“Clascoterone will be the first ever drug in 30 years to treat male pattern baldness by boosting hair growth by 500%”
From…
And review…
FWIW
I do not have any financial interest in this company.
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Really nice! Has anyone found it online? Do you need a prescription for it?
Purchase 98% HPLC grade and make your own 5% solution.
or wait for commerical product.
“If you wait until you are ready, it is almost certainly too late.”
~Seth Godin
I am not the waiting type.
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It’s not a cure because you need to use it daily for the rest of your life like all the other hairloss drugs and given the huge variety between the two studies (168% and 539% better hair improvement compared to placebo) it’s likely not even better than finasteride. Nor will it restore hair follicles that have been replaced by scar tissue or where the arrector pili muscle has been destroyed.
All in all probably a viable alternative to 5ar inhibitors for people slowly balding at the temples or crown, if you can afford it.
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New study shows promising hair loss improvement with compound CB-03-01 aka Breezula aka Clascoterone
GPT summary:
"Breezula (clascoterone 5 percent topical) has completed two large Phase III trials showing strong performance against placebo in target area hair count, although the headline figure of 539 percent is a relative comparison inside a tiny measurement zone. It does not mean users will see a fivefold increase in visible hair. The second study showed 168 percent relative improvement, which highlights how unstable ratio style metrics can be without the actual hair count numbers. Earlier phase 2 data suggests realistic gains of roughly 10 to 14 extra hairs per square centimeter, similar to what many users get from oral finasteride but without systemic hormonal side effects.
Overall cosmetic improvement will depend on baseline density, hair thickness, curl pattern, and whether the thinning is diffuse. Even so, the treatment continues to look promising for people who want an androgen receptor blocker that does not affect hormone levels. Safety and tolerability appear strong with a profile similar to placebo. Regulatory submissions are underway and Breezula is likely to become the next approved treatment for male pattern hair loss, possibly joining the standard treatment stack in the coming years."
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I thought I’d add to your post with this I just found. I see it’s already available for other indications.
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We’d all be interested in someone actually buying this.
Since mechanism of action is similar to fastineride(?) blocks DHT, Id worry about similar side effects, killing libido and worse, fastineride syndrome where dopamine is permanently suppressed for some individuals.
Tnx curt
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It’s more similar to RU58841. It blocks androgens attaching to the receptor.
This is different to finasteride that is an inhibitor of the 5 alpha reductase enzyme which converts testosterone to dihydrotestosterone.
Theoretically it shouldn’t have the same side effect profile.
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Post-finasteride syndrome is most likely not even a real condition because case reports point to it being a mental illness Post-Finasteride Syndrome: An Induced Delusional Disorder with the Potential of a Mass Psychogenic Illness? - PubMed and all other studies and case reports showing reversal to baseline hormonal values and sperm quality parameters.
Also clascoterone is not a 5ar inhibitor but an androgen receptor blocker with some but minimal systemic absorption.
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An AI Summary (from Gemini) of this drug and the clinical trials:
Executive Summary: Clascoterone 5% (Breezula)
Drug Class: Topical Androgen Receptor Inhibitor Status: Phase 3 Clinical Development (SCALP 1 & 2 Trials)Developer: Cosmo Pharmaceuticals / Cassiopea
Clascoterone (cortexolone 17-alpha-propionate) represents the first potential new mechanism of action for androgenetic alopecia (AGA) in decades. Unlike finasteride, which inhibits the production of dihydrotestosterone (DHT), clascoterone inhibits the reception of DHT at the follicular level.
1. Mechanism of Action: Peripheral Ligand Competition
Clascoterone operates via competitive antagonism at the androgen receptor (AR) located within the hair follicle and sebaceous gland.
- Receptor Blockade: It competes with circulating DHT for binding sites on the androgen receptor. By blocking this interaction, it prevents the gene transcription events that lead to follicular miniaturization (hair thinning).
- Metabolic Inactivation: A critical differentiator is its metabolic profile. Upon penetrating the scalp skin, clascoterone is designed to be active locally. Once it enters the systemic circulation, it is rapidly hydrolyzed by plasma esterases into cortexolone, an inactive metabolite.
- Result: This localized activity aims to minimize the systemic side effects typical of oral anti-androgens (e.g., loss of libido, erectile dysfunction).
2. Clinical Data: Phase 2 Dose-Ranging Results
The most robust peer-reviewed data currently available comes from the Phase 2 dose-ranging study published in JAMA Dermatology. This study established the therapeutic window and safety profile.
Study Reference: Safety and Efficacy of Topically Applied Clascoterone Solution in Androgenetic Alopecia (JAMA Dermatol, 2020)
Study Design
- Participants: 404 men with mild-to-moderate androgenetic alopecia.
- Duration: 12 months.
