> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/apalutamide-146fbb79-89a1-420c-bc35-0403bd284412
> Record changed: 2026-10-13

# Apalutamide

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3183409)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3183409)

First approval year

2018

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3183409)

## Development status

**First approval year**

2018

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3183409)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3183409)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3183409)

**Drug name**

Apalutamide

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3183409)

**Molecular weight**

477.44

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3183409)

**Structure (SMILES)**

CNC(=O)c1ccc(N2C(=S)N(c3cnc(C#N)c(C(F)(F)F)c3)C(=O)C23CCC3)cc1F

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3183409)

### Brand names (2)

- erleada
- Erleada

### Other names (27)

- apalutamida
- Apalutamida
- apalutamide
- Apalutamide
- Apalutamide (Erleada™) 60 mg or 240 mg tablets
- Apalutamide \[INN\]
- Apalutamide \[JAN\]
- Apalutamide \[MI\]
- Apalutamide \[ORANGE BOOK\]
- Apalutamide \[WHO-DD\]
- Apalutamide 240 mg
- apalutamide inn
- apalutamide jan
- apalutamide mi
- Apalutamide Oral Tablet
- apalutamide orange book
- apalutamide who dd
- arn 509
- Arn-509
- ARN-509
- ARN-509 (Phase 1)
- ARN-509 (Phase 2)
- jnj 56021927
- JNJ 56021927
- JNJ-56021927

And 2 more, listed on the interactive page.

## Identifiers

**ATC classification codes**

- L02BB05

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3183409)

**CAS registry numbers**

- 956104-40-8

**ChEMBL ID**

CHEMBL3183409

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3183409)

**InChIKey**

HJBWBFZLDZWPHF-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3183409)

**PubChem compound IDs**

- 24872560

**RxNorm IDs (RxCUI)**

- 1999574

**FDA ingredient codes (UNII)**

- 4T36H88UA7

## Regulatory information

### United States

**Applicant**

JANSSEN BIOTECH

**Approval date**

14 Feb 2018

**Application number**

NDA210951

### European Union

**Status**

Authorised

**Status date**

14 Jan 2019

**Authorisation date**

14 Jan 2019

**Approved indications**

Erleada is indicated: in adult men for the treatment of non metastatic castration resistant prostate cancer (nmCRPC) who are at high risk of developing metastatic disease. in adult men for the treatment of metastatic hormone-sensitive prostate cancer (mHSPC) in combination with androgen deprivation therapy (ADT).

**Product number**

EMEA/H/C/004452

**Authorisation holder**

Janssen-Cilag International NV

**Priority medicines scheme**

No

**Generic**

No

**Biosimilar**

No

**Generic medicines**

0

**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

Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/erleada)

### Other regulatory facts

**Patents**

14

**Designations**

2

**Earliest recorded loss of exclusivity**

14 Jan 2041

**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

### Drug classification

**Pharmacology name**

apalutamide

**Type**

Synthetic organic

**Drug name stem**

\-lutamide

**Approval recorded by Guide to Pharmacology**

Yes

#### Administration routes

- Oral

### Mechanisms of action (2)

- **Action**  
Antagonist

**Action type**  
Antagonist

**Target**  
Androgen receptor

**Gene symbol**  
AR

**Protein identifier**  
P10275

**Median affinity**

6.7

**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**  
Inhibitor

**Gene symbol**  
AR

**Protein identifier**  
P10275

**Organism**  
Homo sapiens

**Target development level**  
Clinical

### Investigated indications (10)

- **Condition**  
Prostatic Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0000196

**Subject identifier**  
D011471
- **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**  
Prostatic Neoplasms, Castration-Resistant

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0001663

**Subject identifier**  
D064129
- **Condition**  
Salivary Gland Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0003826

**Subject identifier**  
D012468
- **Condition**  
Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
MONDO:0004992

**Subject identifier**  
D009369
- **Condition**  
Prostatic Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
MONDO:0008315

