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Anti-GPC3 Targeted Therapies – Target Population, Competitive Landscape, and Market Forecast – 2040

Publisher DelveInsight
Published Sep 01, 2025
Length 153 Pages
SKU # DEL20495186

Description

Key Highlights

Anti-GPC3 therapies harness tumor-specific GPC3 expression to induce direct cytotoxicity, block oncogenic signaling pathways, and enhance immune-mediated tumor elimination. Their effectiveness depends on factors such as tumor type, GPC3 expression levels, and the tumor microenvironment, positioning them as promising approaches for HCC and other GPC3-positive cancers.

Therapeutic strategies targeting GPC3 have advanced from monoclonal antibodies to next-generation formats such as antibody-drug conjugates (ADCs), bispecific/trispecific antibodies, radiopharmaceuticals, and CAR-T cell therapies. Many of these are in early clinical studies, aiming to translate GPC3 specificity into meaningful antitumor efficacy.

GPC3 expression is observed in approximately 75% of hepatocellular carcinoma (HCC) cases and 70% of Merkel cell carcinoma (MCC) cases, reinforcing its role as a key biomarker and therapeutic target across both high-burden and rare aggressive malignancies.

The total market for anti-GPC3 targeted therapies in the 7MM is projected to expand dramatically, reaching approximately USD 3.2 billion by 2040, up from USD 24 million in 2032. This rapid growth reflects the increasing clinical adoption of next-generation GPC3 therapies, rising incidence of GPC3-expressing malignancies, and the anticipated introduction of first-in-class approvals.

Emerging GPC3-targeted therapies span diverse modalities for HCC and other tumors, including ZW251 (ADC, Zymeworks), AZD9793 (trispecific T-cell engager, AstraZeneca), and BGB-B2033 ± Tislelizumab (bispecific ± anti-PD-1, BeOne).

Advanced CAR-T and radiopharmaceutical approaches, including RYZ801 (RayzeBio), 225Ac-GPC3 (BAY 3547926, Bayer), ECT204 (Eureka Therapeutics), and BOXR1030 (Sotio Biotech), highlight the multi-pronged clinical potential of GPC3-directed strategies.

No anti-GPC3 targeted therapy is currently approved or commercially available, and the first approvals are anticipated within the forecast period of 2025–2040.

DelveInsight’s “Anti-glypican-3 (GPC3) Targeted Therapies” – Target Population, Competitive Landscape, and Market Forecast – 2040” report delivers an in-depth understanding of the anti- GPC3 targeted therapies, historical and projected epidemiological data, competitive landscape as well as anti-GPC3 targeted therapies market trends in the United States, EU4 (Germany, France, Italy, and Spain), the United Kingdom, and Japan.

The anti-GPC3 targeted therapies market report provides current treatment practices, emerging drugs, market share of individual therapies, and current and forecasted 7MM anti-GPC3 targeted therapies market size from 2020 to 2040. The report also covers emerging anti-GPC3 targeted therapies treatment practices/algorithms and unmet medical needs to curate the best opportunities and assess the market’s potential.

Geography Covered

The United States

EU4 (Germany, France, Italy, and Spain) and the United Kingdom

Japan

Anti-glypican-3 (GPC3) Targeted Therapies Understanding and Treatment Algorithm

Anti-glypican-3 (GPC3) Targeted Therapies Overview

GPC3 is a cell-surface proteoglycan highly expressed in HCC but absent in normal liver tissue, making it a promising diagnostic biomarker and therapeutic target. Its role in key oncogenic pathways, including Wnt/ß-catenin and Hedgehog signaling, drives tumor growth. Measuring GPC3 via biopsy has limitations due to invasiveness and tumor heterogeneity.

Anti-GPC3 targeted therapies has evolved from monoclonal antibodies to next-generation approaches such as antibody-drug conjugates, multispecific/bispecific antibodies, radiopharmaceuticals, and CAR-T cell therapies. Early clinical studies show manageable safety and preliminary activity, while molecular delivery systems and targeted radionuclides aim to enhance efficacy and overcome resistance. Successful translation relies on precise patient selection, combination strategies with immunotherapy, and overcoming the immunosuppressive tumor microenvironment.

Anti-glypican-3 (GPC3) Targeted Therapies Epidemiology

The anti-GPC3 targeted therapies epidemiology chapter in the report provides historical as well as forecasted epidemiology segmented total incident cases of promising indications, GPC3 expressing incident cases of selected indications, GPC3 expressing locally advanced/metastatic cases and GPC3 biomarker positive advanced/metastatic cases in the 7MM covering the United States, EU4 (Germany, France, Italy, and Spain), the United Kingdom, and Japan from 2020 to 2040.