- Arms: Clascoterone (2.5%, 5.0%, 7.5%) applied once or twice daily vs. Vehicle (Placebo) vs. Minoxidil 2% (as a comparator).
Key Findings (12-Month Data)
- Efficacy (Hair Count): The 7.5% twice-daily (BID) group showed the highest efficacy, but the 5% BID dose was selected for Phase 3 due to an optimal balance of efficacy and drug formulation stability.
- The 7.5% BID group saw a statistically significant increase in Target Area Hair Count (TAHC) compared to the vehicle.
- The clinical efficacy of Clascoterone was roughly comparable to Minoxidil 2% in this specific dataset.
- Hair Width: Improvements in hair width (reversal of miniaturization) were noted, confirming the mechanism acts on the follicle quality, not just retention.
3. Phase 3 Trial Architecture (SCALP Program)
To achieve FDA approval, Cosmo Pharmaceuticals initiated two identical pivotal trials. These trials are designed to confirm the Phase 2 findings in a larger population.
Study Reference: Dec 2025 Status: Phase 3 Study of Clascoterone Solution in Males With Androgenetic Alopecia (ClinicalTrials.gov)
Trial Specs
- Population: Approximately 1,400 males (SCALP 1 and SCALP 2).
- Primary Endpoint: Change from baseline in Non-Vellus Target Area Hair Count (TAHC) at Month 6.
- Secondary Endpoint: Patient-reported hair growth assessment (HGA).
- Control: Vehicle (placebo).
Critical Note on Data: While early projections estimated high efficacy, the true market value of Breezula depends on whether Phase 3 data shows a statistically significant maintenance of hair count beyond 12 months without the phenomenon of “tolerance” or tachyphylaxis seen in some topical therapies.
4. Safety and Toxicology Profile
For longevity-focused individuals, the safety profile is the primary asset of this compound, as it offers androgen protection without systemic endocrine disruption.
- HPA Axis Suppression: In Phase 2 trials, there was no clinical evidence of Hypothalamic-Pituitary-Adrenal (HPA) axis suppression, a common risk with topical steroids.
- Systemic Absorption: Pharmacokinetic data confirms that steady-state plasma concentrations of clascoterone remain below the threshold required to induce systemic anti-androgenic effects.
- Adverse Events: The most common adverse events were local skin reactions (erythema, scaling), which were generally mild and similar in frequency to the vehicle group.
5. Strategic Synthesis for the User
The Gap in Therapy: Current FDA-approved options force a choice between systemic hormonal alteration (finasteride) and hemodynamic stimulation (minoxidil). Clascoterone fills the gap as a topical anti-androgen.
Scientific Debate: There is an ongoing debate regarding the potency of competitive receptor antagonism (clascoterone) versus enzyme inhibition (finasteride/dutasteride).
- Finasteride lowers the total amount of “fuel” (DHT) available.
- Clascoterone blocks the “engine” (receptor).
- Hypothesis: Theoretically, these two pathways are synergistic. Using clascoterone to block residual DHT in the scalp that finasteride fails to suppress could provide superior protection.
Practical Limitation: As a topical lipid-soluble molecule, daily application compliance is the primary failure point in real-world settings, rather than drug failure.
Next Step
Would you like me to analyze the comparative binding affinity data of Clascoterone versus RU-58841 (a grey-market experimental anti-androgen) to determine which has a stronger theoretical blockade potential?
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Just checked on IndiaMart, the finished rug is not available, but the API (Active Pharmaceutical ingredient) is. Which got me to wondering…
Prompt:
How many gallons of 5% topical solution could you make with 1kg of Clascoterone API powder?
Gemini Response:
Calculated Yield: ~5.28 Gallons
Based on standard pharmaceutical compounding for topical solutions (Weight-by-Volume), 1 kilogram of Clascoterone API powder yields approximately 5.28 US gallons of 5% solution.
1. The Math (Standard w/v)
Most commercial topical hair loss solutions (e.g., Minoxidil liquids) use a Weight-by-Volume (w/v) metric. This defines potency as a specific weight of the drug (grams) per 100 units of volume (mL).
- Input Mass: 1 kg = 1,000 grams
- Target Concentration: 5% w/v = 5 grams per 100 mL (or 0.05 g/mL)
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Total Volume Calculation:
1,000 grams / 0.05 g/mL = 20,000 mL -
Unit Conversion:
20,000 mL / 3,785.41 mL (per gallon) = 5.283 gallons
2. Critical Variables: Density and Vehicle
If you formulate this by Weight-by-Weight (w/w)—common for creams or gels rather than liquid solutions—the final volume changes based on the density of your solvent (vehicle).
- The Density Factor: Clascoterone is hydrophobic. You cannot use water as the primary solvent. You must use a vehicle like Ethanol or Propylene Glycol.
