Treatment-related adverse events of antibody drug-conjugates in clinical trials

Abstract Background Antibody–drug conjugates (ADCs) aim to enhance the therapeutic index of cytotoxic agents but can cause unexpected toxicities. This study evaluated adverse events (AEs) from phase 1 trials at The Royal Marsden Drug Development Unit (DDU) over a decade and pivotal phase 2 and 3 tri...

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Main Authors: Harold Nathan Tan, Marta Ascanio Morcillo, Juanita Lopez, Anna Minchom, Adam Sharp, Alec Paschalis, Georgina Silva-Fortes, Bindu Raobaikady, Udai Banerji
Format: Article
Language:English
Published: BMC 2025-07-01
Series:Journal of Hematology & Oncology
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Online Access:https://doi.org/10.1186/s13045-025-01720-3
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author Harold Nathan Tan
Marta Ascanio Morcillo
Juanita Lopez
Anna Minchom
Adam Sharp
Alec Paschalis
Georgina Silva-Fortes
Bindu Raobaikady
Udai Banerji
author_facet Harold Nathan Tan
Marta Ascanio Morcillo
Juanita Lopez
Anna Minchom
Adam Sharp
Alec Paschalis
Georgina Silva-Fortes
Bindu Raobaikady
Udai Banerji
author_sort Harold Nathan Tan
collection DOAJ
description Abstract Background Antibody–drug conjugates (ADCs) aim to enhance the therapeutic index of cytotoxic agents but can cause unexpected toxicities. This study evaluated adverse events (AEs) from phase 1 trials at The Royal Marsden Drug Development Unit (DDU) over a decade and pivotal phase 2 and 3 trials leading to FDA registration, correlating AEs with ADC components such as target, antibody, linker, payload, and Drug-to-Antibody Ratio (DAR). Methods We performed a retrospective cohort analysis of patients treated with ADCs in phase 1 trials (January 2014 to January 2024) compared to published phase 2–3 trials of FDA-approved ADCs. Univariate and multivariate logistic regression analyzed ADC components and treatment toxicities. Results One hundred thirty one phase 1 trial patients and 2666 phase 2–3 trial participants were included. High incidences of any-grade treatment-related AEs were observed (89% in phase 1, 93% in phase 2–3), with 58% experiencing grade 3 or higher toxicities in phase 1 and 46% in later phases. Major AEs included fatigue, hematologic toxicities, nausea/vomiting, ocular toxicities, and peripheral neuropathy. Antibody targets were linked to neuropathy, non-cleavable linkers to ocular, pulmonary, and hematologic toxicities, and tubulin-binding payloads to peripheral neuropathy. ADCs with DAR > 4 were associated with higher pulmonary and hematologic AEs. Conclusion Despite their design to minimize toxicity, ADCs were linked to significant AEs. Specific ADC components may contribute to distinct toxicities, necessitating more robust trial data to inform future ADC design. Graphical Abstract
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spelling doaj-art-daf8c53d90374be8979d8a3daeb8fa402025-08-20T03:03:29ZengBMCJournal of Hematology & Oncology1756-87222025-07-0118111110.1186/s13045-025-01720-3Treatment-related adverse events of antibody drug-conjugates in clinical trialsHarold Nathan Tan0Marta Ascanio Morcillo1Juanita Lopez2Anna Minchom3Adam Sharp4Alec Paschalis5Georgina Silva-Fortes6Bindu Raobaikady7Udai Banerji8The Royal Marsden HospitalThe Royal Marsden HospitalThe Royal Marsden HospitalThe Royal Marsden HospitalThe Royal Marsden HospitalThe Royal Marsden HospitalThe Royal Marsden HospitalThe Royal Marsden HospitalThe Royal Marsden HospitalAbstract Background Antibody–drug conjugates (ADCs) aim to enhance the therapeutic index of cytotoxic agents but can cause unexpected toxicities. This study evaluated adverse events (AEs) from phase 1 trials at The Royal Marsden Drug Development Unit (DDU) over a decade and pivotal phase 2 and 3 trials leading to FDA registration, correlating AEs with ADC components such as target, antibody, linker, payload, and Drug-to-Antibody Ratio (DAR). Methods We performed a retrospective cohort analysis of patients treated with ADCs in phase 1 trials (January 2014 to January 2024) compared to published phase 2–3 trials of FDA-approved ADCs. Univariate and multivariate logistic regression analyzed ADC components and treatment toxicities. Results One hundred thirty one phase 1 trial patients and 2666 phase 2–3 trial participants were included. High incidences of any-grade treatment-related AEs were observed (89% in phase 1, 93% in phase 2–3), with 58% experiencing grade 3 or higher toxicities in phase 1 and 46% in later phases. Major AEs included fatigue, hematologic toxicities, nausea/vomiting, ocular toxicities, and peripheral neuropathy. Antibody targets were linked to neuropathy, non-cleavable linkers to ocular, pulmonary, and hematologic toxicities, and tubulin-binding payloads to peripheral neuropathy. ADCs with DAR > 4 were associated with higher pulmonary and hematologic AEs. Conclusion Despite their design to minimize toxicity, ADCs were linked to significant AEs. Specific ADC components may contribute to distinct toxicities, necessitating more robust trial data to inform future ADC design. Graphical Abstracthttps://doi.org/10.1186/s13045-025-01720-3ADCsAEsClinical trials
spellingShingle Harold Nathan Tan
Marta Ascanio Morcillo
Juanita Lopez
Anna Minchom
Adam Sharp
Alec Paschalis
Georgina Silva-Fortes
Bindu Raobaikady
Udai Banerji
Treatment-related adverse events of antibody drug-conjugates in clinical trials
Journal of Hematology & Oncology
ADCs
AEs
Clinical trials
title Treatment-related adverse events of antibody drug-conjugates in clinical trials
title_full Treatment-related adverse events of antibody drug-conjugates in clinical trials
title_fullStr Treatment-related adverse events of antibody drug-conjugates in clinical trials
title_full_unstemmed Treatment-related adverse events of antibody drug-conjugates in clinical trials
title_short Treatment-related adverse events of antibody drug-conjugates in clinical trials
title_sort treatment related adverse events of antibody drug conjugates in clinical trials
topic ADCs
AEs
Clinical trials
url https://doi.org/10.1186/s13045-025-01720-3
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