Elacestrant
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2023
- First approval year
- 2023
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Elacestrant
- Molecular weight
- 458.65
- Structure (SMILES)
- CCNCCc1ccc(CN(CC)c2cc(OC)ccc2[C@@H]2CCc3cc(O)ccc3C2)cc1
- elacestrant
- Elacestrant
- elacestrant [INN]
- Elacestrant [MI]
- ELACESTRANT [USAN]
- Elacestrant [WHO-DD]
- elacestrant inn
- elacestrant mi
- elacestrant usan
- elacestrant who dd
- er 306323
- ER-306323
- rad 1901
- RAD-1901
- rad1901
- Rad1901
- RAD1901
- CAS registry numbers
- 722533-56-4
- ChEMBL ID
- CHEMBL4297509
- InChIKey
- SIFNOOUKXBRGGB-AREMUKBSSA-N
- PubChem compound IDs
- 23642301
- RxNorm IDs (RxCUI)
- 2628469
- FDA ingredient codes (UNII)
- FM6A2627A8
- L02BA
- L02BA04
Sources for recorded values
- Applicant
- STEMLINE THERAP
- Approval date
- 27 Jan 2023
- Application number
- NDA217639
- Status
- Authorised
- Status date
- 15 Sept 2023
- Authorisation date
- 15 Sept 2023
- Approved indications
- Orserdu monotherapy is indicated for the treatment of postmenopausal women, and men, with estrogen receptor (ER) positive, HER2-negative, locally advanced or metastatic breast cancer with an activating ESR1 mutation who have disease progression following at least one line of endocrine therapy including a CDK 4/6 inhibitor.
- Product number
- EMEA/H/C/005898
- Authorisation holder
- Stemline Therapeutics B.V.
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- Yes
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Breast Neoplasms
European medicines record
- Patents
- 0
- Designations
- 2
- First in class
- No
- Fast track
- Yes
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- United States (FDA)
- Approved
- European Union (EMA)
- Authorised
- Pharmacology name
- elacestrant
- Type
- Synthetic organic
- Drug name stem
- -estr-; -estrant
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
Mechanisms of action
- 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
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000305
- Subject identifier
- D001943
- Condition
- Carcinoma, Intraductal, Noninfiltrating
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000432
- Subject identifier
- D002285
- Condition
- Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003869
- Subject identifier
- D001943
- Condition
- Hot Flashes
- Highest recorded phase
- 2
- Condition identifier
- HP:0031217
- Subject identifier
- D019584
- Condition
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0007254
- Subject identifier
- D001943
- Condition identifier
- EFO_0000305
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0003869
- Condition identifier
- EFO_1000649
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000650
- Highest recorded phase
- 2
- Condition identifier
- HP_0031217
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005023
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005210
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0007254
- Condition identifier
- MONDO_0007254
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0011962
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0021100
- Highest recorded phase
- 4
- Event
- disease progression
- Reports
- 296
- Reporting signal score
- 1,084.47
- Event
- drug intolerance
- Reports
- 15
- Reporting signal score
- 8.66005
- Event
- dyspepsia
- Reports
- 12
- Reporting signal score
- 10.3105
- Event
- dysphagia
- Reports
- 12
- Reporting signal score
- 6.3059
- Event
- dyspnoea
- Reports
- 4
- Reporting signal score
- 8.38848
- Event
- foreign body in throat
- Reports
- 4
- Reporting signal score
- 17.9424
- Event
- headache
- Reports
- 4
- Reporting signal score
- 8.29107
- Event
- hospice care
- Reports
- 22
- Reporting signal score
- 78.118
- Event
- hospitalisation
- Reports
- 16
- Reporting signal score
- 8.68825
- Event
- illness
- Reports
- 9
- Reporting signal score
- 14.9014
- Event
- malignant neoplasm progression
- Reports
- 11
