Exatecan, a potent topoisomerase I inhibitor, is an increasingly utilized payload in ADC development due to its efficacy. The drug-to-antibody ratio (DAR) is a critical quality attribute (CQA) of an ADC, …
Abstract 318: Optimal free exatecan payload tumor/plasma ratio of …
Apr 21, 2025 · Free exatecan was detected in tumors 5 min post treatment in LNCaP-abl. Free exatecan concentrations were approximately 80x higher in tumor compared to plasma 2 h post treatment, and …
Harnessing exDNA for precision exatecan delivery in cancer ... - Springer
Oct 13, 2025 · Conclusions V66-exatecan represents a next-generation of ADCs that overcomes key limitations of traditional platforms by exploiting exDNA-driven tumor selectivity and ENT2-mediated …
Development of Optimized Exatecan-Based ... - ScienceDirect
Oct 2, 2025 · Here, we report the development of novel HER2-targeting conjugates, using the camptothecin derivative exatecan and a linker optimized to control hydrophobicity. Three formats …
The stability of Mal-azo-Exatecan and mouse plasma albumin conjugate was slightly poor in mouse plasma and could release 0.68% Exatecan in 7 days. In short, the albumin conjugates formed by the …
8 Commonly Used ADC Payloads and Their ADME and DDI Properties
May 22, 2025 · Exploring eight commonly used ADC payloads, including their toxicity, mechanisms, and highlighting their ADME/DDI characteristics.
Abstract: We herein report the development and evaluation of a novel HER2-targeting antibody–drug conjugate (ADC) based on the topoisomerase I inhibitor payload exatecan, using our hydrophilic …
Tumor-selective, antigen-independent delivery of a pH sensitive …
Jun 4, 2021 · The peptide forms an alpha helix only in the low pH tumor microenvironment, allowing directional insertion of the peptide across the tumor membrane, cleavage of the linker within the …
Preclinical data has shown marked improvement over CatB linkers regarding neutropenia and lung tolerability issues seen with tubulin and TOPO-1 inhibitors in the clinic Exatecan warhead inhibits …
An exatecan derivative based linker-payload platform leads to ADC ...
Background: Camptothecins-based payload ADCs are attracting attentions as a promising anti-tumor modality. One of the most advanced linker-payload combinations approved and in development is …
Exatecan is a Topoisomerase I Inhibitor for Cancer Therapy Research
Dec 24, 2024 · Exatecan is a very potent inhibitor of topoisomerase I and anticancer agent. It has been intensively studied as a single agent, a large macromolecular conjugate and as the payload …