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Alfred001

Androgen receptor blockers and upregulation

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TL DR: Is there anyone here knowledgeable about endocrinology, specifically hormone receptors, blocking them and upregulation?

I'm wondering if you could tell me what is known about how receptor blockers cause regulation, specifically how long must you block a receptor in order to induce that response and how you might avoid that.

 

THE LONG STORY:

This relates to a potential anti-hair loss drug that runs into a problem related to this. The story is this:

Clascoterone is being developed as a potential drug for treating male pattern baldness under the name Breezula (CB-03-01). Male pattern baldness progresses through DHT activating the androgen receptors (AR) in hair follicles, which over time makes the follicle go dormant. CB binds to androgen receptors so that DHT can't, preventing it from exerting its deleterious effect.

Phase II trial data for CB shows that it is very effective up to the 6 month mark and then it stops working.

People in the hairloss community have been speculating as to why that is and one hypothesis has been that, after 6 months of consistently blocking the ARs, AR upregulation is induced.

Assuming it is so, is there some way to avoid that happening? If not for this problem, CB would be a great treatment for hairloss.

Would cycling off the drug before AR upregulation is induced work? Say, taking it for 5 months then going off it and then back on?

Basically, I'm hoping there's someone here knowledgeable about this who might have some ideas about how this might be avoided.

Do you think there's an alternative explanation, other than AR upregulation?

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