In 2024, HCC accounts for the largest GPC3-expressing patient population in the US with approximately 25,000 cases, highlighting GPC3’s relevance as a therapeutic target. Squamous cell carcinoma in NSCLC is the second-largest GPC3-positive group, highlighting further opportunities for targeted therapies.

In 2024, Japan reported approximately 7,800 HCC cases, followed by around 7,500 cases of squamous cell carcinoma in NSCLC. This underscores regional differences in disease incidence and the need to adapt GPC3-targeted therapeutic strategies to specific local patient populations.

Anti-glypican-3 (GPC3) Targeted Therapies Drug Chapters

The drug chapter of the anti-GPC3 targeted therapies report provides a detailed analysis of early-stage candidates (Phase I and Phase II) as well as pipeline drugs under development. It also helps understand the anti-GPC3 targeted therapies clinical trial details, expressive pharmacological action, agreements and collaborations, approval and patent details, advantages and disadvantages of each included drug the latest news and press releases.

Emerging Drugs

RYZ801: RayzeBio/Bristol–Myers Squibb

RYZ801 is a first-in-class proprietary peptide that specifically binds to GPC3 to deliver Ac225 for the treatment of HCC. RYZ801 is currently being investigated in a Phase I/Ib trial to evaluate its safety. Preclinical biodistribution studies in HepG2 xenograft mouse models of liver cancer demonstrated strong tumor uptake and sustained retention, with minimal accumulation in normal tissues. At multiple timepoints, tumor concentrations were roughly three- to twenty-fold greater than those observed in the kidney.

RYZ811 is being developed as a paired diagnostic imaging agent, utilizing the same peptide binder and chelator as RYZ801 but labeled with Gallium-68 (Ga68) as the imaging radioisotope. Uptake of this proprietary peptide binder has been demonstrated in patients with HCC through investigator-initiated clinical use studies using Ga68.

RYZ801 and RYZ811 are being evaluated in a Phase I/Ib open-label trial as a theranostic pair, with RYZ811 for diagnosis and RYZ801 for therapy, targeting patients with GPC3-positive unresectable HCC.

In January 2025, PeptiDream announced that RayzeBio, a Bristol Myers Company, has initiated a Phase I/Ib clinical trial of RYZ801 and RYZ811.

AZD9793: AstraZeneca

AZD9793 is a first-in-class, trispecific IgG1 monoclonal antibody that functions as a CD8-targeted T-cell Engager (TCE). It simultaneously binds tumor-infiltrating T cells and GPC3-positive tumor cells, forming a bridge that triggers T-cell activation, tumor cell killing, and T-cell proliferation.

By preferentially engaging CD8+ T cells, AZD9793 induces potent cytotoxicity against GPC3-positive HCC cells while limiting CD4+ T-cell activation and reducing cytokine release. Its novel mechanism combines bivalent GPC3 binding, CD8-biased engagement, and low-affinity T-cell receptor interaction to enhance tumor cell killing and lower the risk of Cytokine Release Syndrome (CRS) compared with conventional TCEs.

In June 2025, AstraZeneca presented new data from its oncology pipeline at the American Society of Clinical Oncology (ASCO) Annual Meeting, held from May 30, 2025 to June 3, 2025. A key highlight was RHEA-1, the first-in-human study of AZD9793, a first-in-class CD8-guided TCE developed for patients with GPC3+ advanced or metastatic HCC.

Anti-glypican-3 (GPC3) Targeted Therapies Market Outlook

GPC3 is highly expressed in HCC and select solid tumors, with minimal presence in normal tissues, making it an attractive target for precision oncology. Large-scale genomic and IHC analyses confirm its incidence in HCC, , squamous cell carcinoma in NSCLC, and other malignancies, highlighting opportunities to expand GPC3-targeted therapies beyond liver cancer.

Currently, no anti-GPC3 targeted therapy is approved, underscoring a significant unmet need. Next-generation approaches—including ADCs (ZW251), T-cell engagers (AZD9793, BGB-B2033), engineered CAR-T cells (ECT204, BOXR1030), and radiopharmaceuticals (225Ac-GPC3, RYZ801)—aim to enhance tumor-specific cytotoxicity, improve penetration, and overcome immunosuppressive tumor microenvironments. Challenges remain in patient selection, safety, and manufacturing, but ongoing innovation and biomarker-driven strategies position GPC3-targeted therapies to become a major pillar in precision oncology, with first approvals expected post-2032.

