Vol 10, No 3 (2024)
Review paper
Published online: 2024-07-25
Topical solutions for androgenetic alopecia: evaluating efficacy and safety
1
, 2
, 2
DOI: 10.5603/fd.101208
Forum Dermatologicum 2024;10(3):71-78.
Abstract
Androgenetic alopecia (AGA) presents a significant challenge in clinical practice due to its prevalence and impact on patients’ quality of life. With a diverse array of available treatment options, selecting the most appropriate therapy demands careful consideration of factors such as efficacy, safety, practicality, and cost. This review aims to evaluate the efficacy and safety profiles of various topical treatments for AGA, investigating their potential advantages in limiting systemic side effects compared to oral medications. This article explores the pharmacology, mechanisms of action, clinical efficacy, and adverse events associated with topical medications like minoxidil, finasteride, ketoconazole shampoo, clascoterone, latanoprost, spironolactone, flutamide, cetirizine, pyrilutamide, and GT20029.
Keywords: androgenetic alopeciatopicaltreatmentminoxidilfinasterideclascoterone
References
- Hamilton JB. Male hormone stimulation is prerequisite and an incitant in common baldness. Am J Anat. 2005; 71(3): 451–480.
- Ludwig E. Classification of the types of androgenetic alopecia (common baldness) occurring in the female sex. Br J Dermatol. 1977; 97(3): 247–254.
- Kabir Y, Goh C. Androgenetic alopecia. J Egypt Women’s Dermatologic Soc. 2013; 10(3): 107–116.
- Suchonwanit P, Srisuwanwattana P, Chalermroj N, et al. A randomized, double-blind controlled study of the efficacy and safety of topical solution of 0.25% finasteride admixed with 3% minoxidil vs. 3% minoxidil solution in the treatment of male androgenetic alopecia. J Eur Acad Dermatol Venereol. 2018; 32(12): 2257–2263.
- Suchonwanit P, Iamsumang W, Rojhirunsakool S. Efficacy of topical combination of 0.25% finasteride and 3% minoxidil versus 3% minoxidil solution in female pattern hair loss: a randomized, double-blind, controlled study. Am J Clin Dermatol. 2019; 20(1): 147–153.
- Ando Y, Yamaguchi Y, Hamada K, et al. Expression of mRNA for androgen receptor, 5alpha-reductase and 17beta-hydroxysteroid dehydrogenase in human dermal papilla cells. Br J Dermatol. 1999; 141(5): 840–845.
- Irwig MS. Depressive symptoms and suicidal thoughts among former users of finasteride with persistent sexual side effects. J Clin Psychiatry. 2012; 73(9): 1220–1223.
- Irwig MS, Kolukula S. Persistent sexual side effects of finasteride for male pattern hair loss. J Sex Med. 2011; 8(6): 1747–1753.
- Ramos PM, Sinclair RD, Kasprzak M, et al. Minoxidil 1 mg oral versus minoxidil 5% topical solution for the treatment of female-pattern hair loss: a randomized clinical trial. J Am Acad Dermatol. 2020; 82(1): 252–253.
- Randolph M, Tosti A. Oral minoxidil treatment for hair loss: A review of efficacy and safety. J Am Acad Dermatol. 2021; 84(3): 737–746.
- Li M, Marubayashi A, Nakaya Y, et al. Minoxidil-induced hair growth is mediated by adenosine in cultured dermal papilla cells: possible involvement of sulfonylurea receptor 2B as a target of minoxidil. J Invest Dermatol. 2001; 117(6): 1594–1600.
- Galbraith GM, Thiers BH. In vitro suppression of human lymphocyte activity by minoxidil. Int J Dermatol. 1985; 24(4): 249–251.
- Pekmezci E, Turkoğlu M, Gökalp H, et al. Minoxidil downregulates interleukin-1 alpha gene expression in HaCaT cells. Int J Trichology. 2018; 10(3): 108–112.
- Kvedar JC, Baden HP, Levine L. Selective inhibition by minoxidil of prostacyclin production by cells in culture. Biochem Pharmacol. 1988; 37(5): 867–874.
- Navarro MR, Asín M, Martínez MA, et al. Management of androgenetic alopecia: a comparative clinical study between plasma rich in growth factors and topical minoxidil. Eur J Plast Surg. 2016; 39(3): 173–180.
