Research

Understanding the Role of Topical Anti-Androgens in Skincare

Learn how topical anti-androgens can effectively manage PCOS-related skin issues like acne and excess oil with fewer side effects.

July 24, 2025
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Topical anti-androgens offer a targeted way to manage PCOS-related skin concerns like acne, hirsutism, and hair loss. Unlike oral medications, they work directly on the skin, reducing side effects linked to systemic treatments. Key options include FDA-approved clascoterone (Winlevi) and compounded topical spironolactone. Both reduce oil production and inflammation by blocking androgen activity in the skin.

Quick Takeaways:

  • Who benefits? Individuals with PCOS experiencing acne, excess oil, or unwanted hair growth.
  • How it works: Blocks androgen receptors in skin cells to address symptoms locally.
  • Key treatments:
    • Clascoterone (Winlevi): FDA-approved, effective for acne, fewer systemic side effects.
    • Topical spironolactone: Compounded, off-label use for acne and hair loss.

These treatments are safer for long-term use compared to oral options, but they require consistency and dermatologist guidance for best results.

WINLEVI HORMONAL ACNE TREATMENT 🤔 DERMATOLOGIST @DrDrayzday

WINLEVI

How Topical Anti-Androgens Work

Topical anti-androgens are designed to address skin issues related to PCOS by targeting androgen activity directly in the skin. This focused approach helps manage problems like acne, excess oil production, and unwanted hair growth. By working at the skin level, these treatments tackle the root cause of these conditions without affecting the body's overall hormonal balance.

How These Treatments Block Androgens in Skin

The way topical anti-androgens work is quite precise - they block androgen activity right where skin issues arise. Dr. Robert S. Haber explains:

"Antiandrogens are generally considered to be compounds that specifically block androgen activity at target sites."

These treatments disrupt androgen activity by binding to androgen receptors in the skin, effectively preventing androgens from taking action. This can reduce oil production, inflammation, and hair-related concerns. Additionally, many of these treatments inhibit 5-alpha reductase, an enzyme that converts testosterone into dihydrotestosterone (DHT). Since DHT is significantly more potent than testosterone in triggering skin problems, lowering its levels can lead to noticeable improvements, especially in acne and oily skin.

One of the key advantages of topical anti-androgens is their localized action. They work only where applied, allowing for targeted treatment without impacting the entire hormonal system. For best results, dermatologists suggest cleaning the affected area with water before applying a thin layer of the medication. Typically, these treatments are used one to three times daily, and it’s important to gently rub the cream into the skin and wash your hands afterward. This localized method stands in contrast to systemic treatments, which affect the entire body.

Topical vs. Oral Anti-Androgen Treatments

The main difference between topical and oral anti-androgens lies in their range of action and potential side effects. Topical treatments are localized, meaning they primarily affect the area where they’re applied, reducing the risk of systemic side effects. This makes them an appealing option for those looking to address specific skin concerns without disrupting their overall hormonal balance.

Oral anti-androgens, on the other hand, impact the entire body. Because these medications travel through the bloodstream to reach the skin, they can cause a wider range of side effects. These may include menstrual irregularities, breast tenderness, fatigue, gastritis, and headaches. In men, systemic anti-androgens have been linked to gynecomastia, with rates ranging from 30% to 85%. They can also lead to sexual dysfunction and osteoporosis, further highlighting the benefits of the more localized action of topical treatments.

The FDA’s approval of clascoterone in August 2020 underscores the safety of topical treatments. Clinical trials showed that clascoterone was effective while offering a safety profile comparable to a placebo, with no systemic antiandrogenic effects observed. This allows patients to enjoy the benefits of androgen-blocking treatments without the broader side effects associated with oral medications.

For women with PCOS, topical anti-androgens are particularly appealing. They provide a targeted way to manage skin concerns while maintaining existing hormonal treatments. Plus, these treatments can be combined with other topical or oral options, creating personalized skincare routines to address the various skin issues linked to PCOS.

Types of Topical Anti-Androgens for PCOS Skincare

Managing PCOS-related skin issues often involves addressing androgen-driven concerns, like acne and excess oil production. Two topical anti-androgens have gained attention for their effectiveness in treating these problems. Here’s a closer look at both options.

Clascoterone (Winlevi)

Clascoterone 1% cream (Winlevi®) became the first topical anti-androgen approved in 2020 for acne treatment in individuals aged 12 and older. It’s also available in Canada, Australia, New Zealand, and the UK.

