Zibotentan
Highest phase reached
Phase 3
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 3
- Drug type
- Small molecule
- Drug name
- Zibotentan
- Molecular weight
- 424.44
- Structure (SMILES)
- COc1nc(C)cnc1NS(=O)(=O)c1cccnc1-c1ccc(-c2nnco2)cc1
- 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.
- CAS registry numbers
- 186497-07-4
- ChEMBL ID
- CHEMBL1628688
- InChIKey
- FJHHZXWJVIEFGJ-UHFFFAOYSA-N
- PubChem compound IDs
- 9910224
- FDA ingredient codes (UNII)
- 8054MM4902
- First in class
- No
- Orphan designation
- No
- Pharmacology name
- zibotentan
- Type
- Synthetic organic
- Drug name stem
- -entan
- 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
- 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
- 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
- NCT00055471
- NCT00090363
- NCT00314782
- NCT00554229
- NCT00617669
- NCT00626548
- NCT01119118
- NCT00672581
- NCT00745875
- NCT00929162
- NCT00997945
- NCT01134497
- NCT01205711
- NCT01890135
- NCT04724837
- NCT04991571
- NCT05570305
- NCT05516498
- 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
- Recorded assays
- 329
- Active assays
- 10
- 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 Phase 2
- Cancer Phase 1
- Chronic kidney disease Phase 2
- Cirrhosis of liver Phase 2
- Colorectal cancer Phase 2
- Intermittent vascular claudication Phase 2
- Liver disorder Phase 1
- Lung cancer Phase 2
- Non-small cell lung carcinoma Phase 2
- Ovarian cancer Phase 2
- Peripheral arterial disease Phase 2
- Prostate adenocarcinoma Phase 2
- Prostate cancer Phase 3
Targets (1)
- EDNRA Endothelin receptor ET-A antagonist