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 serine/threonine kinase or Ataxia-telangiectasia mutated, symbol ATM, is a serine/threonine protein kinase that is recruited and activated by DNA double-strand breaks. It phosphorylates several key proteins that initiate activation of the DN ...
(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.
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.
In a
UCLA-led study, berzosertib showed promise in treating
COVID-19.
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Enzyme inhibitors