apalutamide 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:

None

Approvals:

DateAgencyCompanyOrphan
March 26, 2019 PMDA Janssen Pharmaceutical K.K.
Jan. 14, 2019 EMA JANSSEN-CILAG INTERNATIONAL N.V.
Feb. 14, 2018 FDA JANSSEN BIOTECH

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC L02BB05 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONE ANTAGONISTS AND RELATED AGENTS
Anti-androgens

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Metastasis from malignant tumor of prostate indication 314994000
Malignant tumor of prostate indication 399068003 DOID:10283
Pregnancy, function contraindication 289908002

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)

None

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 Sept. 17, 2022 TREATMENT OF PATIENTS WITH METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC)
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

External reference:

IDSource
4T36H88UA7 UNII
D11040 KEGG_DRUG
4037326 VANDF
C4329353 UMLSCUI
CHEMBL3183409 ChEMBL_ID
DB11901 DRUGBANK_ID
24872560 PUBCHEM_CID
10118 INN_ID
C572045 MESH_SUPPLEMENTAL_RECORD_UI
9043 IUPHAR_LIGAND_ID
1999574 RXNORM
270303 MMSL
33762 MMSL
d08741 MMSL
017466 NDDF
766972001 SNOMEDCT_US
766973006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ERLEADA HUMAN PRESCRIPTION DRUG LABEL 1 59676-600 TABLET, FILM COATED 60 mg ORAL NDA 30 sections