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)

Associated Therapies: -

Clinical Trials

Study to Evaluate CCS1477 in Advanced Tumours

Phase 1

Recruiting

Conditions: Metastatic Castration-Resistant Prostate Cancer
Non-small Cell Lung Cancer
Metastatic Breast Cancer
Advanced Solid Tumors

Interventions: Drug: CCS1477
Drug: Enzalutamide
Drug: Olaparib
Drug: Atezolizumab
Drug: Abiraterone acetate
Drug: Darolutamide

First Posted Date: 2018-06-26

Last Posted Date: 2024-07-17

Lead Sponsor: CellCentric Ltd.

Target Recruit Count: 350

Registration Number: NCT03568656

Locations: 🇺🇸
Dana-Farber Cancer Institute, Boston, Massachusetts, United States
🇺🇸
Thomas Jefferson University, Sidney Kimmel Cancer Center, Philadelphia, Pennsylvania, United States
🇺🇸
New York-Presbyterian Hospital/Weill Cornell Medical Center, New York, New York, United States

and more 19 locations

Combining CRLX101, a Nanoparticle Camptothecin, With Enzalutamide in People With Progressive Metastatic Castration Resistant Prostate Cancer Following Prior Enzalutamide Treatment

Phase 2

Terminated

Conditions: Metastatic Castration Resistant Prostate Cancer
Prostate Neoplasms

Interventions: Drug: enzalutamide
Drug: CRLX101

First Posted Date: 2018-05-22

Last Posted Date: 2022-07-12

Lead Sponsor: National Cancer Institute (NCI)

Target Recruit Count: 4

Registration Number: NCT03531827

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

ProSTAR: A Study Evaluating CPI-1205 in Patients With Metastatic Castration Resistant Prostate Cancer

Phase 1

Conditions: Metastatic Castration Resistant Prostate Cancer (mCRPC)

Interventions: Drug: CPI-1205
Drug: Enzalutamide
Drug: Abiraterone/Prednisone

First Posted Date: 2018-03-29

Last Posted Date: 2021-07-26

Lead Sponsor: Constellation Pharmaceuticals

Target Recruit Count: 242

Registration Number: NCT03480646

Locations: 🇺🇸
University of Illinois Hospital and Health Systems, Chicago, Illinois, United States
🇺🇸
John Hopkins Kimmel Cancer Center, Baltimore, Maryland, United States
🇺🇸
Dana Farber Cancer Institute, Boston, Massachusetts, United States

and more 38 locations

Mevrometostat Treatment of Relapsed/Refractory SCLC, Castration Resistant Prostate Cancer, and Follicular Lymphoma

Phase 1

Recruiting

Conditions: Follicular Lymphoma (FL)
Small Cell Lung Cancer (SCLC)
Metastatic Castration Resistant Prostate Cancer (mCRPC)

Interventions: Drug: Mervometostat (PF-06821497)
Drug: Enzalutamide

First Posted Date: 2018-03-09

Last Posted Date: 2024-11-01

Lead Sponsor: Pfizer

Target Recruit Count: 343

Registration Number: NCT03460977

Locations: 🇺🇸
Urological Associates of Southern Arizona, P.C ., Tucson, Arizona, United States
🇺🇸
Banner-University Medical Center Tucson, Tucson, Arizona, United States
🇺🇸
The University of Arizona Cancer Center-North Campus, Tucson, Arizona, United States

and more 96 locations

Study of TRC105 With Abiraterone and With Enzalutamide in Prostate Cancer Patients Progressing on Therapy

Phase 2

Completed

Conditions: Prostate Cancer

Interventions: Drug: TRC105
Drug: Abiraterone
Drug: Enzalutamide

First Posted Date: 2018-02-01

Last Posted Date: 2020-12-30

Lead Sponsor: Cedars-Sinai Medical Center

Target Recruit Count: 11

Registration Number: NCT03418324

Locations: 🇺🇸
Cedars Sinai Medical Center, Los Angeles, California, United States

Enzalutamide With or Without Radium Ra 223 Dichloride in Patients With Metastatic, Castration-Resistant Prostate Cancer

Phase 2

Active, not recruiting

Conditions: Castration-Resistant Prostate Carcinoma
Prostate Carcinoma Metastatic in the Bone
Stage IV Prostate Cancer

Interventions: Drug: Enzalutamide
Other: Laboratory Biomarker Analysis
Radiation: Radium Ra 223 Dichloride

First Posted Date: 2017-11-17

Last Posted Date: 2023-11-08

Lead Sponsor: University of Southern California

Target Recruit Count: 30

Registration Number: NCT03344211

Locations: 🇺🇸
City of Hope, Duarte, California, United States
🇺🇸
USC / Norris Comprehensive Cancer Center, Los Angeles, California, United States
🇺🇸
Cedars Sinai Medical Center, Los Angeles, California, United States

An Investigational Immunotherapy Study of Nivolumab in Combination With Rucaparib, Docetaxel, or Enzalutamide in Metastatic Castration-resistant Prostate Cancer

Phase 2

Active, not recruiting

Conditions: Prostate Cancer

Interventions: Biological: nivolumab
Drug: rucaparib
Drug: docetaxel
Drug: enzalutamide
Drug: prednisone

First Posted Date: 2017-11-09

Last Posted Date: 2024-10-15

Lead Sponsor: Bristol-Myers Squibb

Target Recruit Count: 292

Registration Number: NCT03338790

Locations: 🇺🇸
Local Institution - 0037, Miami, Florida, United States
🇺🇸
Local Institution - 0009, Marietta, Georgia, United States
🇺🇸
Local Institution - 0012, Detroit, Michigan, United States

and more 63 locations