Enzalutamide
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2012
- First approval year
- 2012
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Enzalutamide
- Molecular weight
- 464.44
- Structure (SMILES)
- CNC(=O)c1ccc(N2C(=S)N(c3ccc(C#N)c(C(F)(F)F)c3)C(=O)C2(C)C)cc1F
- xtandi
- Xtandi
- 177lu psma 617 plus enzalutamide
- enzalutamida
- Enzalutamida
- enzalutamide
- Enzalutamide
- Enzalutamide (Xtandi)
- Enzalutamide [INN]
- Enzalutamide [JAN]
- Enzalutamide [MI]
- Enzalutamide [ORANGE BOOK]
- Enzalutamide [USAN]
- Enzalutamide [VANDF]
- Enzalutamide [WHO-DD]
- Enzalutamide 160 mg
- Enzalutamide 160mg daily (oral)
- Enzalutamide 40 MG
- Enzalutamide 40 mg capsule
- Enzalutamide 40mg
- Enzalutamide capsule
- Enzalutamide Capsule
- enzalutamide inn
- enzalutamide jan
- enzalutamide mi
- Enzalutamide Oral Capsule
- Enzalutamide Oral Tablet
And 12 more, listed on the interactive page.
- ATC classification codes
- L02BB04
Sources for recorded values
- CAS registry numbers
- 915087-33-1
- ChEMBL ID
- CHEMBL1082407
- InChIKey
- WXCXUHSOUPDCQV-UHFFFAOYSA-N
- PubChem compound IDs
- 15951529
- RxNorm IDs (RxCUI)
- 1307298
- FDA ingredient codes (UNII)
- 93T0T9GKNU
- Applicant
- ASTELLAS
- Approval date
- 31 Aug 2012
- Application number
- NDA203415
- Status
- Authorised
- Status date
- 21 Jun 2013
- Authorisation date
- 21 Jun 2013
- Approved indications
- Xtandi is indicated for: as monotherapy or in combination with androgen deprivation therapy for the treatment of adult men with high risk biochemical recurrent (BCR) non-metastatic hormone sensitive prostate cancer (nmHSPC) who are unsuitable for salvage radiotherapy (see section 5.1). the treatment of adult men with metastatic hormone-sensitive prostate cancer (mHSPC) in combination with androgen deprivation therapy (see section 5.1). the treatment of adult men with high-risk non-metastatic castration-resistant prostate cancer (CRPC) (see section 5.1). the treatment of adult men with metastatic CRPC who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy in whom chemotherapy is not yet clinically indicated (see section 5.1). the treatment of adult men with metastatic CRPC whose disease has progressed on or after docetaxel therapy.
- Product number
- EMEA/H/C/002639
- Authorisation holder
- Astellas Pharma Europe B.V.
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 2
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Prostatic Neoplasms
European medicines record
- Patents
- 11
- Designations
- 2
- Earliest recorded loss of exclusivity
- 23 Feb 2037
- First in class
- No
- Fast track
- Yes
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- enzalutamide
- Type
- Synthetic organic
- Drug name stem
- -lutamide
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Antagonist
- Action type
- Antagonist
- Target
- Androgen receptor
- Gene symbol
- AR
- Protein identifier
- P10275
- Median affinity
- 7.44
- Affinity units
- pIC50
- Primary target
- Yes
- Mechanism
- Androgen Receptor antagonist
- Action type
- Antagonist
- Target
- Androgen receptor
- Protein identifier
- P10275
Open Targets mechanisms
- Mechanism
- Androgen Receptor antagonist
- Action type
- Antagonist
- Target
- Androgen receptor
DrugCentral mechanisms
- Action type
- Antagonist
- Gene symbol
- AR
- Protein identifier
- P10275
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Carcinoma, Hepatocellular
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000182
- Subject identifier
- D006528
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000196
- Subject identifier
- D011471
- Condition
- Adenocarcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000228
- Subject identifier
- D000230
- Condition
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000305
- Subject identifier
- D001943
- Condition
- Carcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000313
- Subject identifier
- D002277
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 0.5
- Condition identifier
- EFO:0000349
- Subject identifier
- D002292
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000673
- Subject identifier
- D011471
- Condition
- Liver Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001421
- Subject identifier
- D008107
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0001663
- Subject identifier
- D011471
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Kidney Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003086
- Subject identifier
- D007674
- Condition
