^
    10ms
    AMEERA-3: Phase 2 Study of Amcenestrant (SAR439859) Versus Physician's Choice in Locally Advanced or Metastatic ER-positive Breast Cancer (clinicaltrials.gov)
    P2, N=367, Terminated, Sanofi | Active, not recruiting --> Terminated; Sponsor decision to prematurely stop the study, not linked to any safety concern.
    Trial termination
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    ER positive • HER-2 negative
    |
    tamoxifen • fulvestrant • letrozole • anastrozole • exemestane • amcenestrant (SAR439859)
    10ms
    New Oral Selective Estrogen Receptor Degraders Redefine Management of Estrogen Receptor-Positive Breast Cancer. (PubMed, Annu Rev Med)
    There are currently five oral SERDs in published and ongoing clinical trials-elacestrant, camizestrant, giredestrant, imlunestrant, and amcenestrant-with more in development. They offer a reasonably well-tolerated oral therapy option with low discontinuation rates in studies. This review summarizes the currently available literature on this new class of drugs.
    Review • Journal
    |
    ER (Estrogen receptor)
    |
    ER positive
    |
    Orserdu (elacestrant) • amcenestrant (SAR439859) • Inluriyo (imlunestrant) • camizestrant (AZD9833) • giredestrant (RG6171)
    10ms
    Pre-Clinical Rationale for Amcenestrant Combinations in HER2+/ER+ Breast Cancer. (PubMed, Int J Mol Sci)
    In this study, the pre-clinical rationale is explored for combining amcenestrant (Amc), a selective oestrogen receptor degrader (SERD), with HER2-targeted therapies including trastuzumab, trastuzumab-emtansine (T-DM1) and tyrosine kinase inhibitors (TKIs)...Additivity and synergy were observed between Amc and the TKIs neratinib, lapatinib and tucatinib in all cell lines...Higher ER expression in MDA-MB-361 and BT-474-T was associated with greater potential for synergy. In conclusion, the combination of Amc- and HER2-targeted treatments has potential as a therapeutic strategy for the treatment of HER2+/ER+ breast cancer and warrants further clinical investigation to validate safety and efficacy in patients.
    Preclinical • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • CASP3 (Caspase 3) • CASP7 (Caspase 7)
    |
    HER-2 positive • ER positive • HER-2 negative
    |
    lapatinib • Nerlynx (neratinib) • Kadcyla (ado-trastuzumab emtansine) • Tukysa (tucatinib) • amcenestrant (SAR439859)
    11ms
    Evaluation of Orally Administered Amcenestrant (SAR439859) in Japanese Postmenopausal Patients With Advanced Breast Cancer (AMEERA-2) (clinicaltrials.gov)
    P1, N=10, Terminated, Sanofi | Active, not recruiting --> Terminated; Sponsor decision to prematurely stop the study, not linked to any safety concern.
    Trial termination
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    amcenestrant (SAR439859)
    12ms
    AMEERA-1: Phase 1/2 Study of Amcenestrant (SAR439859) Single Agent and in Combination With Other Anti-cancer Therapies in Postmenopausal Women With Estrogen Receptor Positive Advanced Breast Cancer (clinicaltrials.gov)
    P1/2, N=136, Terminated, Sanofi | Trial completion date: Dec 2027 --> Nov 2024 | Active, not recruiting --> Terminated | Trial primary completion date: Dec 2027 --> Nov 2024; Sponsor decision to prematurely stop the study, not linked to any safety concern.
    Trial completion date • Trial termination • Trial primary completion date • Combination therapy • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    Ibrance (palbociclib) • everolimus • Piqray (alpelisib) • Verzenio (abemaciclib) • amcenestrant (SAR439859)
    1year
    Oral SERDs changing the scenery in hormone receptor positive breast cancer, a comprehensive review. (PubMed, Cancer Treat Rev)
    Oral SERDs constitute an exciting new drug class. Ongoing and future research will further refine the role of these drugs next to standard endocrine treatments and targeted therapies.