**Subject identifier**  
D011471
- **Condition**  
Prostatic Neoplasms, Castration-Resistant

**Highest recorded phase**  
4

**Condition identifier**  
MONDO:0008315

**Subject identifier**  
D064129

### Open Targets indications (18)

- **Condition identifier**  
EFO\_0000196

**Highest recorded phase**  
2
- **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\_0003826

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0004920

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0000521

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0004956

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0004992

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0005070

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0005082

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005159

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0008315
- **Condition identifier**  
MONDO\_0008315

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0015667
- **Condition identifier**  
MONDO\_0015667

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0021259

**Highest recorded phase**  
4

### Reported adverse events (13)

- **Event**  
blood thyroid stimulating hormone increased

**Reports**  
16

**Reporting signal score**

33.2639
- **Event**  
decreased appetite

**Reports**  
66

**Reporting signal score**

40.9002
- **Event**  
dermatitis exfoliative generalised

**Reports**  
11

**Reporting signal score**

24.452
- **Event**  
disease progression

**Reports**  
49

**Reporting signal score**

36.4677
- **Event**  
fatigue

**Reports**  
164

**Reporting signal score**

60.759
- **Event**  
headache

**Reports**  
13

**Reporting signal score**

20.9081
- **Event**  
hot flush

**Reports**  
71

**Reporting signal score**

127.469
- **Event**  
prostate cancer

**Reports**  
15

**Reporting signal score**

19.1271
- **Event**  
prostatic specific antigen decreased

**Reports**  
5

**Reporting signal score**

22.3018
- **Event**  
prostatic specific antigen increased

**Reports**  
47

**Reporting signal score**

135.867
- **Event**  
pruritus

**Reports**  
65

**Reporting signal score**

21.8574
- **Event**  
rash

**Reports**  
282

**Reporting signal score**

313.942
- **Event**  
vomiting

**Reports**  
10

**Reporting signal score**

21.3464

### Trial references (86)

- NCT01171898  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01171898)
- NCT01790126  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01790126)
- NCT01792687  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01792687)
- NCT02106507  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02106507)
- NCT02489318  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02489318)
- NCT02578797  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02578797)
- NCT02770391  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02770391)
- NCT02772588  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02772588)
- NCT02789878  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02789878)
- NCT02811809  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02811809)
- NCT02849990  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02849990)
- NCT02867020  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02867020)
- NCT02903368  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02903368)
- NCT03009981  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03009981)
- NCT03080116  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03080116)
- NCT03088124  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03088124)
- NCT03093272  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03093272)
- NCT03098836  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03098836)
- NCT03141671  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03141671)
- NCT03279250  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03279250)
- NCT03311555  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03311555)
- NCT03365297  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03365297)
- NCT03436654  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03436654)
- NCT03488810  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03488810)
- NCT03777982  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03777982)

And 61 more, listed on the interactive page.

