Drug intelligence / Profile preview

futibatinib + fulvestrant

Development stage
Unknown
Lead developer
Taiho Oncology
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Futibatinib plus fulvestrant is an investigational combination therapy being studied primarily for the treatment of advanced or metastatic breast cancer with fibroblast growth factor receptor (FGFR) gene amplifications, particularly FGFR1. Futibatinib (TAS-120, brand name Lytgobi) is a small molecule, irreversible covalent inhibitor of FGFR1–4 that blocks aberrant signaling driving tumor growth in cancers with FGFR alterations. Fulvestrant (brand name Faslodex) is a selective estrogen receptor degrader used to treat hormone receptor-positive, HER2-negative advanced breast cancer by binding to and degrading the estrogen receptor. The combination has demonstrated encouraging antitumor activity and clinical benefit in patients who have progressed on prior therapies such as CDK4/6 inhibitors. Adverse events are consistent with known profiles for each agent[1][3][4][6].

Other names
futibatinib + fulvestrant
02

Targets

FGFR4 (Fibroblast growth factor receptor 4)FGFR3 (Fibroblast growth factor receptor 3)ESR1 (ERα)YES1 (YES proto-oncogene 1 tyrosine kinase)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)ESR2 (ERβ)

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