VEGFR-2 Inhibitors Market Set to Transform Oncology Treatment Landscape by 2034 | DelveInsight

The VEGFR-2 inhibitors market is gaining significant traction, driven by the rising global burden of cancer and age-associated conditions such as macular degeneration, especially among the elderly. Progress in angiogenesis research has reinforced the clinical importance of VEGFR-2 as a therapeutic target, leading to increased utilization across various cancers, including gastric, colorectal, and biliary tract malignancies.

LAS VEGAS, Aug. 21, 2025 /PRNewswire/ -- DelveInsight's VEGFR-2 Inhibitors Market Size, Target Population, Competitive Landscape & Market Forecast report includes a comprehensive understanding of current treatment practices, addressable patient population, which includes top indications such as Metastatic colorectal cancer (mCRC), Renal cell carcinoma (RCC), Differentiated thyroid cancer (DTC), Medullary thyroid cancer (MTC), Hepatocellular carcinoma (HCC), Endometrial carcinoma (EC), Metastatic gastric or gastroesophageal junction adenocarcinoma (mGEC), Metastatic non-small cell lung cancer (mNSCLC), Gastric cancer, Adrenocortical carcinoma (ACC), Colorectal cancer (CRC), Unresectable hepatocellular carcinoma (uHCC), Non-clear cell renal cell carcinoma (nccRCC), Head and neck squamous cell carcinoma (HNSCC), Biliary tract cancer (BTC), Squamous cell carcinoma of the head and neck (SCCHN), Various solid tumors, and others. The selected indications are based on approved therapies and ongoing pipeline activity. The report also provides insights into the emerging VEGFR-2 inhibitors, market share of individual therapies, and current and forecasted market size from 2020 to 2034, segmented into 7MM.

Key Takeaways from the VEGFR-2 Inhibitors Market Report

• As per DelveInsight's analysis, the total market size of VEGFR-2 inhibitors in the 7MM is expected to surge significantly by 2034.
• The report provides the total potential number of patients in the indications, such as Metastatic colorectal cancer (mCRC), Renal cell carcinoma (RCC), Differentiated thyroid cancer (DTC), Medullary thyroid cancer (MTC), Hepatocellular carcinoma (HCC), Endometrial carcinoma (EC), Metastatic gastric or gastroesophageal junction adenocarcinoma (mGEC), Metastatic non-small cell lung cancer (mNSCLC), Gastric cancer, Adrenocortical carcinoma (ACC), Colorectal cancer (CRC), Unresectable hepatocellular carcinoma (uHCC), Non-clear cell renal cell carcinoma (nccRCC), Head and neck squamous cell carcinoma (HNSCC), Biliary tract cancer (BTC), Squamous cell carcinoma of the head and neck (SCCHN), Various solid tumors, and others.
• Leading VEGFR-2 inhibitor companies, such as Elevar Therapeutics, Exelixis, Tiumbio, Merck, and others, are developing novel VEGFR-2 inhibitors that can be available in the VEGFR-2 inhibitors market in the coming years. 
• Some of the key VEGFR-2 inhibitors in the pipeline include Rivoceranib, Zanzalintinib (XL092), TU2218, and others.
• In January 2025, Elevar Therapeutics announced the results of a post-hoc analysis from the international CARES-310 study, which evaluated camrelizumab plus rivoceranib versus sorafenib as a first-line treatment for patients with uHCC of viral and non-viral etiology.

Discover which indication is expected to grab the major VEGFR-2 inhibitors market share @ VEGFR-2 Inhibitors Market Report

VEGFR-2 Inhibitors Market Dynamics

The VEGFR-2 inhibitors market has gained strong traction over the past decade due to the growing prevalence of cancer and rising adoption of targeted therapies. VEGFR-2 plays a critical role in tumor angiogenesis, and blocking this pathway has proven effective in slowing tumor growth. Approved drugs like fruquintinib, tivozanib, lenvatinib, ramucirumab, and cabozantinib have demonstrated significant clinical benefits, driving demand for VEGFR-2 inhibitors globally. The increasing number of cancer patients, coupled with a shift toward precision medicine, is accelerating market growth.

Pharmaceutical companies are heavily investing in R&D to develop next-generation VEGFR-2 inhibitors with improved efficacy and safety profiles. Several candidates are in clinical trials, either as monotherapies or in combination with immune checkpoint inhibitors and other targeted agents. These combination approaches are expected to further expand the use of VEGFR-2 inhibitors across multiple tumor types. Moreover, strategic collaborations and licensing agreements among biotech and pharma firms are fostering innovation and expanding product pipelines.

However, the market faces challenges such as high therapy costs, development of drug resistance, and adverse effects like hypertension and proteinuria associated with VEGFR-2 inhibition. Reimbursement hurdles, especially in emerging markets, may also limit patient access. Additionally, the presence of alternative anti-angiogenic therapies and competition from multi-targeted kinase inhibitors could restrain market growth.