## Dosing

**Dose**

240mg

**Route**

Oral

**How often**

Once daily

### Conditions of use (2)

- Can be taken with or without food
- Swallow tablets whole

## Chemical properties

**Hydrogen bond acceptors**

5

**Hydrogen bond donors**

1

**Polar surface area**

89.33

**Calculated partition coefficient (ALogP)**

3.53

**Calculated partition coefficient (XLogP)**

3

**Prodrug**

No

**Chirality**

Achiral

**Inorganic**

No

**Rule-of-five violations**

0

**Rotatable bonds**

3

**Heavy atoms**

33

**Molecular formula**

C21H15F4N5O2S

**Monoisotopic mass**

477.08825856

**Natural product**

No

## National Drug Codes

- 59676-600
- 59676-604

## Evidence counts

**Recorded assays**

470

**Active assays**

102

### Active assay types (3)

- Confirmatory
- Other
- Screening

## Related records

### Trials (147)

- 14C-ARN-509 Microtracer Label AME and Absolute BA Study
- A JNJ-56021927 (ARN-509; Apalutamide) QT/QTc Study
- A Phase I/II Study of Regorafenib Plus Avelumab in Solid Tumors
- A Phase II Neoadjuvant Study of Apalutamide, Abiraterone Acetate, Prednisone, Degarelix and Indomethacin in Men With Localized Prostate Cancer Pre-prostatectomy
- A Registry Study to Observe Clinical Outcomes of Participants With High-risk Metastatic Hormone-naïve Prostate Cancer in Japan
- A Safety and Pharmacokinetics Study of Niraparib Plus an Androgen Receptor-Targeted Therapy in Men With Metastatic Castration-Resistant Prostate Cancer (BEDIVERE)
- A Safety Study of JNJ-56021927 in Participants With Metastatic Castration-Resistant Prostate Cancer
- A Salvage Trial of AR Inhibition With ADT and Apalutamide With Radiation Therapy Followed by Docetaxel in Men With PSA Recurrent Prostate Cancer After Radical Prostatectomy (STARTAR)
- A Study for the Participants With Metastatic Hormone Sensitive Prostate Cancer (mHSPC) Treated With Androgen Deprivation Therapy (ADT) Plus Apalutamide or Enzalutamide
- A Study of Adding Apalutamide to Radiotherapy and LHRH Agonist in High-Risk Patients With Hormone-Sensitive Prostate Cancer
- A Study of an Intermittent ADT Approach With Apalutamide Monotherapy in Participants With mCSPC
- A Study of Androgen Annihilation in High-Risk Biochemically Relapsed Prostate Cancer
- A Study of Androgen Receptor (AR) Antagonist Apalutamide in Chinese Participants With Metastatic Castration-Resistant Prostate Cancer
- A Study of Apalutamide (Adjuvant Treatment) and Androgen Deprivation Therapy (ADT) in Participants Who Have Undergone Radical Prostatectomy (RP) for Non-metastatic Prostate Cancer and Who Are at High Risk for Metastases
- A Study of Apalutamide (ARN-509) in Men With Non-Metastatic Castration-Resistant Prostate Cancer
- A Study of Apalutamide (JNJ-56021927, ARN-509) Plus Androgen Deprivation Therapy (ADT) Versus ADT in Participants With mHSPC
- A Study of Apalutamide Administered Orally as Whole Tablets and as a Mixture in Applesauce in Healthy Participants
- A Study of Apalutamide Combined With GnRH Agonist in Participants With Androgen Receptor Positive Salivary Gland Carcinoma
- A Study of Apalutamide in Chinese Participants With Non Metastatic Castration Resistant Prostate Cancer (NM-CRPC)
- A Study of Apalutamide in Participants With High-Risk, Localized or Locally Advanced Prostate Cancer Who Are Candidates for Radical Prostatectomy

### Approved for (6)

- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md)
- [Metastatic prostate carcinoma](https://trialight.com/data/condition/metastatic-prostate-carcinoma-d5fb1084-bad5-5db6-8240-897dc47ea451.md)
- Neoplasm
- [Prostate adenocarcinoma](https://trialight.com/data/condition/prostate-adenocarcinoma-84e3e3af-1ae1-5760-8157-8d9fc0cff608.md)
- [Prostate cancer](https://trialight.com/data/condition/prostate-cancer-3659fc70-617b-5868-a093-ae819ffc6755.md)
- [Prostate carcinoma](https://trialight.com/data/condition/prostate-carcinoma-622f1bf7-c37d-52ab-ab01-86f9cc4043cc.md)

### In development for (2)

- [Liver disorder](https://trialight.com/data/condition/liver-disorder-8388d30a-2581-5015-9ddf-adc5f6a331d7.md) Phase 1
- Tumor of salivary gland Phase 2

### Other linked conditions (1)

- Acute myeloid leukemia by FAB classification

### Targets (1)

- [AR](https://trialight.com/data/target/ar-a6af2dca-1d81-5967-9bce-dc5b29aacbbc.md) Androgen Receptor antagonist

---

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