- Rundegren J. A one-year observational study with minoxidil 5% solution in Germany: results of independent efficacy evaluation by physicians and patients. J Am Acad Dermatol. 2004; 50(3): P91.
- Olsen EA, Dunlap FE, Funicella T, et al. A randomized clinical trial of 5% topical minoxidil versus 2% topical minoxidil and placebo in the treatment of androgenetic alopecia in men. J Am Acad Dermatol. 2002; 47(3): 377–385.
- McCoy J, Goren A, Kovacevic M, et al. Minoxidil dose response study in female pattern hair loss patients determined to be non-responders to 5% topical minoxidil. J Biol Regul Homeost Agents. 2016; 30(4): 1153–1155.
- Traish AM. Post-finasteride syndrome: a surmountable challenge for clinicians. Fertil Steril. 2020; 113(1): 21–50.
- Coskuner ER, Ozkan B, Culha MG. Sexual problems of men with androgenic alopecia treated with 5-alpha reductase inhibitors. Sex Med Rev. 2019; 7(2): 277–282.
- Liu L, Zhao S, Li F, et al. Effect of 5α-reductase inhibitors on sexual function: a meta-analysis and systematic review of randomized controlled trials. J Sex Med. 2016; 13(9): 1297–1310.
- Mazzarella GF, Loconsole GF, Cammisa GA, et al. Topical finasteride in the treatment of androgenic alopecia. Preliminary evaluations after a 16-month therapy course. J Dermatolog Treat. 2009; 8(3): 189–192.
- Piraccini BM, Blume-Peytavi U, Scarci F, et al. Efficacy and safety of topical finasteride spray solution for male androgenetic alopecia: a phase III, randomized, controlled clinical trial. J Eur Acad Dermatol Venereol. 2022; 36(2): 286–294.
- Suchonwanit P, Srisuwanwattana P, Chalermroj N, et al. A randomized, double-blind controlled study of the efficacy and safety of topical solution of 0.25% finasteride admixed with 3% minoxidil vs. 3% minoxidil solution in the treatment of male androgenetic alopecia. J Eur Acad Dermatol Venereol. 2018; 32(12): 2257–2263.
- Caserini M, Radicioni M, Leuratti C, et al. Effects of a novel finasteride 0.25% topical solution on scalp and serum dihydrotestosterone in healthy men with androgenetic alopecia. Int J Clin Pharmacol Ther. 2016; 54(1): 19–27.
- Fields JR, Vonu PM, Monir RL, et al. Topical ketoconazole for the treatment of androgenetic alopecia: a systematic review. Dermatol Ther. 2020; 33(1): e13202.
- Whiting DA, Waldstreicher J, Sanchez M, et al. Measuring reversal of hair miniaturization in androgenetic alopecia by follicular counts in horizontal sections of serial scalp biopsies: results of finasteride 1 mg treatment of men and postmenopausal women. J Investig Dermatol Symp Proc. 1999; 4(3): 282–284.
- Piérard-Franchimont C, Goffin V, Henry F, et al. Nudging hair shedding by antidandruff shampoos. A comparison of 1% ketoconazole, 1% piroctone olamine and 1% zinc pyrithione formulations. Int J Cosmet Sci. 2002; 24(5): 249–256.
- Piérard-Franchimont C, De Doncker P, Cauwenbergh G, et al. Ketoconazole shampoo: effect of long-term use in androgenic alopecia. Dermatology. 1998; 196(4): 474–477.
- Rafi AW, Katz RM. Pilot study of 15 patients receiving a new treatment regimen for androgenic alopecia: the effects of atopy on AGA. ISRN Dermatol. 2011; 2011: 241953.
- Rosette C, Rosette N, Mazzetti A, et al. Cortexolone 17α-propionate (clascoterone) is an androgen receptor antagonist in dermal papilla cells in vitro. J Drugs Dermatol. 2019; 18(2): 197–201.
- Cartwright M, Mazzetti A, Moro L, et al. A summary of in vitro, phase I, and phase II studies evaluating the mechanism of action, safety, and efficacy of clascoterone (cortexolone 17a propionate, CB-03-01) in androgenetic alopecia. J Am Acad Dermatol. 2019; 81(4): AB13.