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Volume Expansion: Ethanol is less dense than water (approx. 0.789 g/mL). If you create a 5% w/w solution using an ethanol-heavy vehicle, 1 kg of active powder produces a total mass of 20 kg. Because the solvent is light, that 20 kg takes up more space.
- Scenario: 20 kg total mass with a vehicle density of 0.85 g/mL.
- Result: 20,000g / 0.85 = 23,529 mL = 6.21 Gallons.
Bottom Line: For a standard liquid solution comparable to clinical trials, plan for 5.28 gallons. If you formulate a low-density alcoholic tonic by weight, you will end up with closer to 6 gallons of total fluid.
3. Practical Compounding Note
Solubility Constraints:
Do not attempt to dump 1 kg of powder into 5 gallons of vehicle. Clascoterone (Cortexolone 17-alpha-propionate) has specific solubility limits.
- Procedure: You must perform “Geometric Dilution.” Dissolve the API in a smaller volume of the solvent (e.g., Ethanol) first to ensure full solubilization before adding the remaining bulk vehicle (Propylene Glycol/Water) to reach the final volume (Quantity Sufficient).
- Stability: This ester is sensitive to hydrolysis. The pH of the vehicle must be maintained (typically around pH 4.0 - 5.5) to prevent the API from degrading into inactive cortexolone before it even touches the scalp.
Next Step
Would you like me to outline the specific vehicle formulation (percentages of Ethanol, Propylene Glycol, and Water) used in the Cassiopea patent to ensure maximum solubility and shelf-life stability?
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And from Gemini:
I cannot provide specific manufacturing instructions, recipes, or a “how-to” guide for home compounding of pharmaceutical products. I can, however, provide a critical analysis of the formulation chemistry and ingredient lists detailed in the public patent filings for this drug, which highlights the significant chemical stability challenges associated with this molecule.
Formulation Analysis: Clascoterone 5%
The formulation of Clascoterone (Cortexolone 17-alpha-propionate) is not a simple dissolution task. The molecule is an ester, making it chemically fragile.
According to U.S. Patent 8,865,690, assigned to Cassiopea S.p.A., the vehicle requires specific solvents and solubilizers to maintain the drug in an active state. A simple mix of alcohol and powder will likely result in rapid degradation or precipitation.
Patent Reference:
Pharmaceutical compositions comprising cortexolone 17-alpha-propionate (US Patent 8,865,690, 2014)
1. The Ingredients (Based on Patent Data)
The commercial-grade solution described in the patent utilizes a hydroalcoholic base. The following components are critical for a functional 5% (50 mg/mL) solution:
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Ethanol (Anhydrous):
- Function: Primary Solvent and Penetration Enhancer.
- Reality: Clascoterone is highly lipophilic (fat-loving). High concentrations of ethanol are required to dissolve the powder initially. Water alone will not dissolve it.
-
Propylene Glycol:
- Function: Co-solvent and Humectant.
- Reality: Ethanol evaporates rapidly. Without propylene glycol, the ethanol flashes off the scalp immediately, leaving the drug as a dry “dust” on the skin surface which cannot penetrate the follicle. Propylene glycol keeps the product wet long enough for absorption.
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Polysorbate 80:
- Function: Surfactant.
- Reality: This stabilizes the interface between the oil-soluble drug and the water content, preventing the drug from crashing out of the solution (precipitation).
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Purified Water:
- Function: Carrier vehicle.
- Reality: Water is necessary for usability, but it is the enemy of this specific drug due to hydrolysis risks (see below).
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pH Adjusters (Buffers):
- Function: Stability control.
- Reality: The formulation typically requires a pH range of 4.0 to 5.0.
2. The Chemistry: Why “Simple” Mixing Fails
For a biotech specialist, understanding the failure points is more valuable than a recipe.
A. Hydrolysis (The “Inactive” Trap)
Clascoterone is an ester. In the presence of water and uncontrolled pH, esters undergo hydrolysis.
- The Reaction: The ester bond breaks, separating the molecule into Propionic Acid and Cortexolone.
- The Consequence: Cortexolone is the metabolic byproduct; it has no affinity for the androgen receptor. If a DIY solution is not pH-buffered perfectly, you may be applying a solution that is chemically inactive within days, despite appearing clear.
B. Crystallization (The “Delivery” Trap)
Because the drug is 5% concentration (which is high for a topical steroid-like compound), it operates near its saturation point.
- The Consequence: If the ratio of Ethanol to Water is off by even a small margin, the drug will “salt out” or crystallize. Micro-crystals cannot penetrate the stratum corneum. The solution may look cloudy or have sediment, indicating zero bioavailability.
3. Patent-Derived Concentration Ranges
While exact trade secrets are not public, the patent discloses preferred ranges for the vehicle to ensure stability:
- Ethanol: 40% - 50% (w/w)
- Propylene Glycol: 5% - 10% (w/w)
- Water: Balance to 100%
- Polysorbate 80: < 1%
Summary
The clinical data relies on a precise suspension of the active agent in a vehicle that prevents hydrolysis. A home-brew approach lacks the High-Performance Liquid Chromatography (HPLC) required to verify that the active ester has not degraded into inactive cortexolone.
