The Cb (breezula [clascoterone]) Community Thread

[mooreu]

What dosages total? That's my main issue with the anecdotes about people trying it in this thread. Due to how expensive this stuff is and the data we now have, I highly doubt people who have been trying this were using the 7.5% twice daily, let alone 2% twice a day.

I can't recall the dosage from 2011 but in 2018 I used 5% once per day.

 

[FollicleGuardian]

Is there any reason KB solution wouldn't work as a vehicle?

My understanding is that it works

 

[nick123]

Does anyone know whether binding affinity is the direct factor in an androgen receptor blockers efficacy or are there other factors involved?

 

[Mr White]

So according to the Cassiopea website, Phase 3 trials haven't even begun?! There's no way we'll have this in 2021!

 

[nick123]

Don't look for the brand name. Look for Diethylene glycol monoethyl ether.

More info on DEGEE here:

Skin Penetration and Permeation Properties of Transcutol®—Neat or Diluted Mixtures - AAPS PharmSciTech

A heightened interest in (trans)dermal delivery is in part driven by the need to improve the existing skin therapies and also the demand for alternative routes of administration, notably for pharmaceutical actives with undesirable oral absorption characteristics. The premise of delivering...

link.springer.com

I was just looking through the patent https://patents.google.com/patent/EP2503005A2/en and could not find any mention of either the words Transcutol or Diethylene glycol monoethyl ether, have they changed their formulation?

 

[John Difool]

In the Cassiopea patent of trial 2 there is ethanol, pg and transcutol.

The important part is that it dissolves in ethanol, no need for dmso and the other two agents are added as skin penetration enhancers and to reduce ethanol ratio that dries scalp. However you will need to mix it with ethanol first therefore the suggestion to add it to a Rogaine premade solution is not a possibility.

Nothing could be simpler, so a search for the "sacred vehicle" seems to me to make little sense. CB is weak in the first place so instead of optimizing the vehicle, start thinking about replacing the engine.

 

[nick123]

In the Cassiopea patent of trial 2 there is ethanol, pg and transcutol.

The important part is that it dissolves in ethanol, no need for dmso and the other two agents are added as skin penetration enhancers and to reduce ethanol ratio that dries scalp. However you will need to mix it with ethanol first therefore the suggestion to add it to a Rogaine premade solution is not a possibility.

Nothing could be simpler, so a search for the "sacred vehicle" seems to me to make little sense. CB is weak in the first place so instead of optimizing the vehicle, start thinking about replacing the engine.

There's a different patent for the second trial? I can't seem to find it..

Don't worry, I won't be wasting the CB-03-01 by adding it to any premixed solutions such as Minoxidil or Stemoxydine.

CB is weak in the first place so instead of optimizing the vehicle, start thinking about replacing the engine.

Sorry, I just want to be certain I'm understanding this. Are you suggesting to find a stronger alternative to CB-03-01? The reason I'm apprehensive to touch RU58841 is I have a history of hypertension and heart issues already.

 

[nick123]

For anyone else interested, I found the patent that was being referred to and here are some quotes:

Phase 2 clinical trial mention:

"Phase 2 Clinical Study in Males with Androgenetic Alopecia(Androgenetic Alopecia)
The formulation described in Example 4b was studied in a multicenter, randomized, double-blind, phase 2 controlled study. In the study, the formulation of Example 4b (cortexolone-17α-propionate solution 5%) was compared to vehicle solution as placebo. Both the formulation containing the active and the vehicle formulation were applied twice-daily for 26 weeks in males with androgenetic alopecia (Androgenetic Alopecia). "

Example 4b:

"Anhydrous 5% w/v Solution
A 5% (w/v) solution of cortexolone-17α-propionate having the components shown in Table 6, below, was prepared by solubilizing the therapeutic agent in the mixture of solvents followed by the addition of the antioxidant (ascorbyl palmitate) and the emulsifier (polysorbate 80).
TABLE 6 Amount Amount Amount (Kg/20 (Kg/50 Component (g/100 mL) L batch) L batch)
Cortexolone-17α-propionate 5.000 1.000 2.500
Diethylene glycol monoethyl ether (TRANSCUTOL ®) 30.000 6.000 15.000
Alcohol (Ethanol) 30.000 6.000 15.000
Ascorbyl palmitate 0.500 0.100 0.250
Polysorbate 80 0.100 0.020 0.050
Propylene glycol Q.s. Q.s. Q.s. to 100 mL to 20 L to 50 L"

So for a 100ml solution they did: 5% CB-03-01, 30% Diethylene glycol monoethyl ether (TRANSCUTOL ®), 30% Ethanol, 0.5% Ascorbyl palmitate, 0.1% Polysorbate 80 and then the rest filled up with Propylene glycol which would be 34.4%. To confirm if you don't use the antioxidant (ascorbyl palmitate) and the emulsifier (polysorbate 80), the 1:1:1 rule of ethanol, PG and transcutol can apply.

