>[Question by ThomasS]: Would $5-6B be rational, if all pans out?<
Instead of answering directly, let’s examine some background information so that readers may judge for themselves. Let’s first recap the pros and cons of the other classes of acute-care anticoagulants on the market or in development.
(Understanding the discussion below may be facilitated by referring to the clotting-cascade graphic in #msg-26897966.)
FXa inhibition via low-molecular-weight heparins (LMWH) such as Lovenox—or via oral FXa inhibitors in development—works well for preventing DVT. However, FXa inhibition without comparable FIIa inhibition is ineffective against arterial thrombosis. Moreover, LMWH’s and oral FXa inhibitors in development are not reversible, which is a substantial practical drawback in acute-care settings.
FIIa inhibition via Angiomax and related drugs works well for preventing arterial thrombosis; hence, these drugs are widely used in the cath lab. However, FIIa inhibition without FXa inhibition it is ineffective against DVT for either acute treatment or prophylaxis. These drugs are also not reversible.
Unfractionated heparin, the longstanding hospital standby, inhibits FXa and FIIa equally well and is reversible; however, it is unpredictable with respect to dose response and requires close monitoring to prevent life-threatening bleeding episodes.
-- Now, back to M118… it has been designed by MNTA from the ground up to incorporate the best features of unfractionated heparin, LMWH, and direct thrombin inhibitors while omitting the most troublesome features. It does this by using a proprietary mixture of short- and long-chain heparin fragments as shown in #msg-26898084.
The short heparin chains in M118 inhibit FXa but not FIIa, while the long chains inhibit both FXa and FIIa. MNTA believes that the mix of short and long chains is optimized for the therapeutic indications in which M118 will be used. If it works as advertised, it will be a monumental blockbuster, IMO.
A checklist summary of the discussion in this post may be found in #msg-26897124.
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