- Uterine Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003859
- Subject identifier
- D014594
- Condition
- Triple Negative Breast Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005537
- Subject identifier
- D064726
- Condition
- Endometrial Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0007532
- Subject identifier
- D016889
- Condition
- Lymphoma, Mantle-Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:1001469
- Subject identifier
- D020522
- Condition
- Urinary Bladder Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0001187
- Subject identifier
- D001749
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0004992
- Subject identifier
- D009369
- Condition
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0007254
- Subject identifier
- D001943
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0008170
- Subject identifier
- D010051
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0008315
- Subject identifier
- D011471
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0021259
- Subject identifier
- D011471
- Condition
- Severe Acute Respiratory Syndrome
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0100096
- Subject identifier
- D045169
- Condition identifier
- EFO_0000182
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000196
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000228
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000305
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000313
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000349
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000673
- Highest recorded phase
- 3
- Condition identifier
- EFO_0001421
- Highest recorded phase
- 1
- Condition identifier
- EFO_0001663
- Condition identifier
- EFO_0003086
- Highest recorded phase
- 1
- Condition identifier
- EFO_0005537
- Highest recorded phase
- 2
- Condition identifier
- EFO_0009782
- Highest recorded phase
- 2
- Condition identifier
- EFO_0009870
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001469
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001187
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0001187
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002158
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002447
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0002691
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0003330
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004669
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004956
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005005
- Highest recorded phase
- 1
And 25 more, listed on the interactive page.
- Event
- asthenia
- Reports
- 589
- Reporting signal score
- 285.688
- Event
- back pain
- Reports
- 300
- Reporting signal score
- 121.287
- Event
- decreased appetite
- Reports
- 502
- Reporting signal score
- 421.754
- Event
- dysphagia
- Reports
- 359
- Reporting signal score
- 357.877
- Event
- fatigue
- Reports
- 1,436
- Reporting signal score
- 982.902
- Event
- hot flush
- Reports
- 298
- Reporting signal score
- 446.048
- Event
- malignant neoplasm progression
- Reports
- 1,431
- Reporting signal score
- 3,753.53
- Event
- metastases to bone
- Reports
- 104
- Reporting signal score
- 161.902
- Event
- prostate cancer
- Reports
- 145
- Reporting signal score
- 253.046
- Event
- prostatic specific antigen increased
- Reports
- 751
- Reporting signal score
- 2,945.8
- NCT01284920
- NCT02319837
- NCT02384382
- NCT02507570
- NCT02640534
- NCT03196388
- NCT03314324
- NCT03344211
- NCT03531827
- NCT03999515
- NCT04455750
- NCT04471974
- NCT05037500
- NCT05191017
- NCT05730712
- NCT05733351
- NCT05818683
- NCT06236139
- NCT01288911
- NCT01927627
- NCT01949337
- NCT02023463
- NCT02034552
- NCT02058706
- NCT02203695
And 83 more, listed on the interactive page.
- Dose
- 160 mg
- Route
- Oral
- How often
- Once daily
- Do not chew, dissolve, or open the capsules
- Do not cut, crush, or chew the tablets
- Take with or without food
- Hydrogen bond acceptors
- 4
- Hydrogen bond donors
- 1
- Polar surface area
- 76.44
- Calculated partition coefficient (ALogP)
- 3.99
- Calculated partition coefficient (XLogP)
- 3.6
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 3
- Heavy atoms
- 32
- Molecular formula
- C21H16F4N4O2S
- Monoisotopic mass
- 464.09300959
- Natural product
- No
- 0469-0125
- 0469-0625
- 0469-0725
- 0469-1125
- 0469-1725
- Recorded assays
- 1,936
- Active assays
- 204
- Confirmatory
- Other
- Screening
These details could not be displayed.