- Dhillon S. Clascoterone: first approval. Drugs. 2020; 80(16): 1745–1750.
- Mazzetti A, Moro L, Gerloni M, 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.
- Johnstone MA. Hypertrichosis and increased pigmentation of eyelashes and adjacent hair in the region of the ipsilateral eyelids of patients treated with unilateral topical latanoprost. Am J Ophthalmol. 1997; 124(4): 544–547.
- Johnstone MA, Albert DM. Prostaglandin-induced hair growth. Surv Ophthalmol. 2002; 47 Suppl 1: S185–S202.
- Blume-Peytavi U, Lönnfors S, Hillmann K, et al. A randomized double-blind placebo-controlled pilot study to assess the efficacy of a 24-week topical treatment by latanoprost 0.1% on hair growth and pigmentation in healthy volunteers with androgenetic alopecia. J Am Acad Dermatol. 2012; 66(5): 794–800.
- Ioannides D, Lazaridou E. Female pattern hair loss. Curr Probl Dermatol. 2015; 47: 45–54.
- Abdel-Raouf H, Aly UF, Medhat W, et al. A novel topical combination of minoxidil and spironolactone for androgenetic alopecia: Clinical, histopathological, and physicochemical study. Dermatol Ther. 2021; 34(1): e14678.
- Ammar AM, Elshahid AR, Abdel-Dayem HA, et al. Dermoscopic evaluation of the efficacy of combination of topical spironolactone 5% and minoxidil 5% solutions in the treatment of androgenetic alopecia: a cross sectional-comparative study. J Cosmet Dermatol. 2022; 21(11): 5790–5799.
- Sintov A, Serafimovich S, Gilhar A. New topical antiandrogenic formulations can stimulate hair growth in human bald scalp grafted onto mice. Int J Pharm. 2000; 194(1): 125–134.
- Faghihi G, Iraji F, Siadat AH, et al. Comparison between "5% minoxidil plus 2% flutamide" solution vs. "5% minoxidil" solution in the treatment of androgenetic alopecia. J Cosmet Dermatol. 2022; 21(10): 4447–4453.
- Bassiouny EA, El-Samanoudy SI, Abbassi MM, et al. Comparison between topical cetirizine with minoxidil versus topical placebo with minoxidil in female androgenetic alopecia: a randomized, double-blind, placebo-controlled study. Arch Dermatol Res. 2023; 315(5): 1293–1304.
- Hossein Mostafa D, Samadi A, Niknam S, et al. Efficacy of cetirizine 1% versus minoxidil 5% topical solution in the treatment of male alopecia: a randomized, single-blind controlled study. J Pharm Pharm Sci. 2021; 24: 191–199.
- Alavi SM, Layegh P, Vahabi-Amlashi S, et al. Therapeutic effects of topical cetirizine in the treatment of female pattern hair loss: a randomized controlled noninferiority trial. Expert Rev Clin Pharmacol. 2023; 16(10): 1009–1015.
- The safety, tolerability and PK of KX-826 in healthy males with alopecia following topical multiple dose ascending. https://clinicaltrials.gov/study/NCT04502901 (9.06.2024).
- linical Trial Of KX-826 Tincture 1.0% For The Treatment Of Male Adult AGA In China Received Clearance By NMPA. https://en.kintor.com.cn/news/254.html (9.06.2024).
- Kintor Pharma Announces Successful Completion of Phase II Clinical Trial of KX-826 for Treatment of Androgenetic Alopecia in the US. https://en.kintor.com.cn/news/245.html (9.06.2024).
- Kintor Pharma Announces Completion of First Patient Enrollment in KX-826 Long-term Safety Phase III Trial for Treatment of AGA. https://en.kintor.com.cn/news/246.html (9.06.2024).
- Kintor Pharma Announced Completion of Phase I Trial of the World’s First PROTAC Compound (GT20029) for Topical Use. https://en.kintor.com.cn/news/233.html (9.06.2024).
- Kintor Pharma’s GT20029 Phase II trial meets primary endpoint. https://www.clinicaltrialsarena.com/news/kintor-trial-aga-treatment/ (11.06.2024).