Patent: https://patents.google.com/patent/U...coterone)+alopecia&oq=(Clascoterone)+alopecia

 

[nick123]

Does anyone know whether the phase II breezula trials had HPA axis suppressing side effects? Winlevi's trials mentioned HPA axis suppression so I would assume at higher concentrations the HPA axis would be suppressed more?

 

[FollicleGuardian]

Does anyone know whether the phase II breezula trials had HPA axis suppressing side effects? Winlevi's trials mentioned HPA axis suppression so I would assume at higher concentrations the HPA axis would be suppressed more?

Wouldn’t worry about HPA axis shutdown. If I understand correctly 2/42 (?) had it. Surely the company isn’t betting on a chemical that is so harmful. Plus, addisons disease is not listed as a contraindication for Winlevi afaik. FDA doesn’t worry about so me neither. Also it’s completely reversable within 14 days or so.

 

[nick123]

As per the patent I've also compiled a table of all the solvents they tried, I've corrected it a bit as it was very messy and obviously a bad copy and paste job onto the google patent:

Solvent	Ratio	Solubility Result
Room Temperature Water	1	Insoluble
Ethanol	1	Highly soluble
Propylene glycol	1	Sparingly soluble
Isopropyl myristate	1	Insoluble
Isopropyl palmitate	1	Insoluble
Caprylocaproyl polyoxyl-8 glycerides	1	Sparingly soluble
NF (LABRASOL ®) TRANSCUTOL ®/water	1:1	Insoluble
TRANSCUTOL ®/water/ethanol	1:1:1	Soluble
Ethanol/propylene glycol	1:1	Soluble
Ethanol/propylene glycol/TRANSCUTOL ®	1:1:1	Very soluble
Water/propylene glycol/TRANSCUTOL ®	1:1:1	Insoluble
Water/propylene glycol/TRANSCUTOL ®	1:1:2	Soluble

Patent: https://patents.google.com/patent/U...coterone)+alopecia&oq=(Clascoterone)+alopecia

Would an Ethanol/Propylene glycol solution of 1:1 be too irritating on the scalp? The reason I ask is because TRANSCUTOL (Diethylene glycol monoethyl ether) is proving difficult to purchase in the UK?

 

[FollicleGuardian]

As per the patent I've also compiled a table of all the solvents they tried, I've corrected it a bit as it was very messy and obviously a bad copy and paste job onto the google patent:

Solvent	Ratio	Solubility Result
Room Temperature Water	1	Insoluble
Ethanol	1	Highly soluble
Propylene glycol	1	Sparingly soluble
Isopropyl myristate	1	Insoluble
Isopropyl palmitate	1	Insoluble
Caprylocaproyl polyoxyl-8 glycerides	1	Sparingly soluble
NF (LABRASOL ®) TRANSCUTOL ®/water	1:1	Insoluble
TRANSCUTOL ®/water/ethanol	1:1:1	Soluble
Ethanol/propylene glycol	1:1	Soluble
Ethanol/propylene glycol/TRANSCUTOL ®	1:1:1	Very soluble
Water/propylene glycol/TRANSCUTOL ®	1:1:1	Insoluble
Water/propylene glycol/TRANSCUTOL ®	1:1:2	Soluble

Patent: https://patents.google.com/patent/U...coterone)+alopecia&oq=(Clascoterone)+alopecia

Would an Ethanol/Propylene glycol solution of 1:1 be too irritating on the scalp? The reason I ask is because TRANSCUTOL (Diethylene glycol monoethyl ether) is proving difficult to purchase in the UK?

Thanks for sharing @nick123

 

[John Difool]

Try PG 60% Eth 35% Oalic acid 5%. That's the vehicle @pegasus2 suggested when dmso can be avoided and ethanol is good enough for dissolving the powder.

 

[nick123]

Try PG 60% Eth 35% Oalic acid 5%. That's the vehicle @pegasus2 suggested when dmso can be avoided and ethanol is good enough for dissolving the powder.

Potential stupid question but what about dissolving CB in 40% Ethanol, 40% PG then once its dissolved, diluting it with water?

 

[John Difool]

Water in the formulation influences permeation far less than the other solvents

 

[John Difool]

Yesterday I dumped my last 3g of CB I had bought as a large batch a year ago. This will cover the next 10 days of bid application. Then bye bye CB. You won't be missed.

 

[nick123]

Yesterday I dumped my last 3g of CB I had bought as a large batch a year ago. This will cover the next 10 days of bid application. Then bye bye CB. You won't be missed.

No results whatsoever? Are you on finasteride or dutasteride aswell? What vehicle are you using? Did you get your CB tested?

 

[nick123]

CB is week sh*t. I use it but only because Ru gives me sides. It gets the job done for the most part though with my extensive regimen.

Ok cool, vehicle, source, strength?

 

[nick123]

Someone on tressless mentioned there CB-03-01 went dark orange after leaving it there solution for two months?

https://www.reddit.com/r/tressless/comments/kt5hxt

This seems strange, any potential reason to this?

 

[nick123]

Alcohol first to dissolve, then I add in pg. Its a 50/50 split. But When I put it on my head i usually add minoxidil at the same time as I dont really like the consistency.

What % CB-03-01 did you use? Also are you on finasteride or dutasteride?