Chemistry:Berzosertib
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| Formula | C24H25N5O3S |
| Molar mass | 463.56 g·mol−1 |
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Berzosertib (VE-822, VX-970, M6620) 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.[1][2][3]
Phase 1 trial results show promising results in the first clinical trial of the drug class. The new study, designed to test the drug's safety, found that half of patients given the new drug either alone or with platinum chemotherapy saw their cancer stop growing, and two patients saw their tumors shrink or disappear completely.[4][5]
In a UCLA-led study, berzosertib showed promise in treating COVID-19.[6]
References
- ↑ "Molecular Pathways: Targeting ATR in Cancer Therapy". Clinical Cancer Research 21 (21): 4780–5. November 2015. doi:10.1158/1078-0432.CCR-15-0479. PMID 26362996.
- ↑ "Targeting ATR in cancer". Nature Reviews. Cancer 18 (9): 586–595. September 2018. doi:10.1038/s41568-018-0034-3. PMID 29899559.
- ↑ "Discovery of ATR kinase inhibitor berzosertib (VX-970, M6620): Clinical candidate for cancer therapy". Pharmacology & Therapeutics 210: 107518. June 2020. doi:10.1016/j.pharmthera.2020.107518. PMID 32109490.
- ↑ "New Class of Precision Medicine Strips Cancer of its DNA Defenses" (in en). 23 June 2020. http://www.laboratoryequipment.com/565563-New-Class-of-Precision-Medicine-Strips-Cancer-of-its-DNA-Defenses/.
- ↑ "Berzosertib plus gemcitabine versus gemcitabine alone in platinum-resistant high-grade serous ovarian cancer: a multicentre, open-label, randomised, phase 2 trial". The Lancet. Oncology 21 (7): 957–968. July 2020. doi:10.1016/S1470-2045(20)30180-7. PMID 32553118.
- ↑ Goddard, Jack (25 March 2021). "Merck and UCLA find new COVID-19 treatment candidate". http://www.pharmafile.com/news/573896/merck-and-ucla-find-new-covid-19-treatment-candidate.
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