Category Archives: Setipiprant

PGD2 Inhibitors, CRTH2 (DP2), Kythera Biopharmaceuticals, Luis Garza, OC000459, PGD2, PGD2-GPR44 Pathway, Prostaglandin D2, Setipiprant

PGD2 Inhibitors: The Next Big Trend at Hair Clinics?

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Update: South Korea’s Epibiotech (formerly Stemore) was working on a PGD2 inhibitor hair loss product called SM-003. However, in 2023, it was no longer showing up in the company’s pipeline page.

Update: January 2021 — Topical cetirizine 1% (a PGD2 inhibitor) leads to significantly greater hair growth in men with androgenetic alopecia.

Prostaglandin D2

Numerous groundbreaking developments have occurred in hair loss cure research during the past few years. Among the most exciting is Kythera Biopharmaceuticals’ Setipiprant prostaglandin D2 (PGD2) antagonist (inhibiting) product.

For a better understanding of the link between male pattern baldness (MPB) and PGD2, this 2014 paper from the famous Dr. Luis Garza and Dr. Ashley Nieves is excellent reading. Also worth reading is this 2012 paper from Dr. Luis Garza, Dr. George Cotsarelis and others.

In the simplest of terms, prostaglandin D2 levels are elevated in balding scalps, and inhibiting PGD2 could prevent baldness from progressing. In order to do this, you target the PGD2-GPR44 pathway (since PGD2 binds to the GPR44 receptor).

What excited me even more so than the research behind this subject matter is the following 2015 audio interview with Kythera founder and at-the-time CEO Keith Leonard. When I first heard it, I felt like he really knew what he was talking about and was sincere. Mr. Leonard seemed very excited about the “elegant” science (from Dr. Cotsarelis and his team at the University of Pennsylvania) behind this product.

Unfortunately, it seems like Mr. Leonard is no longer with Kythera. Moreover, when I checked Kythera’s website today, the pages with a listing of board of directors and management were missing. I would not read too much into Mr. Leonard’s departure, as the release of Setipiprant is still at least several years away in a best case scenario. To learn more about Kythera and Setipiprant, read my post from 2015 in its entirety.

Clinic Made PGD2 Inhibition Products to Treat Hair Loss

What made me think about this subject matter this week after several months of forgetting about it was an interesting new article published three days ago coming from India. Apparently a local clinic named “Hairline International Hair and Skin Clinic” is now offering PGD2 inhibitor therapy for hair loss. The article is full of typos, bad science and ads. My immediate reaction is that this Indian clinic’s product is likely to be totally ineffective and a sham.

Nevertheless, this development is not surprising at all considering that so many hair loss forum members have been experimenting with similar homemade products for several years now. So perhaps such a product is not too difficult to manufacture/compound? Even something like topical cetirizine is thought to help androgenetic alopecia via reducing PGD2.

Are we about to see more hair loss clinics offer proprietary products that inhibit PGD2 or is this just a one-time thing that will spread to very few other places? A decade ago, very few hair loss clinics offered lasers or platelet-rich plasma therapy to treat hair loss, but now both are commonplace worldwide. Can PGD2 inhibition therapy follow a similar path?  With PGD2 therapy, I do wonder how much the patent held by Kythera negatively impacts the chances of other competing proprietary products from hair loss clinics becoming popular and legal, especially in the US?

Homemade PGD2 Inhibitors to Treat Hair Loss

There is a good chance that Setipiprant will significantly aid patients with androgenetic alopecia. The only problem is that clinical trials for Setipiprant will not be completed for several years. So not surprisingly, many people on hair loss forums are creating their own versions of Setipiprant or PGD2 inhibitors and testing them, or purchasing them from oftentimes sketchy vendors. The vast majority seem to have tested these “ghetto” products with no groundbreaking results to report.

However, as is always the case with such experiments, a majority of people are probably not even remotely correct in getting correct ingredients, dosages, vehicles and more. In any case, I will leave you with some links to the said hair loss forum threads further below.

Also note that I plagiarized the “ghetto” term from “Swisstemples” who I have mentioned on this blog several times before. He used to have an excellent page on his site regarding “The Postaglandin Protocol.”  He also had a page on things to buy and use (where he uses the term “ghetto protocol”) that included products to combat PGD2. I do not take any responsibility if you do what he suggests and get nasty side effects. I would never try any of this myself unless I had a really good chemist friend.

Note that people use various essentially synonymous terms for the products that they are trying in some of the below links, including “PGD2 inhibitors”, “PGD2 receptor antagonist”, “PGD2 blocker”, “PGD2-GPR-44 receptor antagonist” and “CRTH2 receptor antagonist”.

— An excellent poster from the 9th Congress for Hair Research last year  (thanks “Hellouser”) can be found here –> “CRTH2/DP2 Antagonists Reverse Hair Growth Inhibition Caused by PGD2.” Main authors are Cotsarelis, Hsieh, Nace and Zheng.

— 51 page and growing HLT thread titled “dedicated Setipiprant log.”  Seem to be overall negative results, but I have only read 3-4 of those pages.

— BTT thread on homemade  PGD2 inhibitors.

— HLT thread on whether anyone is still on PGD2 blockers?

— HLH thread on OC000459, a CRTH2 antagonist. Also see Oxagen.

— Ramatroban (a PGD2 receptor antagonist) that many people seem to have purchased. I have no idea about safety and legality issues.