Despite these challenges, the long-term outlook remains positive. The emergence of biomarkers to predict response, personalized therapy approaches, and expansion into additional indications such as gastric, hepatocellular, and renal cancers are expected to fuel future demand. Regulatory approvals of new molecules and label expansions of existing VEGFR-2 inhibitors will further propel the market. Overall, the VEGFR-2 inhibitors segment is expected to remain a vital and growing component of the oncology therapeutics landscape.

VEGFR-2 Inhibitors Treatment Market 

Several VEGFR-2 inhibitors have been approved for various oncology indications, including FRUZAQLA (fruquintinib), FOTIVDA (tivozanib), LENVIMA (lenvatinib), CYRAMZA (ramucirumab), and COMETRIQ (cabozantinib), among others.

FRUZAQLA is an oral, selective inhibitor of VEGFR-1, -2, and -3, with IC50 values of 33, 35, and 0.5 nM, respectively. Preclinical studies showed that it effectively inhibited VEGF-driven endothelial proliferation, tube formation, and VEGFR-2 signaling, resulting in significant tumor suppression in colon cancer xenograft models. It is clinically approved for adults with metastatic colorectal cancer (mCRC) who have previously received fluoropyrimidine-, oxaliplatin-, and irinotecan-based regimens, anti-VEGF treatment, and, if RAS wild-type, anti-EGFR therapy. FRUZAQLA has received regulatory approval in major regions: by the US FDA in November 2023, the EMA in June 2024, and in Japan in September 2024.

In November 2024, HUTCHMED announced it would receive a milestone payment following pricing approval and commercial launch of FRUZAQLA 1mg/5mg capsules in Japan, through its partner Takeda, for previously treated mCRC. Additionally, in October 2024, HUTCHMED disclosed it would receive a USD 20 million milestone payment from Takeda after FRUZAQLA sales for mCRC exceeded USD 200 million.

FOTIVDA is a tyrosine kinase inhibitor targeting VEGFR-1/2/3, c-kit, and PDGFRβ, reducing angiogenesis, vascular permeability, and tumor growth in preclinical models, particularly renal cell carcinoma (RCC). It is approved for adults with relapsed or refractory advanced RCC after at least two prior systemic therapies. FOTIVDA received US FDA approval in March 2021 for this use, following earlier EU approval by the European Commission in August 2017.

LENVIMA is a multi-kinase inhibitor targeting VEGFR1–3, FGFR1–4, PDGFRA, KIT, and RET, disrupting angiogenesis and tumor proliferation pathways. It demonstrates anti-proliferative activity in FGFR-driven hepatocellular carcinoma (HCC) models and enhances immune response when combined with PD-1 inhibitors. Preclinically, it also shows synergy with everolimus, enhancing antiangiogenic and antitumor effects. Clinically, LENVIMA is approved for differentiated thyroid cancer (DTC), advanced RCC (as monotherapy or with pembrolizumab/everolimus), unresectable HCC, and advanced endometrial carcinoma in select patients. It was first approved by the US FDA in February 2015, followed by approvals in Japan in March 2015 and in Europe in May 2015.

Learn more about the VEGFR-2 inhibitors @ VEGFR-2 Inhibitors Analysis

Key Emerging VEGFR-2 Inhibitors and Companies

A rich late-stage pipeline, featuring candidates like Rivoceranib (Elevar Therapeutics), Zanzalintinib (Exelixis), and TU2218 (Tiumbio/Merck), among others, highlights sustained innovation and intensifying competition, positioning the market for continued growth across both oncology and ophthalmology sectors.

Rivoceranib is a highly selective VEGFR-2 inhibitor with minimal activity against other tyrosine kinases, offering a focused mechanism of action. It is being studied both as a standalone therapy and in combination with chemotherapy and immunotherapy. Ongoing or planned clinical trials are evaluating it in various cancers, such as hepatocellular carcinoma (paired with camrelizumab), adenoid cystic carcinoma, colorectal cancer (with LONSURF), and gastric cancer.

The drug has received Orphan Drug Designation (ODD) for gastric cancer (in both the US and EU), adenoid cystic carcinoma (in the US), and hepatocellular carcinoma (in the US). The US FDA has accepted a resubmitted New Drug Application (NDA) for rivoceranib in combination with camrelizumab as a first-line systemic treatment for unresectable or metastatic hepatocellular carcinoma (uHCC). A PDUFA date has been set for March 2025, although the therapy has not yet been approved.

Rivoceranib is currently in Phase III trials for third-/fourth-line treatment of gastric cancer, in Phase II trials for adenoid cystic carcinoma and third-line colorectal cancer (with LONSURF), as well as exploratory studies for second-line gastric cancer (with paclitaxel) and in multiple solid tumors (with OPDIVO).

In January 2025, Elevar Therapeutics shared results from a post-hoc analysis of the global CARES-310 study comparing camrelizumab plus rivoceranib to sorafenib as first-line therapy for viral and non-viral uHCC. These findings were presented in a poster at the 2025 ASCO GI Symposium.

