OnCo
ideasIdea

Payload-class switching as the rule for ADC sequencing

When one ADC fails, the next should carry a different kind of poison, not just aim at a different protein.

Cross-resistance among TOP1-payload ADCs is emerging as a clinical reality. The field's instinct to switch antigen (HER2TROP2) may be less important than switching payload mechanism (TOP1 → tubulin, DNA crosslinker, or degrader).

Confidence
50%75%likelyOnCo editors (initial estimate), 2026-09-07 · Cross-resistance among TOP1 payloads is already observed retrospectively; prospective confirmation is likely.
Hypothesis
In patients progressing on a TOP1-payload ADC, a next ADC with a non-TOP1 payload yields longer PFS than a second TOP1-payload ADC regardless of antigen.
Rationale
SLFN11 loss, TOP1 mutations, and ABCG2 upregulation are payload-level resistance mechanisms shared by DXd, SN-38, and exatecan derivatives.
What would test it
A randomised sequencing trial in HER2-low/TNBC after T-DXd or sacituzumab: MMAE- or non-TOP1-payload ADC vs alternate TOP1 ADC; measure SLFN11 and TOP1 status on progression biopsies as predictive biomarkers.
Maturity
preclinical evidence

Key papers

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rctJournal of Clinical Oncology 2024
TROPION-Breast01: datopotamab deruxtecan versus chemotherapy in pretreated hormone-receptor-positive breast cancer, and why a PFS win did not translate to survival

For hormone-receptor-positive metastatic breast cancer that has already had chemotherapy, Dato-DXd controls the disease for longer with fewer severe side effects than chemotherapy, but does not help patients live longer, so it is not a standard option here. The result is a reminder that progression-free survival is a surrogate; regulators and clinicians should wait for survival data before adopting an ADC in a setting where later therapies are effective.

rctNew England Journal of Medicine 2022changed practice
DESTINY-Breast03: trastuzumab deruxtecan beats T-DM1 as second-line treatment of HER2-positive metastatic breast cancer

For HER2-positive metastatic breast cancer that has progressed after trastuzumab and a taxane, trastuzumab deruxtecan is now the standard second-line treatment and T-DM1 has moved later in the sequence. The benefit is large enough that ADC design, not just the target, is understood to be what matters. Patients need lung monitoring because of the risk of pneumonitis.

rctNew England Journal of Medicine 2022changed practice
DESTINY-Breast04: trastuzumab deruxtecan works in HER2-low breast cancer, creating a new treatable group

Patients whose breast cancer was previously called HER2-negative may now be eligible for an effective HER2-directed drug if their tumour has even low-level HER2 staining, so pathology reports must now distinguish HER2-low (1+ or 2+/ISH-negative) from HER2-zero. This applies to metastatic disease after at least one line of chemotherapy; it does not mean these patients benefit from trastuzumab or other older HER2 drugs.

Connected

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