— Note that Kane from China was offering his version of Setipiprant in the past, but I do not know the current status.

— Seems of interest regarding CRTH2.

— PGD2 Regimen — Cetirizine + Water.

— An interesting recent HLT thread on CRISPR type gene therapy to fix the three single nucleotide polymorphisms (SNPs). Specifically, rs545659, rs634681 and rs7167 have been found to be responsible for this PGD2 sensitivity.

— Resvertarol and PGD2?  Not sure about this one.

— Quercetin and PGD2  video. Not sure about this one either, but many other hair loss forum posts on this subject.

Allergan, ATX-101, Bimatoprost, Kybella, KYTH-105, Kythera Biopharmaceuticals, Setipiprant

Is it Time to buy Allergan (AGN) Stock?

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Note: I am no expert in stock market trading and I currently hold no Allergan (AGN) shares in my portfolio.  If I were a bit wealthier, I would seriously consider buying a few hundred shares of the pricey AGN stock.

FYI — The most important part of this lengthy post is probably right towards the end in red.

I have discussed Allergan (of Botox fame) several times on this blog during the past year. The company has had an extremely eventful 2015.  In March of this year, it was acquired by Ireland’s Actavis, but the acquiring company then changed its name to Allergan, probably because the latter is so much more widely known than the former. More importantly for us hair loss sufferers, in June of this year Allergan acquired Kythera Biopharmaceuticals.  As a result, Allergan now holds the rights to three potentially blockbuster products (first two are related to hair loss):

  1. Bimatoprost (prostamide — aka prostaglandin-ethanolamide  — analog).  This is not exactly a PGE2 analog as is often mistakenly cited on internet forums.  Sales will depend on the clinical trial results that I hope will be published any day in the next several months.  If effective, I would guess that sales will be drastically higher than lower-dose Bimatoprost products currently sold by Allergan = i.e., Latisse (around $150 million annual sales) and Lumigan (around $600 million annual sales). Maybe $1 billion in 2017 sales if the product really has a better effect than Minoxidil and it is released in 2016?  I am just throwing around numbers here so a financial expert can perhaps post comments with better forecasting.
  2. Setipiprant (KYTH-105 — selective oral antagonist to the PGD2 receptor).  Still several years before clinical trials for hair loss are completed, but numerous other clinical trials for other conditions have been completed on humans with no major side effects. Maybe this pre-existing safety profile will speed up Allergan’s trials, especially in combination with newer regulations from the 21st Century Cures Act.  Kythera also submitted an Investigational New Drug Application (IND) for Setipiprant to the US FDA a few weeks ago.  If extremely effective, sales would easily hit a few billion dollar per year in say 2020, but this is too much speculation so early in the process.  Note: Numerous people on hair loss forums are already testing Setipiprant, but I have not closely followed how they are getting their product and whether its topical or oral.  If there are many positive anecdotal reports on this in the next year, I will have to seriously consider borrowing money to buy at least several hundred shares of AGN stock.
  3. KybellaTM (ATX -101 — a patented formulation of deoxycholic acid) injected into the face to eliminate double chins.  This product was approved by the FDA in April 2015 and is already in use at 100s of clinics in the US.  Unlike the case with Botox, results from Kybella supposedly last for years.  Waiting lists are already being created in countries that have not yet been granted licenses to use Kybella.  It is worth following realself Kybella reviews to see if the product is all that it is touted to be (keeping in mind fake or flaky reviews). One article I read suggests that Allergan expects annual sales of $500 million for this product in a few years, and the patents on it run out around 2025-2030. However, there are some sources that suggest that that this product could be used for other purposes (love handles?) illegally/with doctor approval too.  Is it possible that Allergan can make much more in Kybella sales than they expect?  Moreover, it seems like it is fairly simple and cheap to manufacture this Kybella product.

Note: Allergan’s total company sales in the first half of 2015 were $10 billion.

Like many hair loss forum members, I have been much more optimistic about Setipiprant than about Bimatoprost.  Clinical trial results of Bimatoprost used at a higher dose on scalp hair have been delayed for many months, although that does not necessarily mean that the results were too weak.  I should note that I have read some positive testimonials about Bimatoprost on hair loss forums, and it is almost impossible that an Allergan representative is posting such testimonials.  Hopefully Bimatoprost turns out to be at the very least as effective as Minoxidil, while Setipiprant turns out to be even more effective and capable of growing new hair (or turning vellus hair back into terminal hair).

Is Allergan Preparing to Release Bimatoprost for Hair Loss?

In any event, the main reason for writing this post was because several days ago a member on the Baldtruthtalk forums posted an interesting link regarding Allergan expanding its plant in Waco, Texas.  The expansion is due to the addition of new processing equipment for packaging.  While the company’s VP of operations declined to name the products for which the packaging would be needed, there is a good chance that it might be for Bimatoprost. The plant already makes weaker versions of Bimatoprost (Latisse and Lumigan).  Moreover, the VP of operations said something very interesting:

We will be producing new packaging for new and existing products, and we could see the need to hire more people by the third quarter of 2016 if demand for these products increases.

Blog readers who live in Texas, please go to Waco and do some ground research!  Buy one of the workers at this plant lunch and beer to get some inside information.  Look around for any paper trails or early arrival of packaging material labeled with anything with the words “Bimatoprost” or “hair” in it.  It might seem like I am joking but I would definitely do this if I were living in Texas.  Why not spend a day in Waco?