Overview
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Indication
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Associated Conditions
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Research Report
A Comprehensive Report on Azenosertib (ZN-c3): A First-in-Class WEE1 Inhibitor for Oncologic Indications
Executive Summary
Azenosertib (also known as ZN-c3) is an investigational, orally bioavailable, small molecule drug being developed by Zentalis Pharmaceuticals as a potentially first-in-class and best-in-class inhibitor of WEE1 kinase. The primary mechanism of action involves the targeted inhibition of WEE1, a critical regulator of the G2/M cell cycle checkpoint. This inhibition abrogates the cell's ability to arrest and repair DNA damage before mitosis, leading to a cascade of events including increased replication stress, premature mitotic entry, and ultimately, cancer cell death via mitotic catastrophe. This therapeutic strategy is particularly effective in tumors characterized by high genomic instability, such as those with p53 mutations or, most notably, overexpression of Cyclin E1, which has emerged as a key predictive biomarker for Azenosertib sensitivity.
The clinical development program for Azenosertib is extensive, evaluating the agent as both a monotherapy and in combination with chemotherapy, PARP inhibitors, and other molecularly targeted agents across a range of solid tumors. The program's strategy has been significantly refined by pharmacokinetic studies that established an optimized intermittent dosing schedule (400 mg daily, 5 days on, 2 days off), which more than doubles drug exposure while improving tolerability compared to continuous dosing.
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2024/04/16 | Phase 2 | Recruiting | Joyce Liu, MD | ||
2024/04/15 | Phase 1 | Recruiting | |||
2024/04/08 | Phase 1 | Recruiting | Filipa Lynce, MD | ||
2023/02/24 | Phase 1 | Terminated | K-Group, Beta, Inc., a wholly owned subsidiary of Zentalis Pharmaceuticals, Inc | ||
2023/01/12 | Phase 1 | Recruiting | K-Group Alpha, Inc., a wholly owned subsidiary of Zentalis Pharmaceuticals, Inc. | ||
2022/06/24 | Phase 1 | Withdrawn | |||
2022/01/20 | Phase 1 | Active, not recruiting | K-Group, Beta, Inc., a wholly owned subsidiary of Zentalis Pharmaceuticals, Inc | ||
2021/11/22 | Phase 2 | Recruiting | K-Group, Beta, Inc., a wholly owned subsidiary of Zentalis Pharmaceuticals, Inc | ||
2021/07/22 | Phase 1 | UNKNOWN | |||
2021/04/06 | Phase 1 | Active, not recruiting | K-Group, Beta, Inc., a wholly owned subsidiary of Zentalis Pharmaceuticals, Inc |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| No FDA approvals found for this drug. | |||||
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
| No EMA approvals found for this drug. | |||
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No HSA approvals found for this drug. | |||||
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| No TGA approvals found for this drug. | |||||
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
|---|---|---|---|---|---|
| No Health Canada approvals found for this drug. | |||||
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
|---|---|---|---|---|---|
| No CIMA AEMPS (Spain) approvals found for this drug. | |||||
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Philippines FDA approvals found for this drug. | |||||
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Saudi SFDA approvals found for this drug. | |||||
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Malaysia NPRA approvals found for this drug. | |||||
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
|---|---|---|---|---|---|
| No UK EMC drug information found for this drug. | |||||
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