Related records
Trials (334)
- A Clinical Study Evaluating The Benefit of Adding Rucaparib to Enzalutamide for Men With Metastatic Prostate Cancer That Has Become Resistant To Testosterone-Deprivation Therapy
- A Clinical Study of Ifinatamab Deruxtecan Based Treatment Combinations or as Monotherapy to Treat Metastatic Castrate Resistant Prostate Cancer (mCRPC) (MK-2400-01A/IDeate-Prostate02)
- A Clinical Study of QLC5508 and/or QLH12016 in Combination With Other Anti-tumor Therapies in Subjects With Advanced Prostate Cancer
- A Dose Optimization Study of Enzalutamide in Elderly Patients With Advanced Prostate Cancer
- A Multi-centre Study to Assess the Safety, Tolerability, and Pharmacokinetics of Capivasertib (AZD5363) in Combination With Novel Agents in Patients With Metastatic Prostate Cancer
- A Phase 1 Clinical Study of AZD4635 in Patients With Advanced Solid Malignancies
- A Phase 1 Study of MDV3100 in Patients With Castration-Resistant (Hormone-Refractory) Prostate Cancer
- A Phase 1/1b Study of MEDI3726 in Adults Subjects With Metastatic Castration Resistant Prostate Cancer
- A Phase 1/2a Study of DB-1311/BNT324 in Advanced/Metastatic Solid Tumors
- A Phase I/IIa Trial of HMBD-001 in Advanced HER3 Positive Solid Tumours
- A Phase Ib/II Open-label Study of AMO959 With Lutetium (177Lu) Vipivotide Tetraxetan (AAA617) in Combination With ARPI in Adult Participants With PSMA-positive mCRPC
- A Phase II Neoadjuvant Study of Enzalutamide, Abiraterone Acetate, Dutasteride and Degarelix in Men With Localized Prostate Cancer Pre-prostatectomy
- A Phase II Study Evaluating the Efficacy of Enzalutamide and the Role of ARv7 in Metastatic Castration Resistant Prostate Cancer (mCRPC) Patients With Visceral Disease.
- A Phase III Clinical Study of Rezvilutamide in Patients With Metastatic Hormone-Sensitive Prostate Cancer
- A Phase III Study Comparing HRS-4357 With Novel Androgen Receptor Pathway Inhibitors in Patients With Progressive, PSMA-Positive Metastatic Castration-Resistant Prostate Cancer
- A Positron Emission Tomography/Computed Tomography (PET/CT) Bone Imaging Study in Patients Receiving Enzalutamide for Castration-Resistant Prostate Cancer (CRPC)
- A Randomized Phase IIa Efficacy and Safety Study of Radium-223 Dichloride With Abiraterone Acetate or Enzalutamide in Metastatic Castration-resistant Prostate Cancer (CRPC)
- A Randomized Study of Enzalutamide in Patients With Localized Prostate Cancer Undergoing Active Surveillance
- A Registry Based Study Evaluating Overall Survival and Treatment Length in mCRPC Patients Treated With Enzalutamide in Sweden
- A Registry Study to Observe Clinical Outcomes of Participants With High-risk Metastatic Hormone-naïve Prostate Cancer in Japan
Approved for (7)
- Cancer
- Metastatic prostate carcinoma
- Neoplasm
- Prostate adenocarcinoma
- Prostate cancer
- Prostate carcinoma
- Prostate neoplasm
In development for (16)
- Adenocarcinoma Phase 2
- Breast cancer Phase 3
- Breast carcinoma Phase 3
- Carcinoma Phase 2
- Clear cell renal carcinoma Early phase 1
- COVID-19 Phase 2
- Exocrine pancreatic carcinoma Phase 1
- Hepatocellular carcinoma Phase 2
- Kidney disorder Phase 1
- Liver disorder Phase 1
- Mantle cell lymphoma Phase 2
- Ovarian cancer Phase 2
- Triple-negative breast carcinoma Phase 2
- Tumor of uterus Phase 2
- Urinary bladder cancer Phase 2
- Uterine corpus cancer Phase 2
Targets (1)
- AR Androgen Receptor antagonist