Selective Estrogen Receptor Degraders (SERDs): A Promising Strategy for Estrogen Receptor Positive Endocrine-Resistant Breast Cancer

Lu, Yunlong; Liu, Wukun

doi:10.1021/acs.jmedchem.0c00913

Cited by 70 publications

(61 citation statements)

References 170 publications

(296 reference statements)

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“…Zanidatamab (ZW25) is a novel bispecific antibody directed against HER2, that can simultaneously bind two non-overlapping epitopes, resulting in HER2 signal blockade [31]. Previously published data have shown promising and durable antitumour activity, as well as good tolerability, in patients with heavily pretreated advanced or metastatic HER2-expressing GEA or in G/GEJ adenocarcinoma [32].…”

Section: Early Results Of Zanidatamab In Her2-positive Gi Tumorsmentioning

confidence: 99%

“…coopERA Breast Cancer: next generation SERD in ER+/ HER2-BC HR+/HER2-is the most common subtype of breast cancer, with an age-adjusted rate of 88.1 new cases per 100,000 women [15]. Endocrine therapy (ET) -including selective estrogen receptor modulators (SERMs), aromatase inhibitors (AIs), or selective estrogen receptor degraders (SERDs) -is the backbone to treat advanced ER+ BC [31]; however, drug resistance remains a challenge [31]. The only approved SERD, fulvestrant, has to be administered through an intramuscular injection and presents poor pharmacokinet- ics [32].…”

Section: Kate3: Adc Combined With Pd-l1 Inhibitionmentioning

confidence: 99%

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A GLOBAL CONGRESS DIGEST ON SOLID TUMORS. Report from the ESMO Virtual Congress, 16th – 21st September 2021

2021

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Section: Early Results Of Zanidatamab In Her2-positive Gi Tumorsmentioning

confidence: 99%

Section: Kate3: Adc Combined With Pd-l1 Inhibitionmentioning

confidence: 99%

A GLOBAL CONGRESS DIGEST ON SOLID TUMORS. Report from the ESMO Virtual Congress, 16th – 21st September 2021

2021

memo

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“…ER-positive breast cancer accounts for 70% of breast cancers in postmenopausal women (48). AIs are the first-line treatment for ER-positive breast cancer and are believed to reduce the risk of local, distant, and contralateral breast recurrence, which ultimately improves overall patient survival (31).…”

Section: Aromatase Inhibitorsmentioning

confidence: 99%

Update on the Role of Neuropeptide Y and Other Related Factors in Breast Cancer and Osteoporosis

Lin

Sun

et al. 2021

Front. Endocrinol.

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Breast cancer and osteoporosis are common diseases that affect the survival and quality of life in postmenopausal women. Women with breast cancer are more likely to develop osteoporosis than women without breast cancer due to certain factors that can affect both diseases simultaneously. For instance, estrogen and the receptor activator of nuclear factor-κB ligand (RANKL) play important roles in the occurrence and development of these two diseases. Moreover, chemotherapy and hormone therapy administered to breast cancer patients also increase the incidence of osteoporosis, and in recent years, neuropeptide Y (NPY) has also been found to impact breast cancer and osteoporosis.Y1 and Y5 receptors are highly expressed in breast cancer, and Y1 and Y2 receptors affect osteogenic response, thus potentially highlighting a potential new direction for treatment strategies. In this paper, the relationship between breast cancer and osteoporosis, the influence of NPY on both diseases, and the recent progress in the research and treatment of these diseases are reviewed.

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“… 22 – 24 The pharmacokinetics of fulvestrant, however, require it to be administered by intramuscular injection. 25 – 27…”

Section: Introductionmentioning

confidence: 99%

AMEERA-5: a randomized, double-blind phase 3 study of amcenestrant plus palbociclib versus letrozole plus palbociclib for previously untreated ER+/HER2– advanced breast cancer

Bardia

Cortés²,

Hurvitz

et al. 2022

Ther Adv Med Oncol

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Background: For estrogen receptor–positive (ER+)/human epidermal growth factor receptor 2–negative (HER2–) advanced breast cancer (ABC), the current standard first-line treatment includes an aromatase inhibitor in combination with a cyclin-dependent kinase 4/6 inhibitor. When resistance occurs, often related to the occurrence of ESR1 mutations, selective estrogen receptor modulators or degraders (SERDs) may be used, alone or in combination regimens. Amcenestrant (SAR439859), an optimized oral SERD, has shown clinical antitumor activity in combination with palbociclib in patients with ER+/HER2– ABC and, as monotherapy, in patients with and without ESR1 mutations. Here, we describe the study design of AMEERA-5, an ongoing, prospective, phase 3, randomized, double-blind, multinational study comparing the efficacy and safety of amcenestrant plus palbociclib versus letrozole plus palbociclib in patients with advanced (locoregional recurrent or metastatic) ER+/HER2– breast cancer. Methods: Patients are pre-/postmenopausal women and men with no prior systemic therapy for ABC. The planned enrollment is 1066 patients. Patients are randomized 1:1 to either amcenestrant 200 mg plus palbociclib 125 mg or letrozole 2.5 mg plus palbociclib 125 mg. Amcenestrant, letrozole, and their matching placebos are taken once daily continuously; palbociclib is taken once daily for 21 days, followed by 7 days off-treatment for a 28-day cycle. Treatment continues until disease progression, unacceptable toxicity, or decision to stop treatment. Pre-/perimenopausal women and men receive goserelin subcutaneously. Randomization is stratified by de novo metastatic disease, menopausal status, and visceral metastases. The primary endpoint is progression-free survival. The key secondary endpoint is overall survival; others are safety, pharmacokinetics, and quality of life. Conclusions: AMEERA-5 is evaluating the efficacy and safety of amcenestrant in combination with palbociclib as first-line therapy in pre-/postmenopausal women and men with ER+/HER2– ABC. ClinicalTrials Identifier: NCT04478266.

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Selective Estrogen Receptor Degraders (SERDs): A Promising Strategy for Estrogen Receptor Positive Endocrine-Resistant Breast Cancer

Cited by 70 publications

References 170 publications

A GLOBAL CONGRESS DIGEST ON SOLID TUMORS. Report from the ESMO Virtual Congress, 16th – 21st September 2021

A GLOBAL CONGRESS DIGEST ON SOLID TUMORS. Report from the ESMO Virtual Congress, 16th – 21st September 2021

Update on the Role of Neuropeptide Y and Other Related Factors in Breast Cancer and Osteoporosis

AMEERA-5: a randomized, double-blind phase 3 study of amcenestrant plus palbociclib versus letrozole plus palbociclib for previously untreated ER+/HER2– advanced breast cancer

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