^
    3d
    ZG005 combination hydrochloride gilteritinib tablets in patients with relapsed or refractory lymphoma: a multicentre, open-label, dose-exploration and dose-expansion phase I/II clinical study. (ChiCTR2500114728)
    P1/2, N=60, Recruiting, The First Affiliated Hospital of Zhejiang University School of Medicine; The First Affiliated Hospital of Zhejiang University School of Medicine
    New P1/2 trial
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    Xospata (gilteritinib) • giredestrant (RG6171) • nilvanstomig (ZG005) • ravoxertinib (RG7842)
    5d
    Optimizing dose selection in oncology: the rationale for the clinical dose selection of giredestrant, an oral selective estrogen receptor degrader. (PubMed, Expert Opin Investig Drugs)
    Data were leveraged from preclinical and phase I/II studies in metastatic and early breast cancer, as a single agent and with palbociclib, to inform giredestrant dose selection. Our learnings challenge the MTD paradigm in drug development, particularly in targeted therapies, and demonstrate the importance of basing dose selection on the totality of evidence, including preclinical data, and may help inform the clinical development of future targeted therapies.
    Journal
    |
    ER (Estrogen receptor)
    |
    ER positive
    |
    Ibrance (palbociclib) • giredestrant (RG6171)
    18d
    PREcoopERA: A Window-of-Opportunity Trial of Giredestrant +/- Triptorelin vs. Anastrozole + Triptorelin in Premenopausal Patients With ER-positive/HER2-negative Early Breast Cancer (clinicaltrials.gov)
    P2, N=231, Completed, ETOP IBCSG Partners Foundation | Recruiting --> Completed | Trial completion date: Jun 2026 --> Sep 2025 | Trial primary completion date: Jun 2026 --> Sep 2025
    Trial completion • Trial completion date • Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    ER positive • HER-2 negative
    |
    anastrozole • triptorelin • giredestrant (RG6171)
    22d
    A Study to Evaluate the Safety, Pharmacokinetics, and Activity of GDC-0587 as a Monotherapy and in Combination With Giredestrant in Participants With Locally Advanced or Metastatic Estrogen Receptor-Positive and Human Epidermal Growth Factor Receptor 2-Negative (ER+/HER2-) Breast Cancer (clinicaltrials.gov)
    P1, N=136, Recruiting, Genentech, Inc. | Not yet recruiting --> Recruiting
    Enrollment open • First-in-human
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    giredestrant (RG6171) • omeprazole
    25d
    Selective Estrogen Receptor Degraders Induce Bradycardia by Modulating Nuclear Estrogen Signaling. (PubMed, JACC Basic Transl Sci)
    Giredestrant and camizestrant induced significant bradycardia in wild-type zebrafish embryos, whereas fulvestrant and amcenestrant (SERDs that do not induce bradycardia in patients) did not alter heart rate. Mutations in gper, esr2a, and esr2b did not confer resistance to SERD-induced bradycardia, whereas esr1 mutant embryos were protected. These findings demonstrate that SERD-associated bradycardia is mediated through Esr1 signaling, supporting an on-target adverse effect.
