Journal of Clinical Oncology June 26, 2026

First-Line Disitamab Vedotin, Tislelizumab, and S-1 in HER2-Overexpressing Advanced Gastric or Gastroesophageal Junction Adenocarcinoma: A Single-Arm, Phase II Trial

Song Li et al.

Bottom Line

A novel first-line triplet regimen combining the HER2-targeted antibody-drug conjugate disitamab vedotin, the PD-1 inhibitor tislelizumab, and S-1 demonstrated a high objective response rate of 89.5% and a median overall survival of 31.9 months in patients with HER2-overexpressing advanced gastric or gastroesophageal junction adenocarcinoma.

Key Findings

1. In the intention-to-treat population (N=57), the confirmed objective response rate (ORR) was 89.5% (95% CI, 78.5-96.0%), including an 8.8% complete response rate and a 98.2% disease control rate.
2. After a median follow-up of 28.2 months, the median progression-free survival (PFS) was 13.8 months (95% CI, 10.3-24.0) and the median overall survival (OS) was 31.9 months (95% CI, 22.1-not reached).
3. Clinical benefit was observed regardless of PD-L1 expression: patients with a Combined Positive Score (CPS) ≥1 achieved an ORR of 92.3% (mPFS 16.7 months, mOS 31.9 months), while those with CPS <1 had an ORR of 87.1% (mPFS 10.0 months, mOS 25.4 months).
4. Treatment-induced T-cell receptor (TCR) clonal expansion was significantly associated with improved PFS (HR 0.34, P=0.017) and OS (HR 0.33, P=0.037), indicating its potential utility as a biomarker of antitumor immune activation.
5. Grade ≥3 treatment-related adverse events occurred in 64.9% of patients, primarily driven by decreased white blood cell count (29.8%), neutropenia (12.3%), anemia (10.5%), and peripheral motor neuropathy (10.5%).

Study Design

Design
Phase II Trial
Open-Label
Sample
57
Patients
Duration
28.2 mo
Median
Setting
Multicenter
Population Adults with histologically confirmed, unresectable or metastatic HER2-overexpressing (IHC 3+ or 2+, regardless of ISH status) gastric or gastroesophageal junction (G/GEJ) adenocarcinoma with no prior systemic therapy for advanced disease.
Intervention Disitamab vedotin (HER2-targeted ADC) plus tislelizumab (anti-PD-1 monoclonal antibody) and S-1 (oral fluoropyrimidine).
Comparator None (Single-Arm).
Outcome Objective response rate (ORR) assessed by independent central review.

Study Limitations

The single-arm, unblinded phase II design prevents direct efficacy comparisons against the current standard of care (trastuzumab plus chemotherapy and pembrolizumab).
The relatively small sample size (N=57) from a single geographic region limits the generalizability of the findings to broader, more diverse patient populations.
The triplet combination makes it difficult to ascertain the exact individual contribution of the antibody-drug conjugate, immune checkpoint inhibitor, and oral chemotherapy to the overall efficacy.
Median overall survival upper bounds had not yet been reached due to the follow-up duration at the time of data cutoff.

Clinical Significance

This phase II trial provides robust preliminary evidence that replacing traditional anti-HER2 monoclonal antibodies and conventional chemotherapy with an MMAE-based antibody-drug conjugate (disitamab vedotin) in combination with immunotherapy (tislelizumab) and S-1 produces profound and durable responses in HER2-overexpressing gastric and gastroesophageal junction (G/GEJ) adenocarcinomas. Most notably, substantial activity was preserved in patients with PD-L1 CPS <1 and those with HER2 IHC 2+/ISH- tumors, subgroups that historically derive limited benefit from standard trastuzumab/pembrolizumab paradigms. These compelling data support advancing this ADC-immuno-chemotherapy triplet into randomized phase III testing as a potential new first-line standard.

Historical Context

Historically, the pivotal ToGA trial (2010) established trastuzumab plus fluoropyrimidine- and platinum-based chemotherapy as the standard first-line treatment for HER2-positive advanced gastric cancer. Recently, the KEYNOTE-811 trial demonstrated that adding pembrolizumab to this backbone improved outcomes, leading to regulatory approvals, but the benefit was largely restricted to patients with strict HER2 positivity and PD-L1 CPS ≥1. Disitamab vedotin is a novel HER2-targeted ADC possessing a cleavable linker and a potent MMAE payload that elicits a 'bystander effect', destroying adjacent tumor cells regardless of their HER2 status. Driven by preclinical evidence showing that ADCs induce immunogenic cell death and synergize with PD-1 blockade, this trial successfully brought an ADC into the first-line setting, moving beyond the traditional ToGA paradigm.

Guided Discussion

High-yield insights from every perspective

Med Student
Medical Student

How does the mechanism of action of an antibody-drug conjugate like disitamab vedotin differ from traditional monoclonal antibodies like trastuzumab in the treatment of HER2-overexpressing gastric cancer?

Key Response

Trastuzumab primarily inhibits HER2 signaling and mediates antibody-dependent cellular cytotoxicity (ADCC). Disitamab vedotin utilizes a HER2-directed antibody to deliver a cytotoxic payload (MMAE) directly into the tumor cell, allowing for targeted cytotoxicity even in tumors with heterogeneous HER2 expression via the bystander effect.

