enzalutamide Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| non-steroid antiandrogens | 4628 | 915087-33-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Enzalutamide is an androgen receptor inhibitor that acts on different steps in the androgen receptor signaling pathway. Enzalutamide has been shown to competitively inhibit androgen binding to androgen receptors and inhibit androgen receptor nuclear translocation and interaction with DNA. A major metabolite, N‑desmethyl enzalutamide, exhibited similar in vitro activity to enzalutamide. Enzalutamide decreased proliferation and induced cell death of prostate cancer cells in vitro, and decreased tumor volume in a mouse prostate cancer xenograft model.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.16 | g | O |
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 31, 2012 | FDA | ASTELLAS | |
| March 24, 2014 | PMDA | Astellas Pharma Inc |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L02BB04 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Anti-androgens |
| FDA MoA | N0000000243 | Androgen Receptor Antagonists |
| FDA EPC | N0000175560 | Androgen Receptor Inhibitor |
| FDA MoA | N0000185506 | Cytochrome P450 3A4 Inducers |
| FDA MoA | N0000185507 | Cytochrome P450 2C9 Inducers |
| FDA MoA | N0000185607 | Cytochrome P450 2C19 Inducers |
| CHEBI has role | CHEBI:35497 | antiandrogen |
| CHEBI has role | CHEBI:35610 | cytostatic |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Metastasis from malignant tumor of prostate | indication | 314994000 | |
| Malignant tumor of prostate | indication | 399068003 | DOID:10283 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.88 | acidic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 40MG | XTANDI | ASTELLAS | N203415 | Aug. 31, 2012 | RX | CAPSULE | ORAL | July 13, 2021 | TREATMENT OF PATIENTS WITH NON-METASTATIC CASTRATION-RESISTANT PROSTATE CANCER |
| 40MG | XTANDI | ASTELLAS | N213674 | Aug. 4, 2020 | RX | TABLET | ORAL | July 13, 2021 | TREATMENT OF PATIENTS WITH NON-METASTATIC CASTRATION-RESISTANT PROSTATE CANCER |
| 80MG | XTANDI | ASTELLAS | N213674 | Aug. 4, 2020 | RX | TABLET | ORAL | July 13, 2021 | TREATMENT OF PATIENTS WITH NON-METASTATIC CASTRATION-RESISTANT PROSTATE CANCER |
| 40MG | XTANDI | ASTELLAS | N203415 | Aug. 31, 2012 | RX | CAPSULE | ORAL | Dec. 16, 2022 | TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) |
| 40MG | XTANDI | ASTELLAS | N213674 | Aug. 4, 2020 | RX | TABLET | ORAL | Dec. 16, 2022 | TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) |
| 80MG | XTANDI | ASTELLAS | N213674 | Aug. 4, 2020 | RX | TABLET | ORAL | Dec. 16, 2022 | TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Androgen receptor | Nuclear hormone receptor | ANTAGONIST | EC50 | 7.31 | CHEMBL | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D10218 | KEGG_DRUG |
| 4031716 | VUID |
| N0000185726 | NUI |
| 4031716 | VANDF |
| C3496793 | UMLSCUI |
| CHEBI:68534 | CHEBI |
| CHEMBL1082407 | ChEMBL_ID |
| DB08899 | DRUGBANK_ID |
| C540278 | MESH_SUPPLEMENTAL_RECORD_UI |
| 15951529 | PUBCHEM_CID |
| 6812 | IUPHAR_LIGAND_ID |
| 9621 | INN_ID |
| 93T0T9GKNU | UNII |
| 1307298 | RXNORM |
| 192757 | MMSL |
| 28802 | MMSL |
| d07900 | MMSL |
| 014630 | NDDF |
| 703125003 | SNOMEDCT_US |
| 703684000 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Xtandi | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0469-0125 | CAPSULE | 40 mg | ORAL | NDA | 28 sections |
| Xtandi | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0469-0625 | TABLET | 40 mg | ORAL | NDA | 28 sections |
| Xtandi | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0469-0725 | TABLET | 80 mg | ORAL | NDA | 28 sections |