apalutamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
non-steroid antiandrogens 5278 956104-40-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • apalutamide
  • ARN-509
  • JNJ-56021927
  • erleada
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.
  • Molecular weight: 477.44
  • Formula: C21H15F4N5O2S
  • CLOGP: 2.14
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 1
  • TPSA: 89.33
  • ALOGS: -5.43
  • ROTB: 4

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.24 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 12.88 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
60MG ERLEADA JANSSEN BIOTECH N210951 Feb. 14, 2018 RX TABLET ORAL Feb. 14, 2023 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA 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:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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