Effect of Tasurgratinib as an Orally Available FGFR1–3 Inhibitor on Resistance to a CDK4/6 Inhibitor and Endocrine Therapy in ER+/HER2− Breast Cancer Preclinical Models DOI Open Access

Satoshi Kawano,

Sayo Fukushima,

Kyoko Nishibata

и другие.

Cancers, Год журнала: 2025, Номер 17(7), С. 1084 - 1084

Опубликована: Март 24, 2025

Fibroblast growth factor (FGF) signaling plays a crucial role in several cellular functions cancer cells. Tasurgratinib, formerly known as E7090, is an orally available FGF receptor (FGFR)1-3 selective inhibitor. Here, we present the effects of tasurgratinib on resistance to CDK4/6 inhibitors and endocrine therapy (ET) preclinical model. Estrogen (ER)+ breast (BC) patient-derived xenograft (PDX) models harboring ESR1 wild-type or mutation were used animal models. An vitro cell proliferation assay ER+ BC lines treated with fulvestrant palbociclib + was conducted presence FGF2 FGF10, without tasurgratinib. Among five PDX models, OD-BRE-0438 OD-BRE-0704 showed higher sensitivities prior than it. In these treatment upregulated expression ligand mRNAs. vitro, FGF10 decreased sensitivity both fulvestrant, which restored by co-treatment Consistently, elacestrant antitumor activity mutation, respectively. ET BC. Tasurgratinib has potential exhibit significant combination against via inhibition. These findings indicate therapeutic treating

Язык: Английский

Effect of Tasurgratinib as an Orally Available FGFR1–3 Inhibitor on Resistance to a CDK4/6 Inhibitor and Endocrine Therapy in ER+/HER2− Breast Cancer Preclinical Models DOI Open Access

Satoshi Kawano,

Sayo Fukushima,

Kyoko Nishibata

и другие.

Cancers, Год журнала: 2025, Номер 17(7), С. 1084 - 1084

Опубликована: Март 24, 2025

Fibroblast growth factor (FGF) signaling plays a crucial role in several cellular functions cancer cells. Tasurgratinib, formerly known as E7090, is an orally available FGF receptor (FGFR)1-3 selective inhibitor. Here, we present the effects of tasurgratinib on resistance to CDK4/6 inhibitors and endocrine therapy (ET) preclinical model. Estrogen (ER)+ breast (BC) patient-derived xenograft (PDX) models harboring ESR1 wild-type or mutation were used animal models. An vitro cell proliferation assay ER+ BC lines treated with fulvestrant palbociclib + was conducted presence FGF2 FGF10, without tasurgratinib. Among five PDX models, OD-BRE-0438 OD-BRE-0704 showed higher sensitivities prior than it. In these treatment upregulated expression ligand mRNAs. vitro, FGF10 decreased sensitivity both fulvestrant, which restored by co-treatment Consistently, elacestrant antitumor activity mutation, respectively. ET BC. Tasurgratinib has potential exhibit significant combination against via inhibition. These findings indicate therapeutic treating

Язык: Английский

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