The US market for anti-GPC3 targeted therapies is projected at approximately USD 25 million in 2032 and is expected to grow steadily throughout the forecast period (2025–2040).

The total market size for anti-GPC3 targeted therapies in the EU4 and the UK is projected at approximately USD 20 million in 2033, with strong growth anticipated through 2040.

In 2034, the total market size for anti-GPC3 targeted therapies in Japan is estimated at approximately USD 10 million and is expected to grow significantly over the forecast period (2025–2040).

Anti-glypican-3 (GPC3) Targeted Therapies Uptake

This section focuses on the uptake rate of potential anti-GPC3 targeted therapies expected to be launched in the market during 2020–2040.

Anti-glypican-3 (GPC3) Targeted Therapies Pipeline Development Activities

The report provides insights into different therapeutic candidates in preregistration, Phase II, and early stage molecule. It also analyzes key players involved in developing targeted therapeutics.

The presence of numerous drugs under different stages is expected to generate immense opportunity for anti-GPC3 targeted therapies market growth over the forecasted period.

Pipeline Development Activities

The report covers information on collaborations, acquisitions and mergers, licensing, and patent details for anti-GPC3 targeted therapies emerging therapies.

KOL Views

To keep up with current and future market trends, we take industry experts’ opinions working in the domain through primary research to fill the data gaps and validate our secondary research. Industry experts were contacted for insights on anti-GPC3 targeted therapies evolving treatment landscape, patient reliance on conventional therapies, patient therapy switching acceptability, drug uptake, along challenges related to accessibility.

DelveInsight’s analysts connected with 25+ KOLs to gather insights; however, interviews were conducted with 10+ KOLs in the 7MM. Centers like the University of Texas, US; University of Rome, Italy; Aix-Marseille University, Marseille, France; National Cancer Center, Kashiwa, Japan.

Their opinion helps understand and validate current and emerging therapy treatment patterns or anti-GPC3 targeted therapies market trends. This will support the clients in potential upcoming novel treatments by identifying the overall scenario of the market and the unmet needs.

As per KOL from the US, “BOXR1030, a metabolically enhanced GPC3-targeting CAR T-cell therapy, has shown strong preclinical activity by maintaining function in tumor microenvironment-like conditions and enhancing T-cell proliferation compared to conventional CAR T cells. With GPC3 established as a tumor-restricted target across multiple solid tumors with high unmet need, BOXR1030 is now being advanced into the DUET-01 clinical study to further explore its therapeutic potential.”

As per KOL from the Italy, “GPC3 is a key marker in HCC, detectable in most cases including early-stage tumors. Its expression is associated with aggressive features, poor prognosis, and shorter disease-free survival. Given its early upregulation in malignancy and minimal presence in normal liver, GPC3 is a valuable target for early detection and risk stratification.”

As per KOL from France, “What makes GPC3 particularly attractive is its compatibility with multiple therapeutic approaches. We're seeing success across the spectrum - monoclonal antibodies, antibody-drug conjugates, CAR-T cells, bispecific antibodies, and now radiopharmaceuticals. Each modality leverages GPC3's cell surface expression differently, providing multiple avenues for therapeutic intervention.”

Qualitative Analysis

We perform Qualitative and market Intelligence analysis using various approaches, such as SWOT analysis. In the SWOT analysis, strengths, weaknesses, opportunities, and threats in terms of disease diagnosis, patient awareness, patient burden, competitive landscape, cost-effectiveness, and geographical accessibility of therapies are provided. These pointers are based on the analyst’s discretion and assessment of the patient burden, cost analysis, and existing and evolving treatment landscape.

Market Access and Reimbursement

The report further details country-wise reimbursement and accessibility status, cost-effectiveness assessments, patient assistance initiatives that improve affordability, and insights into coverage under government prescription drug programs.

Scope of the Report

The report covers a segment of key events, an executive summary, and a descriptive overview of anti-GPC3 targeted therapies, explaining their mechanism and therapies (current and emerging).

Comprehensive insight into the competitive landscape, and forecasts, the future growth potential of treatment rate, drug uptake, and drug information have been provided.

Additionally, an all-inclusive account of the current and emerging therapies and the elaborative profiles of late-stage and prominent therapies will impact the current landscape.

