Drug intelligence / Profile preview

dabogratinib

Development stage
Phase 2
Lead developer
Tyra Biosciences
Modality
Small Molecules
Administration
Oral
01

Overview

Dabogratinib is an investigational, orally available, highly selective small-molecule inhibitor of fibroblast growth factor receptor 3 (FGFR3) being developed by Tyra Biosciences for cancers and skeletal dysplasias driven by FGFR3 alterations.[6][12][14] Designed using Tyra’s SNÅP structure-guided platform, it exhibits isoform selectivity for FGFR3 while sparing FGFR1, FGFR2, and FGFR4, with the goal of maintaining antitumor or growth-modifying efficacy while reducing class-related toxicities such as hyperphosphatemia.[6][12][14] Preclinical data show potent inhibition of FGFR3-activated signaling and tumor growth in xenograft models harboring FGFR3 mutations such as S249C, and early clinical work has demonstrated proof-of-concept activity in metastatic urothelial cancer and supports ongoing trials in intermediate‑risk non‑muscle invasive bladder cancer, low‑grade upper tract urothelial carcinoma, and pediatric achondroplasia.[2][4][6][8][10][14]

Other names
dabogratinib
02

Targets

FGFR3 (Fibroblast growth factor receptor 3)

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