VEGFR-1 Inhibitors Market: Competitive Landscape, Pipeline, and Market Analysis 2024

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Vascular endothelial growth factor receptor 1 is a protein that in humans is encoded by the FLT1 gene. EGFR-1 inhibitors are drugs that target and inhibit the activity of the vascular endothelial growth factor receptor 1 (VEGFR-1), a protein that plays a crucial role in angiogenesis, or the formation of new blood vessels. These inhibitors are used primarily in the treatment of various cancers and certain ocular diseases like age-related macular degeneration (AMD). The mechanism of action of VEGFR-1 inhibitors involves blocking the activation of VEGFR-1 by binding to its receptor site and preventing the binding of its ligands, such as vascular endothelial growth factors (VEGFs). This interference disrupts the signaling pathway that triggers angiogenesis, which is important for tumor growth and the development of abnormal blood vessels in diseases like AMD. When VEGFR-1 is activated by binding to VEGF, it initiates a signaling cascade inside the cell, leading to the activation of various downstream molecules involved in angiogenesis.

By inhibiting VEGFR-1, the inhibitors prevent this cascade from occurring, thereby reducing the formation of new blood vessels. VEGFR-1 Inhibitors have a predominant role in treating leukemia, sarcoma, lymphoma, kidney disorders, respiratory diseases, breast diseases, and digestive system diseases to name a few. According to World Cancer Research Fund 2020, There were an estimated 18.1 million cancer cases around the world and 4,74,519 new cases of Leukaemia in 2020. The global cancer burden is expected to be 28.4 million cases in 2040, a 47% rise from 2020. The launch of newer products by the market players significantly enhances the revenue of the VEGFR-1 Inhibitors market over the forecast years. Moreover, the development of novel molecules by many market players is coming up to overcome challenges in therapy. For instance, Mirati’s Sitravatinib (MGCD516) for the treatment of lung cancer is under the various stages of clinical studies.

Key Market Developments:

  • In September 2021, FDA approved Cabometyx (Cabozantinib), for adult and pediatric patients 12 years of age and older with locally advanced or metastatic differentiated thyroid cancer.
  • In April 2021, GlaxoSmithKline agreed to sell its royalty stake to Royalty Pharma in two Cabozantinib drugs under the trade names Cabometyx and Cometriq.

Approved Drug Molecules for VEGFR-1 Inhibitors along with the Brand Names:

  •  Lenvima (Lenvatinib)
  •  Fotivda (Tivozanib)
  •  Votrient (Pazopanib)
  •  Cabometyx (Cabozantinib Tablet)
  •  Cometriq (Cabozantinib Capsule)
  •  Inlyta (Axitinib) And Others

Drugs under the Pipeline for VEGFR-1 Inhibitors:

  •  Sitravatinib (MGCD516)
  •  Retevmo (Selpercatinib)
  •  Lucitanib (E 3810)
  •  Aplidin (Plitidepsin)
  •  Chiauranib (CS 2164)
  •  CEP-11981
  •  HB-002
  •  3D011
  •  HB0025
  •  SKI-G-801
  •  Tivozanib Reformulated (KHK4951)

Clinical Activity and Developments of VEGFR-1 Inhibitors:

Till July 2023, more than 20 companies have approximately 13 molecules targeting the many cancers. For these molecules, more than 450 clinical trials are being conducted; most are in phase-2 and phase-3 clinical trials by players across the globe. For instance,

  • In August 2018, FDA approved Eisai’s drug Lenvima (Lenvatinib) for expanded indication based on REFLECT, a randomized, multicenter, open-label trial to compare the efficacy and safety of Lenvatinib versus Sorafenib as a first-line systemic treatment in patients (N=954) with unresectable hepatocellular carcinoma (HCC).
  • In March 2021, FDA approved AVEO Oncolog’s drug Fotivda (Tivozanib) based on TIVO-3, a randomized (1:1), open-label, multicenter trial comparing Fotivda to Sorafenib in relapsed or refractory advanced RCC following two or more prior systemic therapies.

Molecule Name

Number of Studies

Sitravatinib (MGCD516)


Retevmo (Selpercatinib)


Lucitanib (E 3810)


Chiauranib (CS 2164)





Target Indication Analysis of VEGFR-1 Inhibitors

The molecules such as Lenvima (Lenvatinib) were developed by Eisai for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer, in combination with everolimus for the treatment of patients with advanced renal cell carcinoma (RCC) following one prior anti-angiogenic therapy, and for the first-line treatment of patients with unresectable hepatocellular carcinoma (HCC). Lenvima is supplied as capsules for oral administration. Moreover, Cabometyx (Cabozantinib tablet) for the treatment of renal cell carcinoma, and  Cometriq (cabozantinib capsule) for the treatment of metastatic medullary thyroid cancer developed by  Exelixis.

Frequently Asked Questions

Lenvima (Lenvatinib), Fotivda (Tivozanib), Cabometyx (cabozantinib tablet), and Cometriq (cabozantinib capsule) is the few approved VEGFR-1 Inhibitors.

Global sales for cabozantinib by Exelixis and its collaboration partners Ipsen Pharma and Takeda in the FY2022 was US$ 1.9 billion.

Major market players include Eisai, Merck (MSD), Advenchen, and Sino Biopharm are a few leading market players.

Major Indications for VEGFR-1 Inhibitors are leukemia, sarcoma, lymphoma, kidney disorders, respiratory diseases, breast diseases, and digestive system diseases

There are around 11 molecules that are in the Phase-1/Phase-2 clinical development for VEGFR-1 Inhibitors.

Key Features of the Reports

  • The report provides granular level information about the market size, regional market share, historic market (2019-2023), and forecast (2024-2030)
  • The report covers in-detail insights about the competitor’s overview, company share analysis, key market developments, and their key strategies
  • The report outlines drivers, restraints, unmet needs, and trends that are currently affecting the market
  • The report tracks recent innovations, key developments, and start-up details that are actively working in the market
  • The report provides a plethora of information about market entry strategies, regulatory framework, and reimbursement scenario
  • Eisai
  •  Merck (MSD)
  •  Advenchen
  •  Sino Biopharm
  •  Novartis
  •  Takeda
  •  Exelixis
  •  Ipsen
  •  Pfizer
  •  Hutchmed
  •  Mirati
  •  Eli Lilly
  •  Clovis
  •  Servier
  •  PharmaMar
  •  Roche
  •  Chipscreen
  •  Teva

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