berzosertib
Berzosertib is a drug originally invented by Vertex Pharmaceuticals and licensed to Merck KGaA, Darmstadt, Germany, for development. It acts as a potent inhibitor of the enzyme ataxia telangiectasia and Rad3 related (ATR) and with lower potency as an inhibitor of ATM serine/threonine kinase (ATM). These enzymes are both involved in detecting DNA damage as part of cell cycle checkpoints during cell division. By inhibiting their activity, berzosertib interferes with the ability of rapidly dividing cells to detect damage to DNA, and this makes it useful as a potential treatment for some forms of cancer by causing accumulation of DNA damage in the cancer cells and thus reducing their viability. It has progressed furthest in trials for the treatment of ovarian cancer, though also shows activity against numerous other cancer types. — Wikipedia
Clinical trial activity
18 trials · 12 clinical orgs · 0 marketing orgs
Earliest trial started Dec 1, 2012 (NCT02157792)
Timeline
Indications
Studied for
- Brain Neoplasms · Phase 1
- Breast Neoplasms · Phase 1
- Carcinoma, Neuroendocrine · Phase 1/Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 1/Phase 2
- Carcinoma, Ovarian Epithelial · Phase 1/Phase 2
- Carcinoma, Squamous Cell · Phase 1
- Carcinoma, Transitional Cell · Phase 2
- Colorectal Neoplasms · Phase 1
- Esophageal Neoplasms · Phase 2
- Fallopian Tube Neoplasms · Phase 2
- Hamartoma · Phase 2
- Leiomyosarcoma · Phase 2
- Lung Neoplasms · Phase 1/Phase 2
- Neoplasms · Phase 1/Phase 2
- Neuroendocrine Tumors · Phase 2
- Ovarian Neoplasms · Phase 2
- Pancreatic Neoplasms · Phase 1
- Prostatic Neoplasms · Phase 2
- Prostatic Neoplasms, Castration-Resistant · Phase 2
- Small Cell Lung Carcinoma · Phase 2
- Squamous Cell Carcinoma of Head and Neck · Phase 1
- Stomach Neoplasms · Phase 2
- Urinary Bladder Neoplasms · Phase 2
- Uterine Cervical Neoplasms · Phase 1/Phase 2
Mechanism of action
- Serine-protein kinase ATRINHIBITOR
ATR inhibitor
Chemistry & pharmacology
SMILES
CNCc1ccc(-c2cc(-c3nc(-c4ccc(S(=O)(=O)C(C)C)cc4)cnc3N)on2)cc1- Mol. weight
- 463.56 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL3989870 ↗
- WikipediaBerzosertib ↗
- ChEMBLCHEMBL3545202 ↗
Also known as
- vx-970
- vx-970
- vx-970
- vx-970
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04807816 | Phase 2 | Oct 31, 2021 | Institut Bergonié, Merck KGaA |
| NCT04826341 | Phase 1/Phase 2 (Phase 2) | Sep 20, 2021 | National Cancer Institute (NCI) |
| NCT04802174 | Phase 1/Phase 2 (Phase 2) | Jun 1, 2021 | National Cancer Institute (NCI) |
| NCT04768296 | Phase 2 | Mar 29, 2021 | Merck KGaA, Merck Serono |
| NCT04216316 | Phase 1/Phase 2 (Phase 2) | Jan 10, 2020 | National Cancer Institute (NCI), University of Pittsburgh |
| NCT04052555 | Phase 1 | Nov 22, 2019 | Harvard University, National Cancer Institute (NCI) |
| NCT03896503 | Phase 2 | Aug 30, 2019 | National Cancer Institute (NCI), National Institutes of Health (NIH) |
| NCT03641313 | Phase 2 | Feb 1, 2019 | National Cancer Institute (NCI), Yale University |
| NCT03517969 | Phase 2 | Oct 6, 2018 | Harvard University, National Cancer Institute (NCI) |
| NCT02627443 | Phase 1/Phase 2 (Phase 2) | Nov 4, 2016 | Mayo Clinic, National Cancer Institute (NCI) |
| NCT02567422 | Phase 1 | Sep 2, 2016 | Johns Hopkins University, National Cancer Institute (NCI) |
| NCT02595892 | Phase 2 | Aug 25, 2016 | Harvard University, National Cancer Institute (NCI) |
| NCT02567409 | Phase 2 | Aug 19, 2016 | City of Hope National Medical Center, National Cancer Institute (NCI) |
| NCT02589522 | Phase 1 | Jul 21, 2016 | Mayo Clinic, National Cancer Institute (NCI) |
| NCT02595931 | Phase 1 | Jun 8, 2016 | National Cancer Institute (NCI), University of Pittsburgh |
| NCT02723864 | Phase 1 | Mar 22, 2016 | National Cancer Institute (NCI) |
| NCT02487095 | Phase 1/Phase 2 (Phase 2) | Jun 18, 2015 | National Cancer Institute (NCI) |
| NCT02157792 | Phase 1 | Dec 1, 2012 | Vertex |
Organizations
Research & Development (12)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| National Cancer Institute (NCI) | Government | 15 | 15 | 2 | 2015 |
| Harvard University | Academic/Hospital | 3 | 0 | 2 | 2016 |
| Mayo Clinic | Academic/Hospital | 2 | 0 | 2 | 2016 |
| Merck KGaA | For profit | 2 | 0 | 1 | 2021 |
| University of Pittsburgh | Academic/Hospital | 2 | 0 | 2 | 2016 |
| City of Hope National Medical Center | Academic/Hospital | 1 | 0 | 1 | 2016 |
| Institut Bergonié | Academic/Hospital | 1 | 1 | 1 | 2021 |
| Johns Hopkins University | Academic/Hospital | 1 | 0 | 1 | 2016 |
| Merck Serono | For profit | 1 | 1 | 1 | 2021 |
| National Institutes of Health (NIH) | Government | 1 | 0 | 1 | 2019 |
| Vertex | For profit | 1 | 1 | 1 | 2012 |
| Yale University | Academic/Hospital | 1 | 0 | 1 | 2019 |