Karenitecin (cositecan) / BioNumerik - LARVOL DELTA

Silyl ethers analogs of SN-38 with unique blue-fluorescent properties exhibit potent anti-cancer activity through topoisomerase I inhibition (AACR 2026) - "Topoisomerase I inhibitors, such as deruxtecan and irinotecan, represent an important class of cell cycle inhibitors in the treatment of cancers. Among these, silylated topoisomerase inhibitors, including DB-67 and karenitecin, have exhibited increased antiproliferative potency...Moreover, direct tissue injection of the siloxytecans has demonstrated exceptional tissue retention and durability, establishing the dimethylthexyl siloxytecan as a preclinical lead for in vivo evaluation. Collectively, these studies demonstrate improved intracellular delivery of topoisomerase inhibitors with the introduction of silicon-containing motifs and highlight the utility of these compounds for enhanced anticancer activity with unique lipophilicity and fluorescent properties that enable quantitative tracking of compound distribution in cancer cells, which is currently being investigated for in vivo activity in triple negative breast cancer studies."

Breast Cancer • Colorectal Cancer • Liver Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Solid Tumor • Triple Negative Breast Cancer • TOP1