rogaratinib   Click here for help

GtoPdb Ligand ID: 9789

Synonyms: BAY-1163877 | BAY1163877 | Example 1 [WO2013087578]
Compound class: Synthetic organic
Comment: Rogaratinib (BAY-1163877) is a FGFR-selective kinase inhibitor that is being investigated for antineoplastic activity. The parent molecular structure is claimed as Example 1 in patent WO2013087578, and the dihydrochloride is claimed as Example 2 [1].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 7
Hydrogen bond donors 2
Rotatable bonds 6
Topological polar surface area 135.25
Molecular weight 466.18
XLogP 1.58
No. Lipinski's rules broken 0
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Canonical SMILES COCc1c(CN2CCNC(=O)C2)n2c(c1c1cc3c(s1)c(OC)cc(c3)C)c(N)ncn2
Isomeric SMILES COCc1c(CN2CCNC(=O)C2)n2c(c1c1cc3c(s1)c(OC)cc(c3)C)c(N)ncn2
InChI InChI=1S/C23H26N6O3S/c1-13-6-14-8-18(33-22(14)17(7-13)32-3)20-15(11-31-2)16(9-28-5-4-25-19(30)10-28)29-21(20)23(24)26-12-27-29/h6-8,12H,4-5,9-11H2,1-3H3,(H,25,30)(H2,24,26,27)
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Summary of Clinical Use Click here for help
The most advanced clinical trial involving rogaratinib is Phase 2/3 trial NCT03410693, which is registerd on, but it is not yet recruiting subjects (Feb 2018). This trial will evaluate rogaratinib vs. chemotherapy in patients with FGFR +ve locally advanced or metastatic urothelial carcinoma.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT03410693 Study of Rogaratinib (BAY1163877) vs Chemotherapy in Patients With FGFR (Fibroblast Growth Factor Receptor)-Positive Locally Advanced or Metastatic Urothelial Carcinoma Phase 2/Phase 3 Interventional Bayer