This cream works by competing with dihydrotestosterone (DHT) for androgen receptor sites in sebaceous glands. By doing so, it reduces oil production and inflammation, which are key contributors to acne. Its safety profile is enhanced by its rapid metabolism in the skin into an inactive form, cortexolone, limiting its impact on the bloodstream.

Clinical studies show promising results. In Phase III trials, clascoterone significantly reduced acne severity - measured by at least a 2-point drop in Investigator Global Assessment scores - compared to a placebo after 12 weeks. It also reduced all types of acne lesions more effectively than the placebo.

For optimal results, clascoterone should be applied as a thin layer to affected areas twice daily, once in the morning and once in the evening. Common side effects include redness, itching, dryness, and scaling. If irritation occurs, reducing the frequency of application or pausing use temporarily may help.

Topical Spironolactone

Unlike clascoterone, topical spironolactone is not commercially manufactured. Instead, it’s available as a compounded medication prepared by specialty pharmacies and is used off-label for acne, hair loss, and other skin conditions.

Topical spironolactone works by blocking 5α-reductase receptors in sebaceous glands, which decreases testosterone production and reduces sebum levels. It also helps with redness and inflammation.

Research supports its effectiveness. In one study, spironolactone significantly reduced comedones, while clindamycin, another acne treatment, showed no effect. Patients also reported higher satisfaction with spironolactone. Another study found that a 5% spironolactone cream applied twice daily for 8 weeks reduced acne severity, including papules and comedones, with no major side effects reported.

As the Curology Team notes:

"Topical spironolactone is different from oral spironolactone, and it minimizes the side effects that are typically associated with oral spironolactone while still effectively combating acne."

However, common side effects include burning (21.7%), dryness (15%), and itching (15%).

Clascoterone vs. Topical Spironolactone

Here’s a side-by-side comparison to help highlight the differences:

Factor Clascoterone (Winlevi) Topical Spironolactone
FDA Status FDA-approved for acne treatment Compounded medication (not FDA-approved)
Availability Commercially available with prescription Requires compounding pharmacy
Age Range Approved for ages 12 and older Used off-label for various ages
Cost $482–$672 per month Varies by compounding pharmacy
Application Applied twice daily Typically applied twice daily
Primary Mechanism Competes with DHT for androgen receptors Blocks 5α-reductase receptors
Common Side Effects Redness, itching, scaling/dryness Burning (21.7%), dryness (15%), itching (15%)

Choosing between these treatments often depends on accessibility and individual response. Clascoterone’s FDA approval ensures consistent quality and efficacy, though its cost may be a challenge for some. On the other hand, topical spironolactone, while potentially more affordable at compounding pharmacies, lacks standardized testing and may vary in quality. Dermatologists often caution patients about these differences and the potential risks tied to compounded medications.

Both options offer targeted solutions for managing PCOS-related skin issues while minimizing systemic side effects. Consulting with a dermatologist can help determine which approach aligns best with individual needs and circumstances.

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How Well Topical Anti-Androgens Work and Their Safety

When it comes to managing PCOS-related skin issues, understanding how effective and safe topical anti-androgens are can help you decide if they’re a good fit for your skincare routine. Research has consistently shown that these treatments offer benefits for addressing common PCOS skin concerns, with a safety profile that makes them worth considering. Here’s what the science says.

Research Results on Treatment Effectiveness

Clinical studies have highlighted the positive impact of topical anti-androgens on skin conditions linked to PCOS. These treatments are often recommended for moderate to severe acne in women who haven’t responded to first-line therapies or show signs of hyperandrogenism.

The connection between androgens and acne in women with PCOS is well-documented. Studies estimate that 30% to 40% of women with PCOS struggle with acne. A meta-analysis found that 42% of adult women with PCOS experience acne, compared to just 17% of women without the condition. Elevated androgen levels are found in about half of women with adult acne, while 50% to 60% of women with normal androgen levels still show increased androgen metabolites.

One commonly used treatment, spironolactone, has proven effective for hormonally driven acne. Research shows it reduces sebum production and may even improve hirsutism, in some cases outperforming oral contraceptives [26-29].

Topical formulations are also gaining attention. For instance, a Phase III trial by Piraccini et al. tested a daily 0.25% topical finasteride spray on 323 patients with androgenetic alopecia. After 24 weeks, patients using the spray saw a significant increase in hair count compared to the placebo group. Interestingly, the topical and oral finasteride groups showed similar results in hair growth, but the plasma concentration of finasteride was over 100 times lower with the topical treatment.