A detailed review of the anti-GPC3 targeted therapies market, historical and forecasted market size, market share by therapies, detailed assumptions, and rationale behind our approach is included in the report, covering the 7MM drug outreach.

The report provides an edge while developing business strategies, by understanding trends, through SWOT analysis, expert insights/KOL views, and treatment preferences that help shape and drive the 7MM anti-GPC3 targeted therapies market.

Anti-glypican-3 (GPC3) Targeted Therapies Report Insights

Anti-GPC3 Targeted Therapies Targeted Patient Pool

Anti-GPC3 Targeted Therapies Therapeutic Approaches

Anti-GPC3 Targeted Therapies Pipeline Analysis

Anti-GPC3 Targeted Therapies Market Size and Trends

Existing and Future Market Opportunity

Anti-glypican-3 (GPC3) Targeted Therapies Report Key Strengths

10 years Forecast

The 7MM Coverage

Key Cross Competition

Attribute Analysis

Drugs Uptake and Key Market Forecast Assumptions

Anti-glypican-3 (GPC3) Targeted Therapies Report Assessment

Current Treatment Practices

Unmet Needs

Pipeline Product Profiles

Market Attractiveness

Qualitative Analysis (SWOT)

Key Questions

What was the anti-GPC3 targeted therapies total market size, the market size by therapies, market share (%) distribution in 2032, and what would it look like in 2040? What are the contributing factors for this growth?

Which drug is going to be the largest contributor in 2040?

Which is the most lucrative market for anti-GPC3 targeted therapies?

What are the risks, burdens, and unmet needs of treatment with anti-GPC3 targeted therapies? What will be the growth opportunities across the 7MM for the patient population anti-GPC3 targeted therapies?

What are the key factors hampering the growth of the anti-GPC3 targeted therapies market?

What are the indications for which recent novel therapies and technologies have been developed to overcome the limitations of existing treatments?

What key designations have been granted to the therapies for anti-GPC3 targeted therapies?

Patient acceptability in terms of preferred therapy options as per real-world scenarios?

Reasons to buy

The report will help develop business strategies by understanding the latest trends and changing dynamics driving the anti-GPC3 targeted therapies market.

Understand the existing market opportunities in varying geographies and the growth potential over the coming years.

Identifying strong upcoming players in the market will help devise strategies to help get ahead of competitors.

Detailed analysis and ranking of indication-wise current and emerging therapies under the attribute analysis section to provide visibility around leading indications.

To understand key opinion leaders’ perspectives around the accessibility, acceptability, and compliance-related challenges of existing treatment to overcome barriers in the future.

Detailed insights on the unmet needs of the existing market so that the upcoming players can strengthen their development and launch strategy.

