Giredestrant
Highest phase reached
Phase 3
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 3
- Drug type
- Small molecule
- Drug name
- Giredestrant
- Molecular weight
- 522.56
- Structure (SMILES)
- C[C@@H]1Cc2c([nH]c3ccccc23)[C@@H](c2c(F)cc(NC3CN(CCCF)C3)cc2F)N1CC(F)(F)CO
- 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
- CAS registry numbers
- 1953133-47-5
- ChEMBL ID
- CHEMBL4650316
- InChIKey
- GQCXHIKRWBIQMD-AKJBCIBTSA-N
- PubChem compound IDs
- 121410806
- FDA ingredient codes (UNII)
- 28P3DU6DB3
- First in class
- No
- Orphan designation
- No
- Pharmacology name
- giredestrant
- Type
- Synthetic organic
- Drug name stem
- -estr-; -estrant
- 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
- 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
- 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
- NCT03332797
- NCT03916744
- NCT04436744
- NCT04546009
- NCT04576455
- NCT04802759
- NCT04961996
- NCT05296798
- NCT05306340
- NCT05659563
- NCT05708235
- NCT05896566
- NCT04486352
- NCT05634499
- 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
- Recorded assays
- 201
- Active assays
- 13
Active assay types
- Confirmatory
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)
- 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 Phase 3
- Endometrial cancer Phase 2
- Neoplasm Phase 1
Targets (1)
- ESR1 Estrogen receptor alpha degrader