apalutamide (erleada) Report issue

Small molecule Approved FDA Fast Track FDA Priority Review FDA
AACT ChEMBL DrugBank Drugs@FDA PubChem

Active Ingredient History

NOW
  • Now
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

Chemistry

  • 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
  • InChIKey: HJBWBFZLDZWPHF-UHFFFAOYSA-N
  • Mol. Mass: 477.435
  • ALogP: 3.53
  • ChEMBL Molecule:
    apalutamide  
More Chemistry

Pharmacology

  • Mechanism of Action:
  • Multi-specific: Missing data
  • Black Box: No
  • Availability: Prescription Only
  • Delivery Methods: Oral
  • Pro Drug: No

Drug Pricing (per unit)

United States

$70.5460 - $90.2514
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

Alternative names

apalutamide | arn-509 | jnj 56021927 | jnj-56021927

Organizations (60)

Research & Development (60)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (1)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (16)

Approved Indications (2)


 

Prostatic Neoplasms (approved 2018)

Prostatic Neoplasms, Castration-Resistant

Experimental Indications - Clinical Trial Phases 1-4 (16)


 

Androgen Antagonists (Phase 2)

Carcinoma, Small Cell (Phase 2)

Carcinoma, Transitional Cell (Phase 1)

Castration (Phase 2)

Drug Therapy (Phase 2)

Healthy Volunteers (Phase 1)

Liver Diseases (Phase 1)

Neoadjuvant Therapy (Phase 2)

Neoplasm Metastasis (Phase 3)

Neoplasms (Phase 2)

Neuroendocrine Tumors (Phase 2)

Prostatectomy (Phase 2)

Prostatic Neoplasms (Phase 4)

Prostatic Neoplasms, Castration-Resistant (Phase 4)

Salivary Gland Neoplasms (Phase 2)

Urinary Bladder Neoplasms (Phase 1)

Overview

  • Highest Phase: Phase 4
  • # of Trials: 97
  • # of Trial Organizations: 60

Trials by Phase

Trial Phase Start Date Organizations Indications

Feedback

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