A comprehensive overview of selective and novel fibroblast growth factor receptor inhibitors as a potential anticancer modality
The arrival of comprehensive genome sequencing has accelerated the understanding of genetically aberrant advanced cancers and target identification for possible cancer treatment. Fibroblast growth factor receptor (FGFR) gene alterations are frequent findings in various rare and advanced cancers refr...
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| Format: | Article |
| Language: | English |
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Sciendo
2024-03-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | https://doi.org/10.2478/acph-2024-0005 |
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| author | Jain Nem Kumar Tailang Mukul Thangavel Neelaveni Makeen Hafiz A. Albratty Mohammed Najmi Asim Alhazmi Hassan Ahmad Zoghebi Khalid Alagusundaram Muthumanickam Jain Hemant Kumar Chandrasekaran Balakumar |
| author_facet | Jain Nem Kumar Tailang Mukul Thangavel Neelaveni Makeen Hafiz A. Albratty Mohammed Najmi Asim Alhazmi Hassan Ahmad Zoghebi Khalid Alagusundaram Muthumanickam Jain Hemant Kumar Chandrasekaran Balakumar |
| author_sort | Jain Nem Kumar |
| collection | DOAJ |
| description | The arrival of comprehensive genome sequencing has accelerated the understanding of genetically aberrant advanced cancers and target identification for possible cancer treatment. Fibroblast growth factor receptor (FGFR) gene alterations are frequent findings in various rare and advanced cancers refractive to mainstay chemo-therapy or surgical interventions. Several FGFR inhibitors have been developed for addressing these genetically altered FGFR-harboring malignancies, and some have performed well in clinical trials. In contrast, others are still being investigated in different phases of clinical trials. FDA has approved four anticancer agents such as erdafitinib, pemigatinib, infigratinib, and futibatinib, for clinical use in oncogenic FGFR-driven malignancies. These include cholangiocarcinoma, urothelial carcinoma, and myeloid/lymphoid malignancies. Pemigatinib is the only FGFR inhibitor globally approved (USA, EU, and Japan) and available as a targeted therapy for two types of cancer, including FGFR2 fusion or other rearrangements harboring cholangiocarcinoma and relapsed/refractory myeloid/lymphoid neoplasms with FGFR1 rearrangements. Myeloid/lymphoid neoplasm is the latest area of application added to the therapeutic armamentarium of FGFR inhibitors. Furthermore, futibatinib is the first-in-class covalent or irreversible pan-FGFR inhibitor that has received FDA approval for locally advanced or metastatic intrahepatic cholangiocarcinoma harboring FGFR2 gene aberrations. This review highlights the current clinical progress concerning the safety and efficacy of all the approved FGFR-TKIs (tyrosine kinase inhibitors) and their ongoing investigations in clinical trials for other oncogenic FGFR-driven malignancies. |
| format | Article |
| id | doaj-art-7b89aa80b68548bb8237cfaba3aee2c1 |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2024-03-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Acta Pharmaceutica |
| spelling | doaj-art-7b89aa80b68548bb8237cfaba3aee2c12025-02-02T21:44:37ZengSciendoActa Pharmaceutica1846-95582024-03-0174113610.2478/acph-2024-0005A comprehensive overview of selective and novel fibroblast growth factor receptor inhibitors as a potential anticancer modalityJain Nem Kumar0Tailang Mukul1Thangavel Neelaveni2Makeen Hafiz A.3Albratty Mohammed4Najmi Asim5Alhazmi Hassan Ahmad6Zoghebi Khalid7Alagusundaram Muthumanickam8Jain Hemant Kumar9Chandrasekaran Balakumar10School of Pharmacy, ITM University Gwalior474001, Madhya Pradesh, IndiaSchool of Studies in Pharmaceutical Sciences, Jiwaji University Gwalior474001, Madhya Pradesh, IndiaDepartment of Pharmaceutical Chemistry and Pharmacognosy, College of Pharmacy, Jazan University, P.O. Box 114, Jazan 82912, Saudi ArabiaPharmacy Practice Research Unit Department of Clinical Pharmacy, College of Pharmacy, Jazan University, P.O. Box 114, Jazan 82912, Saudi ArabiaDepartment of Pharmaceutical