Topical TLR7 agonist and radiotherapy in patients with metastatic breast cancer

Background Toll-like receptor (TLR) agonists and radiation therapy hold promise for cancer immunotherapy. We conducted a phase I/II trial combining topical imiquimod (IMQ, a TLR-7 agonist) and local radiotherapy (RT) in patients with metastatic breast cancer accompanied by longitudinal transcription...

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Main Authors: Ping Jin, Xiaochun Li, Francesco Marincola, Ena Wang, Sandra Demaria, Davide Bedognetti, Darawan Rinchai, Sylvia Adams, Yelena Novik, Ruth Oratz, David Stroncek, Judith Goldberg, Silvia Chiara Formenti, Maria Fenton-Kerimian, Pascale G Levine
Format: Article
Language:English
Published: BMJ Publishing Group 2025-04-01
Series:Journal for ImmunoTherapy of Cancer
Online Access:https://jitc.bmj.com/content/13/4/e011173.full
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author Ping Jin
Xiaochun Li
Francesco Marincola
Ena Wang
Sandra Demaria
Davide Bedognetti
Darawan Rinchai
Sylvia Adams
Yelena Novik
Ruth Oratz
David Stroncek
Judith Goldberg
Silvia Chiara Formenti
Maria Fenton-Kerimian
Pascale G Levine
author_facet Ping Jin
Xiaochun Li
Francesco Marincola
Ena Wang
Sandra Demaria
Davide Bedognetti
Darawan Rinchai
Sylvia Adams
Yelena Novik
Ruth Oratz
David Stroncek
Judith Goldberg
Silvia Chiara Formenti
Maria Fenton-Kerimian
Pascale G Levine
author_sort Ping Jin
collection DOAJ
description Background Toll-like receptor (TLR) agonists and radiation therapy hold promise for cancer immunotherapy. We conducted a phase I/II trial combining topical imiquimod (IMQ, a TLR-7 agonist) and local radiotherapy (RT) in patients with metastatic breast cancer accompanied by longitudinal transcriptional analysis of tumor biopsies.Methods The primary objective of the trial (NCT01421017) was to assess systemic responses by immune-related response criteria (irRC) after an 8-week cycle of topical IMQ and concurrent local RT (cohort 1). An amendment to the trial added two cohorts, both received one dose of cyclophosphamide (CTX) administered 1 week before study treatment initiation, IMQ/RT/CTX (cohort 2) and RT/CTX control (cohort 3). Cutaneous metastases were prospectively assigned to treatment with IMQ and RT (area A) or IMQ alone (area B). Secondary objectives were safety (Common Terminology Criteria for Adverse Events criteria) and local response in skin metastases. In all IMQ cohorts, tumors were biopsied before treatment and at 2 and 3 weeks.Results 31 patients were enrolled (n=12, n=12, and n=7, in cohort 1, 2, and 3, respectively), with 4 out of 24 patients in the IMQ cohorts showing systemic tumor responses (two complete responses (CR) and two partial responses (PR)). No objective responses were observed in the seven patients enrolled in the control arm (RT alone). The treatment was well-tolerated, no grade 4–5 treatment-related adverse events occurred and grade 3 AEs were manageable (anemia, local pain, and local ulceration, n=1 each). Local objective responses were observed in 19/24 (9 CR and 10 PR) and 5/24 (5 PR) in areas treated with combined IMQ-RT and IMQ alone, respectively (p<0.001). All 24 patients treated with IMQ underwent serial biopsies, and 84 samples yielded sufficient material for transcriptional analyses. These revealed that the presence of a T-helper 1 functional orientation of the tumor microenvironment paralleled by the downregulation of DNA-repair genes was associated with CR after IMQ+RT, but not after IMQ alone. No post-treatment activation of immune-effector functions was observed in stable and progressing lesions.Conclusions Our findings support the safety and clinical efficacy of combining topical IMQ with local RT for recurrent breast cancer, with evidence of local and occasional systemic antitumor activity.Trial registration number NCT01421017.
