Clascoterone: a new topical antiandrogen agent.

Authors

  • Magdalena Sitnik a:1:{s:5:"en_US";s:28:"Masovian Brodnowski Hospital";}
  • Jakub Olszewski
  • Maciej Bara
  • Piotr Armański
  • Katarzyna Herjan

DOI:

https://doi.org/10.56782/pps.258

Keywords:

clascoterone, klaskoteron, androgen inhibitor, topical acne therapy, androgenetic alopecia

Abstract

Androgen hormones (androgens) and androgen receptors (ARs) play both a significant role in the pathogenesis of certain skin disorders, such as acne vulgaris (hereafter: acne) and androgenetic alopecia (AGA) in both males and females. Systemic antiandrogen therapies, such as oral contraceptives (DTAs) and spironolactone, are potentially effective strategies for the treatment of acne and AGA. However, they are associated with systemic adverse effects and are unsuitable for use in males. Clascoterone cream, 1%, is a novel topical androgen receptor inhibitor (ARI). The use of a topical antiandrogen drug significantly reduces the risk of these side effects. Clascotereone is currently the only topical ARI approved by the Food and Drug Administration (FDA). It is indicated for patients 12 years of age and older with facial acne vulgaris. Several clinical studies demonstrated the effectiveness of clascoterone in treating acne with a favorable safety profile. The other indications for clascoterone, including the treatment of AGA, are currently under investigation. The promising results from clinical trials suggest that clascoterone may soon play a broader role in dermatology, offering benefits for conditions that currently have limited treatment options.

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References

1. Chen, W.; Zouboulis, C. C.; et al. Evidence of heterogeneity and quantitative differences of the type 1 5alpha-reductase expression in cultured human skin cells – evidence of its presence in melanocytes. J. Invest. Dermatol. 1998, 110 (1), 84-89. DOI: 10.1046/j.1523-1747.1998.00080.x DOI: https://doi.org/10.1046/j.1523-1747.1998.00080.x

2. Lai, J. J.; Chang, P.; et al. The role of androgen and androgen receptor in skin-related disorders. Arch. Dermatol. Res. 2012, 304 (7), 499-510. DOI: 10.1007/s00403-012-1265-x DOI: https://doi.org/10.1007/s00403-012-1265-x

3. Zouboulis, C. C.; Chen, W. C.; et al. Sexual hormones in human skin. Horm. Metab. Res. 2007, 39 (2), 85-95. DOI: 10.1055/s-2007-961807 DOI: https://doi.org/10.1055/s-2007-961807

4. Nestor, M. S.; Ablon, G.; et al. Treatment options for androgenetic alopecia: Efficacy, side effects, compliance, financial considerations, and ethics. J. Cosmet. Dermatol. 2021, 20 (12), 3759-3781. DOI: 10.1111/jocd.14537 DOI: https://doi.org/10.1111/jocd.14537

5. Kircik, L. H. Androgens and acne: perspectives on clascoterone, the first topical androgen receptor antagonist. Expert Opin. Pharmacother. 2021, 22 (13), 1801-1806. DOI: 10.1080/14656566.2021.1918100 DOI: https://doi.org/10.1080/14656566.2021.1918100

6. Rosette, C.; Rosette, N.; et al. Cortexolone 17alpha-Propionate (Clascoterone) is an Androgen Receptor Antagonist in Dermal Papilla Cells In Vitro. J. Drugs Dermatol. 2019, 18 (2), 197-201.

7. Ferraboschi, P.; Chiara Sala, M.; et al. Full spectroscopic characterization of two crystal pseudopolymorphic forms of the antiandrogen cortexolone 17alpha-propionate for topic application. Steroids 2017, 128, 95-104. DOI: 10.1016/j.steroids.2017.09.003 DOI: https://doi.org/10.1016/j.steroids.2017.09.003

8. Mazzetti, A.; Moro, L.; et al. Pharmacokinetic Profile, Safety, and Tolerability of Clascoterone (Cortexolone 17-alpha propionate, CB-03-01) Topical Cream, 1% in Subjects With Acne Vulgaris: An Open-Label Phase 2a Study. J. Drugs Dermatol. 2019, 18 (6), 563-568.

9. Bhatia, N.; Eichenfield, L. F.; et al. Hypothalamic-Pituitary-Adrenal Axis Response in Patients With Acne Vulgaris Treated With Clascoterone. J. Drugs Dermatol. 2024, 23 (6), 433-437. DOI: 10.36849/JDD.7997 DOI: https://doi.org/10.36849/JDD.7997

10. Hebert, A.; Thiboutot, D.; et al. Efficacy and Safety of Topical Clascoterone Cream, 1%, for Treatment in Patients With Facial Acne: Two Phase 3 Randomized Clinical Trials. JAMA Dermatol. 2020, 156 (6), 621-630. DOI: 10.1001/jamadermatol.2020.0465 DOI: https://doi.org/10.1001/jamadermatol.2020.0465

11. Del Rosso, J.; Stein Gold, L.; et al. Is There a Clinically Relevant Risk of Hyperkalemia with Topical Clascoterone Treatment? J. Clin. Aesthet. Dermatol. 2023, 16 (6), 20-24.

