Category Archives: Anti-Androgen

Androgen Receptors, AnHorn Medicines, Anti-Androgen, Aranda Pharma

AnHorn Medicines and Aranda Pharma: Targeting Androgen Receptors

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During the past two years, the number one area of new product development in the hair loss world has entailed the targeting of scalp androgen receptors. Coincidentally, I wrote a post in 2020 that was titled “Destroying Androgen Receptors on the Scalp“.

This is different from the go to 5α-reductase inhibitor hair loss drugs such as Dutasteride and Finasteride, which reduce dihydrotestosterone (DHT) levels.

Balding is caused by DHT binding to scalp androgen receptors, leading to hair follicle miniaturization. Many people have high levels of DHT, but lack the androgen receptor (AR) gene(s) and therefore never go bald. Balding scalps also contain higher levels of androgen receptors compared to non-balding scalps.

Androgen Receptor Targeting for Hair Loss

Among the leading companies that have developed new androgen receptor (AR) targeting products include:

  • Androgen receptor inhibitor Breezula (Clascoterone) from Cosmo Pharmaceuticals (Ireland). Currently in Phase 3 trials.
  • Androgen receptor antagonist Pyrilutamide (KX-826) from Kintor Pharmaceutical (China). Currently in Phase 3 trials, although they released a cosmetic spray version in 2024. The assigned cosmetic ingredient name is Methylpyridinyl Fluoromethoxybenzonitrile Dimethyloxothiooxoimidazolidine.
  • Androgen receptor degrader GT20029 from Kintor Pharmaceutical (China). Phase 3 trials are planned in China in 3Q 2025, with the US six months later.
  • Androgen receptor inhibitor OLX104C from Olix Pharmaceuticals (South Korea). Completed Phase 1 trials in Australia earlier this year.
  • Androgen receptor silencer CosmeRNA from Bioneer (South Korea). This product was released as a cosmetic in 2023 and is also known a SAMiRNA AR68.

We now have two new companies to add to the above list: AnHorn Medicines (Taiwan) and Aranda Pharma (Finland). However, neither is advanced enough in its clinical trial process to warrant significant interest for the time being.

AnHorn Medicines AH-001: Androgen Receptor Degrader

In November 2024, AnHorn Medicines (Taiwan) received US FDA Investigational New Drug (IND) clearance for its novel protein degrader program (h/t “John Doe”). AH-001 is described as:

“A novel, topically applied protein degrader, designed to selectively target and degrade the androgen receptor, a known driver of several challenging dermatological and hair loss disorders.”

Phase 1 clinical trials are expected to begin in the US by the end of 2024. Check out their pipeline page for more details.

Aranda Pharma ADA-308: Androgen Receptor Inhibitor

Aranda Pharma (Finland) is developing an androgen receptor inhibitor product called ADA-308 to tackle androgenetic alopecia (AGA) and acne. Below is an image from their site showing the mechanism of action of ADA-308 for both acne and AGA.

Aranda Pharma ADA-308 Androgen Receptor
Aranda Pharma ADA-308: Androgen Receptor Inhibitor for Acne and Androgenetic Alopecia. Source: Company Website.

In August 2024, Aranda Pharma in collaboration with Vancouver Prostate Centre (Canada) published an article in the journal Oncology Reports titled:

“Targeting adenocarcinoma and enzalutamide-resistant prostate cancer using the novel anti-androgen inhibitor ADA-308”

The results demonstrated the efficacy of ADA-308 in inhibiting prostate cancer cell growth.

Anti-Androgens

Note that for decades, there have already existed many anti-androgens that target the androgen receptors to combat hair loss. All of the popular anti-androgens that are used for hair growth purposes are also classified as AR antagonists. Among the ones that I have covered on this blog include Bicalutamide, Flutamide and Fluridil, RU-58841 and Spironolactone.

However, all of these anti-androgens are likely much weaker at destroying the androgen receptor strength in comparison to the newer products being developed specifically for that purpose.

Bicalutamide, Acne, Anti-Androgen, Casodex, Female Hair Loss, Hirsutism

Bicalutamide for Female Pattern Hair Loss

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Bicalutamide Female Pattern Hair Loss
Bicalutamide to treat female pattern hair loss. Before and after 6 months of treatment with 50 mg per day. © 2020 by the American Academy of Dermatology, Inc.

Over the past several years, I have increasingly been hearing about an oral anti-androgen called bicalutamide (brand name Casodex). While originally approved to treat prostate cancer in 1995, it is becoming a popular option in treating female pattern hair loss (FPHL).

Bicalutamide is a nonsteroidal antiandrogen (NSAA). It is also called a selective androgen receptor (AR) antagonist. Among the skin and hair conditions that it is being used to treat include acne, hirsutism and female pattern hair loss. Bicalutamide was originally derived from a structural modification of flutamide.

Update: August 2023 — A new paper from Brazil on treating female pattern hair loss covers bicalutamide in detail.

Update: April 2023 — From yesterday’s ISHRS Webinar:

April 19, 2023

Bicalutamide for Female Pattern Hair Loss

A number of recent reviews, studies and presentations conclude favorably in regards to the use of oral bicalutamide to treat female pattern hair loss (FPHL).

  • In 2022, researchers from Brazil reviewed various studies and concluded that oral bicalutamide seems to be a promising option to expand the arsenal of FPHL treatment. They do point out the need for clinical trials to establish the ideal dose and efficacy of the drug.
  • At the 2022 ISHRS conference, Dr. Sergio Vañó Galván discussed two “new medications” to treat hair loss: bicalutamide and clascoterone (aka Breezula).
  • Moreover, at the same conference, Dr. Alba Gómez-Zubiaur had a presentation titled: “Mesotherapy with Bicalutamide: A New Treatment for Androgenetic Alopecia.” In April 2023, he published a study on this interesting mesotherapy delivery method for bicalutamide. Make sure to also read my post on mesotherapy and dutasteride.
  • In 2020, a group of Spanish researchers retrospectively reviewed all patients who were receiving oral bicalutamide (OB) for FPHL at their hair clinic between February 2018 and February 2020. A total of 44 women receiving OB 25-50 mg daily were included. They concluded that OB had favorable hair growth results and a very good safety profile, even when used in combination with oral minoxidil or spironolactone. One of their patient’s before and after photo is shown at the top of this post.
  • In 2020, a team from Australia led by Dr. Rodney Sinclair reviewed the safety results in 316 women treated with bicalutamide. Doses ranged from 5 mg per day to 50 mg per day. The vast majority of them were also using oral minoxidil or spironolactone. In general, the safety profile was excellent and the drug benefitted female androgenetic alopecia (AGA) patients. The few patients who got a mild elevation in liver enzymes saw no adverse symptoms.

Side Effects

Bicalutamide has no diuretic effect and it does not cross the blood brain barrier. In comparison to another popular anti-androgen called flutamide, bicalutamide has a much lower rate of liver toxicity. Moreover, unlike the former, the latter does not affect serum luteinizing hormone and testosterone levels.

Bicalutamide can cause a mild elevation of liver transaminases (enzymes), peripheral edema and gastrointestinal complaints in a very small percentage of users. These side effects are usually reversible. Overall, this medication seems to cause fewer side effects than Spironolactone, the most popular anti-androgen that is used for reducing hair loss.

Note that bicalutamide is often used as an antiandrogen in feminizing hormone therapy for transgender women. And also as a puberty blocker in adolescent transgender girls.

In 2017, the combination of bicalutamide and a birth control pill was evaluated in a phase III clinical trial for the treatment of severe hirsutism in women with PCOS. The combination was found to be significantly more effective than a birth control pill alone.