apalutamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| non-steroid antiandrogens | 5278 | 956104-40-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Apalutamide is an Androgen Receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR. Apalutamide inhibits AR nuclear translocation, inhibits DNA binding, and impedes AR-mediated transcription. A major metabolite, N-desmethyl apalutamide, is a less potent inhibitor of AR, and exhibited one-third the activity of apalutamide in an in vitro transcriptional reporter assay. Apalutamide administration caused decreased tumor cell proliferation and increased apoptosis leading to decreased tumor volume in mouse xenograft models of prostate cancer.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.24 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 14, 2019 | EMA | JANSSEN-CILAG INTERNATIONAL N.V. | |
| Feb. 14, 2018 | FDA | JANSSEN BIOTECH | |
| March 26, 2019 | PMDA | Janssen Pharmaceutical K.K. |
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 |
|---|---|---|---|---|---|---|
| Rash | 528.50 | 23.81 | 380 | 5834 | 222372 | 34728345 |
| Hot flush | 293.54 | 23.81 | 113 | 6101 | 17953 | 34932764 |
| Death | 285.09 | 23.81 | 349 | 5865 | 397700 | 34553017 |
| Prostatic specific antigen increased | 179.91 | 23.81 | 75 | 6139 | 14605 | 34936112 |
| Fatigue | 109.41 | 23.81 | 217 | 5997 | 370436 | 34580281 |
| Therapy cessation | 69.11 | 23.81 | 41 | 6173 | 16932 | 34933785 |
| Hospitalisation | 68.16 | 23.81 | 66 | 6148 | 56836 | 34893881 |
| Dermatitis exfoliative generalised | 66.61 | 23.81 | 25 | 6189 | 3682 | 34947035 |
| Fall | 49.18 | 23.81 | 110 | 6104 | 202775 | 34747942 |
| Interstitial lung disease | 48.73 | 23.81 | 59 | 6155 | 65223 | 34885494 |
| Decreased appetite | 38.91 | 23.81 | 89 | 6125 | 166303 | 34784414 |
| Prostate cancer metastatic | 31.69 | 23.81 | 17 | 6197 | 5786 | 34944931 |
| Drug eruption | 31.46 | 23.81 | 27 | 6187 | 19871 | 34930846 |
| Therapy interrupted | 28.89 | 23.81 | 22 | 6192 | 13675 | 34937042 |
| Hypertension | 28.62 | 23.81 | 70 | 6144 | 136373 | 34814344 |
| Blood thyroid stimulating hormone increased | 27.63 | 23.81 | 14 | 6200 | 4241 | 34946476 |
| Prostatic specific antigen decreased | 26.10 | 23.81 | 6 | 6208 | 155 | 34950562 |
| Metastases to bone | 24.75 | 23.81 | 19 | 6195 | 11951 | 34938766 |
| Rash erythematous | 24.43 | 23.81 | 26 | 6188 | 24951 | 34925766 |
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 |
|---|---|---|---|---|---|---|
| Rash | 241.90 | 25.27 | 215 | 3938 | 578143 | 79162092 |
| Death | 200.36 | 25.27 | 192 | 3961 | 566322 | 79173913 |
| Hot flush | 200.24 | 25.27 | 83 | 4070 | 54794 | 79685441 |
| Prostatic specific antigen increased | 154.73 | 25.27 | 45 | 4108 | 10341 | 79729894 |
| Fatigue | 76.36 | 25.27 | 156 | 3997 | 929571 | 78810664 |
| Dermatitis exfoliative generalised | 67.89 | 25.27 | 22 | 4131 | 7219 | 79733016 |
| Interstitial lung disease | 63.26 | 25.27 | 50 | 4103 | 112550 | 79627685 |
| Decreased appetite | 48.09 | 25.27 | 73 | 4080 | 342345 | 79397890 |
| Fall | 37.56 | 25.27 | 80 | 4073 | 487549 | 79252686 |
| Drug eruption | 37.13 | 25.27 | 25 | 4128 | 43910 | 79696325 |
| Prostatic specific antigen abnormal | 32.76 | 25.27 | 7 | 4146 | 454 | 79739781 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L02BB05 | 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 |
|---|---|---|---|
| Metastasis from malignant tumor of prostate | indication | 314994000 | |
| Malignant tumor of prostate | indication | 399068003 | DOID:10283 |
| Castration-resistant prostate cancer | indication | 427492003 | |
| Pregnancy, function | contraindication | 289908002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
