darolutamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| non-steroid antiandrogens | 5334 | 1297538-32-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Darolutamide is an androgen receptor (AR) inhibitor. Darolutamide competitively inhibits androgen binding, AR nuclear translocation, and AR-mediated transcription. A major metabolite, keto-darolutamide, exhibited similar in vitro activity to darolutamide. In addition, darolutamide functioned as a progesterone receptor (PR) antagonist in vitro (approximately 1% activity compared to AR). Darolutamide decreased prostate cancer cell proliferation in vitro and tumor volume in mouse xenograft models of prostate cancer
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.20 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.01 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 27, 2020 | EMA | Bayer AG | |
| July 30, 2019 | FDA | BAYER HEALTHCARE PHARMACEUTICALS INC | |
| Jan. 23, 2020 | PMDA | Bayer Yakuhin, Ltd |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Prostatic specific antigen increased | 174.32 | 34.12 | 45 | 803 | 14635 | 34941448 |
| Metastases to bone | 48.58 | 34.12 | 16 | 832 | 11954 | 34944129 |
| Fatigue | 35.60 | 34.12 | 44 | 804 | 370609 | 34585474 |
| Off label use | 34.35 | 34.12 | 46 | 802 | 419478 | 34536605 |
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 |
|---|---|---|---|---|---|---|
| Prostatic specific antigen increased | 145.73 | 35.72 | 29 | 525 | 10357 | 79733477 |
| Off label use | 39.38 | 35.72 | 39 | 515 | 907176 | 78836658 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L02BB06 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Anti-androgens |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Metastatic prostate cancer | indication | 94503003 | |
| Hormone refractory prostate cancer | indication | 427492003 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.99 | acidic |
| pKa2 | 12.59 | acidic |
| pKa3 | 1.18 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 300MG | NUBEQA | BAYER HEALTHCARE | N212099 | July 30, 2019 | RX | TABLET | ORAL | 9657003 | Oct. 27, 2030 | TREATMENT OF PATIENTS WITH NON-METASTATIC CASTRATION RESISTANT PROSTATE CANCER |
| 300MG | NUBEQA | BAYER HEALTHCARE | N212099 | July 30, 2019 | RX | TABLET | ORAL | 8975254 | March 25, 2033 | TREATMENT OF PATIENTS WITH NON-METASTATIC CASTRATION RESISTANT PROSTATE CANCER |
| 300MG | NUBEQA | BAYER HEALTHCARE | N212099 | July 30, 2019 | RX | TABLET | ORAL | 10835515 | Jan. 28, 2036 | TREATMENT OF PATIENTS WITH NON-METASTATIC CASTRATION RESISTANT PROSTATE CANCER |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 300MG | NUBEQA | BAYER HEALTHCARE | N212099 | July 30, 2019 | RX | TABLET | ORAL | July 30, 2024 | NEW CHEMICAL ENTITY |
| 300MG | NUBEQA | BAYER HEALTHCARE | N212099 | July 30, 2019 | RX | TABLET | ORAL | Aug. 5, 2025 | TREATMENT OF ADULT PATIENTS WITH METASTATIC HORMONE‐SENSITIVE PROSTATE CANCER (MHSPC) IN COMBINATION WITH DOCETAXEL |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Androgen receptor | Nuclear hormone receptor | INHIBITOR | IC50 | 7.19 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Progesterone receptor | Nuclear hormone receptor | ANTAGONIST | DRUG LABEL | ||||||
| Androgen receptor | Transcription factor | ANTAGONIST | Ki | 7.96 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| X05U0N2RCO | UNII |
| C4547776 | UMLSCUI |
| CHEMBL4297185 | ChEMBL_ID |
| 67171867 | PUBCHEM_CID |
| DB12941 | DRUGBANK_ID |
| D11045 | KEGG_DRUG |
| 10227 | INN_ID |
| 10439 | IUPHAR_LIGAND_ID |
| 018070 | NDDF |
| 789148001 | SNOMEDCT_US |
| 789166006 | SNOMEDCT_US |
| 4038612 | VANDF |
| 2180325 | RXNORM |
| 321167 | MMSL |
| 37249 | MMSL |
| d09337 | MMSL |
| C000607739 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| NUBEQA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50419-395 | TABLET, FILM COATED | 300 mg | ORAL | NDA | 29 sections |
| NUBEQA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50419-395 | TABLET, FILM COATED | 300 mg | ORAL | NDA | 29 sections |
| NUBEQA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50419-395 | TABLET, FILM COATED | 300 mg | ORAL | NDA | 29 sections |