Erdafitinib
エルダフィチニブ
JNJ-42756493
CAS 1346242-81-6
MF, C25H30N6O2, MW 446.54
UNII-890E37NHMV
890E37NHMV
2019/4/12, FDA APPROVED, BALVERSA (Janssen Products LP)
| Balversa |
Эрдафитиниб [Russian] [INN]
N‘-(3,5-dimethoxyphenyl)-N‘-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-N-propan-2-ylethane-1,2-diamine
Erdafitinib is an orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Upon oral administration, erdafitinib binds to and inhibits FGFR, which may result in the inhibition of FGFR-related signal transduction pathways and thus the inhibition of tumor cell proliferation and tumor cell death in FGFR-overexpressing tumor cells. FGFR, upregulated in many tumor cell types, is a receptor tyrosine kinase essential to tumor cell proliferation, differentiation and survival
Erdafitinib has been used in trials studying the basic science and treatment of Tumor or Lymphoma.
Erdafitinib[1] is a small molecule inhibitor of FGFR approved for treatment of cancer and marketed under the name Balversa. FGFRs are a subset of tyrosine kinases which are unregulated in some tumors and influence tumor cell differentiation, proliferation, angiogenesis, and cell survival.[2] Astex Pharmaceuticals discovered the drug and licensed it to Janssen Pharmaceuticals for further development.
Researchers have investigated erdafitinib for safety and efficacy in treatment of cholangiocarcinoma, gastric cancer, non-small cell lung cancer, and esophageal cancer.[3]
In March 2018, erdafitinib was granted Breakthrough Therapy Designation by the U.S. Food and Drug Administration for treatment of urothelial cancer.[2],
In April 2019, erdafitinib was granted approval by the FDA for treatment of metastatic or locally advanced bladder cancer with an FGFR3 or FGFR2 alteration that has progressed beyond traditional platinum-based therapies, subject to a confirmatory trial.
PATENT
WO 2011135376
https://patents.google.com/patent/WO2011135376A1/ru
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References
- ^ https://searchusan.ama-assn.org/usan/documentDownload?uri=%2Funstructured%2Fbinary%2Fusan%2Ferdafitinib.pdf
- ^ Jump up to:a b “Janssen Announces U.S. FDA Breakthrough Therapy Designation for Erdafitinib in the Treatment of Metastatic Urothelial Cancer – Johnson & Johnson”. http://www.jnj.com.
- ^ “Erdafitinib – Janssen Pharmaceutica – AdisInsight”. adisinsight.springer.com.
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| Synonyms | JNJ-42756493 |
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| UNII | |
| KEGG | |
| ECHA InfoCard | 100.235.008  |
| Chemical and physical data | |
| Formula | C25H30N6O2 |
| Molar mass | 446.555 g·mol−1 |
| 3D model (JSmol) | |
Patent IDTitleSubmitted DateGranted Date
US2018186775QUINOXALINE DERIVATIVES USEFUL AS FGFR KINASE MODULATORS2017-12-28
US2018127397PYRAZOLYL QUINOXALINE KINASE INHIBITORS2017-11-13
US20172601682-ARYL- AND 2-HETEROARYL-SUBSTITUTED 2-PYRIDAZIN-3(2H)-ONE COMPOUNDS AS INHIBITORS OF FGFR TYROSINE KINASES2016-10-24
US2017267684A DEUTERATED TRIAZOLOPYRIDAZINE AS A KINASE MODULATOR2015-12-03
US9464071PYRAZOLYL QUINOXALINE KINASE INHIBITORS2014-10-022015-04-16
US8895601Pyrazolyl quinoxaline kinase inhibitors2011-04-282014-11-25
US2017100406COMBINATIONS OF AN FGFR INHIBITOR AND AN IGF1R INHIBITOR2015-03-26
US9850228PYRAZOLYL QUINOXALINE KINASE INHIBITORS2016-04-28
US9902714QUINOXALINE DERIVATIVES USEFUL AS FGFR KINASE MODULATORS2015-03-26
US2018296558COMBINATIONS2018-04-17
US2018021332PHARMACEUTICAL COMPOSITIONS COMPRISING N-(3,5-DIMETHOXYPHENYL)-N’-(1-METHYLETHYL)-N-[3-(1-METHYL-1H-PYRAZOL-4-YL)QUINOXALIN-6-YL]ETHANE-1,2-DIAMINE2016-02-09
US2017119763COMBINATIONS2015-03-26
US2016090633USE OF FGFR MUTANT GENE PANELS IN IDENTIFYING CANCER PATIENTS THAT WILL BE RESPONSIVE TO TREATMENT WITH AN FGFR INHIBITOR2015-09-182016-03-31
US2016287699FGFR/PD-1 COMBINATION THERAPY FOR THE TREATMENT OF CANCER2016-03-24
/////////Erdafitinib, FDA 2019, エルダフィチニブ, BALVERSA, Janssen Products LP, JNJ-42756493, Эрдафитиниб , إيردافيتينيب , 厄达替尼 ,
CC(C)NCCN(C1=CC2=NC(=CN=C2C=C1)C3=CN(N=C3)C)C4=CC(=CC(=C4)OC)OC