Competitive differences
Dabigatran is a thrombin inhibitor and, compared to DD217, which is an factor Xa inhibitor, can have significantly more adverse effects.
Xarelto (Rivaroxaban), Eliquis (Apixaban) and Lixiana (Edoxaban), as well as DD217 are factor Xainhibitors, but DD217 showed the highest activity in the study of its anticoagulant properties on human plasma, and compared to Xarelto showed a twofold excess of efficacy when administered orally to primates in the same dosages. The figure shows that DD217 is more than 2 times more active than Xarelto (Rivaroxaban) and lasts 2 times longer than Xarelto - “softness of action”.
DD217 FDF (Finished Dosage Form) compared to Xarelto, per os, Rhesus Monkeys
Unique activity of the drug substance to the most modern target factor Xa allows to suggest that the drug based on DD217 will be the best in class of direct oral factor Xa inhibitors in terms of efficacy and safety.
|
Analogues |
Stage (presented on the market/under development) |
Concentration doubling the prothrombin time, mM |
|
DD217 |
Under development |
0.1 |
|
Rivaroxaban (Bayer and Johnson & Johnson) |
Presented on the market |
0.23 |
|
Apixaban (Pfizer and Bristol-Myers Squibb) |
Presented on the market |
0.23 |
|
Edoxaban (Daiichi Sankyo) |
Presented on the market |
0.26 |
|
Betrixaban (Portola pharmaceuticals) |
At the 3rd stage of clinical trials |
0.4 |
Source:
Bioorganic & Medicinal Chemistry Letters 21 (2011) 6228–6235- Arterioscler Thromb Vasc Biol. June 2007 1238-1247
The biological in vitro activity of the compound DD217 developed by us is the best among all known compounds.
According to results of the analysis of the interim report on results of the 1st phase of clinical trials (CT), it can be concluded that DD217 is superior to competitors over a longer half-life (by several times). This will lead to the fact that as a result of daily intake once a day, average concentration of the drug in blood will experience smaller deviations than other currently known drugs (Xarelto, Eliquis and Edoxaban).
Thus, the following advantages will be achieved:
Marketing advantage - the ease of use compared to Eliquis (Apixaban), ordered twice a day.
Safety of use - smaller deviations of concentration in blood lead to a reduction in the risk of uncontrolled internal bleeding that occurs most often in the first hours after taking medications such as Rivaroxaban or Edoxaban (prescribed once a day) and are associated pharmacokinetically with high drug concentrations in blood after administration. Moreover, a preliminary analysis of the results predicts a better safety profile even compared to Apixaban, which patients are forced to take twice a day.