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apalutamide

Trade name: erleada

Small moleculeapprovedFast Track FDA

Approved

Feb 14, 2018

Apalutamide (developmental code name ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM, useful for prostate cancer treatment. Apalutamide binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes. This ultimately inhibits the expression of genes that regulate prostate cancer cell proliferation and may lead to an inhibition of cell growth in AR-expressing tumor cells. Apalutamide is currently in phase III clinical trials for castration-resistant prostate cancer. — NCATS

Clinical trial activity

107 trials · 77 clinical orgs · 2 marketing orgs

Phase 1
24
Phase 2
79
Phase 3
24
Phase 4
2

Earliest trial started Jul 26, 2010 (NCT01171898)

Timeline

2010s

  1. Jan 1, 2010

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2013

    Earliest Phase 2 Sponsor(trial)

  3. Jan 1, 2013

    Earliest Phase 3 Sponsor(trial)

  4. Feb 14, 2018

    Johnson and Johnson — Earliest FDA Approval

  5. Feb 14, 2018

    Johnson and Johnson — NDA Secondary Org

  6. Feb 14, 2018

    Johnson and Johnson — NDA Organization

2020s

  1. Mar 17, 2025

    Zydus Discovery DMCC — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewFast trackFeb 14, 2018

Chemistry & pharmacology

Loading structure…

SMILES

CNC(=O)C1=CC=C(C=C1F)N2C(=S)N(C(=O)C23CCC3)C4=CC(=C(N=C4)C#N)C(F)(F)F
Mol. weight
477.435 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • apalutamide
  • apalutamide
  • apalutamide
  • apalutamide
  • arn-509
  • arn-509
  • arn-509
  • jnj 56021927
  • jnj 56021927
  • jnj-56021927
  • jnj-56021927
  • jnj-56021927

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06931340Phase 3Nov 8, 2025National Cancer Institute (NCI)
NCT07002320Phase 1/Phase 2 (Phase 2)Apr 28, 2025Janssen Pharmaceutica NV, Ospedale S. Giovanni Bellinzona, Prostate Cancer UK, Queen's University, Belfast, Royal Marsden Hospital NHS Trust, Syntrix Biosystems, Inc., University of Cambridge, University of London
NCT06832774Phase 2Apr 1, 2025Jiao Tong University
NCT06592924Phase 3Jan 15, 2025Canadian Cancer Trials Group, ECOG-ACRIN Cancer Research Group, National Cancer Institute (NCI), NRG Oncology, SWOG Cancer Research Network
NCT06758882Phase 2Nov 25, 2024Azienda Sanitaria Ospedaliera Molinette S. Giovanni Battista
NCT06274047Phase 3Sep 10, 2024Janssen Pharmaceutica NV, University of Texas at Houston
NCT06505278Phase 2Aug 31, 2024Sun Yat-Sen University
NCT06320067Phase 3Jun 11, 2024Cancer Research UK, Janssen Pharmaceutica NV, Medical Research Council, Novartis, University of London
NCT06378866Phase 2Jun 3, 2024Mayo Clinic
NCT07260435Phase 3Feb 20, 2024Erasmus University Rotterdam, Stichting Treatmeds
NCT05960578Phase 2Jan 7, 2024Janssen Pharmaceutica NV, University of Washington
NCT06067269Phase 2Dec 1, 2023Janssen Pharmaceutica NV, University of California, Los Angeles
NCT05884398Phase 3Aug 31, 2023—
NCT05790213Phase 2Aug 17, 2023Janssen Pharmaceutica NV, University of Cincinnati
NCT05717582Phase 2May 1, 2023Fudan University
NCT05778097Phase 2Apr 1, 2023Johnson and Johnson, Nanjing University
NCT05717660Phase 2Mar 11, 2023University of Florence
NCT05740488N/AFeb 28, 2023Southern Medical University
NCT05751941Phase 2Feb 14, 2023Dendreon, University of South Florida
NCT05521698Phase 1Feb 12, 2023National Cancer Institute (NCI), University of Wisconsin
Showing 20 of 107 trials
Page 1 / 6

Organizations

Research & Development (77)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Janssen Pharmaceutica NVFor profit37442014
Johnson and JohnsonFor profit22932013
Aragon PharmaceuticalsFor profit171632010
National Cancer Institute (NCI)Government13332017
University of Texas at HoustonAcademic/Hospital9822016
Harvard UniversityAcademic/Hospital5432016
NRG OncologyAcademic/Hospital4322018
Cornell UniversityAcademic/Hospital3322014
Department of Veteran AffairsGovernment3322017
University of California, San FranciscoAcademic/Hospital3222017
University of CambridgeAcademic/Hospital3222018
University of WashingtonAcademic/Hospital3312017
Duke UniversityAcademic/Hospital2212017
ECOG-ACRIN Cancer Research GroupAcademic/Hospital2112020
Fudan UniversityAcademic/Hospital2212022
Nanjing UniversityAcademic/Hospital2212020
Southern Medical UniversityAcademic/Hospital2212021
University of California, Los AngelesAcademic/Hospital2212019
University of LondonAcademic/Hospital2222024
AccelovanceFor profit1012018
77 organizations
Page 1 / 4

Marketing (3)

OrganizationOrg typeRelationshipDate
Johnson and JohnsonFor profitNDA2Feb 14, 2018
Johnson and JohnsonFor profitNDAFeb 14, 2018
Zydus Discovery DMCCFor profitMKTGMar 17, 2025