Zanzalintinib is a third-generation oral tyrosine kinase inhibitor that targets VEGF receptors, MET, AXL, and MER, kinases involved in tumor progression, angiogenesis, metastasis, and resistance to therapies, including immune checkpoint inhibitors.

Exelixis has partnered with multiple pharma companies to evaluate zanzalintinib in combination regimens, including with atezolizumab (Roche), nivolumab, ipilimumab, relatlimab (BMS), and pembrolizumab and belzutifan (Merck). These collaborations are part of a broad development strategy to assess their safety and efficacy alongside established cancer treatments.

The drug is being studied in several trials: Phase III trials in colorectal cancer (STELLAR-303) and non-clear cell renal cell carcinoma (STELLAR-304), a Phase II/III study in squamous cell carcinoma of the head and neck (STELLAR-305), and two Phase II studies (STELLAR-001 and STELLAR-002) in multiple solid tumors.

A Phase III pivotal trial comparing zanzalintinib to everolimus as a first-line oral therapy in advanced neuroendocrine tumors (NET), regardless of primary site, is expected to begin in the first half of 2025.

In January 2025, Exelixis reported data from an expansion cohort in the Phase Ib/II STELLAR-001 trial examining zanzalintinib alone or with atezolizumab (TECENTRIQ) in previously treated metastatic CRC. These results, presented at ASCO GI 2025, support the launch of STELLAR-303, studying zanzalintinib plus atezolizumab vs regorafenib in metastatic CRC, with results expected in the latter half of 2025 depending on trial events.

TU2218 is an innovative oral immuno-oncology drug that dual inhibits TGFR1 and VEGFR2, simultaneously targeting TGF-β and VEGF signaling pathways, which are known to suppress immune checkpoint inhibitor (ICI) effectiveness. As a potential first-in-class therapy, TU2218 is designed to enhance responses to ICIs like PD-1 and CTLA-4 inhibitors and address unmet needs in cancer immunotherapy.

In October 2024, TiumBio began dosing patients in a Phase II clinical trial evaluating TU2218 in combination with KEYTRUDA for head and neck squamous cell carcinoma (HNSCC), biliary tract cancer (BTC), and colorectal cancer (CRC). This Phase II study builds upon Phase Ia/Ib findings that established safety, pharmacokinetic, and pharmacodynamic profiles in patients with advanced solid tumors and helped determine dosing.

The anticipated launch of these emerging therapies are poised to transform the VEGFR-2 inhibitors market landscape in the coming years. As these cutting-edge therapies continue to mature and gain regulatory approval, they are expected to reshape the VEGFR-2 inhibitors market landscape, offering new standards of care and unlocking opportunities for medical innovation and economic growth.

To know more about VEGFR-2 inhibitors clinical trials, visit @ VEGFR-2 Inhibitors Treatment 

VEGFR-2 Inhibitors Overview

Abnormal blood vessel formation is essential for tumors to grow and spread, with VEGF signaling being a major driver of this process. VEGF family members, VEGF-A, VEGF-B, VEGF-C, VEGF-D, and PlGF, bind selectively to receptors VEGFR-1, VEGFR-2, and VEGFR-3, each associated with different types of endothelial cells. Although these receptors share structural similarities, they differ in how they are activated and the signaling pathways they trigger. Importantly, VEGFR-2 is the primary receptor involved in angiogenesis in vascular endothelial cells, making it a critical focus for anti-cancer strategies that aim to block the tumor's blood supply.

Due to its pivotal role in tumor angiogenesis, VEGFR-2 is a prime target in oncology. Inhibiting VEGFR-2 selectively has shown encouraging results in reducing tumor blood vessel formation and slowing disease progression. However, many available inhibitors lack specificity, causing off-target effects that can reduce their clinical benefit. Current research efforts are focused on designing more selective VEGFR-2 inhibitors to limit adverse effects and enhance treatment outcomes. VEGFR-2 is overexpressed in numerous cancers, such as breast, cervical, non-small cell lung, liver, and renal cancers, underscoring its relevance across various tumor types.

VEGFR-2 Inhibitors Epidemiology Segmentation

The VEGFR-2 inhibitors market report proffers epidemiological analysis for the study period 2020–2034 in the 7MM, segmented into:

• Total Cases in Selected Indications for VEGFR-2 Inhibitor
• Total Eligible Patient Pool in Selected Indications for VEGFR-2 Inhibitor
• Total Treated Cases in Selected Indications for VEGFR-2 Inhibitor

Scope of the VEGFR-2 Inhibitors Market Report

• VEGFR-2 Inhibitors Therapeutic Assessment: VEGFR-2 Inhibitors' current marketed and emerging therapies
• VEGFR-2 Inhibitors Market Dynamics: Conjoint Analysis of Emerging VEGFR-2 Inhibitor Drugs
• Competitive Intelligence Analysis: SWOT analysis and Market entry strategies
• Unmet Needs, KOL's views, Analyst's views, VEGFR-2 Inhibitors Market Access and Reimbursement

Discover more about VEGFR-2 inhibitors in development @ VEGFR-2 Inhibitors Clinical Trials

Table of Contents

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