Response from Grok.ai
Here’s an example of a 5% clascoterone (cortexolone-17α-propionate) anhydrous topical solution, drawn from patented formulations developed for treating conditions like alopecia. This is a high-concentration liquid composition designed for stability and skin penetration, using a solvent mixture in roughly equal parts. Note that this is for illustrative purposes; actual preparation should be done in a controlled pharmaceutical setting with proper safety measures, as clascoterone is a prescription active ingredient.
Ingredients List (for 100 g of solution)
- Clascoterone (cortexolone-17α-propionate): 5 g (5% w/w)
- Diethylene glycol monoethyl ether (e.g., Transcutol): 31.5 g (31.5% w/w)
- Ethanol (96°): 31.5 g (31.5% w/w)
- Propylene glycol: 31.4 g (31.4% w/w)
- Ascorbyl palmitate (antioxidant): 0.5 g (0.5% w/w)
- Polysorbate 80 (emulsifier): 0.1 g (0.1% w/w)
This formulation is anhydrous (less than 3% water content) to enhance solubility and reduce degradation.
Mixing Instructions
- In a suitable container (e.g., glass or stainless steel beaker), add the diethylene glycol monoethyl ether and ethanol. Stir gently to combine.
- Gradually add the clascoterone powder to the solvent mixture while stirring continuously (use a magnetic stirrer or paddle mixer at moderate speed) until fully dissolved. This may take 10-30 minutes at room temperature; gentle heating (up to 40°C) can be applied if needed to aid dissolution, but avoid exceeding this to prevent degradation.
- Slowly incorporate the propylene glycol while maintaining stirring to ensure homogeneity.
- Add the ascorbyl palmitate and polysorbate 80, stirring for an additional 5-10 minutes until the mixture is clear and uniform.
- Check the pH if equipment is available (target 4-5 for stability); adjust with a small amount of citric acid if necessary, though anhydrous versions often don’t require it.
- Filter the solution through a fine mesh or pharmaceutical filter to remove any undissolved particles.
- Store in airtight, light-protected containers (e.g., amber glass bottles) at room temperature or refrigerated for up to 2 years, based on stability data showing minimal degradation.
This example yields a clear, viscous solution suitable for topical application, such as via dropper or spray. Scaling up (e.g., to 1 kg) involves multiplying quantities proportionally while maintaining the process.
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Used DMSO as the carrier…
Quick AI search…
'Clascoterone is soluble in DMSO, with reported solubilities of at least 100 mg/mL (248.43 mM)
, 80 mg/mL
, and 2 mg/mL.
For in vitro use, a stock solution can be prepared by dissolving the compound in DMSO, with recommendations to use fresh DMSO to avoid moisture-related solubility issues.
The stock solution should be stored at 0–4°C for short-term use (days to weeks) or at -20°C for long-term storage (months).
When preparing in vivo formulations, DMSO is used as a component in the mixture, such as in a 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline formulation, where the DMSO serves as a solubilizing agent"
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Thoughts on PFS: Opinion about Finasteride and DHT - #397 by Barnabas
I’d keep an eye on clascoterone. It looks interesting.
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This is actually pretty disappointing, especially since they used minoxidil 2% instead of minoxidil 5%, which is the concentration recommended these days (5% twice daily for men, once daily for women). I wonder why the pharma company compared clascoterone to the weaker version of minoxidil? 
I have yet to prescribe Winlevi for acne, since it’s expensive and has the same mechanism of action as topical spironolactone, which can be bought in topical form from compounding pharmacies for a very reasonable price. The problem with using topical spiro for hair loss is that apparently it smells pretty bad when put into a liquid solution formulation (but not in cream form). If one is willing to use the cream in the scalp (maybe once at night, wash hair in the morning?) then this would be reasonable.
Also, a very easy and cheap topical androgen blocker for the scalp is 2% ketoconazole shampoo. It only needs to be used 3x weekly (leave on for several minutes prior to rinsing) and its anti-androgen effect has been proven to help androgenetic alopecia, although the effect is likely weaker than clascoterone/spironolactone. I prescribe ketoconazole shampoo mainly as an adjunct therapy for hair loss that complements whatever else we’re doing.
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What I doubt are permanently changed baselines. The couple of case reports we have for fertility issues point to a complete reversal to baseline after three months. Dutasteride side effects can linger for up to 6-12 months, given its long half life.
I’d keep an eye on clascoterone. It looks interesting.
If it wasn’t so expensive and sensitive to solvents, it’d be a perfect addition to the fin/dut + min stack. Should definitely give some more density.