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)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 8802689 | March 27, 2027 | TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 8802689 | March 27, 2027 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 8802689 | March 27, 2027 | TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 8802689 | March 27, 2027 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 8445507 | Sept. 15, 2030 | TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 8445507 | Sept. 15, 2030 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 8445507 | Sept. 15, 2030 | TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 8445507 | Sept. 15, 2030 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 9481663 | June 4, 2033 | TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 9481663 | June 4, 2033 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 9481663 | June 4, 2033 | TREATMENT OF METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 9481663 | June 4, 2033 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 10849888 | Sept. 23, 2033 | TREATMENT IN COMBINATION WITH ORCHIECTOMY OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NMCRPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 9884054 | Sept. 23, 2033 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | RE49353 | Sept. 23, 2033 | TREATMENT IN COMBINATION WITH A GNRH AGONIST OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 10052314 | Sept. 23, 2033 | TREATMENT IN COMBINATION WITH A GNRH AGONIST OF HIGH RISK NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 10052314 | Sept. 23, 2033 | TREATMENT IN COMBINATION WITH A GNRH AGONIST OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 10849888 | Sept. 23, 2033 | TREATMENT IN COMBINATION WITH ORCHIECTOMY OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NMCRPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 9884054 | Sept. 23, 2033 | TREATMENT OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | RE49353 | Sept. 23, 2033 | TREATMENT IN COMBINATION WITH A GNRH AGONIST OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NM-CRPC) |
| 240MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 17, 2023 | RX | TABLET | ORAL | 10702508 | April 30, 2038 | TREATMENT IN COMBINATION WITH ANDROGEN DEPRIVATION THERAPY OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NMCRPC) THAT IMPROVES METASTASIS FREE SURVIVAL |
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | 10702508 | April 30, 2038 | TREATMENT IN COMBINATION WITH ANDROGEN DEPRIVATION THERAPY OF NON-METASTATIC, CASTRATION-RESISTANT PROSTATE CANCER (NMCRPC) THAT IMPROVES METASTASIS FREE SURVIVAL |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 60MG | ERLEADA | JANSSEN BIOTECH | N210951 | Feb. 14, 2018 | RX | TABLET | ORAL | Feb. 14, 2023 | NEW CHEMICAL ENTITY |
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 | 7.80 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Androgen receptor | Transcription factor | ANTAGONIST | Ki | 7.03 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4T36H88UA7 | UNII |
| D11040 | KEGG_DRUG |
| C4329353 | UMLSCUI |
| CHEMBL3183409 | ChEMBL_ID |
| 24872560 | PUBCHEM_CID |
| DB11901 | DRUGBANK_ID |
| 10118 | INN_ID |
| 9043 | IUPHAR_LIGAND_ID |
| 270303 | MMSL |
| 33762 | MMSL |
| d08741 | MMSL |
| 017466 | NDDF |
| 766972001 | SNOMEDCT_US |
| 766973006 | SNOMEDCT_US |
| 4037326 | VANDF |
| 1999574 | RXNORM |
| C572045 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| ERLEADA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59676-600 | TABLET, FILM COATED | 60 mg | ORAL | NDA | 32 sections |
| ERLEADA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59676-600 | TABLET, FILM COATED | 60 mg | ORAL | NDA | 32 sections |
| ERLEADA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59676-600 | TABLET, FILM COATED | 60 mg | ORAL | NDA | 32 sections |
| ERLEADA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59676-600 | TABLET, FILM COATED | 60 mg | ORAL | NDA | 32 sections |
| ERLEADA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59676-604 | TABLET, FILM COATED | 240 mg | ORAL | NDA | 32 sections |