12. Eichenfield, L. F.; Hebert, A. A.; et al. Long-Term Safety and Efficacy of Twice-Daily Topical Clascoterone Cream 1% in Patients Greater Than or Equal to 12 Years of Age With Acne Vulgaris. J. Drugs Dermatol. 2023, 22 (8), 810-816. DOI: 10.36849/jdd.7592 DOI: https://doi.org/10.36849/jdd.7592

13. Heng, A. H. S.; Chew, F. T. Systematic review of the epidemiology of acne vulgaris. Sci. Rep. 2020, 10 (1), Art. No: 5754. DOI: 10.1038/s41598-020-62715-3 DOI: https://doi.org/10.1038/s41598-020-62715-3

14. Williams, H. C.; Dellavalle, R. P.; et al. Acne vulgaris. Lancet 2012, 379 (9813), 361-372. DOI: 10.1016/S0140-6736(11)60321-8 DOI: https://doi.org/10.1016/S0140-6736(11)60321-8

15. Zaenglein, A. L.; Pathy, A. L.; et al. Guidelines of care for the management of acne vulgaris. J. Am. Acad. Dermatol. 2016, 74 (5), 945-973.e33. DOI: 10.1016/j.jaad.2015.12.037 DOI: https://doi.org/10.1016/j.jaad.2015.12.037

16. Ghosh, S.; Chaudhuri, S.; et al. Profiling and hormonal therapy for acne in women. Indian J. Dermatol. 2014, 59 (2), 107-115. DOI: 10.4103/0019-5154.127667 DOI: https://doi.org/10.4103/0019-5154.127667

17. Chalker, D. K.; Lesher, J. L., Jr.; et al. Efficacy of topical isotretinoin 0.05% gel in acne vulgaris: results of a multicenter, double-blind investigation. J. Am. Acad. Dermatol. 1987, 17 (2 Pt 1), 251-254. DOI: 10.1016/s0190-9622(87)70200-x DOI: https://doi.org/10.1016/S0190-9622(87)70200-X

18. Thiboutot, D.; Pariser, D. M.; et al. Adapalene gel 0.3% for the treatment of acne vulgaris: a multicenter, randomized, double-blind, controlled, phase III trial. J. Am. Acad. Dermatol. 2006, 54 (2), 242-250. DOI: 10.1016/j.jaad.2004.10.879 DOI: https://doi.org/10.1016/j.jaad.2004.10.879

19. Gollnick, H. P.; Draelos, Z.; et al. Adapalene-benzoyl peroxide, a unique fixed-dose combination topical gel for the treatment of acne vulgaris: a transatlantic, randomized, double-blind, controlled study in 1670 patients. Br. J. Dermatol. 2009, 161 (5), 1180-1189. DOI: 10.1111/j.1365-2133.2009.09209.x DOI: https://doi.org/10.1111/j.1365-2133.2009.09209.x

20. Chalker, D. K.; Shalita, A.; et al. A double-blind study of the effectiveness of a 3% erythromycin and 5% benzoyl peroxide combination in the treatment of acne vulgaris. J. Am. Acad. Dermatol. 1983, 9 (6), 933-936. DOI: 10.1016/s0190-9622(83)70211-2 DOI: https://doi.org/10.1016/S0190-9622(83)70211-2

21. Lookingbill, D. P.; Chalker, D. K.; et al. Treatment of acne with a combination clindamycin/benzoyl peroxide gel compared with clindamycin gel, benzoyl peroxide gel and vehicle gel: combined results of two double-blind investigations. J. Am. Acad. Dermatol. 1997, 37 (4), 590-595. DOI: 10.1016/s0190-9622(97)70177-4 DOI: https://doi.org/10.1016/S0190-9622(97)70177-4

22. Babaeinejad, S.; Khodaeiani, E.; et al. Comparison of therapeutic effects of oral doxycycline and azithromycin in patients with moderate acne vulgaris: What is the role of age? J. Dermatolog. Treat. 2011, 22 (4), 206-210. DOI: 10.3109/09546631003762639 DOI: https://doi.org/10.3109/09546631003762639

23. Bossuyt, L.; Bosschaert, J.; et al. Lymecycline in the treatment of acne: an efficacious, safe and cost-effective alternative to minocycline. Eur. J. Dermatol. 2003, 13 (2), 130-135.

