Dr. Costarelis’ clinical trials of SETIPIPRANT are something to watch. Surprisingly, this drug is not being administered topically in the trials. (I would have thought that a prostaglandin inhibitor would best be delivered closest to the target tissue – that is, topically – but now it makes sense to me that this stuff is being delivered orally, to reach peak concentration levels in the blood – because once full systemic absorption and equilibrium is reached, that will deliver high concentrations to the target tissue).
Setipiprant is a selective oral antagonist of the PGD2 receptor (actually, we know there are at least two different PGD2 receptors in the body, so which one are they targeting, specifically?)
What is promising about this, is that all or almost all of the people who have “home tested” prostaglandin inhibitors on themselves (like me with cromoglicic acid), and getting no results, have been doing it topically. Home experimentation with topicals involves a lot of uncertainties in dosing, formulation, vehicles, and drug absorption problems. Unless a home experimenter is also a pharmacologist, pharmacist or Ph.D. biochemist, with the proper laboratory experience and tools, one can never trust the results of home experimenters, because it’s very likely they’re not mixing the drug correctly, not using the proper vehicle to dissolve it well enough and get enough of it absorbed into the skin, etc.
The fact that Dr. Costarelis’ Setipiprant trials are oral is promising, because this is likely the best bet for getting enough of the drug into the system and the target tissues. Here is the dosing they’re using:
1000 mg setipiprant (two 500 mg tablets) twice daily (BID) at 12-hour intervals for 24 weeks.
That is very encouraging because, anyway you slice this, that is a HIGH dose. That shows they’re serious about getting enough of the drug into the tissues for it to have an effect. If this stuff works at all, these trials should prove it.