For those that have suffered a myocardial infarction, a wealth of drugs will be prescribed to them to aid in their recovery. Newly released data from a group of 21,000 patients has shown that Brilinta (generic name Ticagrelor) aids in the prevention of further infarcts and thus increasing life expectancy and overall quality of life, especially since it reduces the chances of further hospital stays.

What is Ticagrelor?

Ticagrelor is a platelet aggregation inhibitor from AstraZeneca. Under normal circumstances it’s use will be in conjunction with the over the counter medication aspirin on the basis that the patient has not previously suffered any ADR’s (adverse drug reactions) to aspirin.  In the trials that have been conducted, it’s effectiveness has only been assessed for those that have suffered from a heart attack in which there has been ST elevation, and said effectiveness is only at doses of 60 and 90mg when aspirin is co-prescribed.

Further whilst this is a breakthrough medication for the aforementioned group, it can hinder those that are also on digoxin. The reason behind this is due to the interactions that Ticagrelor forms within the body in that it will cause the inhibition of P-glycoprotein. This in turn will raise the circulating levels of digoxin and can have a negative effect on the patient since digoxin is dose dependent on the individual, so special consideration should be used when given to digoxin users.

How does Ticagrelor work?

As it’s drug class suggests, platelets are involved in the mechanism of action for Ticagrelor. In this regard, its mechanism of action is fairly simple. In this respect, the G-PCR (G-Protein Coupling Receptors) on platelets, namely the P2Y12 protein also contains receptors for ADP (adeonsine di-phosphate. Due to this receptor being one of the crucial proteins for initiating platelet aggregation. Ticagrelor therefore results in the blockage of the ADP receptors of P2Y12, but not as a direct and irreversible role. Rather, it is allosteric in that it binds to a site elsewhere on the molecule rather than directly on the receptor. Further, this association away from the active site on the protein allows the interaction to be reversible, which also makes any potential antidote (yet to be developed) to be able to be administered if and when needed.

 

This is certainly an exciting time for AstaZeneca, and time will tell if Ticagrelor will be able to regain the investment costs and continue to show the impressive results that has been displayed in its most recent trial.