These findings suggest that topical anti-androgens can be a practical option for treating moderate to severe acne, regardless of androgen levels. While their effectiveness is clear, safety is always a critical consideration.

Side Effects and Safety Concerns

Topical anti-androgens generally work well, but like any medication, they can cause side effects. Most are mild and temporary, such as dryness, flaking, burning, redness, or itching, which often improve as your skin adjusts.

However, there are rare but more serious side effects to be aware of, including skin thinning, telangiectasia (visible blood vessels), hyperkalemia, or allergic reactions. If any of these occur, it’s important to stop using the product and consult a doctor.

Pregnancy is a major contraindication for these treatments. Topical anti-androgens can interfere with fetal development, so they should never be used during pregnancy. Women who are trying to conceive or could become pregnant should use effective contraception and work closely with their healthcare provider [12, 14].

Another advantage of topical formulations is their reduced systemic exposure. For example, topical finasteride has been shown to stimulate hair growth similar to oral finasteride but with minimal impact on plasma DHT levels, making it a safer option for many patients.

To ensure the best results and minimize risks, proper application and hygiene are essential. It’s also critical to inform your doctor about all medications and supplements you’re taking, including over-the-counter or herbal products, as these could interact with hormone therapies.

Adding Topical Anti-Androgens to Your Skincare Routine

Incorporating topical anti-androgens into your skincare routine requires consistency and proper application. These prescription treatments work best when used regularly as part of a structured regimen. Knowing how to apply them correctly, tracking your progress, and working closely with your dermatologist can help you achieve better outcomes.

How to Apply Topical Anti-Androgens

To get the most out of topical anti-androgens, apply them as directed by your dermatologist - usually once or twice daily, depending on your skin's tolerance. Start with clean, dry skin by gently cleansing with a non-comedogenic cleanser twice a day. Avoid harsh scrubbing, as it can aggravate inflammation. After cleansing, ensure your skin is completely dry before applying the treatment.

When layering products, apply the topical anti-androgen immediately after cleansing. If you’re using chemical exfoliants like salicylic acid or glycolic acid, alternate their use as advised by your dermatologist to minimize irritation. After applying the treatment, follow up with a light, oil-free moisturizer containing humectants like glycerin or hyaluronic acid. Don’t forget to finish with a broad-spectrum SPF 50+ sunscreen to protect your skin from increased sun sensitivity caused by the treatment.

For acne related to polycystic ovary syndrome (PCOS), which often appears on the chin, jawline, and neck, focus your application on these areas. Be careful to avoid sensitive areas like the eyes and mouth. Consistent application is key - stick with the routine and adjust as needed with your dermatologist's guidance.

Monitoring Results and Working with Dermatologists

Tracking your progress is essential to determine if the treatment is effective. Improvements often take 8–12 weeks to become noticeable, so patience is important. Keep an eye on changes in acne, oiliness, unwanted hair growth, and scalp hair loss. A simple log or weekly photos can help you document progress, such as fewer breakouts or reduced oiliness. Pay particular attention to hormonal acne, which typically shows up as painful cysts or nodules along the jawline and chin.

Because PCOS-related acne is largely influenced by hormonal fluctuations, you may see a gradual decline in the frequency and severity of breakouts over time. Your dermatologist might suggest additional treatments, such as chemical peels, laser therapy, or drainage for larger cysts, to complement your regimen. They may also discuss lifestyle factors, like diet and stress, that can impact inflammation and overall results.

Regular follow-ups with your dermatologist, typically every 6–8 weeks, allow for a review of your progress and adjustments to your treatment plan. During these visits, discuss any side effects, changes in your menstrual cycle, or other concerns. Your doctor may also conduct blood tests or imaging to evaluate hormone levels and further investigate PCOS.

If you don’t see improvements after 12–16 weeks, your dermatologist may modify your treatment or suggest additional therapies. They may also explore whether dietary adjustments, such as reducing dairy or high-glycemic foods, could improve your results.

Insurance Coverage and Costs

The cost of topical anti-androgens can be high, so it’s important to explore ways to make treatment more affordable. Insurance coverage for newer options like Winlevi can be limited, with many plans placing it in higher copay tiers.

