> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/darolutamide-58582cea-cd7f-464d-b5cc-049941dce9c1
> Record changed: 2026-10-13

# Darolutamide

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297185)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297185)

First approval year

2019

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297185)

## Development status

**First approval year**

2019

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297185)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297185)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297185)

**Drug name**

Darolutamide

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297185)

**Molecular weight**

398.85

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297185)

**Structure (SMILES)**

CC(O)c1cc(C(=O)N\[C@@H\](C)Cn2ccc(-c3ccc(C#N)c(Cl)c3)n2)n\[nH\]1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297185)

### Brand names (2)

- nubeqa
- Nubeqa

### Other names (36)

- bay 1841788
- BAY 1841788
- bay 1841788 odm 201
- BAY 1841788(ODM-201)
- BAY-1841788
- bay1841788
- BAY1841788
- BAY1841788 (darolutamide)
- BAY1841788 (ODM-201)
- darolutamida
- Darolutamida
- darolutamide
- Darolutamide
- Darolutamide (BAY 1841788)
- Darolutamide (BAY1841788)
- Darolutamide (Nubeqa®) 300 mg tablets
- darolutamide \[INN\]
- DAROLUTAMIDE \[JAN\]
- DAROLUTAMIDE \[MI\]
- DAROLUTAMIDE \[ORANGE BOOK\]
- DAROLUTAMIDE \[USAN\]
- Darolutamide \[WHO-DD\]
- Darolutamide 300 mg
- darolutamide inn
- darolutamide jan

And 11 more, listed on the interactive page.

## Identifiers

**CAS registry numbers**

- 1297538-32-9

**ChEMBL ID**

CHEMBL4297185

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297185)

**InChIKey**

BLIJXOOIHRSQRB-PXYINDEMSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297185)

**PubChem compound IDs**

- 67171867

**RxNorm IDs (RxCUI)**

- 2180325

**FDA ingredient codes (UNII)**

- X05U0N2RCO

### ATC classification codes (2)

- L02BB
- L02BB06

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4297185)

## Regulatory information

### United States

**Applicant**

BAYER HEALTHCARE

**Approval date**

30 Jul 2019

**Application number**

NDA212099

### European Union

**Status**

Authorised

**Status date**

27 Mar 2020

**Authorisation date**

27 Mar 2020

**Approved indications**

NUBEQA is indicated for the treatment of adult men with non‑metastatic castration resistant prostate cancer (nmCRPC) who are at high risk of developing metastatic disease (see section 5.1). metastatic hormone‑sensitive prostate cancer (mHSPC) in combination with androgen deprivation therapy (see section 5.1). metastatic hormone‑sensitive prostate cancer (mHSPC) in combination with docetaxel and androgen deprivation therapy (see section 5.1).

**Product number**

EMEA/H/C/004790

**Authorisation holder**

Bayer AG

**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, Castration-Resistant

European medicines record

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

### Other regulatory facts

**Patents**

9

**Designations**

2

**Earliest recorded loss of exclusivity**

17 Jun 2042

**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**

darolutamide

**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**

7.59

**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 (2)

- **Action type**  
Antagonist

**Gene symbol**  
PGR

**Protein identifier**  
P06401

**Organism**  
Homo sapiens

**Target development level**  
Clinical
- **Action type**  
Inhibitor

**Gene symbol**  
AR

**Protein identifier**  
P10275

**Organism**  
Homo sapiens

**Target development level**  
Clinical

### Investigated indications (12)

- **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**  
Prostatic Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0001663

**Subject identifier**  
D011471
- **Condition**  
Salivary Gland Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0000521

**Subject identifier**  
D012468
- **Condition**  
Salivary Gland Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0004669

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

**Highest recorded phase**  
4

**Condition identifier**  
MONDO:0004992

**Subject identifier**  
D009369
- **Condition**  
Breast Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0007254

**Subject identifier**  
D001943
- **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
- **Condition**  
Granulosa Cell Tumor

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0020541

**Subject identifier**  
D006106
- **Condition**  
Prostatic Neoplasms, Castration-Resistant

**Highest recorded phase**  
4

**Condition identifier**  
MONDO:0021259

**Subject identifier**  
D064129

### Open Targets indications (21)

- **Condition identifier**  
EFO\_0000196

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0000616
- **Condition identifier**  
EFO\_0000673

