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

Combining EPI-7386 With Enzalutamide and Androgen Deprivation Therapy for Metastatic Hormone-Sensitive Prostate Cancer

Phase 2

Active, not recruiting

Conditions: Prostate Cancer
Metastatic Hormone-sensitive Prostate Cancer (mHSPC)
Prostate Adenocarcinoma

Interventions: Drug: EPI-7386
Drug: Enzalutamide
Drug: Androgen Deprivation Therapy (ADT)

First Posted Date: 2024-03-15

Last Posted Date: 2024-11-15

Lead Sponsor: Pedro Barata, MD, MSc

Target Recruit Count: 13

Registration Number: NCT06312670

Locations: 🇺🇸
University Hospitals Cleveland Medical Center Seidman Cancer Center, Case Comprehensive Cancer Center, Cleveland, Ohio, United States
🇺🇸
Cleveland Clinic Taussig Cancer institute, Case Comprehensive Cancer Center, Cleveland, Ohio, United States

Enzalutamide Implants (Enolen) in Patients With Prostate Cancer

Phase 1

Recruiting

Conditions: Prostate Adenocarcinoma

Interventions: Drug: enzalutamide

First Posted Date: 2024-02-14

Last Posted Date: 2024-06-28

Lead Sponsor: Alessa Therapeutics Inc.

Target Recruit Count: 20

Registration Number: NCT06257693

Locations: 🇺🇸
National Institutes of Health Clinical Center, Bethesda, Maryland, United States

Cell Therapy (STEAP1 CART) With Enzalutamide for the Treatment of Patients With Metastatic Castration-Resistant Prostate Cancer

Phase 1

Recruiting

Conditions: Castration-Resistant Prostate Carcinoma
Metastatic Prostate Adenocarcinoma
Stage IVB Prostate Cancer AJCC v8

Interventions: Biological: Anti-STEAP1 CAR T-cells
Procedure: Biopsy
Procedure: Biospecimen Collection
Procedure: Bone Scan
Procedure: Computed Tomography
Drug: Cyclophosphamide
Procedure: Echocardiography
Drug: Enzalutamide
Drug: Fludarabine
Procedure: Leukapheresis
Procedure: Magnetic Resonance Imaging
Procedure: Multigated Acquisition Scan
Procedure: Positron Emission Tomography

First Posted Date: 2024-02-01

Last Posted Date: 2025-03-30

Lead Sponsor: Fred Hutchinson Cancer Center

Target Recruit Count: 48

Registration Number: NCT06236139

Locations: 🇺🇸
Fred Hutch/University of Washington Cancer Consortium, Seattle, Washington, United States

Study of SX-682 Plus Enzalutamide in Men With Abiraterone-Resistant Metastatic Castration Resistant Prostate Cancer

Phase 2

Recruiting

Conditions: Metastatic Castration-resistant Prostate Cancer

Interventions: Drug: SX-682
Drug: Enzalutamide

First Posted Date: 2024-01-29

Last Posted Date: 2025-04-23

Lead Sponsor: Syntrix Biosystems, Inc.

Target Recruit Count: 53

Registration Number: NCT06228053

Locations: 🇺🇸
University of California, Los Angeles, Los Angeles, California, United States
🇺🇸
University of California, San Francisco, San Francisco, California, United States
🇺🇸
University of Michigan, Ann Arbor, Michigan, United States

and more 3 locations

An Observational Study to Learn More About the Use of Androgen Receptor Inhibitors and How They Affect Men With Nonmetastatic Prostate Cancer in Routine Medical Care in the United States

Completed

Conditions: Non-metastatic Castration-resistant Prostate Cancer
Non-metastatic Prostate Cancer

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

First Posted Date: 2024-01-12

Last Posted Date: 2024-04-09

Lead Sponsor: Bayer

Target Recruit Count: 1800

Registration Number: NCT06204302

Locations: 🇺🇸
Bayer, Whippany, New Jersey, United States

A Study of Opevesostat (MK-5684) Versus Alternative Next-generation Hormonal Agent (NHA) in Metastatic Castration-resistant Prostate Cancer (mCRPC) Post One NHA (MK-5684-004)

