Drug intelligence / Profile preview

BBI-355 + futibatinib

Development stage
Unknown
Lead developer
Boundless Bio
Modality
Small Molecules
Administration
Oral
01

Overview

BBI-355 + futibatinib is an investigational oral combination therapy being evaluated for the treatment of locally advanced or metastatic solid tumors harboring specific oncogene amplifications, especially those involving EGFR or FGFR genes. BBI-355 is a highly selective, orally bioavailable checkpoint kinase 1 (CHK1) small molecule inhibitor developed as an extrachromosomal DNA (ecDNA)-directed therapy, disrupting the cell-cycle checkpoint and DNA damage response in cancer cells with oncogene amplification on ecDNA. Futibatinib (brand name LYTGOBI) is an oral, selective, irreversible pan-FGFR (fibroblast growth factor receptor) inhibitor. The combination aims to achieve synergistic antitumor activity: BBI-355 sensitizes ecDNA-driven tumors to FGFR inhibition, reducing resistance mechanisms seen with FGFR inhibitors alone. Ongoing trials primarily target solid tumors, including gastric, bladder, endometrial, lung, and other cancers with this molecular profile[1][2][3][5][7].

Other names
BBI-355 + LYTGOBI
02

Targets

FGFR4 (Fibroblast growth factor receptor 4)FGFR3 (Fibroblast growth factor receptor 3)CHEK1 (Checkpoint kinase 1)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)

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