Overview
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.
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
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/06/19 | Phase 3 | Not yet recruiting | |||
2025/05/28 | Phase 2 | Recruiting | |||
2025/04/10 | Phase 2 | Not yet recruiting | |||
2025/03/07 | Phase 1 | Recruiting | |||
2025/01/08 | Phase 3 | Recruiting | |||
2024/11/25 | Phase 1 | Recruiting | Evopoint Biosciences Inc. | ||
2024/11/18 | Phase 3 | Recruiting | |||
2024/10/22 | N/A | Recruiting | |||
2024/10/09 | Phase 2 | Recruiting | |||
2024/10/08 | Phase 3 | Recruiting |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Astellas Pharma US, Inc. | 0469-0725 | ORAL | 80 mg in 1 1 | 11/20/2023 | |
| Astellas Pharma US, Inc. | 0469-0125 | ORAL | 40 mg in 1 1 | 11/20/2023 | |
| Astellas Pharma US, Inc. | 0469-0625 | ORAL | 40 mg in 1 1 | 11/20/2023 | |
| Astellas Pharma US, Inc. | 0469-1725 | ORAL | 40 mg in 1 1 | 11/20/2023 | |
| Astellas Pharma US, Inc. | 0469-1125 | ORAL | 40 mg in 1 1 | 11/20/2023 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 8/22/2024 | ||
Authorised | 6/21/2013 | ||
Authorised | 6/21/2013 | ||
Authorised | 8/22/2024 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| XTANDI™ SOFT CAPSULES 40MG | SIN14829P | CAPSULE, LIQUID FILLED | 40.0 mg | 8/24/2015 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| Enzalutamide Soft Capsules | 国药准字HJ20240126 | 化学药品 | 胶囊剂 | 10/29/2024 | |
| Enzalutamide Soft Capsules | 国药准字HJ20200043 | 化学药品 | 胶囊剂 | 5/22/2024 | |
| Enzalutamide Soft Capsules | 国药准字H20244129 | 化学药品 | 胶囊剂 | 6/25/2024 | |
| Enzalutamide Soft Capsules | 国药准字H20253584 | 化学药品 | 胶囊剂 | 3/11/2025 | |
| Enzalutamide Soft Capsules | H20190056 | 化学药品 | 胶囊剂 | 11/18/2019 | |
| Enzalutamide Soft Capsules | 国药准字H20213660 | 化学药品 | 胶囊剂 | 8/25/2021 | |
| Enzalutamide Soft Capsules | 国药准字H20233027 | 化学药品 | 胶囊剂 | 1/10/2023 | |
| Enzalutamide Soft Capsules | 国药准字H20233306 | 化学药品 | 胶囊剂 | 3/21/2023 | |
| Enzalutamide Soft Capsules | 国药准字H20243257 | 化学药品 | 胶囊剂 | 2/23/2024 | |
| Enzalutamide Soft Capsules | 国药准字H20243243 | 化学药品 | 胶囊剂 | 2/23/2024 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| CIP ENZALUTAMIDE enzalutamide 40 mg soft capsule bottle | 390962 | Medicine | A | 5/13/2024 | |
| ENZALINE enzalutamide 40 mg soft capsule bottle | 390968 | Medicine | A | 5/13/2024 | |
| LUTACIP enzalutamide 40 mg soft capsule bottle | 390967 | Medicine | A | 5/13/2024 | |
| XTANDI enzalutamide 40 mg soft capsule blister pack | 210494 | Medicine | A | 7/1/2014 | |
| ENZACIP enzalutamide 40 mg soft capsule bottle | 390966 | Medicine | A | 5/13/2024 |