"Winlevi cream, a prescription acne treatment that targets testosterone's effects on skin oil production, can cost nearly $800 without insurance." – SingleCare

Prescription discount programs can help lower these costs. For example, using a SingleCare savings card may reduce the price of Winlevi to about $507 for a 60 g tube. It’s also worth comparing prices at different pharmacies, as costs can vary between chain stores, independent pharmacies, and online retailers.

Discuss all treatment options and costs with your dermatologist. Ask about generic versions or alternative treatments that might be more affordable. Some dermatology offices may offer samples or payment plans to help manage expenses.

Online dermatology services are another budget-friendly option for consultations and prescriptions. Platforms like Miiskin offer consultations starting at $39 for returning patients and $59 for new ones. Keep in mind that while topical spironolactone is sometimes prescribed off-label for acne, it is not FDA-approved for this use. Your dermatologist will determine the best treatment based on your needs.

Finally, contact your insurance provider to clarify your coverage, including prior authorization requirements, copays, and deductibles. Factor in the long-term costs of treatment, such as complementary skincare products, regular dermatologist visits, and any additional therapies. Sticking to your routine and attending follow-ups can make the investment worthwhile by delivering noticeable results.

Key Points About Topical Anti-Androgens for PCOS Skincare

Topical anti-androgens provide a targeted solution for managing skin concerns related to PCOS. By blocking androgen receptors in the skin, they help reduce sebum production and formation of comedones, all while minimizing the risk of systemic side effects.

PCOS affects many women of reproductive age, with androgen excess being a common issue. Around 70% of women with PCOS experience symptoms of excess androgens, and studies show that 30–40% of them deal with acne. A meta-analysis revealed that acne is present in 42% of adult women with PCOS, compared to just 17% in women without the condition. These numbers highlight the importance of localized treatments like topical anti-androgens.

The effectiveness of these treatments is well-established. Research shows they can lower sebum production by about 30% and significantly reduce comedone development.

Topical anti-androgens also offer practical benefits compared to systemic therapies. They are ideal for women who cannot tolerate oral contraceptives or for those where such treatments are not suitable. These topical options work well alongside hair removal methods like waxing, shaving, laser treatments, or electrolysis. Evidence suggests they are particularly useful when oral therapies fail to deliver results after six months. Additionally, combining anti-androgen treatments with lifestyle changes may outperform metformin plus lifestyle adjustments for addressing hirsutism and improving insulin-related markers.

One example is clascoterone cream, which is applied twice daily and fits seamlessly into daily routines.

For women with PCOS, topical anti-androgens present a scientifically supported way to address skin issues. With proper application and guidance from a dermatologist, these treatments can lead to clearer skin and an enhanced quality of life.

FAQs

What side effects can occur with topical anti-androgens, and how can they be managed?

Using topical anti-androgens can sometimes lead to mild skin issues like dryness, redness, flaking, or a slight burning sensation at the application site. These reactions are typically short-lived and tend to improve as your skin gets used to the treatment. In rare cases, some individuals might experience headaches or minor hormonal changes, though this is uncommon when the product is applied correctly.

To ease these side effects, consider using a gentle moisturizer to calm irritated skin and combat dryness. You might also reduce how often you apply the product - switching to every other day instead of daily can help. If the discomfort continues or worsens, it’s a good idea to reach out to your healthcare provider for advice. Serious side effects are extremely rare when used as recommended.

Topical anti-androgens are a popular choice for managing PCOS-related skin concerns like acne and oily skin. They generally cause fewer systemic side effects compared to oral options. On the other hand, oral medications like spironolactone may be more effective for addressing broader symptoms but can come with drawbacks, such as hormonal shifts or stomach issues.

For targeted issues like acne, topical treatments such as clascoterone work well and are often considered safer. Deciding between oral and topical options ultimately depends on the severity of the symptoms and individual health needs. Speaking with a healthcare professional can help you choose the best treatment for your skin.

Can I use topical anti-androgens with other skincare products for PCOS safely?

Yes, you can usually use topical anti-androgens along with other skincare products, but it’s wise to approach this carefully. These treatments are often paired with ingredients like benzoyl peroxide, salicylic acid, or retinol, but the combination should be customized to suit your skin type and monitored for any irritation or unwanted effects.

To ensure the best outcome, it’s a good idea to consult a dermatologist or healthcare provider before adding new products to your routine. They can guide you in creating a skincare plan that’s effective and minimizes potential risks.

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