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 NUV-422 in Combination With Enzalutamide in Patients With mCRPC

Phase 1

Withdrawn

Conditions: Cancer of Prostate
Prostate Cancer
Castration Resistant Prostatic Neoplasms
Prostatic Cancer
Cancer of the Prostate
Prostate Neoplasm
Castrate Resistant Prostate Cancer
Castration Resistant Prostatic Cancer

Interventions: Drug: NUV-422
Drug: Enzalutamide

First Posted Date: 2022-01-13

Last Posted Date: 2022-08-05

Lead Sponsor: Nuvation Bio Inc.

Registration Number: NCT05191017

Locations: 🇺🇸
Pennsylvania Cancer Specialists and Research Institute, Gettysburg, Pennsylvania, United States
🇺🇸
Gabrail Cancer Center Research, Canton, Ohio, United States
🇺🇸
NEXT Virginia, Fairfax, Virginia, United States

An Extension Study in Participants Previously Enrolled in a Genentech and/or F. Hoffmann-La Roche Ltd Sponsored Atezolizumab Study (IMbrella C)

Phase 3

Active, not recruiting

Conditions: Neoplasms

Interventions: Drug: Atezolizumab
Drug: Pemetrexed
Drug: Bevacizumab
Drug: Paclitaxel
Drug: Enzalutamide

First Posted Date: 2021-11-09

Last Posted Date: 2025-04-11

Lead Sponsor: Hoffmann-La Roche

Target Recruit Count: 49

Registration Number: NCT05112965

Locations: 🇨🇳
Changchun Cancer Hospital, Changchun, China
🇨🇳
Henan Cancer Hospital, Zhengzhou, China
🇨🇳
Union Hospital of Tongji Medical College, Dept. of Cancer Center, Wuhan, Hubei, China

and more 16 locations

Safety and Efficacy of Oral Testosterone Undecanoate Followed by Enzalutamide as Therapy for Men With Metastatic Castrate Resistant Prostate Cancer

Phase 2

Active, not recruiting

Conditions: Metastatic Castration-resistant Prostate Cancer
Prostate Cancer
Castration-resistant Prostate Cancer

Interventions: Drug: Testosterone Undecanoate
Drug: Enzalutamide

First Posted Date: 2021-10-18

Last Posted Date: 2025-05-11

Lead Sponsor: Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins

Target Recruit Count: 30

Registration Number: NCT05081193

Locations: 🇺🇸
Johns Hopkins Hospital, Baltimore, Maryland, United States
🇺🇸
Allegheny Health Network, Pittsburgh, Pennsylvania, United States

EPI-7386 in Combination with Enzalutamide Compared with Enzalutamide Alone in Subjects with MCRPC

Phase 1

Terminated

Conditions: Prostate Cancer

Interventions: Drug: EPI-7386 with Enzalutamide
Drug: Enzalutamide

First Posted Date: 2021-10-13

Last Posted Date: 2025-02-28

Lead Sponsor: ESSA Pharmaceuticals

Target Recruit Count: 77

Registration Number: NCT05075577

Locations: 🇺🇸
Arizona Urology, Tucson, Arizona, United States
🇺🇸
Hematology Oncology Associates of the Treasure Coast, Port Saint Lucie, Florida, United States
🇺🇸
Moffitt Cancer Center, Tampa, Florida, United States

and more 21 locations

A Phase I/IIa Trial of HMBD-001 in Advanced HER3 Positive Solid Tumours

Phase 1

Recruiting

Conditions: Bladder Cancer
Castration-resistant Prostate Cancer
Melanoma
Non-small Cell Lung Cancer (NSCLC)
Triple Negative Breast Cancer
Gastric Cancer
Ovarian Cancer
Pancreatic Cancer
Squamous Cell Cancer of the Head and Neck
Cervical Cancer