Resident
Resident

Given the standard of care established by the KEYNOTE-811 trial for HER2-positive advanced gastric cancer, how does the regimen in this Phase II trial conceptually modify the current standard first-line treatment?

Key Response

The current standard is trastuzumab, fluoropyrimidine and platinum chemotherapy, plus pembrolizumab. This trial substitutes the standard monoclonal antibody with an ADC (disitamab vedotin), drops the platinum agent, uses S-1 instead of 5-FU or capecitabine, and swaps pembrolizumab for tislelizumab, attempting to maximize efficacy while potentially altering the toxicity profile.

Fellow
Fellow

Disitamab vedotin uses monomethyl auristatin E (MMAE) as its payload. What specific overlapping toxicities might you anticipate when combining an MMAE-based ADC with a fluoropyrimidine (S-1) and an immune checkpoint inhibitor, and how might this impact dose intensity?

Key Response

MMAE is known for causing peripheral neuropathy and neutropenia. S-1 can also cause myelosuppression and gastrointestinal toxicities. Combining an ADC that causes neutropenia with standard chemotherapy can lead to significant additive myelosuppression, potentially requiring dose interruptions that compromise the dose intensity and long-term efficacy.

Attending
Attending

While an ORR of 89.5% and median OS of 31.9 months are historically unprecedented in this population, why must we be cautious about integrating single-arm Phase II survival data into routine practice for advanced gastric cancer?

Key Response

Single-arm trials are subject to significant selection bias, often enrolling fitter patients with lower disease burden. Furthermore, survival endpoints in Phase II trials can be heavily confounded by subsequent lines of therapy and lack a concurrent control arm (like the KEYNOTE-811 control arm) to account for stage migration and improvements in supportive care, making randomized Phase III data essential.

Scholarly Review

Critical appraisal through the lens of expert reviewers and guideline development

PhD
PhD

How does the lack of a randomized control arm in this Phase II trial impact the ability to delineate the independent contribution of the PD-1 inhibitor (tislelizumab) versus the HER2-ADC (disitamab vedotin), and what trial design would best address this?

Key Response

In a single-arm triplet study, it is impossible to determine whether the synergistic effect is driven by the ADC plus chemo, the PD-1 plus chemo, or the full triplet. A factorial design or a multi-arm randomized trial is required to parse out the relative contributions and justify the added toxicity and cost of the triplet regimen.

Journal Editor
Journal Editor

As a reviewer evaluating this manuscript, what critical baseline demographic and molecular data, such as PD-L1 CPS score and HER2 immunohistochemistry distribution, would you require the authors to report to assess the true generalizability of this 89.5% ORR?

Key Response

Gastric cancer response to PD-1 inhibitors is highly dependent on PD-L1 CPS, and ADC efficacy can vary by HER2 expression levels. A tough reviewer would flag that if the cohort is disproportionately skewed toward CPS greater than 10 or exclusively IHC 3+ patients, the remarkable ORR might just reflect a highly selected, biologically favorable subgroup rather than a broad regimen effect.

Guideline Committee
Guideline Committee

The NCCN and ESMO guidelines currently recommend trastuzumab, chemotherapy, and pembrolizumab for HER2-positive first-line gastric cancer based on KEYNOTE-811. What level of evidence does this study provide, and what threshold of data is required before guidelines would adopt this triplet regimen?

Key Response

This single-arm Phase II trial provides Level 3 (or Category 2B) evidence, which is insufficient to supplant a Category 1 recommendation. For guidelines to update the standard of care to include an ADC in the first-line setting, a randomized Phase III trial demonstrating superiority or non-inferiority in OS and PFS compared to the KEYNOTE-811 standard regimen is strictly required.

Clinical Landscape

Noteworthy Related Trials

2010

ToGA Trial

n = 594 · Lancet

Tested

Trastuzumab + chemotherapy

Population

Patients with HER2-positive advanced gastric or gastroesophageal junction cancer

Comparator

Chemotherapy alone

Endpoint

Overall survival

Key result: Adding trastuzumab to chemotherapy significantly improved median overall survival from 11.1 months to 13.8 months.
2020

DESTINY-Gastric01

n = 188 · NEJM

Tested

Trastuzumab deruxtecan (T-DXd)

Population

Patients with HER2-positive advanced gastric cancer progressed on at least two prior regimens

Comparator

Physician's choice of chemotherapy (irinotecan or paclitaxel)

Endpoint

Objective response rate

Key result: T-DXd led to a significantly higher response rate (51% vs 14%) and longer overall survival (12.5 vs 8.4 months) than standard chemotherapy.
2021

KEYNOTE-811

n = 732 · Nature

Tested

Pembrolizumab + trastuzumab + chemotherapy

Population

Patients with previously untreated, HER2-positive advanced gastric or gastroesophageal junction adenocarcinoma

Comparator

Placebo + trastuzumab + chemotherapy

Endpoint

Progression-free survival and overall survival

Key result: The addition of pembrolizumab significantly increased the objective response rate to 74.4% compared to 51.9% with the control, leading to FDA accelerated approval.

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