- Reporting signal score
- 7.49036
- Event
- metastases to bone
- Reports
- 8
- Reporting signal score
- 14.1109
- Event
- nausea
- Reports
- 81
- Reporting signal score
- 41.6888
- Event
- positron emission tomogram abnormal
- Reports
- 2
- Reporting signal score
- 7.64616
- Event
- pyrexia
- Reports
- 1
- Reporting signal score
- 9.83858
- Event
- salivary hyposecretion
- Reports
- 1
- Reporting signal score
- 7.36255
- Event
- tumour marker increased
- Reports
- 12
- Reporting signal score
- 41.0652
- Event
- vomiting
- Reports
- 32
- Reporting signal score
- 6.10383
- NCT00875420
- NCT02653417
- NCT02338349
- NCT02650817
- NCT03778931
- NCT04791384
- NCT05512364
- NCT05618613
- NCT04797728
- NCT06075953
- Dose
- 345 mg
- Route
- Oral
- How often
- Once daily
Conditions of use
- Take with food
- Hydrogen bond acceptors
- 4
- Hydrogen bond donors
- 2
- Polar surface area
- 44.73
- Calculated partition coefficient (ALogP)
- 5.85
- Calculated partition coefficient (XLogP)
- 6.3
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 10
- Heavy atoms
- 34
- Molecular formula
- C30H38N2O2
- Monoisotopic mass
- 458.293328459
- Natural product
- No
- 72187-0101
- 72187-0102
- Recorded assays
- 167
- Active assays
- 50
Active assay types
- Confirmatory
- Antineoplastic Agents
Related records
Trials (38)
- A First-in-Human Study of MEN2312 in Adults With Advanced Breast Cancer
- A Phase 2 Bridging Study of Elacestrant Monotherapy in Advanced or Metastatic Breast Cancer
- A Phase I, Multicenter, Open-Label, Multi-Part, Dose-escalation Study of RAD1901 in Postmenopausal Women With Advanced Estrogen Receptor Positive and HER2-Negative Breast Cancer
- A Rollover Protocol of Elacestrant, in Combination With Onapristone, for Patients With ER+, PR+, HER2- Advanced or Metastatic Breast Cancer
- A Short-term Preoperative, Evaluating Activity and Safety of Elacestrant Monotherapy as Compared to Elacestrant + Ovarian Function Suppression (LHRH Agonist) in Premenopausal Patients With Stage I-II ER+/HER2- Breast Cancer
- A Study of Elacestrant Alone or in Combination With Abemaciclib in People With Endometrial Cancer
- A Study of Elacestrant Versus Standard Endocrine Therapy in Women and Men With ER+,HER2-, Early Breast Cancer With High Risk of Recurrence
- A Study to Evaluate the Effects of RAD1901 in the Treatment of Vasomotor Symptoms in Postmenopausal Women
- BGB-43395 Alone or as Part of Combination Therapies in Participants With Breast Cancer and Other Advanced Solid Tumors
- Circulating Tumor DNA
- DCIS: RECAST Trial Ductal Carcinoma In Situ: Re-Evaluating Conditions for Active Surveillance Suitability as Treatment
- Elacestrant + Everolimus in Patients ER+/HER2-, ESR1mut, Advanced Breast Cancer Progressing to ET and CDK4/6i.
- Elacestrant and Exemestane for Patients With Pretreated HR+/HER2- Metastatic Breast Cancer and [18F] FES-avid Lesions (COMBINE)
- Elacestrant for Treating ER+/HER2- Breast Cancer Patients With ctDNA Relapse (TREAT ctDNA)
- Elacestrant in Advanced Triple Positive Breast Cancer
- Elacestrant in Patients With ER+ HER2- ESR1-mutated Locally Advanced or Metastatic Breast Cancer
- Elacestrant in Preoperative Setting, a Window of Opportunity Study
- ELACESTRANT in Women and Men With CDK4/6 Inhibitor-Naive Estrogen Receptor Positive, HER-2 Negative Metastatic Breast Cancer Study
- Elacestrant vs Elacestrant Plus a CDK4/6 Inhibitor in Patients With ERpositive/HER2-negative Advanced or Metastatic Breast Cancer
- Elacestrant With Everolimus for the Treatment of Recurrent Advanced or Metastatic ER-Positive Endometrial Cancer
In development for (10)
- Breast cancer Phase 3
- Breast carcinoma Phase 3
- Breast neoplasm Phase 3
- Cancer Phase 1
- Ductal breast carcinoma in situ Phase 2
- Endometrial cancer Phase 2
- Estrogen-receptor negative breast cancer Phase 2
- Estrogen-receptor positive breast cancer Phase 2
- Neoplasm Phase 3
- Uterine corpus sarcoma Phase 2
Targets (1)
- ESR1 Estrogen receptor alpha degrader