Phase 3

Recruiting

Conditions: Prostatic Neoplasms
Metastatic Castration-resistant Prostate Cancer (mCRPC)

Interventions: Drug: Abiraterone acetate
Drug: Opevesostat
Drug: Dexamethasone
Drug: Prednisone acetate
Drug: Fludrocortisone acetate
Drug: Enzalutamide
Drug: Hydrocortisone

First Posted Date: 2023-11-18

Last Posted Date: 2025-05-16

Lead Sponsor: Merck Sharp & Dohme LLC

Target Recruit Count: 1500

Registration Number: NCT06136650

Locations: 🇺🇸
The University of Arizona Cancer Center - North Campus ( Site 0073), Tucson, Arizona, United States
🇺🇸
UCLA Hematology/Oncology - Santa Monica ( Site 0044), Los Angeles, California, United States
🇺🇸
University of California, Irvine (UCI) Health - UC Irvine Medical Center ( Site 0040), Orange, California, United States

and more 305 locations

Study of Opevesostat (MK-5684) Versus Alternative NHA in mCRPC (MK-5684-003)

Phase 3

Recruiting

Conditions: Prostate Cancer Metastatic

Interventions: Drug: Opevesostat
Drug: Abiraterone acetate
Drug: Hydrocortisone
Drug: Enzalutamide
Drug: Fludrocortisone acetate
Drug: Prednisone
Drug: Dexamethasone

First Posted Date: 2023-11-18

Last Posted Date: 2025-05-16

Lead Sponsor: Merck Sharp & Dohme LLC

Target Recruit Count: 1200

Registration Number: NCT06136624

Locations: 🇵🇪
Aliada-Oncologìa ( Site 1257), Lima, Peru
🇺🇸
University of California, Irvine (UCI) Health - UC Irvine Medical Center ( Site 0040), Orange, California, United States
🇺🇸
Stanford Cancer Center ( Site 0036), Palo Alto, California, United States

and more 276 locations

Combination Study of Antibiotics With Enzalutamide (PROMIZE)

Phase 1

Recruiting

Conditions: Metastatic Castration-Resistant Prostate Cancer (mCRPC)

Interventions: Drug: Enzalutamide 40mg
Drug: Amoxicillin 500mg
Drug: Metronidazole 400mg
Drug: Vancomycin 125mg
Drug: Ciprofloxacin 500g

First Posted Date: 2023-11-13

Last Posted Date: 2025-04-24

Lead Sponsor: Institute of Cancer Research, United Kingdom

Target Recruit Count: 39

Registration Number: NCT06126731

Locations: 🇨🇭
Oncolgy Institute of Southern Switzerland (IOSI), Bellinzona, Switzerland
🇬🇧
The Royal Marsden NHS Foundation Trust, London Borough of Sutton, United Kingdom

Saruparib (AZD5305) vs Placebo in Men With Metastatic Castration-Sensitive Prostate Cancer Receiving Physician's Choice New Hormonal Agents

Phase 3

Recruiting

Conditions: Metastatic Castration-Sensitive Prostate Cancer

Interventions: Drug: Placebo
Drug: Saruparib
Drug: Abiraterone Acetate
Drug: Darolutamide
Drug: Enzalutamide

First Posted Date: 2023-11-07

Last Posted Date: 2025-05-15

Lead Sponsor: AstraZeneca

Target Recruit Count: 1800

Registration Number: NCT06120491

Locations: 🇬🇧
Research Site, Truro, United Kingdom

A Study of Enzalutamide, Enzalutamide in Combination With Mifepristone, or Chemotherapy in People With Metastatic Breast Cancer

Phase 2

Recruiting

Conditions: Metastatic Breast Cancer

Interventions: Drug: TPC
Drug: Enzalutamide
Drug: Mifepristone

First Posted Date: 2023-10-25

Last Posted Date: 2025-04-10

Lead Sponsor: Memorial Sloan Kettering Cancer Center

Target Recruit Count: 201

Registration Number: NCT06099769

Locations: 🇺🇸
University of Alabama at Birmingham, Birmingham, Alabama, United States
🇺🇸
University of California San Francisco (Data collection only), San Francisco, California, United States
🇺🇸
University of Chicago Medical Center, Chicago, Illinois, United States

and more 9 locations

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