Oral Selective Estrogen Receptor Degraders (SERDs) in Breast Cancer: Advances, Challenges, and Current Status

Downton, Teesha; Zhou, Fiona H.; Segara, Davendra; Jeselsohn, Rinath; Lim, Elgene

doi:10.2147/dddt.s380925

Cited by 26 publications

(22 citation statements)

References 89 publications

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“…Nevertheless, its effectiveness in metastatic disease has been validated, the challenges of drug resistance remain even for this drug [ 65 ] and it has the limit of being an injectable with considerable pharmaceutical liabilities [ 66 ]. Thus, several SERDs available as oral formulations are under study as monotherapy or in combination with other drugs [ 67 , 68 , 69 , 70 ]. GDC-9545 (giredestrant) was identified as an oral SERD with an exceptional preclinical profile [ 71 ].…”

Section: Breast Cancer Therapiesmentioning

confidence: 99%

Targeting Breast Cancer: An Overlook on Current Strategies

Iacopetta

Ceramella

Baldino

et al. 2023

IJMS

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Breast cancer (BC) is one of the most widely diagnosed cancers and a leading cause of cancer death among women worldwide. Globally, BC is the second most frequent cancer and first most frequent gynecological one, affecting women with a relatively low case-mortality rate. Surgery, radiotherapy, and chemotherapy are the main treatments for BC, even though the latter are often not aways successful because of the common side effects and the damage caused to healthy tissues and organs. Aggressive and metastatic BCs are difficult to treat, thus new studies are needed in order to find new therapies and strategies for managing these diseases. In this review, we intend to give an overview of studies in this field, presenting the data from the literature concerning the classification of BCs and the drugs used in therapy for the treatment of BCs, along with drugs in clinical studies.

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Section: Breast Cancer Therapiesmentioning

confidence: 99%

Targeting Breast Cancer: An Overlook on Current Strategies

Iacopetta

Ceramella

Baldino

et al. 2023

IJMS

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“…There are several emerging novel classes of ET, of which the oral SERDs are the largest group and are reviewed in detail elsewhere ( Downton et al, 2022 ). To date there have been four completed randomized trials of oral SERDs in advanced ER+/HER2-breast cancer, after progression on prior ET with or without a CDK4/6 inhibitor, and results have been mixed.…”

Section: Therapeutic Strategies Following Progression On Cdk4/6 Inhib...mentioning

confidence: 99%

CDK4/6 inhibitor resistance in estrogen receptor positive breast cancer, a 2023 perspective

Zhou

Downton

Freelander

et al. 2023

Front. Cell Dev. Biol.

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CDK4/6 inhibitors have become game-changers in the treatment of estrogen receptor-positive (ER+) breast cancer, and in combination with endocrine therapy are the standard of care first-line treatment for ER+/HER2-negative advanced breast cancer. Although CDK4/6 inhibitors prolong survival for these patients, resistance is inevitable and there is currently no clear standard next-line treatment. There is an urgent unmet need to dissect the mechanisms which drive intrinsic and acquired resistance to CDK4/6 inhibitors and endocrine therapy to guide the subsequent therapeutic decisions. We will review the insights gained from preclinical studies and clinical cohorts into the diverse mechanisms of CDK4/6 inhibitor action and resistance, and highlight potential therapeutic strategies in the context of CDK4/6 inhibitor resistance.

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“…The most diagnosed type of cancer globally is breast cancer (BC) [1] . Furthermore, it is the second most lethal illness for women [2] .…”

Section: Introductionmentioning

confidence: 99%

Selenium Analogue of LSZ102 as a Highly Potent ER‐α Binder

Paegle

Arsenyan

2023

Eur J Org Chem

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Nowadays, selective estrogen receptor modulators (SERMs) and downregulators (SERDs) are used as the first-line medical treatment for estrogen receptor positive (ER +) tumors. Herein we report synthesis, ER-α binding activity, and cytotoxicity of LSZ102 selenium analogues 11 and 28. TR-FRET competitive ERα binding experiments and cytotoxicity assays have shown that the selenium analogues exhibit closely related activity to LSZ102. Furthermore, the prepared selenium analogues are not toxic in rat cardiomyoblasts (H9C2), indicating that substituted benzo[b]selenophene is a prospective scaffold for the development of ER-α modulators and downregulators for the treatment of ER + cancers.

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Oral Selective Estrogen Receptor Degraders (SERDs) in Breast Cancer: Advances, Challenges, and Current Status

Cited by 26 publications

References 89 publications

Targeting Breast Cancer: An Overlook on Current Strategies

Targeting Breast Cancer: An Overlook on Current Strategies

CDK4/6 inhibitor resistance in estrogen receptor positive breast cancer, a 2023 perspective

Selenium Analogue of LSZ102 as a Highly Potent ER‐α Binder

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