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

A Study of Sipuleucel-T With Administration of Enzalutamide in Men With Metastatic Castrate-Resistant Prostate Cancer

Phase 2

Completed

Conditions: Metastatic Prostate Cancer

Interventions: Biological: sipuleucel-T
Drug: enzalutamide

First Posted Date: 2013-11-11

Last Posted Date: 2018-10-24

Lead Sponsor: Dendreon

Target Recruit Count: 52

Registration Number: NCT01981122

Locations: 🇺🇸
Urology of Virginia, Virginia Beach, Virginia, United States
🇺🇸
Northwest Medical Specialties, Rainier Physicians, Tacoma, Washington, United States
🇺🇸
USC/Norris Comprehensive Cancer Center, Los Angeles, California, United States

and more 16 locations

A Study to Evaluate the Potential Increased Risk of Seizures Among Metastatic Castration-Resistant Prostate Cancer (mCRPC) Patients Treated With Enzalutamide

Phase 4

Completed

Conditions: Metastatic Castration-resistant Prostate Cancer (mCRPC)

Interventions: Drug: Enzalutamide

First Posted Date: 2013-11-07

Last Posted Date: 2024-12-06

Lead Sponsor: Astellas Pharma Global Development, Inc.

Target Recruit Count: 424

Registration Number: NCT01977651

Locations: 🇦🇺
Site AU61011, Sydney, New South Wales, Australia
🇺🇸
Site US10039, Syracuse, New York, United States
🇺🇸
Site US10008, Dallas, Texas, United States

and more 73 locations

Enzalutamide in Patients With Androgen Receptor Positive (AR+) Ovarian, Primary Peritoneal or Fallopian Tube Cancer and One, Two or Three Prior Therapies

Phase 2

Completed

Conditions: Advanced Epithelial Ovarian
Primary Peritoneal Carcinoma
Recurrent Epithelial Ovarian
Fallopian Tube

Interventions: Drug: Enzalutamide

First Posted Date: 2013-11-03

Last Posted Date: 2023-04-28

Lead Sponsor: Memorial Sloan Kettering Cancer Center

Target Recruit Count: 59

Registration Number: NCT01974765

Locations: 🇺🇸
Memorial Sloan Kettering Cancer Center, New York, New York, United States
🇺🇸
Memorial Sloan Kettering Cancer Center at Basking Ridge, Basking Ridge, New Jersey, United States
🇺🇸
Memorial Sloan Kettering Westchester, Harrison, New York, United States

and more 3 locations

Enzalutamide With or Without Abiraterone and Prednisone in Treating Patients With Castration-Resistant Metastatic Prostate Cancer

Phase 3

Active, not recruiting

Conditions: Adenocarcinoma of the Prostate
Stage IV Prostate Cancer
Hormone-resistant Prostate Cancer
Recurrent Prostate Cancer

Interventions: Drug: enzalutamide
Drug: abiraterone
Drug: prednisone

First Posted Date: 2013-09-24

Last Posted Date: 2023-09-28

Lead Sponsor: Alliance for Clinical Trials in Oncology

Target Recruit Count: 1311

Registration Number: NCT01949337

Locations: 🇺🇸
Greenville Health System Cancer Institute-Easley, Easley, South Carolina, United States
🇺🇸
University of Pittsburgh Cancer Institute (UPCI), Pittsburgh, Pennsylvania, United States
🇺🇸
UT Southwestern/Simmons Cancer Center-Dallas, Dallas, Texas, United States

and more 533 locations

Abiraterone Acetate Plus LHRH Agonist and Abiraterone Acetate Plus LHRH Agonist and Enzalutamide

Phase 2

Completed

Conditions: Prostate Cancer

Interventions: Drug: Abiraterone Acetate
Drug: Prednisone
Drug: Enzalutamide
Drug: LHRHa

First Posted Date: 2013-09-19

Last Posted Date: 2019-12-06

Lead Sponsor: M.D. Anderson Cancer Center

Target Recruit Count: 69

Registration Number: NCT01946165

Locations: 🇺🇸
University of Texas MD Anderson Cancer Center, Houston, Texas, United States

Study of Enzalutamide in Patients With Castration-resistant Prostate Cancer

Phase 2

Completed

Conditions: Metastatic Castration-resistant Prostate Cancer

Interventions: Drug: Enzalutamide

First Posted Date: 2013-09-16

Last Posted Date: 2022-10-24

Lead Sponsor: Dana-Farber Cancer Institute

Target Recruit Count: 67

Registration Number: NCT01942837

Locations: 🇺🇸
South Shore Hospital, Weymouth, Massachusetts, United States
🇺🇸
University of Washington Medical Center/Seattle Cancer Care Alliance, Seattle, Washington, United States
🇺🇸
Brigham and Women's Hospital, Boston, Massachusetts, United States

and more 2 locations