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    Home > Active Ingredient News > Antitumor Therapy > AACR 2022: First-in-human trial results of second-generation PARP1 selective inhibitor announced

    AACR 2022: First-in-human trial results of second-generation PARP1 selective inhibitor announced

    • Last Update: 2022-05-18
    • Source: Internet
    • Author: User
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    On September 7, 2021 , CDE's official website showed that AstraZeneca's PARP1 selective inhibitor was approved for clinical use in advanced malignant solid tumors .


    On September 7, CDE's official website showed that AstraZeneca's PARP1 selective inhibitor was approved for clinical use in advanced malignant solid tumors


    PARP, namely polyADP-ribose polymerase (poly ADP-ribose polymerase), is a kind of ribozyme that exists in eukaryotic cells and catalyzes the synthesis of poly(ADP-ribose) [PAR].


    Part of the adverse reactions of the first-generation dual PARP1/2 inhibitor (PARPi) may come from the inhibition of PARP2, which is not necessary for efficacy


    First report of PETRA (NCT04644068) trial results


    breast cancer ovarian cancer pancreatic cancer

    As of November 17, 2021, 46 patients were taking AZD5305 10-90 mg orally daily (43.


     

    At 10-40mg QD dose, AZD5305 inhibited ≥90% polyadenosine diphosphate ribosylation (PARylation), confirming its effective binding to the target


    Results published last year showed that AZD5305 caused accumulation of DNA damage only in BRCA mutant cells and was not harmful to BRCA wild-type cells; in animal experiments, the antitumor activity of AZD5305 at a dose of 0.


    AZD5305 caused accumulation of DNA damage only in BRCA mutant cells, but was not harmful to BRCA wild-type cells; in animal experiments, the antitumor activity of AZD5305 at 0.




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