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spelling doaj-art-db35775e3570437e924ff51a8a67b4ef2025-08-20T03:08:06ZengBMJ Publishing GroupJournal for ImmunoTherapy of Cancer2051-14262025-04-0113410.1136/jitc-2024-011173Topical TLR7 agonist and radiotherapy in patients with metastatic breast cancerPing Jin0Xiaochun Li1Francesco Marincola2Ena Wang3Sandra Demaria4Davide Bedognetti5Darawan Rinchai6Sylvia Adams7Yelena Novik8Ruth Oratz9David Stroncek10Judith Goldberg11Silvia Chiara Formenti12Maria Fenton-Kerimian13Pascale G Levine148 National Institutes of Health, Bethesda, Maryland, USA6 Division of Biostatistics, NYU Langone Health, New York, New York, USA7 TAM Bioscience, Nashville, Tennessee, USA3 Sidra Medical and Research Center, Ar-Rayyan, Qatar2 Department of Radiation Oncology, Weill Cornell Medicine, New York, New York, USA11 Sidra Medicine, Doha, Ad Dawhah, Qatar3 Sidra Medical and Research Center, Ar-Rayyan, Qatar1 Perlmutter Cancer Center, NYU Langone Health, New York, New York, USA4 Department of Medicine, NYU Langone Health, New York, New York, USA1 Perlmutter Cancer Center, NYU Langone Health, New York, New York, USA8 National Institutes of Health, Bethesda, Maryland, USA9 Population Health, NYU Grossman School of Medicine, New York, New York, USA2 Department of Radiation Oncology, Weill Cornell Medicine, New York, New York, USA2 Department of Radiation Oncology, Weill Cornell Medicine, New York, New York, USA5 Pathology, NYU Langone Health, New York, New York, USABackground Toll-like receptor (TLR) agonists and radiation therapy hold promise for cancer immunotherapy. We conducted a phase I/II trial combining topical imiquimod (IMQ, a TLR-7 agonist) and local radiotherapy (RT) in patients with metastatic breast cancer accompanied by longitudinal transcriptional analysis of tumor biopsies.Methods The primary objective of the trial (NCT01421017) was to assess systemic responses by immune-related response criteria (irRC) after an 8-week cycle of topical IMQ and concurrent local RT (cohort 1). An amendment to the trial added two cohorts, both received one dose of cyclophosphamide (CTX) administered 1 week before study treatment initiation, IMQ/RT/CTX (cohort 2) and RT/CTX control (cohort 3). Cutaneous metastases were prospectively assigned to treatment with IMQ and RT (area A) or IMQ alone (area B). Secondary objectives were safety (Common Terminology Criteria for Adverse Events criteria) and local response in skin metastases. In all IMQ cohorts, tumors were biopsied before treatment and at 2 and 3 weeks.Results 31 patients were enrolled (n=12, n=12, and n=7, in cohort 1, 2, and 3, respectively), with 4 out of 24 patients in the IMQ cohorts showing systemic tumor responses (two complete responses (CR) and two partial responses (PR)). No objective responses were observed in the seven patients enrolled in the control arm (RT alone). The treatment was well-tolerated, no grade 4–5 treatment-related adverse events occurred and grade 3 AEs were manageable (anemia, local pain, and local ulceration, n=1 each). Local objective responses were observed in 19/24 (9 CR and 10 PR) and 5/24 (5 PR) in areas treated with combined IMQ-RT and IMQ alone, respectively (p<0.001). All 24 patients treated with IMQ underwent serial biopsies, and 84 samples yielded sufficient material for transcriptional analyses. These revealed that the presence of a T-helper 1 functional orientation of the tumor microenvironment paralleled by the downregulation of DNA-repair genes was associated with CR after IMQ+RT, but not after IMQ alone. No post-treatment activation of immune-effector functions was observed in stable and progressing lesions.Conclusions Our findings support the safety and clinical efficacy of combining topical IMQ with local RT for recurrent breast cancer, with evidence of local and occasional systemic antitumor activity.Trial registration number NCT01421017.https://jitc.bmj.com/content/13/4/e011173.full
spellingShingle Ping Jin
Xiaochun Li
Francesco Marincola
Ena Wang
Sandra Demaria
Davide Bedognetti
Darawan Rinchai
Sylvia Adams
Yelena Novik
Ruth Oratz
David Stroncek
Judith Goldberg
Silvia Chiara Formenti
Maria Fenton-Kerimian
Pascale G Levine
Topical TLR7 agonist and radiotherapy in patients with metastatic breast cancer
Journal for ImmunoTherapy of Cancer
title Topical TLR7 agonist and radiotherapy in patients with metastatic breast cancer
title_full Topical TLR7 agonist and radiotherapy in patients with metastatic breast cancer
title_fullStr Topical TLR7 agonist and radiotherapy in patients with metastatic breast cancer
title_full_unstemmed Topical TLR7 agonist and radiotherapy in patients with metastatic breast cancer
title_short Topical TLR7 agonist and radiotherapy in patients with metastatic breast cancer
title_sort topical tlr7 agonist and radiotherapy in patients with metastatic breast cancer
url https://jitc.bmj.com/content/13/4/e011173.full
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