Modeling the novel SERD elacestrant in cultured fulvestrant-refractory HR-positive breast circulating tumor cells

Summary: First-line therapy with ribociclib plus letrozole showed a significant overall survival benefit as compared with placebo plus letrozole in patients with HR-positive, HER2-negative advanced breast cancer. Median overall survival was more than 12 months longer with ribociclib than with placebo.

NEW ENGLAND JOURNAL OF MEDICINE (2022)

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Article Oncology

Elacestrant (oral selective estrogen receptor degrader) Versus Standard Endocrine Therapy for Estrogen Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Advanced Breast Cancer: Results From the Randomized Phase III EMERALD Trial

Francois-Clement Bidard et al.

Summary: Elacestrant, a novel oral selective estrogen receptor degrader, demonstrated significant improvement in progression-free survival in patients with pretreated estrogen receptor-positive/human epidermal growth factor receptor 2-negative advanced breast cancer, including those with ESR1 mutations, with manageable adverse events.

JOURNAL OF CLINICAL ONCOLOGY (2022)

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Meeting Abstract Oncology

AMEERA-3, a phase II study of amcenestrant (AMC) versus endocrine treatment of physician's choice (TPC) in patients (pts) with endocrine-resistant ER+/HER2-advanced breast cancer (aBC)

S. M. Tolaney et al.

ANNALS OF ONCOLOGY (2022)

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Review Oncology

Next-generation selective estrogen receptor degraders and other novel endocrine therapies for management of metastatic hormone receptor-positive breast cancer: current and emerging role

Maxwell R. Lloyd et al.

Summary: Endocrine therapy is a pivotal strategy for managing ER+ breast cancer, but resistance remains a major challenge. ESR1 mutations induce ER activity and resistance. Oral SERDs and other novel ETs show promise in treating ER+ breast cancer.

THERAPEUTIC ADVANCES IN MEDICAL ONCOLOGY (2022)

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Article Oncology

The Lipogenic Regulator SREBP2 Induces Transferrin in Circulating Melanoma Cells and Suppresses Ferroptosis

Xin Hong et al.

Summary: Circulating tumor cells shed by cancer into the bloodstream coordinately upregulate lipogenesis and iron homeostasis pathways, contributing to resistance to BRAF inhibitors. The lipogenesis regulator SREBP2 induces transcription of iron carrier TF, reducing oxidative stress and conferring resistance to ferroptosis inducers. Presence of CTCs with high lipogenic and iron metabolic signatures is correlated with adverse clinical outcome in melanoma patients.

CANCER DISCOVERY (2021)

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Article Oncology

Phase I Study of Elacestrant (RAD1901), a Novel Selective Estrogen Receptor Degrader, in ER-Positive, HER2-Negative Advanced Breast Cancer

Aditya Bardia et al.

Summary: This phase I study evaluated elacestrant in heavily pretreated women with estrogen receptor-positive metastatic breast cancer. The results showed that elacestrant 400 mg orally once daily has an acceptable safety profile and demonstrated single-agent activity, particularly in patients with ESR1 mutation. A phase III trial investigating elacestrant versus standard endocrine therapy is ongoing.

JOURNAL OF CLINICAL ONCOLOGY (2021)

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Review Biochemistry & Molecular Biology

Oral Selective Estrogen Receptor Degraders (SERDs) as a Novel Breast Cancer Therapy: Present and Future from a Clinical Perspective

Cristina Hernando et al.

Summary: ER+ breast cancer is the most common subtype, with endocrine therapy being the fundamental treatment. However, some patients develop endocrine resistance, with ESR1 gene mutations being a studied mechanism. SERDs have become a weapon against endocrine resistance in research and development, showing promise for improving patient outcomes.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

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Article Oncology

Distinct mechanisms of resistance to fulvestrant treatment dictate level of ER independence and selective response to CDK inhibitors in metastatic breast cancer

Kamila Kaminska et al.

Summary: Resistance to endocrine treatment in metastatic breast cancer poses a major clinical challenge, with complex mechanisms contributing to the development of diverse resistance patterns, impacting levels of estrogen receptor independence and potential cross-resistance to CDK inhibitors.

BREAST CANCER RESEARCH (2021)

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Article Medicine, General & Internal