pemigatinib   Click here for help

GtoPdb Ligand ID: 9767

Synonyms: example 126 [WO2014007951] | INCB 54828 | INCB-54828 | INCB054828 | INCB54828 | Pemazyre®
Approved drug
pemigatinib is an approved drug (FDA (2020))
Compound class: Synthetic organic
Comment: Pemigatinib (INCB54828) is a FGFR inhibitor claimed in Incyte Corporation's patent WO2014007951 [3]. It is equipotent at FGFR subtypes 1-3 [3].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 6
Hydrogen bond donors 1
Rotatable bonds 6
Topological polar surface area 83.16
Molecular weight 487.2
XLogP 2.02
No. Lipinski's rules broken 0
SMILES / InChI / InChIKey
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Canonical SMILES CCN1C(=O)N(Cc2c1c1cc([nH]c1nc2)CN1CCOCC1)c1c(F)c(OC)cc(c1F)OC
Isomeric SMILES CCN1C(=O)N(Cc2c1c1cc([nH]c1nc2)CN1CCOCC1)c1c(F)c(OC)cc(c1F)OC
InChI InChI=1S/C24H27F2N5O4/c1-4-30-21-14(11-27-23-16(21)9-15(28-23)13-29-5-7-35-8-6-29)12-31(24(30)32)22-19(25)17(33-2)10-18(34-3)20(22)26/h9-11H,4-8,12-13H2,1-3H3,(H,27,28)
InChI Key HCDMJFOHIXMBOV-UHFFFAOYSA-N
No information available.
Summary of Clinical Use Click here for help
Pemigatinib (INCB54828) progressed to Phase 3 cancer clinical trials. Click here to see all INCB54828 trials registered with ClinicalTrials.gov. In April 2020 the FDA approved the use of pemigatinib as a treatment for locally advanced/metastatic cholangiocarcinoma with a verified fibroblast growth factor receptor 2 (FGFR2) fusion [4] or other rearrangement [2]. It is indicated for tumours that have been previously treated and which cannot be resected. Pemigatinib holds EMA orphan designations for myeloid/lymphoid neoplasms with eosinophilia and rearrangement of PDGFRA, PDGFRB, or FGFR1, or with PCM1-JAK2 (2019) and cholangiocarcinoma (2018).
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Pemigatinib inhibits aberrant FGFR-related signal transduction activation in FGFR1/2/3-overexpressing tumour cells and thereby inhibits cancer cell proliferation.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT02924376 Efficacy and Safety of Pemigatinib in Subjects With Advanced/Metastatic or Surgically Unresectable Cholangiocarcinoma Who Failed Previous Therapy - (FIGHT-202) Phase 2 Interventional Incyte Corporation 1