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

LHRH Analogue Therapy With Enzalutamide or Bicalutamide in Treating Patients With Hormone Sensitive Prostate Cancer

Phase 2

Completed

Conditions: Adenocarcinoma of the Prostate
Recurrent Prostate Cancer
Stage IV Prostate Cancer

Interventions: Drug: enzalutamide
Drug: bicalutamide
Procedure: orchiectomy
Drug: leuprolide acetate
Drug: goserelin acetate
Other: laboratory biomarker analysis

First Posted Date: 2014-02-10

Last Posted Date: 2023-05-10

Lead Sponsor: Barbara Ann Karmanos Cancer Institute

Target Recruit Count: 71

Registration Number: NCT02058706

Locations: 🇺🇸
Barbara Ann Karmanos Cancer Institute, Detroit, Michigan, United States
🇺🇸
University of Alabama at Birmingham, Birmingham, Alabama, United States
🇺🇸
Henry Ford Hospital, Detroit, Michigan, United States

and more 1 locations

Salvage Therapeutic Radiation With Enzalutamide and ADT in Men With Recurrent Prostate Cancer (STREAM)

Phase 2

Completed

Conditions: Prostate Cancer

Interventions: Drug: enzalutamide
Drug: Androgen Deprivation
Radiation: Radiation Therapy

First Posted Date: 2014-02-07

Last Posted Date: 2019-06-26

Lead Sponsor: Duke University

Target Recruit Count: 38

Registration Number: NCT02057939

Locations: 🇺🇸
Wake Forest Baptist Health, Winston-Salem, North Carolina, United States
🇺🇸
Rutgers Cancer Institute of New Jersey, New Brunswick, New Jersey, United States
🇺🇸
Duke University Medical Center, Durham, North Carolina, United States

A Randomized Phase IIa Efficacy and Safety Study of Radium-223 Dichloride With Abiraterone Acetate or Enzalutamide in Metastatic Castration-resistant Prostate Cancer (CRPC)

Phase 2

Completed

Conditions: Prostatic Neoplasms

Interventions: Drug: Radium-223 dichloride (Xofigo, BAY88-8223)
Drug: Abiraterone acetate
Drug: Enzalutamide
Drug: Prednisone

First Posted Date: 2014-01-13

Last Posted Date: 2019-07-23

Lead Sponsor: Bayer

Target Recruit Count: 68

Registration Number: NCT02034552

Enzalutamide + External Beam Rt For Prostate

Phase 2

Completed

Conditions: Intermediate Risk Prostate Cancer

Interventions: Drug: Enzalutamide
Radiation: External Beam Radiation

First Posted Date: 2014-01-07

Last Posted Date: 2023-05-06

Lead Sponsor: Dana-Farber Cancer Institute

Target Recruit Count: 64

Registration Number: NCT02028988

Locations: 🇺🇸
Dana Farber Cancer Institute, Boston, Massachusetts, United States
🇺🇸
Beth Israel Deaconess Medical Center, Boston, Massachusetts, United States
🇺🇸
Brigham and Women's Hospital, Boston, Massachusetts, United States

Enzalutamide, Radiation Therapy and Hormone Therapy in Treating Patients With Intermediate or High-Risk Prostate Cancer

Phase 1

Active, not recruiting

Conditions: Stage IV Prostate Cancer
Recurrent Prostate Cancer
Stage IIB Prostate Cancer
Adenocarcinoma of the Prostate
Stage III Prostate Cancer

Interventions: Drug: Enzalutamide
Drug: Goserelin acetate
Drug: Leuprolide acetate
Radiation: Radiation therapy

First Posted Date: 2013-12-30

Last Posted Date: 2024-10-23

Lead Sponsor: Thomas Jefferson University

Target Recruit Count: 25

Registration Number: NCT02023463

Locations: 🇺🇸
Thomas Jefferson University, Philadelphia, Pennsylvania, United States

