Nitroglycerin, TOP-M119, Topadur Pharma, Vasodilation, Viagra

Topadur Pharma TOP-M119: Increased Scalp Blood Circulation

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A few people have commented or emailed me about Topadur Pharma (Switzerland)’s TOP-M119 hair growth compound in the past year. The company has yet to even begin Phase 1 clinical trials, so I was reluctant to write a post about this new product. However, two news items about Topadur in June 2024 have changed my mind.

Topadur Pharma: TOP-M119 for Hair Loss

Topadur Pharma’s TOP-M119 hair loss drug candidate promotes hair growth by activating the cyclic guanosine monophosphate (cGMP) enzyme regulatory system. This results in increased scalp blood flow via the restoration of optimal intracellular cGMP levels. The increased blood supply to the hair bulb subsequently allows for better hair growth. Cell-to-cell communication is also improved.

On Topadur’s website, they have an image that compares TOP-M119 0.002% (1.2 new hairs) versus Minoxidil 2% (0.5 new hairs). So this is not a cure, but a potentially superior treatment. The website also mentions that TOP-M119 and its structurally-related compound TOP-M111 were both very potent hair growth promoters in a predictive animal model.

Topadur Pharma TOP-M119
Topadur Pharma: TOP-M119 for Hair Growth. Source: Company website.

Topadur Pharma and Oshen Holdings Partner to Develop Alopecia Treatment

On June 6th, it was announced that Topadur Pharma AG and Oshen Holdings SA (Switzerland) would partner to develop the former’s treatment for androgenetic alopecia. According to Topadur CEO Pascal Brenneisen:

“Based on our pre-clinical data, we believe that TOP-M119 can become a game changer in treating hair loss and improving hair quality.”

The contract between Topadur and Oshen includes the following:

  • Co-development, licensing and commercialization rights for China.
  • Initial focus on the completion of IND studies, followed by Phase 1 and Phase 2 clinical trials.
  • An initial investment of CHF 3 million ($3.4 million) by Oshen in Topadur. Thereafter, milestone payments totaling CHF 12 million ($13.6 million).

In addition to the topical formulation of TOP-M119, Topadur is also developing intradermal sustained release formulations. Note that Topadur is also working on treatments for chronic wounds.

TOP-M119: Same Active Ingredient as Viagra

Yesterday, two new articles about Topadur got published and both highlight the fact that TOP-M119 has the same active ingredient (Sildenafil) as Viagra, plus Nitroglycerin and possibly other compounds. Note that in pill form, the combination of Viagra and Nitroglycerin can cause a major decrease in blood pressure. Topadur, however, is working on a slow release localized scalp formulation.

The first of these two articles is far more detailed, while the second one (link no longer works) is on a site with too many ads. The author of the first article managed to interview the ex-CEO and founder of Topadur, Mr. Reto Naef. Among the highlights:

  • TOP-M119 can increasing scalp blood circulation levels 1,000-fold.
  • This new candidate drug will be administered into the scalp through dissolving microneedles (DMNs), allowing transdermal release.
  • Human clinical trials will start in 1-2 years.
  • It has been shown that Viagra improves the active phase in the hair growth of rodents
  • The active ingredients of the candidate drug can protect against hair loss triggered by chemotherapy drug cyclophosphamide.

It should be noted that one of the ways that Minoxidil works is via its vasodilatory effects. If they add other compounds into the drug, I would not be surprised if one of them is caffeine, due its hair growth stimulatory effect.

Finasteride

US Finasteride Prescriptions Rise a Massive 200% in 7 Years

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Finasteride (5 mg) was originally approved by the US FDA in 1992 to treat enlarged prostates (BPH) in older men under the brand name Proscar. In 1997, the manufacturer Merck got FDA approval to treat hair loss with finasteride (1 mg) under the brand name Propecia. It is one of only two drugs that have ever been approved to treat hair loss in the US or Europe, with the other being minoxidil (brand name Rogaine).

Finasteride blocks the 5α-reductase enzyme (type II and III isoforms), drastically limiting the conversion of testosterone to dihydrotestosterone (DHT). DHT is the main hormone responsible for increased body hair and reduced scalp hair.

Note that dutasteride (a stronger 5α-reductase inhibitor than finasteride, including type I and II isoforms) is approved to treat hair loss in Japan and South Korea. In the US, many people use dutasteride off-label to treat their male pattern hair loss (aka androgenetic alopecia). See my posts on finasteride and dutasteride dosage comparisons and finasteride and dutasteride combination treatment.

Finasteride and Dutasteride Dosage and DHT Reduction
A comparison of DHT reduction via Finasteride and Dutasteride.

Finasteride Prescriptions in the US Rise 200 Percent in 7 years

A new report from Epic Research (conducted on behalf of NBC News) has made a startling finding. The number of men in the US with finasteride prescriptions increased nearly 200% in the last seven years.

Note that the above data does not even include topical finasteride, which is now sold by a large number of companies via online consultations. And many people get the oral drug imported from various foreign nations via sketchy websites without a prescription. Some are even getting finasteride injections into their scalps.

According to the ClinCalc DrugStats Database, finasteride was the 88th most prescribed drug in the US in 2021. Based on these latest findings from Epic Research, this ranking must have gone up significantly in 2023.

While the Epic report looked at all men 25 and older, the increase in prescriptions is likely driven mostly by young and middle-aged hair loss patients. The older enlarged prostate patient segment is already well established and not targeted by all the new ads promoting finasteride for hair growth. Moreover, there are other popular medications for enlarged prostates (e.g., Flomax); and a host of new minimally invasive surgical procedures to permanently reduce prostate size.

Doctors also say that they are seeing more and more young men seeking treatment for hair loss at an earlier age, including some in their late teens. Social media, YouTube videos and Reddit before and after finasteride hair growth photos are all contributing factors.

Moreover, there has been a proliferation or telemedicine companies such as Hims, Keeps and Ro. And these well funded companies all promote finasteride very heavily via online ads, billboards, social media and sponsorship of sporting events.

The earlier you start treating hair loss, the better the results. Of course this assumes that you get no sexual or other side effects from using finasteride. Per most findings, any such side effects are almost never permanent. However, you could be one of unlucky few, so it is always best to shave your head first and see if you can handle the appearance. That way, you never need to get on any lifelong drug treatment plan in the first place. Finasteride also impacts testosterone and estrogen levels, though usually not by much.

Note that finasteride can work for a very very long time in treating your hair loss, at least in Japanese men. As an added bonus, recent findings suggest that the drug could also lower the risk of heart disease via reducing cholesterol levels.