24. Villani, A.; Nastro, F.; et al. Oral isotretinoin for acne: a complete overview. Expert Opin. Drug Saf. 2022, 21 (8), 1027-1037. DOI: 10.1080/14740338.2022.2102605 DOI: https://doi.org/10.1080/14740338.2022.2102605

25. Trivedi, M. K.; Shinkai, K.; et al. A Review of hormone-based therapies to treat adult acne vulgaris in women. Int. J. Womens Dermatol. 2017, 3 (1), 44-52. DOI: 10.1016/j.ijwd.2017.02.018 DOI: https://doi.org/10.1016/j.ijwd.2017.02.018

26. Trifu, V.; Tiplica, G. S.; et al. Cortexolone 17alpha-propionate 1% cream, a new potent antiandrogen for topical treatment of acne vulgaris. A pilot randomized, double-blind comparative study vs. placebo and tretinoin 0.05% cream. Br. J. Dermatol. 2011, 165 (1), 177-183. DOI: 10.1111/j.1365-2133.2011.10332.x DOI: https://doi.org/10.1111/j.1365-2133.2011.10332.x

27. Mazzetti, A.; Moro, L.; et al. A Phase 2b, Randomized, Double-Blind Vehicle Controlled, Dose Escalation Study Evaluating Clascoterone 0.1%, 0.5%, and 1% Topical Cream in Subjects With Facial Acne. J. Drugs Dermatol. 2019, 18 (6), 570-575.

28. Piszczatoski, C. R.; Powell, J. Topical Clascoterone: The First Novel Agent for Acne Vulgaris in 40 Years. Clin. Ther. 2021, 43 (10), 1638-1644. DOI: 10.1016/j.clinthera.2021.08.007 DOI: https://doi.org/10.1016/j.clinthera.2021.08.007

29. Reynolds, R. V.; Yeung, H.; et al. Guidelines of care for the management of acne vulgaris. J. Am. Acad. Dermatol. 2024, 90 (5), 1006.e1001-1006.e1030. DOI: 10.1016/j.jaad.2023.12.017 DOI: https://doi.org/10.1016/j.jaad.2023.12.017

30. Riis, P. T.; Ring, H. C.; et al. The Role of Androgens and Estrogens in Hidradenitis Suppurativa - A Systematic Review. Acta Dermatovenerol. Croat. 2016, 24 (4), 239-249.

31. Der Sarkissian, S. A.; Sun, H. Y.; et al. Cortexolone 17alpha-propionate for hidradenitis suppurativa. Dermatol. Ther. 2020, 33 (6), Art. No: e14142. DOI: 10.1111/dth.14142 DOI: https://doi.org/10.1111/dth.14142

32. Cunningham, K. N.; Moody, K.; et al. Use of topical clascoterone for the treatment of hidradenitis suppurativa. JAAD Case Rep. 2023, 36, 38-39. DOI: 10.1016/j.jdcr.2023.04.002 DOI: https://doi.org/10.1016/j.jdcr.2023.04.002

33. Adil, A.; Godwin, M. The effectiveness of treatments for androgenetic alopecia: A systematic review and meta-analysis. J. Am. Acad. Dermatol. 2017, 77 (1), 136-141.e135. DOI: 10.1016/j.jaad.2017.02.054 DOI: https://doi.org/10.1016/j.jaad.2017.02.054

34. Lolli, F.; Pallotti, F.; et al. Androgenetic alopecia: a review. Endocrine 2017, 57 (1), 9-17. DOI: 10.1007/s12020-017-1280-y DOI: https://doi.org/10.1007/s12020-017-1280-y

35. Kanti, V.; Messenger, A.; et al. Evidence-based (S3) guideline for the treatment of androgenetic alopecia in women and in men - short version. J. Eur. Acad. Dermatol. Venereol. 2018, 32 (1), 11-22. DOI: 10.1111/jdv.14624 DOI: https://doi.org/10.1111/jdv.14624

36. Dhillon, S. Clascoterone: First Approval. Drugs 2020, 80 (16), 1745-1750. DOI: 10.1007/s40265-020-01417-6 DOI: https://doi.org/10.1007/s40265-020-01417-6

37. Sun, H. Y.; Sebaratnam, D. F. Clascoterone as a novel treatment for androgenetic alopecia. Clin. Exp. Dermatol. 2020, 45 (7), 913-914. DOI: 10.1111/ced.14292 DOI: https://doi.org/10.1111/ced.14292

38. FDA-approved Winlevi® is the first novel topical mechanism for acne in nearly 40 years. . https://www.cosmopharma.com/products/winlevi (accessed 10 Dec 2024).

39. How much is Winlevi without insurance? . https://www.singlecare.com/blog/winlevi-without-insurance/ (accessed 10 Dec2024).

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Published

2025-02-07

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Clascoterone: a new topical antiandrogen agent. (2025). Prospects in Pharmaceutical Sciences, 23(1), 47-52. https://doi.org/10.56782/pps.258

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