Two deals for antibody-drug conjugates inked since May between Merck & Co. Inc. and Sichuan Kelun-Biotech Pharmaceutical Co. Ltd. have blossomed eight months later into the year’s biggest agreement, one that could bring Kelun-Biotech up to $9.3 billion in development, regulatory and sales milestones. The exclusive license and collaboration deal has Merck paying an up-front $175 million to Kelun-Biotech plus promising to make an equity investment in the Sichuan, China-based company.

Trastuzumab deruxtecan (DS-8201a) is an antibody-drug conjugate used for the treatment of metastatic HER2+ breast cancer that is refractory to anti-HER2 therapy such as T-DM1, however, there is a lack of knowledge on acquired or innate resistance to the drug.

Approximately 20,000 patients diagnosed with non-Hodgkin lymphomas died in 2022 despite current treatments; 30-40% of these cases involved diffuse large B-cell lymphoma (DLBCL). Monoallelic mutations in histone acetyltransferases (HATs) occur in over 39% of germinal center DLBCLs. Activation of intact wild-type alleles offers an opportunity to overcome the mutated allele.

Researchers from Taipei Medical University presented the discovery of novel store-operated calcium channel (SOC) inhibitors as potential anticancer candidates. Synthesis and optimization of a series of difluorobenzamide derivatives led to the discovery of MPT-0M004 as the lead candidate with promising SOC inhibitory activity. In vitro, both migration and invasion of colorectal cancer cells were significantly suppressed after 48 hours of treatment with MPT-0M004, with the growth inhibitory effect of the compound being similar to that seen for the reference SOC inhibitor.