    Journal
    |
    ER (Estrogen receptor)
    |
    ER positive • BRAF wild-type • ESR1 mutation
    |
    fulvestrant • amcenestrant (SAR439859) • camizestrant (AZD9833) • giredestrant (RG6171)
    1m
    MiRaDoR: A PoC Study to Evaluate Treatments' Efficacy by Monitoring MRD Using ctDNA in HR-positive/HER2-negative EBC Population (clinicaltrials.gov)
    P2, N=1260, Recruiting, MedSIR | Active, not recruiting --> Recruiting
    Enrollment open • Minimal residual disease • Circulating tumor DNA
    |
    HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
    |
    HR positive • HER-2 negative • PIK3CA mutation
    |
    Prosigna™ Breast Cancer Prognostic Gene Signature Assay • MammaPrint® • Oncotype DX Breast Recurrence Score®Test
    |
    Verzenio (abemaciclib) • Itovebi (inavolisib) • giredestrant (RG6171)
    1m
    MORPHEUS BC: A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Participants With Breast Cancer (clinicaltrials.gov)
    P1/2, N=316, Recruiting, Hoffmann-La Roche | Trial completion date: Nov 2027 --> May 2029 | Trial primary completion date: Nov 2027 --> May 2029
    Trial completion date • Trial primary completion date
    |
    ER (Estrogen receptor) • CDK4 (Cyclin-dependent kinase 4)
    |
    HER-2 positive • ER positive
    |
    Herceptin (trastuzumab) • Tecentriq (atezolizumab) • Ibrance (palbociclib) • everolimus • Verzenio (abemaciclib) • Kisqali (ribociclib) • ipatasertib (RG7440) • Itovebi (inavolisib) • giredestrant (RG6171) • Pegasys (pegylated interferon α -2a) • Phesgo (pertuzumab/trastuzumab/hyaluronidase-zzxf) • samuraciclib (CT7001)
    3ms
    A Study to Evaluate the Efficacy and Safety of Giredestrant in Combination With Phesgo (Pertuzumab, Trastuzumab, and Hyaluronidase-zzxf) Versus Phesgo in Participants With Locally Advanced or Metastatic Breast Cancer (heredERA Breast Cancer) (clinicaltrials.gov)
    P3, N=922, Active, not recruiting, Hoffmann-La Roche | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    ER positive • EGFR positive
    |
    paclitaxel • docetaxel • tamoxifen • giredestrant (RG6171) • Phesgo (pertuzumab/trastuzumab/hyaluronidase-zzxf)
    4ms
    A Study to Evaluate Efficacy and Safety of Giredestrant Compared With Fulvestrant (Plus a CDK4/6 Inhibitor), in Participants With ER-Positive, HER2-Negative Advanced Breast Cancer Resistant to Adjuvant Endocrine Therapy (pionERA Breast Cancer) (clinicaltrials.gov)
    P3, N=1050, Recruiting, Hoffmann-La Roche | Trial primary completion date: Jul 2026 --> Feb 2027
    Trial primary completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • CDK4 (Cyclin-dependent kinase 4)
    |
    ER positive • HER-2 negative • ESR1 mutation • HER-2 negative + ER positive • HER-2 negative + ER positive + ESR1 mutation
    |
    FoundationOne® Liquid CDx
    |
    Ibrance (palbociclib) • Verzenio (abemaciclib) • Kisqali (ribociclib) • fulvestrant • giredestrant (RG6171)
    4ms
    EndomERA: A Study of Giredestrant in Participants With Grade 1 Endometrial Cancer (clinicaltrials.gov)
    P2, N=30, Active, not recruiting, Hoffmann-La Roche | Trial completion date: Dec 2025 --> Jun 2026 | Trial primary completion date: Dec 2025 --> Jun 2026
    Trial completion date • Trial primary completion date
    |
    giredestrant (RG6171)
    4ms
    acelERA BC: A Study Evaluating the Efficacy and Safety of Giredestrant Compared With Physician's Choice of Endocrine Monotherapy in Participants With Previously Treated Estrogen Receptor-Positive, HER2-Negative Locally Advanced or Metastatic Breast Cancer (acelERA Breast Cancer) (clinicaltrials.gov)
    P2, N=303, Active, not recruiting, Hoffmann-La Roche | Trial completion date: Jun 2025 --> Aug 2027
    Trial completion date
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor)
    |
    ER positive • HER-2 negative • HER-2 negative + ER positive
    |
    fulvestrant • giredestrant (RG6171)
    4ms
    A Study to Evaluate the Safety, Pharmacokinetics, and Activity of GDC-0587 as a Monotherapy and in Combination With Giredestrant in Participants With Locally Advanced or Metastatic Estrogen Receptor-Positive and Human Epidermal Growth Factor Receptor 2-Negative (ER+/HER2-) Breast Cancer (clinicaltrials.gov)
    P1, N=136, Not yet recruiting, Genentech, Inc.
    New P1 trial
    |
    giredestrant (RG6171) • omeprazole