R290-CPT2

**R290-CPT2** is a research-stage RSPO2-based peptide-drug conjugate designed to target leucine-rich repeat-containing G protein-coupled receptors 4, 5, and 6. It comprises the R290 peptibody, derived from a signaling-inactive mutant RSPO2 furin domain, conjugated to the camptothecin analog payload CPT2. R290-CPT2 retains high-affinity binding to LGR4, LGR5, and LGR6, enabling receptor-mediated uptake and delivery of the cytotoxic camptothecin payload to receptor-positive tumor cells. It showed potent activity in colorectal cancer and neuroblastoma models, including SKNAS xenografts, and remains a preclinical candidate reported in a bioRxiv preprint. ([biorxiv.org](https://www.biorxiv.org/content/10.1101/2025.04.25.650662v4.full.pdf))