MedPath

Apalutamide

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

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
Associated Therapies
Androgen Deprivation Therapy

Neoadjuvant Intense Endocrine Therapy for High Risk and Locally Advanced Prostate Cancer

Phase 2
Recruiting
Conditions
Intense Endocrine Therapy
Neoadjuvant Therapy
High Risk Prostate Cancer
Locally Advanced Prostate Cancer
Interventions
Drug: ADT
Drug: PARP inhibitor
Drug: Darotamide
Drug: Abiraterone Acetate
Drug: Enzalutamide
Drug: Apalutamide
Drug: Rezvilutamide
Procedure: Robot-assisted radical prostatectomy
Drug: Prednisolone tablets
First Posted Date
2022-06-07
Last Posted Date
2022-08-16
Lead Sponsor
The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School
Target Recruit Count
900
Registration Number
NCT05406999
Locations
🇨🇳

Department of Urology, Drum Tower Hospital, Medical School of Nanjing University, Institute of Urology, Nanjing University, Nanjing, Jiangsu, China

Study of AZD5305 When Given in Combination With New Hormonal Agents in Patients With Metastatic Prostate Cancer

Phase 1
Recruiting
Conditions
Metastatic Prostate Cancer
Interventions
First Posted Date
2022-05-10
Last Posted Date
2024-12-18
Lead Sponsor
AstraZeneca
Target Recruit Count
190
Registration Number
NCT05367440
Locations
🇬🇧

Research Site, Plymouth, United Kingdom

An Observational Study, Called DEAR, to Learn More About Treatment With Darolutamide, Enzalutamide and Apalutamide in Men With Non-metastatic Castration-resistant Prostate Cancer in Real World Settings

Completed
Conditions
Non-metastatic Castration-resistant Prostate Cancer
Interventions
First Posted Date
2022-05-05
Last Posted Date
2024-03-20
Lead Sponsor
Bayer
Target Recruit Count
870
Registration Number
NCT05362149
Locations
🇺🇸

Bayer, Whippany, New Jersey, United States

A Study of EPI-7386 in Combination With Abiraterone Acetate Plus Prednisone, or Apalutamide in Metastatic Castration-resistant Prostate Cancer (mCRPC)

Phase 1
Terminated
Conditions
Prostatic Neoplasms
Interventions
First Posted Date
2022-03-25
Last Posted Date
2023-05-09
Lead Sponsor
Janssen Research & Development, LLC
Target Recruit Count
3
Registration Number
NCT05295927
Locations
🇺🇸

GU Research Network, Omaha, Nebraska, United States

🇺🇸

Chesapeake Urology Research Associates, Towson, Maryland, United States

🇺🇸

Carolina Urologic Research Center, Myrtle Beach, South Carolina, United States

and more 1 locations

Enhanced Systemic Combined With Local Treatment for Primary and Metastatic Lesions in Oligo-metastatic Prostate Cancer

Phase 2
Recruiting
Conditions
Prostate Cancer
Interventions
Drug: Leuprolide acetate
Drug: Goserelin acetate
Drug: Triptorelin acetate
Drug: Degarelix acetate
Drug: Abiraterone acetate
Drug: Apalutamide
Drug: Enzalutamide
Procedure: Local treatment for primary lesion
Radiation: Radiotherapy for primary lesion
Radiation: Radiotherapy for metastatic lesion
First Posted Date
2022-01-28
Last Posted Date
2022-03-16
Lead Sponsor
Fudan University
Target Recruit Count
160
Registration Number
NCT05212857
Locations
🇨🇳

Fudan University Shanghai Cancer Center, Shanghai, Shanghai, China

A Study Using Available Data to Learn to What Extent Patients With Prostate Cancer Who Received Second Generation Androgen Receptor Inhibitors Took Their Medication as Prescribed or Stopped Taking Their Medication Completely

Active, not recruiting
Conditions
Prostate Cancer
Interventions
First Posted Date
2022-01-21
Last Posted Date
2024-12-13
Lead Sponsor
Bayer
Target Recruit Count
13779
Registration Number
NCT05202301
Locations
🇺🇸

Bayer, Whippany, New Jersey, United States

The Finnish National Study to Facilitate Patient Access to Targeted Anti-cancer Drugs

Phase 2
Recruiting
Conditions
Advanced Cancer
Solid Tumor
Haematological Malignancy
Interventions
First Posted Date
2021-12-16
Last Posted Date
2024-07-15
Lead Sponsor
Helsinki University Central Hospital
Target Recruit Count
250
Registration Number
NCT05159245
Locations
🇫🇮

Turku University Hospital Cancer Centre, Turku, Varsinais-Suomi, Finland

🇫🇮

Kuopio University Hospital, Kuopio, Finland

🇫🇮

Oulu University Hospital OYS Cancer Center, Oulu, Finland

and more 2 locations

An Evaluation of the Efficacy and Safety of Apalutamide as Neoadjuvant Endocrine Therapy in High-Risk and Oligometastatic Prostate Cancer

Not Applicable
Recruiting
Conditions
High-Risk and Oligometastatic Prostate Cancer
Interventions
First Posted Date
2021-08-09
Last Posted Date
2024-03-18
Lead Sponsor
Zhujiang Hospital
Target Recruit Count
50
Registration Number
NCT04997252
Locations
🇨🇳

zhujiang Hospital of Southern Medical University, Guangzhou, Guangdong, China

Androgen Ablation Therapy With or Without Niraparib After Radiation Therapy for the Treatment of High-Risk Localized or Locally Advanced Prostate Cancer

Phase 2
Recruiting
Conditions
Prostate Carcinoma
Stage III Prostate Cancer AJCC v8
Stage IIC Prostate Cancer AJCC v8
Stage IVA Prostate Cancer AJCC v8
Stage IIIA Prostate Cancer AJCC v8
Stage IIIB Prostate Cancer AJCC v8
Stage IIIC Prostate Cancer AJCC v8
Interventions
Drug: Antiandrogen Therapy
Drug: Abiraterone Acetate
Drug: Apalutamide
Procedure: Biopsy
Radiation: Radiation Therapy
Drug: Niraparib
Drug: Prednisone
First Posted Date
2021-07-01
Last Posted Date
2024-06-06
Lead Sponsor
M.D. Anderson Cancer Center
Target Recruit Count
200
Registration Number
NCT04947254
Locations
🇺🇸

M D Anderson Cancer Center, Houston, Texas, United States

Apalutamide Plus Cetrelimab in Patients With Treatment-Emergent Small Cell Neuroendocrine Prostate Cancer

Phase 2
Active, not recruiting
Conditions
Prostate Cancer
Small Cell Neuroendocrine Carcinoma
Small Cell Carcinoma
Interventions
Drug: Apalutamide
Biological: Cetrelimab
First Posted Date
2021-06-15
Last Posted Date
2024-04-26
Lead Sponsor
Rahul Aggarwal
Target Recruit Count
2
Registration Number
NCT04926181
Locations
🇺🇸

University of California, San Francisco, San Francisco, California, United States

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