Antidote for Ticagrelor Coming

March 15, 2015

AstraZeneca researchers report that a new drug call MED12452 is being developed as an antidote for patients who need to reverse the effects of ticagrelor (Brilinta/AstraZeneca) on an emergency basis. That could be important for patients taking ticagrelor who need emergency surgery or are bleeding from an accident.

AstraZeneca researchers report that a new drug call MED12452 is being developed as an antidote for patients who need to reverse the effects of ticagrelor (Brilinta/AstraZeneca) on an emergency basis. That could be important for patients taking ticagrelor who need emergency surgery or are bleeding from an accident.

Sven Nylander, PhD, of AstraZeneca Research and Development in Molndal Sweden the experimental drug works quickly to reverse the anti-clotting properties of ticagrelor.

The findings are due to be reported in a poster session Monday, March 16 at the American College of Cardiology meeting in San Diego, CA. The drug has been tested in human platelet rich plasma, Nylander said. It has also been tested in mice given the drug intravenously. Blood samples were collected at intervals of 5 minutes, 30 minutes, and 60 minutes afterwards. The experiemental drug showed an affinity for ticagrelor its active metabolite with no significant binding to adenosine, ADP, ATP or any structurally related compounds.

The recovery of platelet aggregation occurred quickly, reversing the aggregation response by 34% at 5 min., 94% at 30 min. and 83% at 60 minutes.

The researchers concluded that the experimental drug “specifically binds to ticagrelor and tricagrelor active metabolite with high affinity,” and that it “neutralizes the plasma unbound fraction of ticagrelor and reverses ticagrelor mediated inhibition of platelet aggregations in vitro”, at least in mice.


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