one more from DR. DAN
Strong Buy
From the Yahoo board. Thank you Dr. Daniel
This post is to answer some of the important questions brought up from my previous post regarding the advantage of Temanogrel over other antithrombotic meds on the market.
From the study I posted we read the following - a very important point:
"5HT2A receptor antagonists, including ketanserin, sarpogrelate,and AR246686, can effectively block arterial thrombosis without increasing bleeding.
However, lack of selectivity and suboptimal pharmacokinetics limit the usefulness of these compounds in the clinic.
Thus, our goal was to improve the selectivity and pharmacokinetic profiles, which resulted in the discovery of APD791.
Recently, APD791 was tested in the Folts dog model of coronary stenosis and was shown to effectively block coronary thrombosis without increasing bleeding time .
The separation of antithrombosis effects and bleeding is of potential clinical relevance."
Someone asked what drugs would Temangrel replace.
Here is the list:
We are all familiar with warfarin (coumadin) and plavix - both of which have problems with bleeding.
The others include dabigatran, rivaroxaban, and apixaban.
Anticoagulation with each of these newer agents leads to similar or lower rates both of ischemic stroke and major bleeding compared to warfarin.
However, the risk of gastrointestinal bleeding was increased in these agents.
There is a potentially higher rate of myocardial infarction with dabigatran and twice daily regimen (dabigatran and apixaban) Though they may have lower rates of major bleeding compared to warfarin it is still a risk with these drugs.
Therefore, if the second phase 1 trial and subsequent phase 2a and 3 trials confirm the preclinical study results of blocking thrombosis through its unique and very specific 5HT2a receptor antagonist with no increased bleeding then Temanogrel will become a major player in antithrombotic therapy
Daniel
UCLA MD
