Target Information
| Target General Information | Top | |||||
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| Target ID |
T17687
(Former ID: TTDR00314)
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| Target Name |
Fibroblast growth factor receptor (FGFR)
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| Synonyms |
FGF receptor
Click to Show/Hide
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| Gene Name |
NO-GeName
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Bladder cancer [ICD-11: 2C94] | |||||
| 2 | Liver cancer [ICD-11: 2C12] | |||||
| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 4 Approved Drugs | + | ||||
| 1 | Erdafitinib | Drug Info | Approved | Bladder cancer | [2] | |
| 2 | Futibatinib | Drug Info | Approved | Intrahepatic cholangiocarcinoma | [3] | |
| 3 | Infigratinib | Drug Info | Approved | Cholangiocarcinoma | [4] | |
| 4 | HIF-1alpha | Drug Info | Phase 4 | Lymphoma | [5] | |
| Clinical Trial Drug(s) | [+] 6 Clinical Trial Drugs | + | ||||
| 1 | ARQ-087 | Drug Info | Phase 3 | Intrahepatic cholangiocarcinoma | [6] | |
| 2 | AZD4547 | Drug Info | Phase 2/3 | Solid tumour/cancer | [7], [8] | |
| 3 | BAY1163877 | Drug Info | Phase 2 | Bladder cancer | [9] | |
| 4 | Debio 1347 | Drug Info | Phase 2 | Solid tumour/cancer | [10] | |
| 5 | ICP-192 | Drug Info | Phase 2 | Bladder cancer | [11] | |
| 6 | PRN1371 | Drug Info | Phase 1 | Solid tumour/cancer | [6] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Inhibitor | [+] 5 Inhibitor drugs | + | ||||
| 1 | Erdafitinib | Drug Info | [2] | |||
| 2 | Infigratinib | Drug Info | [6] | |||
| 3 | AZD4547 | Drug Info | [6] | |||
| 4 | ICP-192 | Drug Info | [15] | |||
| 5 | PRN1371 | Drug Info | [6] | |||
| Antagonist | [+] 7 Antagonist drugs | + | ||||
| 1 | Futibatinib | Drug Info | [12] | |||
| 2 | HIF-1alpha | Drug Info | [1] | |||
| 3 | ARQ-087 | Drug Info | [6] | |||
| 4 | BAY1163877 | Drug Info | [13] | |||
| 5 | PD173074 | Drug Info | [1] | |||
| 6 | SU4984 | Drug Info | [1] | |||
| 7 | SU5403 | Drug Info | [1] | |||
| Modulator | [+] 2 Modulator drugs | + | ||||
| 1 | Debio 1347 | Drug Info | [14] | |||
| 2 | ARO 087 | Drug Info | [16] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| References | Top | |||||
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| REF 1 | Tumor angiogenesis as a therapeutic target. Drug Discov Today. 2001 Oct 1;6(19):1005-1024. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019 | |||||
| REF 3 | FDA Approved Drug Products from FDA Official Website. 2022. Application Number: 214801. | |||||
| REF 4 | FDA Approved Drug Products from FDA Official Website. 2021. Application Number: 214622. | |||||
| REF 5 | ClinicalTrials.gov (NCT00880672) Effect of Dutasteride on HIF-1alpha and VEGF in the Prostate. U.S. National Institutes of Health. | |||||
| REF 6 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 7 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7707). | |||||
| REF 8 | ClinicalTrials.gov (NCT02154490) Lung-MAP: S1400 Biomarker-Targeted Second-Line Therapy in Treating Patients With Recurrent Stage IIIB-IV Squamous Cell Lung Cancer. U.S. National Institutes of Health. | |||||
| REF 9 | ClinicalTrials.gov (NCT04040725) Rogaratinib for BCG Refractory High Risk Non-Muscle Invasive Bladder Cancer With FGFR1/2 Overexpression. U.S. National Institutes of Health. | |||||
| REF 10 | ClinicalTrials.gov (NCT03834220) Basket Trial in Solid Tumors Harboring a Fusion of FGFR1, FGFR2 or FGFR3- (FUZE Clinical Trial). U.S. National Institutes of Health. | |||||
| REF 11 | ClinicalTrials.gov (NCT04492293) An Efficacy and Safety Study of ICP-192 in Subjects With Bladder Urothelial Cancer. U.S. National Institutes of Health. | |||||
| REF 12 | TAS-120, a highly potent and selective irreversible FGFR inhibitor, is effective in tumors harboring various FGFR gene abnormalities. Molecular Cancer Therapeutics. 01/2014; 12(11_Supplement):A270-A270. | |||||
| REF 13 | Preclinical profile of BAY 1163877 - a selective pan-FGFR inhibitor in phase 1 clinical trial. Cancer Research. 10/2014; 74(19 Supplement):1739-1739. | |||||
| REF 14 | The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor. Mol Cancer Ther. 2014 Nov;13(11):2547-58. | |||||
| REF 15 | Clinical pipeline report, company report or official report of InnoCare Pharma. | |||||
| REF 16 | J Clin Oncol 33, 2015 (suppl; abstr 2545). | |||||
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