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elacestrant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| estrogen antagonists, including estrogen receptor down-regulators | 5710 | 722533-56-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Elacestrant is an estrogen receptor antagonist that binds to estrogen receptor-alpha (ERalfa). In ER-positive (ER+) HER2-negative (HER2-) breast cancer cells, elacestrant inhibited 17beta-estradiol mediated cell proliferation at concentrations inducing degradation of ERalfa protein mediated through proteasomal pathway. Elacestrant demonstrated in vitro and in vivo antitumor activity including in ER+ HER2- breast cancer models resistant to fulvestrant and cyclin-dependent kinase 4/6 inhibitors and those harboring estrogen receptor 1 gene (ESR1) mutations.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.727 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 22.182 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.724 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 13.459 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.090 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 1.330 | % | High | 1 |
| herg | hERG pIC50 | 5.271 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 7.379 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 11.722 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.200 | % | High | 1 |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 9.484 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 77.446 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.130 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 32.285 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 0.960 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.080 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 50.119 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 0.300 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.140 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 4.140 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 27, 2023 | FDA | STEMLINE THERAPEUTICS INC | |
| Sept. 15, 2023 | EMA | Stemline Therapeutics B.V. |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Disease progression | 1219.50 | 48.69 | 305 | 1049 | 156310 | 90470783 |
| Death | 347.66 | 48.69 | 156 | 1198 | 456395 | 90170698 |
| Nausea | 108.33 | 48.69 | 105 | 1249 | 1110211 | 89516882 |
| Hospice care | 104.13 | 48.69 | 25 | 1329 | 9679 | 90617414 |
| Tumour marker increased | 57.33 | 48.69 | 14 | 1340 | 5793 | 90621300 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Disease progression | 1085.88 | 52.14 | 286 | 938 | 243748 | 110344327 |
| Death | 326.67 | 52.14 | 155 | 1069 | 698714 | 109889361 |
| Hospice care | 105.37 | 52.14 | 25 | 1199 | 12448 | 110575627 |
| Nausea | 88.01 | 52.14 | 86 | 1138 | 1235604 | 109352471 |
| Tumour marker increased | 63.44 | 52.14 | 14 | 1210 | 5046 | 110583029 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L02BA04 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Anti-estrogens |
| MeSH PA | D000970 | Antineoplastic Agents |
| FDA MoA | N0000000145 | Estrogen Receptor Antagonists |
| FDA EPC | N0000175582 | Estrogen Receptor Antagonist |
| FDA MoA | N0000185503 | P-Glycoprotein Inhibitors |
| FDA MoA | N0000190113 | Breast Cancer Resistance Protein Inhibitors |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:50751 | anti-estrogen |
| CHEBI has role | CHEBI:50792 | estrogen receptor antagonist |
Related Drugs by ATC class:
L02BA Anti-estrogens 3 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Estrogen receptor positive advanced or metastatic breast cancer | indication | 254837009 | DOID:1612 |
| HER2-negative advanced or metastatic breast cancer | indication | 254837009 | DOID:1612 |
| ESR1-mutated advanced or metastatic breast cancer | indication | 254837009 | DOID:1612 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 86MG BASE | ORSERDU | STEMLINE THERAP | N217639 | Jan. 27, 2023 | RX | TABLET | ORAL | 7612114 | Aug. 18, 2026 | TREATMENT OF AN ER-POSITIVE BREAST CANCER |
| EQ 86MG BASE | ORSERDU | STEMLINE THERAP | N217639 | Jan. 27, 2023 | RX | TABLET | ORAL | 10071066 | Oct. 10, 2034 | TREATMENT OF AN ER-POSITIVE BREAST CANCER FOLLOWING AT LEAST ONE LINE OF ENDOCRINE THERAPY |
| EQ 86MG BASE | ORSERDU | STEMLINE THERAP | N217639 | Jan. 27, 2023 | RX | TABLET | ORAL | 11779552 | Oct. 10, 2034 | TREATMENT OF AN ER-POSITIVE BREAST CANCER FOLLOWING AT LEAST ONE LINE OF ENDOCRINE THERAPY |
| EQ 86MG BASE | ORSERDU | STEMLINE THERAP | N217639 | Jan. 27, 2023 | RX | TABLET | ORAL | 10420734 | Oct. 3, 2036 | TREATMENT OF AN ER-POSITIVE BREAST CANCER FOLLOWING AT LEAST ONE LINE OF ENDOCRINE THERAPY |
| EQ 86MG BASE | ORSERDU | STEMLINE THERAP | N217639 | Jan. 27, 2023 | RX | TABLET | ORAL | 11819480 | Feb. 28, 2037 | TREATMENT OF AN ER-POSITIVE BREAST CANCER |
| EQ 86MG BASE | ORSERDU | STEMLINE THERAP | N217639 | Jan. 27, 2023 | RX | TABLET | ORAL | 10745343 | Jan. 5, 2038 | TREATMENT OF AN ER-POSITIVE BREAST CANCER |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 86MG BASE | ORSERDU | STEMLINE THERAP | N217639 | Jan. 27, 2023 | RX | TABLET | ORAL | Jan. 27, 2028 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Estrogen receptor | Nuclear hormone receptor | ANTAGONIST | IC50 | 7.32 | DRUG LABEL | DRUG LABEL | |||
| Estrogen receptor beta | Nuclear hormone receptor | ANTAGONIST | IC50 | 6.06 | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| CHEBI:229213 | CHEBI |
| CHEMBL4297509 | ChEMBL_ID |
| C000626176 | MESH_SUPPLEMENTAL_RECORD_UI |
| 12339 | IUPHAR_LIGAND_ID |
| DB06374 | DRUGBANK_ID |
| 43186711000001103 | SNOMEDCT_US |
| 43186811000001106 | SNOMEDCT_US |
| 4042013 | VANDF |
| C4682404 | UMLSCUI |
| I0V | PDB_CHEM_ID |
| CHEMBL4594273 | ChEMBL_ID |
| 10247 | INN_ID |
| 23642301 | PUBCHEM_CID |
| 364875 | MMSL |
| 41206 | MMSL |
| d09981 | MMSL |
| 019283 | NDDF |
| 019284 | NDDF |
| D11671 | KEGG_DRUG |
| FM6A2627A8 | UNII |
| 2628469 | RXNORM |
| C000626184 | MESH_SUPPLEMENTAL_RECORD_UI |
| FM6A2627A8 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| ORSERDU | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72187-0101 | TABLET, FILM COATED | 86 mg | ORAL | NDA | 27 sections |
| ORSERDU | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72187-0102 | TABLET, FILM COATED | 345 mg | ORAL | NDA | 27 sections |