> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/giredestrant-c67ceef7-88fc-49f5-b635-5568fc80cd3c
> Record changed: 2026-10-13

# Giredestrant

Highest phase reached

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650316)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650316)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650316)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650316)

**Drug name**

Giredestrant

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650316)

**Molecular weight**

522.56

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650316)

**Structure (SMILES)**

C\[C@@H\]1Cc2c(\[nH\]c3ccccc23)\[C@@H\](c2c(F)cc(NC3CN(CCCF)C3)cc2F)N1CC(F)(F)CO

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650316)

### Other names (17)

- abemaciclib 150 mg giredestrant 30 mg
- gdc 9545
- Gdc-9545
- GDC-9545
- GDC-9545 Solution for Infusion
- giredestrant
- Giredestrant
- giredestrant \[INN\]
- GIREDESTRANT \[USAN\]
- Giredestrant \[WHO-DD\]
- giredestrant inn
- giredestrant usan
- giredestrant who dd
- ro 7197597
- RO-7197597
- ro7197597
- RO7197597

## Identifiers

**CAS registry numbers**

- 1953133-47-5

**ChEMBL ID**

CHEMBL4650316

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650316)

**InChIKey**

GQCXHIKRWBIQMD-AKJBCIBTSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650316)

**PubChem compound IDs**

- 121410806

**FDA ingredient codes (UNII)**

- 28P3DU6DB3

## Regulatory information

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

## Pharmacology

### Drug classification

**Pharmacology name**

giredestrant

**Type**

Synthetic organic

**Drug name stem**

\-estr-; -estrant

### Mechanisms of action (2)

- **Action**  
Antagonist

**Action type**  
Antagonist

**Target**  
Estrogen receptor-α

**Gene symbol**  
ESR1

**Protein identifier**  
P03372

**Median affinity**

10.3

**Affinity units**  
pIC50
- **Mechanism**  
Estrogen receptor alpha degrader

**Action type**  
DEGRADER

**Target**  
Estrogen receptor

**Protein identifier**  
P03372

### Open Targets mechanisms

- **Mechanism**  
Estrogen receptor alpha degrader

**Action type**  
DEGRADER

**Target**  
Estrogen receptor

### Investigated indications (3)

- **Condition**  
Neoplasms

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369
- **Condition**  
Breast Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
MONDO:0007254

**Subject identifier**  
D001943
- **Condition**  
Endometrial Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0011962

**Subject identifier**  
D016889

### Open Targets indications (7)

- **Condition identifier**  
EFO\_0000616
- **Condition identifier**  
MONDO\_0002229

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005070
- **Condition identifier**  
MONDO\_0006512

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0007254

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0011962

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0021092

**Highest recorded phase**  
2

### Trial references (14)

- NCT03332797  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03332797)
- NCT03916744  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03916744)
- NCT04436744  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04436744)
- NCT04546009  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04546009)
- NCT04576455  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04576455)
- NCT04802759  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04802759)
- NCT04961996  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04961996)
- NCT05296798  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05296798)
- NCT05306340  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05306340)
- NCT05659563  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05659563)
- NCT05708235  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05708235)
- NCT05896566  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05896566)
- NCT04486352  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04486352)
- NCT05634499  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05634499)

## Chemical properties

**Hydrogen bond acceptors**

4

**Hydrogen bond donors**

3

**Polar surface area**

54.53

**Calculated partition coefficient (ALogP)**

4.87

**Calculated partition coefficient (XLogP)**

4.8

**Prodrug**

No

**Chirality**

Single enantiomer

**Inorganic**

No

**Rule-of-five violations**

1

**Rotatable bonds**

9

**Heavy atoms**

37

**Molecular formula**

C27H31F5N4O

**Monoisotopic mass**

522.24180244

**Natural product**

No

## Evidence counts

**Recorded assays**

201

**Active assays**

13

### Active assay types

- Confirmatory

## Biological measurements

These details could not be displayed.

## Related records

### Trials (24)

- A PoC Study to Evaluate Treatments' Efficacy by Monitoring MRD Using ctDNA in HR-positive/HER2-negative EBC Population
- 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)
- 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)
- A Study Evaluating the Efficacy and Safety of Biomarker-Driven Therapies in Patients With Persistent or Recurrent Rare Epithelial Ovarian Tumors
- 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)
- 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)
- 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)
- A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Participants With Breast Cancer
- A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Patients With Metastatic or Locally Advanced Breast Cancer
- A Study of GDC-9545 Alone or in Combination With Palbociclib and/or Luteinizing Hormone-Releasing Hormone (LHRH) Agonist in Locally Advanced or Metastatic Estrogen Receptor-Positive Breast Cancer
- A Study of Giredestrant (GDC-9545) in Postmenopausal Women With Stage I-III Operable, Estrogen Receptor-Positive Breast Cancer
- A Study of Giredestrant in Participants With Grade 1 Endometrial Cancer
- A Study of Targeted Agents for Patients With Recurrent or Persistent Endometrial Cancer
- [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)](https://trialight.com/data/trial/a-study-to-evaluate-efficacy-and-safety-of-giredestrant-8ed24989-15f7-4e80-bfbc-75c0b49f45cd.md)
- 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
- 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)
- A Study to Evaluate the Efficacy, Safety, and Pharmacokinetics of Giredestrant Plus Palbociclib Compared With Anastrozole Plus Palbociclib for Postmenopausal Women With Estrogen Receptor-Positive and HER2-Negative Untreated Early Breast Cancer (coopERA Breast Cancer)
- 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
- A Window-of-Opportunity Trial of Giredestrant +/- Triptorelin vs. Anastrozole + Triptorelin in Premenopausal Patients With ER-positive/HER2-negative Early Breast Cancer
- Evaluation of the Relative Bioavailability and Food Effect of GDC-9545 in Healthy Females of Non-Childbearing Potential

### In development for (3)

- [Breast cancer](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md) Phase 3
- [Endometrial cancer](https://trialight.com/data/condition/endometrial-cancer-4da2a0bc-7943-502b-a698-cc2beccbed8c.md) Phase 2
- Neoplasm Phase 1

### Targets (1)

- [ESR1](https://trialight.com/data/target/esr1-e58c882c-75fc-5507-bf76-2d7a172c0a28.md) Estrogen receptor alpha degrader

---

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