Androgen Biosynthesis Inhibitors (cyp17a, Cyp17a1). Thoughts?

DHTpolice

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As a guy who biased towards hardcore treatment, I did some cursory research on the subject of CYP17 inhibitors. Seems like Abiraterone acetate is a most potent representative of this class of medication. This drug was designed specifically for the treatment of castration-resistant prostate cancer and, currently, this is the only one CYP17A1-inhibitor which medical use was approved by FDA. I checked, it's extremely expensive: 1 250 mg pill costs more that $70. In one study patients with no response to ADT were required as much as 2000 mg of Abiraterone acetate a day and the duration of therapy was not less than 12 weeks. That's crazy!

Ketoconazole (for oral use) is another CYP17A1 inhibitor. Its antiandrogenic properties are very impressive too, but unfortunately, this drug wasn't approved by FDA due to high incidence rate of severe liver toxicity. It's stronger than cyproterone acetate, flutamide, bicalutamide and other commonly used antiandrogens.

Seviteronel (VT-464) seems to be a best option, cause apart from castration-resistant and breast cancers, it was directly intended for treatment of androgen dependent conditions such as precocious puberty, PCOS, congential adrenal hyperplasia. So, I suppose it should also be effective in the treatment of androgenic hair loss and seborrhea. It selectively inhibits CYP17 lyase, an enzyme necessary for the synthesis of androgen and estrogen and also directly blocks the androgen receptor, so it can be a better solution than spironolactone, cyproterone acetate, flutamide and bicalutamide. The good thing is that no serious cardiac issues or liver enzyme elevations have been observed when this drug was administered to the group of 100 patients. Preliminary results from a breast cancer trial are expected by the end of this month. I hope this drug will successfully replace cyproterone acetate as a most potent oral antiandrogen on the market. If it happens, I am seriously willing to try it, lol. Only sky-high price would be a biggest drawback for me...

What do you guys think about that?
 
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ALightInTheDark

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Estrogen is benefic for hairs. If you kill it, you'll have problem with your hair.
The probleme isn't DHT or anything else, the problem is hair's sensitivity to it.
Daro is better than this and have a better profile I belive.
 

arnoldd

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Estrogen is benefic for hairs. If you kill it, you'll have problem with your hair.
The probleme isn't DHT or anything else, the problem is hair's sensitivity to it.
Daro is better than this and have a better profile I belive.

Why topical estrogens ( estradiol) dont work for regrowth ?
 

DHTpolice

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Estrogen is benefic for hairs. If you kill it, you'll have problem with your hair.
The probleme isn't DHT or anything else, the problem is hair's sensitivity to it.
Daro is better than this and have a better profile I belive.
Sure, but it shoudn't be a problem, cause I am going to use it only with estrogen therapy. These drugs don't block estrogen receptor, from what I've read. Cyproterone acetate also suppresses estrogen production, btw.
 

DHTpolice

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Do you know if keto has the same affect if applied topically?
I am not sure, have to find a study, but I guess, in order to be highly effective, topical ketoconazole should go systemic, so it can damage the liver in the long run too.
 

IdealForehead

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I am not sure, have to find a study, but I guess, in order to be highly effective, topical ketoconazole should go systemic, so it can damage the liver in the long run too.

Topical keto actually has a strange property of probably not going too much systemic. It's partly why it's so controversial as to the mechanism of action.

I can't find the link right now but there was a study where they soaked dogs head to toe in the stuff for days on end, and they didn't register any significant absorption into the blood.

A TINY bit might absorb but it must be very tiny. I don't know why it works so well topically for hair. No one really does. Maybe it's a combination of very shallow penetration, androgen receptor antagonism, and some other unknown effect. The Japanese nizoral cream study said they thought it had androgen independent growth stimulant activity as well as working as just as an antiandrogen.

Here's from Drugs.com:

Although hepatotoxicity, decreased testosterone concentrations, and decreased ACTH-induced corticosteroid concentrations have been reported with oral ketoconazole,32 105 110 these adverse effects have not been reported with topical ketoconazole105 110 and are unlikely since the drug does not appear to be appreciably absorbed following topical application to skin.2 56 57

https://www.drugs.com/monograph/ketoconazole-topical.html
 

bridgeburn

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Topical keto actually has a strange property of probably not going too much systemic. It's partly why it's so controversial as to the mechanism of action.

I can't find the link right now but there was a study where they soaked dogs head to toe in the stuff for days on end, and they didn't register any significant absorption into the blood.

A TINY bit might absorb but it must be very tiny. I don't know why it works so well topically for hair. No one really does. Maybe it's a combination of very shallow penetration, androgen receptor antagonism, and some other unknown effect. The Japanese nizoral cream study said they thought it had androgen independent growth stimulant activity as well as working as just as an antiandrogen.

Here's from Drugs.com:

Although hepatotoxicity, decreased testosterone concentrations, and decreased ACTH-induced corticosteroid concentrations have been reported with oral ketoconazole,32 105 110 these adverse effects have not been reported with topical ketoconazole105 110 and are unlikely since the drug does not appear to be appreciably absorbed following topical application to skin.2 56 57

https://www.drugs.com/monograph/ketoconazole-topical.html
Keto does something with the vitamin d receptor as well. which is supposed to be involved in anagen initiation.

Estrogen is benefic for hairs. If you kill it, you'll have problem with your hair.
Cyproterone acetate also suppresses estrogen production, btw.
yeah, but any antiandrogen which reduces T also reduces E because E is made from T. but blocking the androgen receptor causes any amount of E to be stronger because it doesnt have any antagonization from male hormones.
 

bridgeburn

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I hope this drug will successfully replace cyproterone acetate as a most potent oral antiandrogen on the market.
I wish I knew where to buy it! no liver problems sounds great. is it really stronger than cypro? now you got me curious.
 
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