Chemistry and Pharmacognosy, College of Pharmacy, Jazan University, P.O. Box 114, Jazan 82912, Saudi ArabiaDepartment of Pharmaceutical Chemistry and Pharmacognosy, College of Pharmacy, Jazan University, P.O. Box 114, Jazan 82912, Saudi ArabiaDepartment of Pharmaceutical Chemistry and Pharmacognosy, College of Pharmacy, Jazan University, P.O. Box 114, Jazan 82912, Saudi ArabiaDepartment of Pharmaceutical Chemistry and Pharmacognosy, College of Pharmacy, Jazan University, P.O. Box 114, Jazan 82912, Saudi ArabiaSchool of Pharmacy, ITM University Gwalior474001, Madhya Pradesh, IndiaDepartment of General Medicine Government Medical CollegeDatia475661, Madhya Pradesh, IndiaFaculty of Pharmacy, Philadelphia UniversityP.O. Box 1, Amman19392JordanThe arrival of comprehensive genome sequencing has accelerated the understanding of genetically aberrant advanced cancers and target identification for possible cancer treatment. Fibroblast growth factor receptor (FGFR) gene alterations are frequent findings in various rare and advanced cancers refractive to mainstay chemo-therapy or surgical interventions. Several FGFR inhibitors have been developed for addressing these genetically altered FGFR-harboring malignancies, and some have performed well in clinical trials. In contrast, others are still being investigated in different phases of clinical trials. FDA has approved four anticancer agents such as erdafitinib, pemigatinib, infigratinib, and futibatinib, for clinical use in oncogenic FGFR-driven malignancies. These include cholangiocarcinoma, urothelial carcinoma, and myeloid/lymphoid malignancies. Pemigatinib is the only FGFR inhibitor globally approved (USA, EU, and Japan) and available as a targeted therapy for two types of cancer, including FGFR2 fusion or other rearrangements harboring cholangiocarcinoma and relapsed/refractory myeloid/lymphoid neoplasms with FGFR1 rearrangements. Myeloid/lymphoid neoplasm is the latest area of application added to the therapeutic armamentarium of FGFR inhibitors. Furthermore, futibatinib is the first-in-class covalent or irreversible pan-FGFR inhibitor that has received FDA approval for locally advanced or metastatic intrahepatic cholangiocarcinoma harboring FGFR2 gene aberrations. This review highlights the current clinical progress concerning the safety and efficacy of all the approved FGFR-TKIs (tyrosine kinase inhibitors) and their ongoing investigations in clinical trials for other oncogenic FGFR-driven malignancies.https://doi.org/10.2478/acph-2024-0005fgfrtyrosine kinase inhibitorsfda approvalerdafitinibinfigratinibpemigatinibfutibatinib |
| spellingShingle | Jain Nem Kumar Tailang Mukul Thangavel Neelaveni Makeen Hafiz A. Albratty Mohammed Najmi Asim Alhazmi Hassan Ahmad Zoghebi Khalid Alagusundaram Muthumanickam Jain Hemant Kumar Chandrasekaran Balakumar A comprehensive overview of selective and novel fibroblast growth factor receptor inhibitors as a potential anticancer modality Acta Pharmaceutica fgfr tyrosine kinase inhibitors fda approval erdafitinib infigratinib pemigatinib futibatinib |
| title | A comprehensive overview of selective and novel fibroblast growth factor receptor inhibitors as a potential anticancer modality |
| title_full | A comprehensive overview of selective and novel fibroblast growth factor receptor inhibitors as a potential anticancer modality |
| title_fullStr | A comprehensive overview of selective and novel fibroblast growth factor receptor inhibitors as a potential anticancer modality |
| title_full_unstemmed | A comprehensive overview of selective and novel fibroblast growth factor receptor inhibitors as a potential anticancer modality |
| title_short | A comprehensive overview of selective and novel fibroblast growth factor receptor inhibitors as a potential anticancer modality |
| title_sort | comprehensive overview of selective and novel fibroblast growth factor receptor inhibitors as a potential anticancer modality |
| topic | fgfr tyrosine kinase inhibitors fda approval erdafitinib infigratinib pemigatinib futibatinib |
| url | https://doi.org/10.2478/acph-2024-0005 |
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