> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/zibotentan-f4c9c1df-415a-4617-939f-43a7b5eda0ea
> Record changed: 2026-10-13

# Zibotentan

Highest phase reached

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1628688)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1628688)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1628688)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1628688)

**Drug name**

Zibotentan

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1628688)

**Molecular weight**

424.44

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1628688)

**Structure (SMILES)**

COc1nc(C)cnc1NS(=O)(=O)c1cccnc1-c1ccc(-c2nnco2)cc1

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1628688)

### Other names (28)

- dapagliflozin and zibotentan
- n 3 methoxy 5 methylpyrazin 2 yl 2 4 1 3 4 oxadiazol 2 yl phenyl pridine 3 sulfonamide
- N-(3-METHOXY-5-METHYLPYRAZIN-2-YL)-2-(4-(1,3,4-OXADIAZOL-2-YL)PHENYL)PRIDINE-3-SULFONAMIDE
- zd 4054
- ZD-4054
- zd4054
- ZD4054
- ZD4054 (Zibotentan)
- ZD4054 10 mg
- ZD4054 15 mg
- ZD4054 22.5 mg
- ZD4054 Zibotentan
- zibotentan
- Zibotentan
- Zibotentan (Treatment A)
- Zibotentan (ZD4054)
- zibotentan \[INN\]
- ZIBOTENTAN \[JAN\]
- ZIBOTENTAN \[MART.\]
- ZIBOTENTAN \[MI\]
- ZIBOTENTAN \[USAN\]
- Zibotentan \[WHO-DD\]
- zibotentan inn
- zibotentan jan
- zibotentan mart

And 3 more, listed on the interactive page.

## Identifiers

**CAS registry numbers**

- 186497-07-4

**ChEMBL ID**

CHEMBL1628688

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1628688)

**InChIKey**

FJHHZXWJVIEFGJ-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1628688)

**PubChem compound IDs**

- 9910224

**FDA ingredient codes (UNII)**

- 8054MM4902

## Regulatory information

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

## Pharmacology

### Drug classification

**Pharmacology name**

zibotentan

**Type**

Synthetic organic

**Drug name stem**

\-entan

### Mechanisms of action (2)

- **Action**  
Antagonist

**Action type**  
Antagonist

**Target**  
ETA receptor

**Gene symbol**  
EDNRA

**Protein identifier**  
P25101

**Median affinity**

8.3

**Affinity units**  
pIC50

**Primary target**  
Yes
- **Mechanism**  
Endothelin receptor ET-A antagonist

**Action type**  
Antagonist

**Target**  
Endothelin-1 receptor

**Protein identifier**  
P25101

### Open Targets mechanisms

- **Mechanism**  
Endothelin receptor ET-A antagonist

**Action type**  
Antagonist

**Target**  
Endothelin-1 receptor

### Investigated indications (14)

- **Condition**  
Prostatic Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000673

**Subject identifier**  
D011471
- **Condition**  
Liver Diseases

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0001421

**Subject identifier**  
D008107
- **Condition**  
Liver Cirrhosis

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0001422

**Subject identifier**  
D008103
- **Condition**  
Carcinoma, Non-Small-Cell Lung

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0003060

**Subject identifier**  
D002289
- **Condition**  
Intermittent Claudication

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0003876

**Subject identifier**  
D007383
- **Condition**  
Renal Insufficiency, Chronic

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0003884

**Subject identifier**  
D051436
- **Condition**  
Peripheral Arterial Disease

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0004265

**Subject identifier**  
D058729
- **Condition**  
Neoplasm Metastasis

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0009708

**Subject identifier**  
D009362
- **Condition**  
Neoplasms

**Highest recorded phase**  
1

**Condition identifier**  
MONDO:0004992

**Subject identifier**  
D009369
- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0005575

**Subject identifier**  
D015179
- **Condition**  
Breast Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0007254

**Subject identifier**  
D001943
- **Condition**  
Ovarian Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0008170

**Subject identifier**  
D010051
- **Condition**  
Prostatic Neoplasms, Castration-Resistant

**Highest recorded phase**  
3

**Condition identifier**  
MONDO:0008315

**Subject identifier**  
D064129
- **Condition**  
Lung Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
MONDO:0008903

**Subject identifier**  
D008175

### Open Targets indications (23)

- **Condition identifier**  
EFO\_0000673

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0001421

**Highest recorded phase**  
1
- **Condition identifier**  
EFO\_0001422

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0003876

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0003884

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0004265

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0004285

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0009708

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0009870

**Highest recorded phase**  
2
- **Condition identifier**  
HP\_0000093

**Highest recorded phase**  
3
- **Condition identifier**  
HP\_0001394

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

**Highest recorded phase**  
1
- **Condition identifier**  
MONDO\_0005016

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005148

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005233

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005240

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005295

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005300

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0005386

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005575

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

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0008170

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

**Highest recorded phase**  
3

### Trial references (18)

- NCT00055471  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00055471)
- NCT00090363  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00090363)
- NCT00314782  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00314782)
- NCT00554229  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00554229)
- NCT00617669  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00617669)
- NCT00626548  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00626548)
- NCT01119118  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01119118)
- NCT00672581  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00672581)
- NCT00745875  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00745875)
- NCT00929162  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00929162)
- NCT00997945  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00997945)
- NCT01134497  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01134497)
- NCT01205711  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01205711)
- NCT01890135  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01890135)
- NCT04724837  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04724837)
- NCT04991571  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04991571)
- NCT05570305  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05570305)
- NCT05516498  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05516498)

