination deficiency (HRD). Targeting USP1 has emerged as a promising approach to overcome resistance observed in BRCA/HRD-driven tumors. Aigen Sciences Inc. developed and presented data for AIG-07025, a potent and selective USP1 inhibitor.