Search
For optimal search results, please limit to 2 product keywords
If you are searching for information related to a product:
- For optimal results, please enter at least 2 search terms in addition to product name
- Example: [product name] [search term] [search term]
- Example: Product + clinical trials
- For an exact match, please include search terms in double quotations. For example: "Elevatum"
Other names: RG6171; RO7197597; GDC-9545
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 | |
|---|---|---|---|---|
| NCT07100106 | Phase I / Phase II | 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 |
| 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 |
| NCT07541079 | Phase III | Recruiting | A Study Evaluating Adherence, Tolerability, and Patient Reported Outcomes of Giredestrant in Participants With ER+/HER2- Early Breast Cancer Who Are Intolerant to Adjuvant Aromatase Inhibitor Therapy (novERA 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 |
| 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 |
| 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 |
| 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 |
Proposed Mechanism of Action
Giredestrant (RG6171, GDC-9545) is an investigational, orally bioavailable, non-steroidal, selective estrogen receptor degrader (SERD) and antagonist. The molecule is designed to bind to the estrogen receptor (ER) and outcompeting estradiol. Through this action, giredestrant may block the assembly of ER transcription factors and immobilizes the receptor. As a consequence of this ER immobilization, the receptor undergoes a conformational change that causes ubiquitination, resulting in the elimination of the ER via proteosomes as seen in preclinical models. Ultimately, this process suppresses ER-mediated signaling, stops the transcription of ER target genes, and suppresses cellular proliferation.
CBP=CREB-binding protein; CCND1=Cyclin D1 gene; DNA=Deoxyribonucleic acid; E2F=E2F transcription factors; GREB1=Growth regulation by estrogen in breast cancer 1; GRIP-1=Glucocorticoid receptor-interacting protein 1; p300=E1A-binding protein p300; PGR=Progesterone receptor; Rb=Retinoblastoma protein; SRC=Steroid receptor coactivator; TFF1=Trefoil factor 1
Looking for more information?
Reach out to a Genentech Medical Science Liaison near you, or connect with the contact center.
Call the Trial Information Support Team: 1-888-662-6728 Hours: Monday-Friday, 5am-5pm PT