Development

Astellas pushes CLDN18.2 bispecific ASP2138 into Phase III

Astellas pushes CLDN18.2 bispecific ASP2138 into Phase III

Astellas Pharma (TSE: 4503) has dosed the first patient in a Phase III trial of ASP2138, its subcutaneously administered CLDN18.2 × CD3 bispecific antibody, in first-line CLDN18.2-positive, HER2-negative locally advanced unresectable or metastatic gastric or gastroesophageal junction (GEJ) adenocarcinoma. The trial tests whether layering a T-cell engager onto the combination of chemotherapy and Merck's Keytruda (pembrolizumab) can improve on outcomes that remain poor despite recent advances in the biomarker-selected population. The median progression-free survival on non-CLDN18.2-directed standard of care in this population remains 6 to 7 months, per Astellas' cited reference to KEYNOTE-859 data.

ASP2138 simultaneously binds CLDN18.2 on tumor cells and CD3 on T cells, physically bridging the two to activate cytotoxic killing. Unlike Astellas' own approved CLDN18.2-directed monoclonal antibody Vyloy (zolbetuximab-clzb), which depletes tumor cells through antibody-dependent cellular cytotoxicity and complement-dependent cytotoxicity, ASP2138 recruits T cells directly. The subcutaneous route also distinguishes it from the intravenous infusions required by all currently approved agents in this setting.

The randomized, double-blind, placebo-controlled study plans to enroll 570 participants across multiple countries. The experimental arm receives ASP2138 plus chemotherapy (CAPOX or mFOLFOX6) with pembrolizumab; the control arm receives placebo plus chemotherapy with or without pembrolizumab. Co-primary endpoints are overall survival and progression-free survival. Phase I/Ib data presented at ESMO 2025 provided the proof of concept that supported Phase III initiation, with first clinical results covering monotherapy and combination cohorts in CLDN18.2-positive gastric and GEJ adenocarcinoma.

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In terms of the competitive environment, Astellas' own Vyloy received US FDA approval in October 2024 in combination with chemotherapy for CLDN18.2-positive, HER2-negative disease, following earlier approvals in Japan, the UK, the EU, and South Korea. Pembrolizumab and Bristol Myers Squibb's Opdivo (nivolumab) are also approved for the broader HER2-negative population. ASP2138's trial design — adding the bispecific on top of both chemotherapy and pembrolizumab — is therefore testing incremental benefit over a backbone of established therapies. AstraZeneca is also developing the CLDN18.2-targeted antibody-drug conjugate sonesitatug vedotin, which delivered a Phase III overall survival benefit across the second-line-and-later population in CLDN18.2-positive advanced gastric cancer. Meanwhile, China's Innovent Biologics has filed arcotatug tavatecan for approval in China, the first global regulatory submission for a CLDN18.2-directed ADC.

For Astellas, ASP2138 carries milestone and royalty obligations to Xencor (Nasdaq: XNCR), whose XmAb 2+1 bispecific format underpins the molecule's design. Xencor is eligible to receive up to USD 232.5 million in future milestones linked to the molecule's development.


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