Enzalutamide

Generic Name: Enzalutamide

Brand Names: Xtandi, Enzalutamide Viatris

Drug Type: Small Molecule

Chemical Formula: C_₂₁H_₁₆F_₄N_₄O_₂S

CAS Number: 915087-33-1

Unique Ingredient Identifier: 93T0T9GKNU

Background: Enzalutamide is an androgen receptor (AR) inhibitor for the treatment of castration-resistant prostate cancer (CRPC), both metastatic and non-metastatic. It is a second-generation antiandrogen agent that the FDA approved on August 31, 2012. Although androgen deprivation therapy (ADT) is the first-line treatment of prostate cancer and remission can be achieved, arising resistance is inevitable, becoming castration-resistant prostate cancer. Until recently, docetaxel is the only treatment available for metastatic CRPC; however, AR inhibitors have been developed for more targeted therapy, although first-generation AR inhibitors like bicalutamide did not substantially increase the survival rate. Second-generation such as enzalutamide is more efficacious due to a higher affinity to AR and no partial agonist activity compared to bicalutamide.

Due to a favorable pharmacological profile, a phase 1 study of enzalutamide was initiated in July 2007. Compared to the average time of 10 to 15 years for a drug to go from pre-clinical to clinical studies, enzalutamide was developed relatively rapidly.

Indication: Enzalutamide is indicated for the treatment of castration-resistant prostate cancer and metastatic castration-sensitive prostate cancer (mCRPC). It is also used in combination with talazoparib for the treatment of adult patients with HRR gene-mutated mCRPC.

Associated Conditions: Castration Resistant Prostate Cancer, Metastatic Castration Sensitive Prostate Cancer (mCSPC), Metastatic Castration-Resistant Prostate Cancer (mCRPC)

Clinical Trials

Study of AMG 509 in Participants With Metastatic Castration-Resistant Prostate Cancer

Phase 1

Recruiting

Conditions: Prostate Cancer

Interventions: Drug: AMG 509
Drug: Abiraterone
Drug: Enzalutamide

First Posted Date: 2020-01-09

Last Posted Date: 2025-04-03

Lead Sponsor: Amgen

Target Recruit Count: 470

Registration Number: NCT04221542

Locations: 🇨🇭
HOCH Health Ostschweiz, Sankt Gallen, Switzerland
🇺🇸
United States Oncology Regulatory Affairs Corporate Office, Nashville, Tennessee, United States
🇺🇸
US Oncology Research Investigational Products Center, Irving, Texas, United States

and more 51 locations

Addition of Opaganib to Androgen Antagonists in Patients With mCRPC

Phase 2

Active, not recruiting

Conditions: Prostate Cancer

Interventions: Drug: Enzalutamide
Drug: Abiraterone
Drug: Opaganib

First Posted Date: 2019-12-20

Last Posted Date: 2024-06-25

Lead Sponsor: Medical University of South Carolina

Target Recruit Count: 67

Registration Number: NCT04207255

Locations: 🇺🇸
Medical University of South Carolina, Charleston, South Carolina, United States
🇺🇸
Emory University, Atlanta, Georgia, United States

Efficacy and Safety of Pembrolizumab (MK-3475) Plus Enzalutamide Plus Androgen Deprivation Therapy (ADT) Versus Placebo Plus Enzalutamide Plus ADT in Participants With Metastatic Hormone-Sensitive Prostate Cancer (mHSPC) (MK-3475-991/KEYNOTE-991)

Phase 3

Active, not recruiting

Conditions: Metastatic Hormone-Sensitive Prostate Cancer

Interventions: Biological: Pembrolizumab
Drug: Enzalutamide
Drug: Androgen Deprivation Therapy (ADT)
Other: Placebo

First Posted Date: 2019-12-09

Last Posted Date: 2025-02-14

Lead Sponsor: Merck Sharp & Dohme LLC

Target Recruit Count: 1251

Registration Number: NCT04191096

Locations: 🇺🇸
UCLA Hematology/Oncology - Santa Monica ( Site 0241), Los Angeles, California, United States
🇲🇽
Grupo Medico Camino SC ( Site 2613), Mexico City, Mexico
🇩🇪
Klinikum der Universitaet Muenchen - Grosshadern ( Site 1210), Muenchen, Bayern, Germany

and more 210 locations

Study of Oral Rucaparib With Other Anticancer Agents in Metastatic Castration Resistant Prostate Cancer Patients (RAMP)

Phase 1

Completed

Conditions: Metastatic Castration Resistant Prostate Cancer

Interventions: Drug: Rucaparib
Drug: Abiraterone
Drug: Enzalutamide

First Posted Date: 2019-11-27

Last Posted Date: 2023-06-29

Lead Sponsor: pharmaand GmbH

Target Recruit Count: 8

Registration Number: NCT04179396

Locations: 🇺🇸
University of Minnesota, Minneapolis, Minnesota, United States
🇺🇸
Urology Associates, P.C., Nashville, Tennessee, United States
🇺🇸
Piedmont Cancer Institute, P.C., Atlanta, Georgia, United States

A Study of Tazemetostat With Enzalutamide or Abiraterone/Prednisone in Participants With Advanced Prostate Cancer

Phase 1

Terminated

Conditions: Metastatic Castration-resistant Prostate Cancer
Metastatic Prostate Cancer

Interventions: Drug: Tazemetostat
Drug: Abiraterone/prednisone
Drug: Enzalutamide

First Posted Date: 2019-11-27

Last Posted Date: 2024-12-09

Lead Sponsor: Epizyme, Inc.

