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Modality: Oral selective estrogen receptor degrader (SERD)
Disease State: ER+/HER2- breast cancer, ER+/HER2+ breast cancer
Summary
Giredestrant (RG6171, GDC-9545) is an investigational oral selective estrogen receptor degrader (SERD) that is designed to bind to the estrogen receptor (ER) and limit its function by outcompeting estrogen.[1-3] Giredestrant-bound ER was shown to remain in an inactive conformation and directed for proteasome-dependent degradation.
Clinical Trials
Giredestrant
| NCT ID | Study Phase | Enrollment Status | Study Title | |
|---|---|---|---|---|
| NCT06065748 | Phase III | Recruiting | 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) | View details |
| NCT04802759 | Recruiting | A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Participants With Breast Cancer | View details | |
| NCT05306340 | Phase III | Active, not recruiting | A Study Evaluating the Efficacy and Safety of Giredestrant Plus Everolimus Compared With the Physician's Choice of Endocrine Therapy Plus Everolimus in Participants With Estrogen Receptor-Positive, HER2-Negative, Locally Advanced or Metastatic Breast Cancer (evERA Breast Cancer) | View details |
| NCT05634499 | Phase II | Active, not recruiting | A Study of Giredestrant in Participants With Grade 1 Endometrial Cancer | View details |
| NCT04961996 | Phase III | Active, not recruiting | A Study Evaluating the Efficacy and Safety of Adjuvant Giredestrant Compared With Physician's Choice of Adjuvant Endocrine Monotherapy in Participants With Estrogen Receptor-Positive, HER2-Negative Early Breast Cancer (lidERA Breast Cancer) | View details |
| NCT04546009 | Phase III | Active, not recruiting | A Study Evaluating the Efficacy and Safety of Giredestrant Combined With Palbociclib Compared With Letrozole Combined With Palbociclib in Participants With Estrogen Receptor-Positive, HER2-Negative Locally Advanced or Metastatic Breast Cancer (persevERA Breast Cancer) | View details |
| NCT04576455 | Phase II | Active, not recruiting | 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) | View details |
| NCT05296798 | Phase III | Active, not recruiting | 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) | View details |
| NCT07100106 | Recruiting | A Study to Evaluate the Effect of GDC-4198 Alone and in Combination With Giredestrant Versus Abemaciclib and Giredestrant in Participants With Locally Advanced or Metastatic Estrogen Receptor-Positive (ER+), Human Epidermal Growth Factor Receptor-Negative (HER2-) Breast Cancer | View details | |
Proposed Mechanism of Action
Giredestrant (RG6171, GDC-9545) is an investigational selective estrogen receptor degrader (SERD) that is designed to bind to the estrogen receptor (ER) and limit its function by outcompeting estrogen.[1-3] It is thought that giredestrant-bound ER changes the shape of the receptor in such a way that the cell eliminates it by degradation.
ER, estrogen receptor; HR, hormone receptor; mTOR, mammalian target of rapamycin; PIP2, phosphatidylinositol (4,5)-bisphosphate; PIP3, phosphatidylinositol (3,4,5)-trisphosphate; RTK, receptor tyrosine kinase; SERD, selective estrogen receptor degrader
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