Enzalutamide and Mifepristone in Treating Patients With Metastatic Hormone Resistant Prostate Cancer

Phase 1

Completed

Conditions: Hormone-resistant Prostate Cancer
Stage IV Prostate Cancer
Recurrent Prostate Cancer

Interventions: Drug: enzalutamide
Other: laboratory biomarker analysis
Drug: mifepristone
Other: pharmacological study

First Posted Date: 2013-12-16

Last Posted Date: 2022-07-13

Lead Sponsor: University of Chicago

Target Recruit Count: 88

Registration Number: NCT02012296

Locations: 🇺🇸
University of Chicago Comprehensive Cancer Center, Chicago, Illinois, United States
🇺🇸
Cancer Care Specialists of Central Illinois (Decatur) /Decatur Memorial Hospital, Decatur, Illinois, United States
🇺🇸
NorthShore University Health System, Evanston, Illinois, United States

and more 1 locations

Efficacy and Safety Study of Enzalutamide in Combination With Exemestane in Patients With Advanced Breast Cancer

Phase 2

Completed

Conditions: Breast Cancer

Interventions: Drug: exemestane
Drug: Enzalutamide
Drug: Placebo (for enzalutamide)

First Posted Date: 2013-12-10

Last Posted Date: 2024-10-21

Lead Sponsor: Pfizer

Target Recruit Count: 247

Registration Number: NCT02007512

Locations: 🇺🇸
Indiana University Health Hospital, Indianapolis, Indiana, United States
🇺🇸
Indiana University Health Melvin and Bren Simon Cancer Center, Indianapolis, Indiana, United States
🇺🇸
Investigational Drug Services, Indianapolis, Indiana, United States

and more 76 locations

Safety and Efficacy Study of Enzalutamide in Patients With Nonmetastatic Castration-Resistant Prostate Cancer

Phase 3

Active, not recruiting

Conditions: Prostate Cancer
Nonmetastatic Castration-Resistant Prostate Cancer
Cancer of the Prostate

Interventions: Drug: Placebo
Drug: Enzalutamide

First Posted Date: 2013-12-06

Last Posted Date: 2025-02-14

Lead Sponsor: Pfizer

Target Recruit Count: 1402

Registration Number: NCT02003924

Locations: 🇺🇸
Urological Associates of Southern Arizona, PC, Tucson, Arizona, United States
🇺🇸
Ronald Reagan UCLA Medical Center, Los Angeles, California, United States
🇺🇸
UCLA Clark Urology Center, Los Angeles, California, United States

and more 384 locations

Safety Study of Continued Enzalutamide Treatment In Prostate Cancer Patients

Phase 4

Completed

Conditions: Prostate Cancer

Interventions: Drug: Enzalutamide
Drug: Placebo for Enzalutamide
Drug: Abiraterone
Drug: Prednisone

First Posted Date: 2013-11-26

Last Posted Date: 2023-09-18

Lead Sponsor: Pfizer

Target Recruit Count: 509

Registration Number: NCT01995513

Locations: 🇺🇸
Dana Farber Cancer Institute, Boston, Massachusetts, United States
🇦🇺
Box Hill Hospital, Box Hill, Victoria, Australia
🇧🇪
Universitaire Ziekenhuizen Leuven, Leuven, Belgium

and more 86 locations

Neoadjuvant Phase 2 Study Comparing the Effects of AR Inhibition With/Without SRC or MEK Inhibition in Prostate Cancer

Phase 2

Active, not recruiting

Conditions: Prostate Cancer

Interventions: Drug: degarelix
Drug: enzalutamide
Drug: trametinib
Drug: dasatinib

First Posted Date: 2013-11-21

Last Posted Date: 2024-10-01

Lead Sponsor: Jonsson Comprehensive Cancer Center

Target Recruit Count: 45

Registration Number: NCT01990196

Locations: 🇺🇸
University of California, Los Angeles, Los Angeles, California, United States

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