Target Recruit Count: 102

Registration Number: NCT04179864

Locations: 🇺🇸
Dana Farber Cancer Institute, Boston, Massachusetts, United States
🇺🇸
Beth Israel Deaconess Medical Center, Boston, Massachusetts, United States
🇺🇸
Genesis Healthcare Partners, San Diego, California, United States

and more 21 locations

Study to Compare the Effects of Drug Darolutamide and Drug Enzalutamide on Physical Function, Including Balance and Daily Activity, in Patients With Castration-resistant Prostate Cancer (CRPC)

Phase 2

Terminated

Conditions: Prostatic Cancer, Castration-Resistant

Interventions: Drug: Darolutamide (Nubeqa, BAY1841788)
Drug: Enzalutamide

First Posted Date: 2019-11-08

Last Posted Date: 2023-08-04

Lead Sponsor: Bayer

Target Recruit Count: 30

Registration Number: NCT04157088

Locations: 🇺🇸
Oregon Health and Science University, Portland, Maine, United States
🇺🇸
Duke University Medical Center, Durham, North Carolina, United States
🇺🇸
MidLantic Urology - Bala Cynwyd, Bala-Cynwyd, Pennsylvania, United States

and more 4 locations

Continuation Protocol for ZEN003694 in Patients Experiencing Clinical Benefit While Enrolled in a ZEN003694 Protocol

Phase 1

Conditions: mCRPC

Interventions: Drug: ZEN003694
Drug: Enzalutamide

First Posted Date: 2019-10-30

Last Posted Date: 2025-03-19

Lead Sponsor: Zenith Epigenetics

Target Recruit Count: 40

Registration Number: NCT04145375

Locations: 🇺🇸
Oregon Health & Science University, Portland, Oregon, United States
🇺🇸
University of California San Francisco Medical Center, San Francisco, California, United States

Targeting the PAM50 Her2-Enriched Phenotype With Enzalutamide in Hormone Receptor-Positive/Her2-Negative Metastatic BC

Phase 2

Terminated

Conditions: Breast Cancer

Interventions: Drug: Enzalutamide

First Posted Date: 2019-10-29

Last Posted Date: 2022-10-28

Lead Sponsor: SOLTI Breast Cancer Research Group

Target Recruit Count: 34

Registration Number: NCT04142060

Locations: 🇪🇸
ICO Badalona, Badalona, Barcelona, Spain
🇪🇸
Hospital Universitari Vall d' Hebrón, Barcelona, Spain
🇪🇸
Hospital Clinic de Barcelona, Barcelona, Spain

and more 5 locations

Fecal Microbiota Transplant and Pembrolizumab for Men With Metastatic Castration Resistant Prostate Cancer.

Phase 2

Conditions: Prostate Cancer Metastatic
Prostate Cancer

Interventions: Biological: Fecal microbiota transplant
Drug: Pembrolizumab
Drug: Enzalutamide

First Posted Date: 2019-10-07

Last Posted Date: 2022-06-23

Lead Sponsor: Julie Graff, MD

Target Recruit Count: 32

Registration Number: NCT04116775

Locations: 🇺🇸
VA Portland Health Care System, Portland, Oregon, United States

A Study of Tulmimetostat DZR123 (CPI-0209) in Patients With Advanced Solid Tumors and Lymphomas

Phase 1

Recruiting

Conditions: Advanced Solid Tumor
Diffuse Large B Cell Lymphoma
Lymphoma, T-Cell
Mesothelioma, Malignant
Prostatic Neoplasms, Castration-Resistant
Endometrial Cancer
Ovarian Clear Cell Carcinoma
Metastatic Castration-resistant Prostate Cancer

Interventions: Drug: Tulmimetostat
Drug: Enzalutamide

First Posted Date: 2019-09-26

Last Posted Date: 2025-05-15

Lead Sponsor: Novartis Pharmaceuticals

Target Recruit Count: 275

Registration Number: NCT04104776

Locations: 🇺🇸
Winship Cancer Institute of Emory University, Atlanta, Georgia, United States
🇺🇸
University of Chicago Medical Center, Chicago, Illinois, United States
🇺🇸
University of Maryland - Marlene and Stewart Greenebaum Cancer Center, Baltimore, Maryland, United States

and more 57 locations

Drug Development Updates

Stay informed with timely notifications on clinical trials, regulatory changes, and research advancements related to this medication.

Home Terms & Conditions Privacy Policy