    Review • Journal
    |
    ER (Estrogen receptor) • CDK4 (Cyclin-dependent kinase 4)
    |
    HR positive • ER mutation • ESR1 mutation
    |
    fulvestrant • Orserdu (elacestrant) • amcenestrant (SAR439859) • Inluriyo (imlunestrant) • camizestrant (AZD9833) • giredestrant (RG6171) • rintodestrant (G1T48)
    over1year
    Randomized Phase III Study of Amcenestrant Plus Palbociclib Versus Letrozole Plus Palbociclib in Estrogen Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Advanced Breast Cancer: Primary Results From AMEERA-5. (PubMed, J Clin Oncol)
    The AMEERA-5 study was discontinued on the basis of the recommendation of the data monitoring committee at the interim futility analysis. No new safety signals were identified.
    P3 data • Journal • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    Ibrance (palbociclib) • letrozole • amcenestrant (SAR439859)
    over1year
    I-SPY2 Endocrine Optimization Pilot (EOP): Neoadjuvant amcenestrant +/- abemaciclib +/- letrozole in molecularly selected patients (pts) with HR+ HER2- stage 2/3 breast cancer (BC). (ASCO 2024)
    Six months of neoadjuvant endocrine therapy (NET) with the oral SERD amcenestrant is feasible, well-tolerated, and demonstrates anti-proliferative and anti-tumor activity in pre- and postmenopausal pts. NET provides a rich platform for biomarker discovery and investigating response to endocrine therapy.
    Clinical
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    MammaPrint
    |
    Verzenio (abemaciclib) • letrozole • amcenestrant (SAR439859)
    over1year
    AMEERA-3: Phase 2 Study of Amcenestrant (SAR439859) Versus Physician's Choice in Locally Advanced or Metastatic ER-positive Breast Cancer (clinicaltrials.gov)
    P2, N=367, Active, not recruiting, Sanofi | Trial completion date: Mar 2024 --> Sep 2024
    Trial completion date • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    ER positive • HER-2 negative
    |
    tamoxifen • fulvestrant • letrozole • anastrozole • exemestane • amcenestrant (SAR439859)
    almost2years
    Pharmacological insights on novel oral selective estrogen receptor degraders in breast cancer. (PubMed, Eur J Pharmacol)
    Fulvestrant is the first approved SERD with proven efficacy and good tolerability in clinical practice...Elacestrant is an orally bioavailable SERD that has been recently approved by the FDA for postmenopausal women with ER+, human epidermal growth factor receptor 2-negative (HER2-), estrogen receptor 1 (ESR1)-mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy. Other molecules of the same class currently tested in clinical trials are amcenestrant, giredestrant, camizestrant, and imlunestrant. The current review article offers a detailed pharmacological perspective of this emerging drug class, which may help with their possible future clinical applications.
    Review • Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    ER positive • HER-2 negative • HER-2 mutation • ESR1 mutation
    |
    fulvestrant • Orserdu (elacestrant) • amcenestrant (SAR439859) • Inluriyo (imlunestrant) • camizestrant (AZD9833) • giredestrant (RG6171)
    almost2years
    AMEERA-3: Phase 2 Study of Amcenestrant (SAR439859) Versus Physician's Choice in Locally Advanced or Metastatic ER-positive Breast Cancer (clinicaltrials.gov)
    P2, N=367, Active, not recruiting, Sanofi | Trial completion date: Dec 2023 --> Mar 2024
    Trial completion date • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    ER positive • HER-2 negative
    |
    tamoxifen • fulvestrant • letrozole • anastrozole • exemestane • amcenestrant (SAR439859)
    almost2years
    Evaluation of Orally Administered Amcenestrant (SAR439859) in Japanese Postmenopausal Patients With Advanced Breast Cancer (AMEERA-2) (clinicaltrials.gov)
    P1, N=10, Active, not recruiting, Sanofi | Trial completion date: Nov 2023 --> Nov 2024
    Trial completion date • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    amcenestrant (SAR439859)