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).
- 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.
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.