MedPath

Apalutamide

Generic Name
Apalutamide
Brand Names
Erleada
Drug Type
Small Molecule
Chemical Formula
C21H15F4N5O2S
CAS Number
956104-40-8
Unique Ingredient Identifier
4T36H88UA7

Overview

Apalutamide is a potent androgen receptor (AR) antagonist that selectively binds to the ligand-binding domain of AR and blocks AR nuclear translocation or binding to androgen response elements . It has been used in trials studying the treatment of Prostate Cancer, Hepatic Impairment, Prostatic Neoplasms, Castration-Resistant Prostate Cancer, and Prostatic Neoplasms, Castration-Resistant, among others. Exerting an antitumor action, apalutamide blocking the effect of androgens that promote tumor growth. It targets the AR ligand-binding domain and prevents AR nuclear translocation, DNA binding, and transcription of AR gene targets in prostate tumors . In mice bearing human CRPC xenograft models, apalutamide treatment produced tumor regressions in a dose-dependent manner that was more effective than that of Bicalutamide or Enzalutamide. Unlike bicalutamide, apalutamide antagonized AR-mediated signaling in AR overexpressing human CRPC cell lines . Androgen-deprivation therapy, or hormone therapy, can be used as part of maintenance therapy for patients with non-metastatic prostate cancer. Although most patients achieve therapeutic responses at the initial hormone therapy, many patients progress to non-metastatic castration-resistant (resistance to hormone therapy) prostate cancer which is the second-most common cause of cancer-related deaths in American males . Castration-resistant prostate cancer is often incurable, which poses significant clinical challenges for patients. Approximately 10 to 20 % of prostate cancer cases are castration-resistant, and up to 16% of these patients show no evidence of cancer metastasis at the time of castration-resistant diagnosis . Higher prostate-specific antigen (PSA) and shorter PSA doubling time (PSA DT) are associated with a higher risk for metastases and death . In a phase-2 multicenter open-label study, 89% of patients with non-metastatic, castration-resistant prostate cancer had ≥50% PSA decline at week 12 of apalutamide treatment . In a randomized trial, the median metastasis-free survival for patients taking apalutamide was 40.5 months compared to 16.2 months for patients taking a placebo . Apalutamide displayed good tolerability and safety profile in clinical studies. Apalutamide was approved in February 2018 by the FDA as Erleada for the treatment of patients with non-metastatic prostate cancer that is resistant to treatment with hormone therapy (castration-resistant). It is available as oral tablets. Apalutamide is the first FDA-approved treatment for non-metastatic, castration-resistant prostate cancer .

Indication

Apalutamide is indicated for the treatment of patients with metastatic castration-sensitive prostate cancer and non-metastatic castration-resistant prostate cancer.

Associated Conditions

  • Metastatic Castration Sensitive Prostate Cancer (mCSPC)
  • Metastatic Hormone-Sensitive Prostate Cancer (mHSPC)
  • Non-Metastatic Castration-Resistant Prostate Cancer

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2025/07/25
N/A
Not yet recruiting
2025/06/03
Phase 1
Recruiting
Institute of Cancer Research, United Kingdom
2025/04/17
Phase 3
Not yet recruiting
2025/01/06
Phase 2
Recruiting
Marco Oderda
2024/10/22
N/A
Recruiting
2024/09/19
Phase 3
Recruiting
2024/06/25
N/A
Recruiting
Santa Chiara Hospital
2024/05/28
N/A
Not yet recruiting
2024/04/23
Phase 2
Recruiting
2024/03/20
Phase 3
Recruiting

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
Janssen Products, LP
59676-600
ORAL
60 mg in 1 1
1/17/2024
Janssen Products, LP
59676-604
ORAL
240 mg in 1 1
1/17/2024

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
ERLEADA FILM-COATED TABLET 60MG
SIN15698P
TABLET, FILM COATED
60mg
5/27/2019

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
No NMPA approvals found for this drug.

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
ERLEADA TABLETS 60MG
N/A
N/A
N/A
12/14/2018

TGA Drug Approvals

Health Canada Drug Approvals

Approved Product
Company
DIN
Dosage Form
Strength
Market Date
ERLEADA
02540185
Tablet - Oral
240 MG
11/1/2023
ERLEADA
02478374
Tablet - Oral
60 MG
7/27/2018

CIMA AEMPS Drug Approvals

Approved Product
Company
Registration Number
Pharmaceutical Form
Prescription Type
Status
No CIMA AEMPS (Spain) approvals found for this drug.

Philippines FDA Drug Approvals

Approved Product
Company
License Number
Dosage Form
Strength
Approval Date
No Philippines FDA approvals found for this drug.

Saudi SFDA Drug Approvals

Approved Product
Company
License Number
Dosage Form
Strength
Approval Date
No Saudi SFDA approvals found for this drug.

Malaysia NPRA Drug Approvals

Approved Product
Company
Registration Number
Dosage Form
Strength
Approval Date
No Malaysia NPRA approvals found for this drug.

UK EMC Drug Information

Medicine Name
MA Holder
MA Number
Pharmaceutical Form
Active Ingredient
Authorization Date
No UK EMC drug information found for this drug.

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