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0001663

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0006461

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

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0004669

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

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0004992

**Highest recorded phase**  
2
- **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\_0005233

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005494

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0007254

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008315
- **Condition identifier**  
MONDO\_0008315

**Highest recorded phase**  
4
- **Condition identifier**  
MONDO\_0020541

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0021259
- **Condition identifier**  
MONDO\_0023283

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0044881

**Highest recorded phase**  
1

### Reported adverse events (12)

- **Event**  
brainstem compression

**Reports**  
1

**Reporting signal score**

8.64902
- **Event**  
fatigue

**Reports**  
22

**Reporting signal score**

13.1482
- **Event**  
gastric cancer recurrent

**Reports**  
1

**Reporting signal score**

5.8774
- **Event**  
hormone-refractory prostate cancer

**Reports**  
7

**Reporting signal score**

39.6865
- **Event**  
hospitalisation

**Reports**  
11

**Reporting signal score**

14.2687
- **Event**  
malignant neoplasm of renal pelvis

**Reports**  
1

**Reporting signal score**

5.48603
- **Event**  
metastases to bone

**Reports**  
4

**Reporting signal score**

9.31887
- **Event**  
nothing by mouth order

**Reports**  
1

**Reporting signal score**

7.39642
- **Event**  
parvovirus b19 test positive

**Reports**  
1

**Reporting signal score**

5.97574
- **Event**  
product dose omission issue

**Reports**  
5

**Reporting signal score**

6.23357
- **Event**  
prostatic specific antigen increased

**Reports**  
6

**Reporting signal score**

18.9081
- **Event**  
stoma obstruction

**Reports**  
1

**Reporting signal score**

5.62241

### Trial references (60)

- NCT01317641  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01317641)
- NCT01429064  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01429064)
- NCT01784757  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01784757)
- NCT02200614  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02200614)
- NCT02799602  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02799602)
- NCT02933801  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02933801)
- NCT02972060  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02972060)
- NCT03385655  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03385655)
- NCT03568656  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03568656)
- NCT03724747  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03724747)
- NCT03903835  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03903835)
- NCT04025372  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04025372)
- NCT04136353  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04136353)
- NCT04157088  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04157088)
- NCT04176081  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04176081)
- NCT04237584  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04237584)
- NCT04558866  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04558866)
- NCT04737109  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04737109)
- NCT04916613  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04916613)
- NCT05059236  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05059236)
- NCT05116475  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05116475)
- NCT05171387  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05171387)
- NCT05249712  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05249712)
- NCT05346848  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05346848)
- NCT05348876  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05348876)

And 35 more, listed on the interactive page.