Interventions: Drug: HMBD-001
Drug: HMBD-001 and enzalutamide

First Posted Date: 2021-09-27

Last Posted Date: 2024-12-27

Lead Sponsor: Cancer Research UK

Target Recruit Count: 81

Registration Number: NCT05057013

Locations: 🇬🇧
The Christie Hospital, Manchester, United Kingdom
🇬🇧
Freeman Hospital, Newcastle, Newcastle, United Kingdom
🇬🇧
Royal Marsden NHS Foundation Trust, London, United Kingdom

and more 1 locations

Decitabine/Cedazuridine and Enzalutamide for the Treatment of Metastatic Castrate Resistant Prostate Cancer

Phase 1

Terminated

Conditions: Stage IV Prostate Cancer AJCC v8
Stage IVA Prostate Cancer AJCC v8
Stage IVB Prostate Cancer AJCC v8
Castration-Resistant Prostate Carcinoma

Interventions: Drug: Decitabine and Cedazuridine
Drug: Enzalutamide

First Posted Date: 2021-09-08

Last Posted Date: 2025-02-28

Lead Sponsor: Roswell Park Cancer Institute

Target Recruit Count: 8

Registration Number: NCT05037500

Locations: 🇺🇸
Roswell Park Cancer Institute, Buffalo, New York, United States

FOR46 in Combination With Enzalutamide in Patients With Metastatic Castration Resistant Prostate Cancer

Phase 1

Recruiting

Conditions: Prostate Cancer
Metastatic Castration-resistant Prostate Cancer

Interventions: Biological: FOR46
Biological: Enzalutamide
Drug: Pegfilgrastim
Procedure: Blood Samples

First Posted Date: 2021-08-18

Last Posted Date: 2023-09-15

Lead Sponsor: Rahul Aggarwal

Target Recruit Count: 36

Registration Number: NCT05011188

Locations: 🇺🇸
University of California, San Francisco, San Francisco, California, United States

ZEN003694 and Enzalutamide Versus Enzalutamide Monotherapy in Metastatic Castration-Resistant Prostate Cancer

Phase 2

Recruiting

Conditions: Metastatic Castration-Resistant Prostate Cancer

Interventions: Drug: ZEN003694
Drug: Enzalutamide

First Posted Date: 2021-08-02

Last Posted Date: 2025-01-24

Lead Sponsor: Zenith Epigenetics

Target Recruit Count: 200

Registration Number: NCT04986423

Locations: 🇨🇳
Hubei Cancer Hospital, Wuhan, Hubei, China
🇺🇸
California Research Institute, Los Angeles, California, United States
🇺🇸
University of California, San Francisco, San Francisco, California, United States

and more 28 locations

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)-China Extension

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: 2021-06-22

Last Posted Date: 2025-03-18

Lead Sponsor: Merck Sharp & Dohme LLC

Target Recruit Count: 186

Registration Number: NCT04934722

Locations: 🇨🇳
Zhejiang Provincial People's Hospital ( Site 0809), Hangzhou, Zhejiang, China
🇨🇳
The First Affiliated Hospital of Wenzhou Medical University ( Site 0834), Wenzhou, Zhejiang, China
🇨🇳
The first affiliated Hospital of Xi an Jiaotong University ( Site # 0812), XI An, Shanxi, China

and more 21 locations

A Trial of SHR3162 Combined With Apatinib Mesylate Tablets or SHR3162 Monotherapy in Patients With Metastatic Castration Resistant Prostate Cancer

Phase 2

Completed

Conditions: Metastatic Castration Resistant Prostate Cancer

Interventions: Drug: Fluzoparib
Drug: Enzalutamide OR abiraterone acetate With Prednisone Acetate Tablets
Drug: Fluzoparib Combined With Apatinib

First Posted Date: 2021-05-03

Last Posted Date: 2025-01-24

Lead Sponsor: Jiangsu HengRui Medicine Co., Ltd.

Target Recruit Count: 93

Registration Number: NCT04869488

Locations: 🇨🇳
Fudan University Shanghai Cancer Center, Shanghai, Shanghai, China

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