## Chemical properties

**Hydrogen bond acceptors**

9

**Hydrogen bond donors**

1

**Polar surface area**

132.99

**Calculated partition coefficient (ALogP)**

2.71

**Calculated partition coefficient (XLogP)**

1.4

**Prodrug**

No

**Chirality**

Achiral

**Inorganic**

No

**Rule-of-five violations**

0

**Rotatable bonds**

6

**Heavy atoms**

30

**Molecular formula**

C19H16N6O4S

**Monoisotopic mass**

424.09537419

**Natural product**

Yes

## Evidence counts

**Recorded assays**

329

**Active assays**

10

### Active assay types (3)

- Confirmatory
- Other
- Screening

## Related records

### Trials (32)

- 10mg ZD4054 (Zibotentan) PK Study in Male, Elderly Chinese Patients With Advanced Solid Malignancies
- A Phase IIa. Open-label, Multicenter, Dose-escalation Study to Assess the Tolerability and Pharmacokinetics of ZD4054 (Zibotentan) Given Orally Once Daily in Subjects With Metastatic Prostate Cancer
- A Phase IIb Study to Evaluate the Safety of Zibotentan/Dapagliflozin in Participants With Cirrhosis-ZEAL-UNLOCK
- A Phase III Trial of ZD4054 (Zibotentan) (Endothelin A Antagonist) and Docetaxel in Metastatic Hormone Resistant Prostate Cancer
- A Phase III Trial of ZD4054 (Zibotentan) (Endothelin A Antagonist) in Hormone Resistant Prostate Cancer With Bone Metastases
- A Phase III Trial of ZD4054 (Zibotentan) (Endothelin A Antagonist) in Non-metastatic Hormone Resistant Prostate Cancer
- A Safety Study of ZD4054 in Prior Chemotherapy Treated Patients With Metastatic Hormone-resistant Prostate Cancer
- A Study to Assess Zibotentan Pharmacokinetics in Participants With Moderate Hepatic and Moderate Renal Impairment
- A Study to Investigate the Blood Concentrations of 4 Different Oral Doses of Zibotentan in Healthy Non-Asian and Japanese Participants
- A Study to Investigate the Concentrations of Zibotentan and Dapagliflozin in Blood When Given With and Without Food
- A Study to Investigate the Effects of Zibotentan/Dapagliflozin Combination Compared to Dapagliflozin Alone in Adult Participants With Chronic Kidney Disease and High Proteinuria
- Assessing the Effect of Multiple Doses of Zibotentan on the Pharmacokinetics of Single Doses of Combined Oral Contraceptives in Healthy Female Participants of Non-childbearing Potential.
- Carboplatin With or Without ZD4054 in Patients With Metastatic Breast Cancer
- Drug Interaction Study to Asses Multiple Doses of ZD4054 (Zibotentan)
- Food Effect Study of a Single Dose of ZD4054 (Zibotentan)
- Four-period Crossover Study to Assess the Effects of Single Oral Doses of ZD4054 (Zibotentan) (10mg and 30mg) on QTc Interval
- Irinotecan Hydrochloride, Fluorouracil, and Leucovorin Calcium With or Without Zibotentan in Treating Patients With Metastatic Colorectal Cancer
- Pharmacokinetics, Safety & Tolerability of ZD4054 (Zibotentan) in Subjects With Normal, Mild, Moderate and Severe Hepatic Impairment
- Phase I Study of ZD4054 (Zibotentan) and Docetaxel in Patients With Metastatic HRPC
- Precision Medicine With Zibotentan in Microvascular Angina

### In development for (13)

- [Breast cancer](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md) Phase 2
- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md) Phase 1
- [Chronic kidney disease](https://trialight.com/data/condition/chronic-kidney-disease-dc1fecbb-338b-5bbc-8d68-08e49db49918.md) Phase 2
- [Cirrhosis of liver](https://trialight.com/data/condition/cirrhosis-of-liver-d90e4a84-9e82-54fc-a553-1e42086e8382.md) Phase 2
- [Colorectal cancer](https://trialight.com/data/condition/colorectal-cancer-09c643cf-146c-5e27-a5b7-3c891b3368c2.md) Phase 2
- Intermittent vascular claudication Phase 2
- [Liver disorder](https://trialight.com/data/condition/liver-disorder-8388d30a-2581-5015-9ddf-adc5f6a331d7.md) Phase 1
- [Lung cancer](https://trialight.com/data/condition/lung-cancer-c4ca1fe0-9b3d-5957-a668-2d6cf26bd16a.md) Phase 2
- [Non-small cell lung carcinoma](https://trialight.com/data/condition/non-small-cell-lung-carcinoma-a86c1d60-523f-5ea7-a5e1-39ed4a2296f8.md) Phase 2
- [Ovarian cancer](https://trialight.com/data/condition/ovarian-cancer-f64f2018-55a5-553a-8960-76cb4906aa17.md) Phase 2
- [Peripheral arterial disease](https://trialight.com/data/condition/peripheral-arterial-disease-660376f2-3d22-5c83-86ea-1d146307e09b.md) Phase 2
- [Prostate adenocarcinoma](https://trialight.com/data/condition/prostate-adenocarcinoma-84e3e3af-1ae1-5760-8157-8d9fc0cff608.md) Phase 2
- [Prostate cancer](https://trialight.com/data/condition/prostate-cancer-3659fc70-617b-5868-a093-ae819ffc6755.md) Phase 3

### Targets (1)

- [EDNRA](https://trialight.com/data/target/ednra-89941d39-d02d-5fd8-ae9f-905322fa3386.md) Endothelin receptor ET-A antagonist

---

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