Cybrexa Therapeutics' CBX-12, a 26-amino-acid pH-targeted peptide-drug conjugate that delivers a topoisomerase-1 inhibitor selectively to the acidic tumor microenvironment, completed Phase 1 in September 2024 and has moved into Phase 2 for platinum-resistant ovarian cancer. The peptide-drug conjugate field continues to broaden beyond the bicyclic-peptide and FAP-activated approaches already covered at ASCO, with smaller direct-acting peptide carriers gaining traction.
Avacta Therapeutics's AVA6000, a fibroblast activation protein (FAP)-activated peptide-drug conjugate releasing doxorubicin selectively in the tumor microenvironment, will be presented at ASCO 2026 (Chicago, May 29-June 2) covering Phase Ia/Ib data in FAP-positive solid tumors with activity against salivary gland cancers — a rare cancer subset with no approved targeted therapies. The pre|CISION platform attaches a peptide tetrazolyl moiety that is cleaved by FAP, an enzyme overexpressed in cancer-associated fibroblasts and selectively present in the tumor stroma, allowing systemic dosing without the cardiotoxicity that limits free doxorubicin. AVA6000 joins Bicycle's nuzefatide pevedotin and Lilly's CRN09682 in the broader peptide-drug conjugate Phase 2/3 cohort.