Category Archives: Bimatoprost

Increasing PGE2 and PGF2α for Hair Growth

I originally wrote this post in 2020 and covered the hair growth effects of increasing prostaglandin E2 (PGE2) and prostaglandin F2α (PGF2α). Not to be confused with decreasing prostaglandin D2 (PGD2) for more hair.

Update: December 14, 2022

Dermaliq Therapeutics: Prostaglandin F2α Analogue Clinical Trials

Earlier today, Dermaliq Therapeutics (US) announced that it has begun Phase 1b/2a clinical trials for its DLQ01 solution (h/t “Nick”). This product is a topical Prostaglandin F2α analogue (thought to contain latanoprost) that will be used to grow hair in men with androgenetic alopecia (aka male pattern baldness). You can check out Dermaliq’s home page for its pipeline.

The DLQ01 topical formulation is based on hyliQ®, Dermaliq’s novel and proprietary platform technology. The trials will be conduced at Dr. Rodney Sinclair’s cliinic in Australia and will last for six months. Dr. Sinclair is currently also conducting trials for Hope Medicine’s HMI-115 prolactin blocker. Make sure to read that post for one trial volunteer’s biweekly updates.

According to Dr. Betsy Hughes-Formella (Chief Scientific Officer at Dermaliq):

“Dermaliq’s hyliQ® technology has the potential to transform follicular and dermal delivery of a broad range of active ingredients. DLQ01 is just the start of a promising pipeline targeting follicular delivery.”

June 27, 2020

In a number of past posts, I have discussed how hair loss is impacted by prostaglandins (lipids). Most of my focus has been on how a reduction in prostaglandin D2 (PGD2) levels benefits hair growth. In this post, I will discuss how an increase in levels of prostaglandin E2 (PGE2) and PGF2a (PGF2α) leads to hair growth.

PGE2, PGF2α and Hair Growth.
Increase PGE2 and PGF2α for hair growth. Reduce PGD2.

It has also been hypothesized that the balance between PGE2 and PGD2 levels controls hair growth. Increased levels of PGD2 and reduced levels of PGE2 have been observed in the scalps of men suffering from androgenetic alopecia (AGA). Also of note, PGE2 is known to act synergistically with PGF2 alpha

PGE2 and Hair Growth

PGE2 (also known as dinoprostone) is a naturally occurring prostaglandin that is also known to interact with Wnt signaling. A number of studies have shown that increasing PGE2 levels on the scalp can benefit hair growth.

An interesting 2019 study found that one of the ways in which skin and tissue injury can sometimes lead to hair growth is via an increase in PGE2.

A 2018 case report from Spain found that the drug Omeprazole induced hypertrichosis (excessive body hair) in two children. This side effect resulted from a significant increase in prostaglandin E2 levels. Once Omeprazole therapy was stopped, the excess body hair entirely disappeared after six months.

One of the ways in which Minoxidil works to grow hair is via increasing PGE2 levels.

Dexamethasone and Sulfasalazine can both increase prostaglandin E2 levels significantly.

Natural products such as castor oil are thought to raise PGE2 levels, and potentially benefit hair growth. Even if true, such gains will be modest at best in my opinion.

PGF2α (aka PGF2a) and Hair Growth

PGF2α acts by binding to the prostaglandin F2α receptor. When injected into the body or amniotic sac, PGF2α can either induce labor or cause an abortion in a pregnant woman. PGF2a levels are higher in people with non-balding scalps.

In the past, I have written in detail about the glaucoma drug Bimatoprost. This drug is an analog of prostamide F2a, which is almost the same as prostaglandin F2a. Bimatoprost raises both PGF2a and PGE2 levels, and is therefore the key ingredient in eyelash hair growth drug Latisse.

Another analogue of prostaglandin F2a is the well known drug Latanaprost. It prolongs the anagen phase of the hair cycle via the prostaglandin effect.

Another glaucoma and high eye pressure relief drug named Travoprost has a patent related to its scalp hair growth properties. Travaprost raises both PGF2α and PGE2 levels on the scalp when applied topically.

The only other major PGF2a analogue pharmaceutical on the market is called Carboprost.