Table of Contents

153 Pages
1. Key Insights
2. Report Introduction
3. Executive Summary
4. Key Events
4.1. Key Transactions and Collaborations
4.2. News Flow
5. Epidemiology and Market Methodology
6. Anti-GPC3 targeted therapies Market Overview at a Glance
6.1. Clinical Landscape (Analysis by Molecule Type, Phase, and Route of Administration [RoA])
6.2. Market Share (%) Distribution of anti-GPC3 targeted therapies in 2032
6.3. Market Share (%) Distribution of anti-GPC3 targeted therapies in 2040
7. Anti-GPC3 Targeted Therapies Background and Overview
7.1. Introduction
7.2. Mechanism of Action
7.3. Potential of Anti-GPC3 Targeted Therapies
7.4. Adverse Reactions to Anti-GPC3 Targeted Therapies
7.5. Emerging Anti-GPC3 Targeted Therapies
7.5.1. Radiotherapy/Radioisotopes
7.5.2. Monoclonal Antibodies
7.5.2.1. ADCs.
7.5.2.2. Trispecific T-cell Engagers
7.5.2.3. Bispecific Antibody
7.5.3. Engineered T-cell Therapies/CAR-T
7.6. Anti-GPC3 Targeted Therapies in Different Indications
7.6.1. HCC.
7.6.1.1. GPC3 in Hepatocellular Carcinoma
7.6.2. Non-small Cell Lung Cancer (NSCLC)
7.6.2.1. GPC3 in NSCLC
7.6.3. Merkel Cell Carcinoma (MCC)
7.6.3.1. GPC3 in MCC
7.6.4. Liposarcoma
7.6.4.1. GPC3 in Liposarcoma
7.6.5. Gastric Cancer
7.6.5.1. GPC3 in Gastric Cancer
7.6.6. Colorectal Cancer
7.6.6.1. GPC3 in Colorectal Cancer
7.6.7. Yolk Sac Tumors
7.6.7.1. GPC3 in Yolk Sac Tumors
7.6.8. Thyroid Cancer
7.6.8.1. GPC3 in Thyroid Cancer
7.6.9. Bladder Cancer
7.6.9.1. GPC3 in Bladder Cancer
7.6.10. Breast Cancer
7.6.10.1. GPC3 in Breast Cancer
8. Epidemiology and Patient Population
8.1. Key Findings
8.2. Assumptions and Rationale: 7MM
8.3. Epidemiology Scenario in the 7MM
8.3.1. Total Incident Cases of Promising Indications for Anti-GPC3 targeting Therapies in the 7MM
8.3.2. GPC3 Expressing Incident Cases of Selected Indications in the 7MM
8.3.3. GPC3 Expressing Advanced/Metastatic Cases in the 7MM
8.3.4. GPC3 Biomarker Positive Advanced/Metastatic Cases in the 7MM
9. Emerging Therapies
9.1. Key Cross Competition
9.2. RYZ801: RayzeBio/Bristol–Myers Squibb
9.2.1. Product Description
9.2.2. Other Developmental Activities
9.2.3. Ongoing Clinical Development Activity
9.2.4. Safety and Efficacy
9.2.5. Analyst Views
9.3. AZD9793: AstraZeneca
9.3.1. Product Description
9.3.2. Other Developmental Activities
9.3.3. Ongoing Clinical Development Activity
9.3.4. Safety and Efficacy
9.3.5. Analyst Views
9.4. BGB-B2033 ± Tislelizumab: BeOne Medicine
9.4.1. Product Description
9.4.2. Ongoing Clinical Development Activity
9.4.3. Safety and Efficacy
9.4.4. Analyst Views
9.5. ECT204: Eureka Therapeutics
9.5.1. Product Description
9.5.2. Other Developmental Activities
9.5.3. Ongoing Clinical Development Activity
9.5.4. Safety and Efficacy
9.5.5. Analyst Views
9.6. BOXR1030: Sotio Biotech
9.6.1. Product Description
9.6.2. Other Developmental Activities
9.6.3. Ongoing Clinical Development Activity
9.6.4. Safety and Efficacy
9.6.5. Analyst Views
9.7. ZW251: Zymeworks
9.7.1. Product Description
9.7.2. Other Developmental Activities
9.7.3. Ongoing Clinical Development Activity
9.7.4. Safety and Efficacy
9.7.5. Analyst Views
9.8. 225Ac-GPC3 (BAY 3547926): Bayer
9.8.1. Product Description
9.8.2. Other Developmental Activities
9.8.3. Ongoing Clinical Development Activity
9.8.4. Safety and Efficacy
9.8.5. Analyst Views
10. Anti-GPC3 targeted Therapies: Seven Major Market Analysis
10.1. Key Findings
10.2. Market Outlook
10.3. Conjoint Analysis
10.4. Key Market Forecast Assumptions
10.4.1. Cost Assumptions
10.4.2. Launch Year Assumptions
10.5. Total Market Size by Country in the 7MM
10.6. Total Market Size by Therapies in the 7MM
10.7. The United States Market Size
10.7.1. Total Market Size of Anti-GPC3 targeted Therapies in the United States
10.7.2. Total Market Size by Therapies in the United States
10.8. EU4 and the UK Market Size
10.8.1. Total Market Size of Anti-GPC3 targeted Therapies in EU4 and the UK
10.8.2. Total Market Size by Therapies in EU4 and the UK
10.9. Japan Market Size
10.9.1. Total Market Size of Anti-GPC3 targeted Therapies in Japan
10.9.2. Total Market Size by Therapies in Japan
11. Unmet Needs
12. SWOT Analysis
13. KOL Views
14. Market Access and Reimbursement
14.1. The United States
14.2. In EU4 and the UK
14.2.1. Germany.
14.2.2. France.
14.2.3. Italy.
14.2.4. Spain.
14.2.5. United Kingdom
14.3. Japan.
14.4. Summary and Comparison of Market Access and Pricing Policy Developments in 2025
15. Appendix.
15.1. Bibliography
15.2. Report Methodology
16. DelveInsight Capabilities
17. Disclaimer
18. About DelveInsight
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