Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors, Potential Market Opportunity & Clinical Pipeline Insights, 2019

  • OI-101
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  • Published date: Apr, 2019
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  • Life Sciences & Healthcare
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  • 0 Pages

Fibroblast growth factor receptor 4 (FGFR4) is a tyrosine kinase receptor for FGFs and is involved in diverse cellular processes like the regulation of cell proliferation, differentiation, migration, metabolism, and bile acid biosynthesis. FGF exerts its actions through four of these: FGFR1, FGFR2, FGFR3, and FGFR4. Compared to the other three FGFR family members, the signaling pathways and mechanisms of FGFR4 involved in cancer development are less characterized. The fibroblast growth factor (FGF)-FGFR signaling system has been implicated in diverse biological processes during embryo development, wound healing, and angiogenesis. Recently, elevated FGFR4 has been correlated with cancer development and progression that makes it an attractive target for developing novel and effective anticancer therapeutics. More efforts have been focusing on developing selective inhibitors for targeting FGFR4, which will show particular promise as an adjunct treatment or an anticancer monotherapy.

Market Overview

As a promising target, FGFR4 is attracting intensive pharmaceutical and academic attention for developing novel target therapy against cancers driven by FGFR4. The three strategies that have been developed to target FGFR4 include neutral antibodies, antisense oligonucleotides, and small molecule inhibitors. Not surprisingly, multi-targeted tyrosine kinase inhibitors (mTKIs) can be used to inactivate FGFR4 by disrupting ATP binding in its TK domains. The anticancer activity of many mTKIs, including lenvatinib and ponatinib, has been tested on FGFR-driven solid tumors in animals or in clinical trials. However, the limited selective activity of mTKIs on FGFRs induces less efficiency and increases side effects in these treatments. Therefore, pan-FGFR inhibitors are developed and are being evaluated in clinical trials to treat cancers driven by abnormal FGFR pathways. Other inhibitors in this category include ATP-competitive inhibitors NVP-BGJ398 and AZD4547, ATP-binding pocket inhibitor LY2874455, and FGFRs-FIIN-3. At present, FGFR blockers, such as multi-kinase inhibitors, specific FGFR inhibitors, and FGF ligand traps are being tested in clinical trials.

Small molecule inhibitors of FGFR tyrosine kinase, selective or nonselective, are under clinical evaluation, although mainly in the early stages of trials. Efforts are being made for increasing the selectivity to the intracellular ATP-binding domain of the receptor to minimize the toxicity. AZD4547 is another TKI, which has shown strong activity against FGFR-3, yet weaker activity against FGFR4. The development of non-selective TKI-targeting FGFRs recently shown to be very successful in preclinical studies. Some of these inhibitors have known to be passed the phase I trial showing encouraging results in terms of safety and tolerability. Less number of studies is found to be in clinical trials. The drugs that are in clinical trails include Rogaratinib by Bayer, Ensartinib by Betta Pharmaceuticals, Roblitinib (FGF401) by Novartis, Lenvatinib by Esai Co Ltd, Nintedanib by Boehringer Ingelheim, FGF19 by Genentech, and ponatinib hydrochloride by Ariad pharmaceuticals for malignant neoplasm. BLU-554, a potent fibroblast growth factor receptor 4 (FGFR4) inhibitor is a new drug that is approved by Neil Bifulco, Lucian V. Dipietro, Brian L. Hodous, Chandrashekar V. MIDITURU.

A long series of evidence is said to be pointing towards the expectation that deregulated FGFRs can work as driving oncogenes in several types of tumor. The FGFRs/FGFs (Fibroblast growth factor receptors / Fibroblast growth factors) axis is offering interesting molecular targets to be pursued in clinical development. FGFR is an already established breast cancer oncogenic driver involved in various mechanisms leading to the formation of vessels, tumor growth and avoidance of apoptosis. The therapeutic strategies have been implemented in order to inhibit FGFRs. In fact, several anti-FGF/FGFR therapies have been tested at phase I and II clinical trials.

Key Developments

  • In Jan 2019, CStone Pharmaceuticals has received approval from China’s National Medical Products Administration (NMPA) for its clinical trial application (CTA) to begin a Phase I clinical trial of BLU-554 (CS3008) for the treatment of hepatocellular carcinoma (HCC).

  • In Jan 2019, Boehringer Ingelheim plans a phase III trial of Nintedanib for treating interstitial lung disease.


This Pipeline research report segments the Fibroblast Growth Factor Receptor inhibitors pipeline on the basis of therapies employed (combination therapy, and monotherapy + combination therapy), therapeutic modality (small molecules, and unknown), RoA (oral and unknown), drugs under development (discovery, pre-clinical, phase I, phase I/II, phase II, and phase III), and recruitment status (recruiting, active not recruiting, enrolling by invitation, and undisclosed).

The Key players analyzed in Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors pipeline include Ionis Pharmaceutical, H3 BiomedicineInc, Daiichi SankyoInc, Blueprint MedicinesCorp., IncyteCorporation, Genosco, AstraZeneca, and others.

Report Description: The report covers in-depth analysis on Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors Pipeline Insights, 2019. The report assesses the Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors pipeline by stage of development (early development, pre-clinical, clinical and in approval), by application (pancreatic cancer, colorectal cancer, melanoma, breast cancer, lung diseases, and others). In addition, the report includes key insights on other development activities, including (but not limited to) – licensing (In and Out), collaborations, acquisitions, reimbursement, patent, and regulatory designations.

The report includes in-depth company profiles of key players in Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors Pipeline. The company profile includes key information on overview, financial highlights, product portfolio, business strategies, and key recent developments.

The report highlights information on emerging companies with potentially disruptive technologies and new market entrants.


  • Provides detailed analysis of the product pipeline structure along with forecast of the various segments and sub-segments of the Fibroblast Growth Factor Receptor 4 (FGFR4) InhibitorsPipeline.

  • Provides a comparative analysis of key marketed products and pipeline Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors products.

  • Provides key information on players involved on the Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors Pipeline.

  • Provides a complete overview of market segments and the regional outlook of Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors Pipeline.

  • Provides in-depth coverage of key news related toFibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors Pipeline, including major mergers and acquisitions and product development updates such as clinical trial progression updates and regulatory updates

Our research works on a holistic 360° approach to deliver high quality, validated and reliable information in our market reports. The Market estimation and forecasting involve the following steps:

  • Data Collation (Primary & Secondary)

  • In-house Estimation (Based on proprietary databases and Models)

  • Market Triangulation

  • Forecasting

  • Market-related information is assembled from both primary and secondary sources. 

  • Primary sources involved participants from all global stakeholders such as experts from several related industries and suppliers that have been interviewed to obtain and verify critical information as well as to assess prospects of the market. The participants included are CXOs, VPs, and managers. Plus, our in-house industry experts having decades of industry experience contribute their consulting and advisory services. 

  • Secondary sources include public sources such as regulatory frameworks, government IT spending, government demographic indicators, industry association statistics, and company publications annual reports press releases along with paid sources such as Factiva, OneSource, Bloomberg among others. 

  • Top-down and bottom-up approaches: The overall market size was used in the top-down approach to estimate the sizes of other individual submarkets (mentioned in the market segmentation by product, type of manufacturing, and disease) through percentage splits from secondary and primary research. The bottom-up approach was also implemented (wherever applicable) for data extracted from secondary research to validate the market segment revenues obtained. 


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