Synonyms: compound A-1 [WO2022023450]
Compound class:
Synthetic organic
Comment: The chemical structure for flezurafenib was obtained from proposed INN list 130 (Feb. 2024), in which the compound is described as a rapidly accelerated fibrosarcoma (Raf) kinase inhibitor with proposed antineoplastic action. It is one of the Raf inhibitors claimed in patent WO2022023450A1 [1]. Investigation of Jazz Pharmaceuticals' pipeline suggests that flezurafenib may be their oral pan-Raf inhibitor clinical lead JZP815. This lead is being explored for efficacy against solid tumours and haematologic malignancies harbouring oncogenic mutations that activate the RAS-RAF-MAPK pathway. We will update this entry when the structure for flezurafenib or JZP815 is publicly disclosed.
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Bioactivity Comments |
Inhibition of ERK phosphorylation in cancer cell lines by flezurafenib (compound A-1) is reported in patent WO2022023450A1 [1]. The patent does not provide potency values for inhibition of RAF kinases. |