## Dosing

**Dose**

600 mg

**Route**

Oral

**How often**

Twice daily

### Conditions of use (2)

- Swallow tablets whole
- Take with food

## Chemical properties

**Hydrogen bond acceptors**

6

**Hydrogen bond donors**

3

**Polar surface area**

119.62

**Calculated partition coefficient (ALogP)**

2.67

**Calculated partition coefficient (XLogP)**

1.8

**Prodrug**

No

**Chirality**

Racemic

**Inorganic**

No

**Rule-of-five violations**

0

**Rotatable bonds**

6

**Heavy atoms**

28

**Molecular formula**

C19H19ClN6O2

**Monoisotopic mass**

398.1258016

**Natural product**

Yes

## National Drug Codes

- 50419-395

## Evidence counts

**Recorded assays**

288

**Active assays**

26

### Active assay types

- Confirmatory

## Biological measurements

### Observed measurements

#### Solubility

**Median**

24,460

**Mean**

24,460

**Minimum**

24,460

**Maximum**

24,460

**Unit**

nM

**Assays**

1

**Standard deviation**

0

**Summary method**

median

**Censored results excluded**

0

**Other units excluded**

0

**Unknown units excluded**

0

#### Measurement types

- Solubility

## Related records

### Trials (120)

- 177Lu-PSMA-617 Combined With Darolutamide in Neoadjuvant Treatment of High-risk Localized Prostate Cancer: a Prospective, Single-arm, Multi-center Clinical Trial
- [A Clinical Study of KTX-2001 in Subjects With Metastatic Castration-Resistant Prostate Cancer (STRIKE-001)](https://trialight.com/data/trial/a-clinical-study-of-ktx-2001-in-subjects-with-metastatic-91eebe70-94e2-44ca-b197-78e0187bba9a.md)
- A Phase 1b/2a Study of Pocenbrodib as Monotherapy and in Combination With Darolutamide in Participants With mCRPC
- A Phase 2 Trial of Darolutamide as a Prostate-Specific Membrane Antigen (PSMA) Expression Enhancer in Patients With Localized Prostate Cancer
- A Phase II Neoadjuvant Study of Darolutamide Plus ADT in Men With Localized Prostate Cancer
- A Study Called ARAMON to Learn to What Extent Does Study Treatment With Darolutamide Affects Testosterone Levels in Men With Prostate Cancer That Had Not Been Treated With Hormonal Therapy Compared to Treatment With Enzalutamide
- A Study Comparing ARB With Radium-223 vs ARB Therapy With Placebo and the Effect Upon Survival for mCRPC Patients
- A Study in Which Non-metastatic Castration-resistant Prostate Cancer (nmCRPC) Patients for Whom a Decision to Treat With Darolutamide Has Been Made Before Enrollment Are Observed and Certain Outcomes Are Described
- A Study of HRS-5041 Tablets Combined With Antitumor Therapy in Subjects With Advanced Prostate Cancer
- [A Study of Pasritamig (JNJ-78278343) in Combination With Other Agents for Metastatic Prostate Cancer](https://trialight.com/data/trial/a-study-of-pasritamig-jnj-78278343-in-combination-with-other-e6590381-7e15-4bbc-982a-d0945f86d1f5.md)
- A Study of Patient Preference Between ODM-201 and Enzalutamide in Men With Metastatic Castrate-resistant Prostate Cancer
- A Study of Valemetostat (DS-3201b) in Combination With Darolutamide in Metastatic Castration Resistant Prostate Cancer (mCRPC)
- A Study to Compare Darolutamide Given With Androgen Deprivation Therapy (ADT) and Placebo Given With ADT in Men With Hormone Sensitive Prostate Cancer and Raise of Prostate Specific Antigen (PSA) Levels After Local Therapies
- A Study to Evaluate Changes in Human Breast Cancer Tissue Following Short-Term Use of Darolutamide
- A Study to Investigate the Biological Effects of Saruparib (AZD5305), Darolutamide, and in Combination in Men With Newly Diagnosed Prostate Cancer.
- A Study to Learn About How Safe Darolutamide is and How Well it Works in Combination With Androgen Deprivation Therapy and Docetaxel in Routine Medical Care for Japanese Men With Low Volume Metastatic Hormone-Sensitive Prostate Cancer
- A Study to Learn About Real-world Utilization and Outcomes of Darolutamide and Other Androgen Receptor Pathway Inhibitors (ARPIs) for Newly Diagnosed Metastatic Hormone-sensitive Prostate Cancer (de Novo mHSPC) in US Urology Clinics
- A Study to Learn About the Investigational Drug Rinzimetostat (ORIC-944) in Patients With mCRPC Who Were Previously Treated With Abiraterone Acetate (Himalayas-1)
- A Study to Learn About the Outcomes Between Study Medicines, Enzalutamide and Darolutamide Among Men With Metastatic Castration Sensitive Prostate Cancer (mCSPC)
- A Study to Learn How Men With Advanced Prostate Cancer Respond to Treatment With Darolutamide and Hormone Therapy, With or Without Chemotherapy, in Real-world Medical Practice

### Approved for (7)

- [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)
- [Prostate neoplasm](https://trialight.com/data/condition/prostate-neoplasm-28a8a0a9-1d2f-5539-80c9-7eb822c444fc.md)

### In development for (4)

- [Breast cancer](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md) Phase 2
- Maligant granulosa cell tumor of ovary Phase 2
- Salivary gland cancer Phase 2
- Salivary gland carcinoma Phase 2

### Targets (1)

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

---

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