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Nectin-4 PET for predicting enfortumab vedotin dose-response in urothelial carcinoma

Akhilesh Mishra, Ajay Sharma, Kuldeep Gupta, Dhanush S. Banka, Burles A. Johnson, Hoffman-Censits Jean, Peng Huang, David J. McConkey, S. Nimmagadda

2026Science Advances6 citationsDOIOpen Access PDF

Abstract

Optimizing dosing strategies is critical to balance effectiveness and toxicity, especially for drugs with narrow therapeutic windows such as antibody-drug conjugates (ADCs). This study evaluates whether positron emission tomography (PET) imaging targeting Nectin-4 can noninvasively quantify the real-time interaction of the ADC enfortumab vedotin (EV) with tumors in urothelial carcinoma. Using the imaging agent [ 68 Ga]AJ647, dynamic changes in the interaction of EV with Nectin-4 were measured across preclinical models and correlated with therapeutic responses. PET imaging identified dose-dependent variations in Nectin-4 engagement, with suboptimal EV doses resulting in incomplete Nectin-4 engagement and increased tumor growth. Crucially, PET-measured target engagement predicted therapeutic outcomes more reliably than either drug dose or baseline target expression. By defining effective target engagement levels needed for optimal therapeutic outcomes, PET imaging provides a clear benchmark for dosing decisions, maximizing efficacy while potentially reducing exposure to higher, toxic doses and thereby enhancing patient safety.

Topics & Concepts

MedicineDosingPet imagingPositron emission tomographyOncologyTherapeutic drug monitoringTherapeutic indexTherapeutic effectDrugUrothelial carcinomaCancer researchInternal medicinePharmacologyUrothelial cancerPharmacokineticsImaging biomarkerMaximum tolerated doseTherapeutic approachEffective dose (radiation)Functional imagingCancerPreclinical testingBiomarkerPreclinical researchNuclear medicineMolecular imagingText miningBladder and Urothelial Cancer TreatmentsWnt/β-catenin signaling in development and cancerHER2/EGFR in Cancer Research
Nectin-4 PET for predicting enfortumab vedotin dose-response in urothelial carcinoma | Litcius