Bimatoprost Results are Finally Out

At the beginning of this year, I published a detailed post on Allergan’s Bimatoprost product. In that post, I stated the following:

My feeling is that Bimatoprost may result in slightly superior results to Minoxidil, but nothing extraordinary.

I am pleased as well as disappointed to say that I was correct (read the rest of this post). At the end of January 2015, Allergan finished its phase II clinical trials regarding using Bimatoprost to treat scalp hair loss.

Update: January 18, 2022 — Preparation of topical Bimatoprost with enhanced skin infiltration for hair growth.

Bimatoprost Hair Growth
Bimatoprost hair growth mechanism. Source: FASEB Journal, Randall et al, Feb 2013.

Allergan Releases Bimatoprost Results

On November 4, Allergan published two interesting pdfs on its website (can no longer be downloaded). On pages 16 and 17 of one of those pdfs, there is a surprising and unexpected summary of the initial results of using Bimatoprost to treat people with hair loss. I am assuming that these results are from the earlier mentioned clinical trials.

Update: March 2016 official safety and efficacy clinical trial results.

It seems like Bimatoprost 1% and Bimatoprost 3% both result in slightly superior hair growth in comparison to Minoxidil 5%. This is based on an “Expert Panel Review” and based on an “Investigator Global Assessment.”  Hopefully the experts and investigators involved in those reviews are unbiased and not employed or funded by Allergan.

Funnily enough, Bimatoprost 1% has slightly better results than the higher dose Bimatoprost 3% according to the “Expert Panel Review”. However, the “Investigator Global Assessment” finds the opposite to be true as one would have expected. When it comes to actual volunteer opinions based on non-scientific self-assessments, Minoxidil results seemed to be slightly better than Bimatoprost results.

We Have Become Spoilt

The overall mood of hair loss forum members regarding this news has been slightly pessimistic per my analysis. This is a bit surprising considering that to date there have only ever been two FDA approved drugs to treat hair loss on the market: Finasteride and Minoxidil. Bimatoprost will match or slightly exceed the results of one of those two (Minoxidil), and work via a different mechanism.

Just a few years ago, millions of people around the world were delighted that Minoxidil (Rogaine brand) was finally released in a foam version. The old liquid version was extremely irritating for many people and often dripped down people’s foreheads. Last year, women were also pleased that Rogaine had finally released a 5% version for females. All in all, there are numerous people out there who find Minoxidil to be very useful to slow their hair loss progression and sometimes even halt it entirely. I hope that Bimatoprost finds similar success.

At the same time, I can also understand some of the pessimism. In today’s extremely fast paced world, groundbreaking medical and technological advances are announced on a weekly basis (and popular smartphone brands come out with new versions every year). Many hair loss sufferers expect a 100 percent foolproof hair loss cure immediately. Nothing less is worth getting excited over.

While not particularly impressed by these results, I am still pleased that we could finally have a third FDA approved weapon in the fight against hair loss. And one that acts via an entirely different mechanism (prostamide F2α analog) to Finasteride or Minoxidil. With hopefully even fewer side effects.

Bimatoprost and Allergan Notes

— Even if Bimatoprost does consistently produce superior results to Minoxidil with no significant side effects, we are still at least 2-3 years away from actual product release. However, lower dose versions of Bimatoprost have already been in use for eyelash growth (via the brand name Latisse) for a few years now. I am guessing that some hair loss forum members will continue to try to make their own higher dose versions and play around with topical delivery mechanisms for the scalp. Do note that the current cost of Bimatoprost makes it very prohibitive at higher doses.

— In my post on Allergan from a month ago, I was thinking that it was worth buying the company’s stock. Since then, AGN has gone up by 10 percent. The main reason for this is due to the fact that the world’s largest drug company, Pfizer, has recently expressed interest in purchasing Allergan for $160 billion.

The primary reason given is that Pfizer would then benefit by drastically lowering its tax bill by adopting Allergan’s headquarters in Ireland. The US corporate tax rate is 35%, while Ireland’s corporate tax rate is 12.5%. However, it remains to be seen if the US government will allow Pfizer to get even bigger than it already is and also pay far less taxes to Uncle Sam. Update: Merger plans cancelled in 2016.

— Allergan plans to commence further clinical trials for Bimatoprost on scalp hair in the first quarter of 2016.