fulvestrant + tasurgratinib

Fulvestrant + tasurgratinib is a combination therapy under clinical investigation for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2−) advanced or metastatic breast cancer, particularly in patients who have progressed after prior CDK4/6 inhibitor therapy. Fulvestrant is a selective estrogen receptor degrader (SERD) that binds to and accelerates degradation of the estrogen receptor, thereby inhibiting estrogen signaling in breast cancer cells. Tasurgratinib (E7090; brand name TASFYGO) is an orally available small molecule tyrosine kinase inhibitor that selectively targets fibroblast growth factor receptors FGFR1, FGFR2, and FGFR3. The rationale for this combination stems from evidence that FGF signaling contributes to resistance against endocrine therapies such as fulvestrant; inhibition of FGFR1–3 by tasurgratinib can restore sensitivity and enhance antitumor activity when combined with endocrine therapy. Preclinical models and early-phase clinical trials have shown promising antitumor activity with manageable safety profiles for this combination[1][2][3].

Brand names

Faslodex

Other names

fulvestrant + E7090fulvestrant + TASFYGO