Drug intelligence / Profile preview

rogaratinib

Development stage
Phase 3
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral
01

Overview

Rogaratinib is an investigational, orally administered small-molecule pan-fibroblast growth factor receptor inhibitor developed by Bayer. It inhibits FGFR1, FGFR2, FGFR3, and FGFR4, thereby suppressing oncogenic FGFR signaling and downstream proliferative pathways in tumors with FGFR pathway activation. Clinical development initially used tumor FGFR mRNA overexpression as a selection biomarker, particularly in urothelial carcinoma and squamous non-small cell lung cancer; however, the randomized FORT-1 urothelial carcinoma study did not show superiority over chemotherapy, while exploratory analyses suggested higher activity in tumors also harboring FGFR3 DNA alterations. A National Cancer Institute-sponsored phase 2 study remains active in FGFR1-4-altered sarcoma and SDH-deficient gastrointestinal stromal tumor. ([pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/30807645/?dopt=Abstract))

Other names
BAY1213802BAY-1213802BAY 1213802
02

Targets

FGFR4 (Fibroblast growth factor receptor 4)FGFR2 (Keratinocyte growth factor receptor)FGFR3 (Fibroblast growth factor receptor 3)FGFR1 (Fibroblast growth factor receptor 1)

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