Table 1: Drugs currently available (post-2010)
or under clinical trials for PAH.
Drug Name |
Type of Drug |
Stage |
Route of Delivery |
Working Mechanism |
Work on animal Models |
Amlodipine |
Calcium Channel Blocker |
Currently Available |
Oral |
CCBs prevent Ca2+ entry into cells, Ca2+
will not serve as an intracellular messenger. CCBs will act as a
smooth-muscle dilator. |
Tested in rats [25]. |
Epoprostenol |
Prostanoid |
Currently Available |
I.V. |
Acts as a selective IP-prostacyclin receptor agonist.
This will promote vasodilation and inhibition of vascular smooth muscle
cells. |
|
Treprostinil |
Prostanoid |
Clinical Trial (phase 3) |
I.V. or Inhaled |
Acts as a selective IP-prostacyclin receptor agonist.
This will promote vasodilation and inhibition of vascular smooth muscle
cells. |
Tested in male and female rat models [6]. |
Macitentan |
Endothelian Receptor Antagonist |
Clinical Trial (phase 2) |
Oral |
ERAs will either interact with ERA-A or ERB. When the
antagonist interacts with either of these receptors, it will either promote
vasoconstriction or vasodilation – respectively. |
|
Ambrisentan |
Endothelian Receptor Antagonist |
Currently Available |
Oral |
ERAs will either interact with ERA-A or ERB. When the
antagonist interacts with either of these receptors, it will either promote
vasoconstriction or vasodilation – respectively. |
Work in rat models [16]. |
Riociguat |
Phosphodiesterase-5 (PDE5) Inhibitors |
Currently Available |
Oral |
Prevents hydrolysis of cGMP. cGMP prevents vasoconstriction.
Nitric oxide is release as a mediator which will promote vasodilation. |
|
Sildenafil |
Soluble Guanylyl Cyclase stimulants |
Currently Available |
Oral |
sGC stimulator will promote NO binding
on heme group. Allows for cGMP
synthesis, which will interact with the Nitric oxide cycle and promote
vasodilation. |