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Topilutamide
Chemical compound From Wikipedia, the free encyclopedia
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Topilutamide, known more commonly as fluridil and sold under the brand name Eucapil, is an antiandrogen medication which is used in the treatment of pattern hair loss in men and women.[6][1][2][3][4][5] It is used as a topical medication and is applied to the scalp.[1][2][3][4][5] Topilutamide belongs to a class of molecules known as perfluoroacylamido-arylpropanamides.[6]
Topilutamide is a nonsteroidal antiandrogen (NSAA), or an antagonist of the androgen receptor (AR), the biological target of androgens like testosterone and dihydrotestosterone (DHT).[1][2][3][4][5]
Topilutamide was introduced for medical use in 2003.[7] It is marketed only in the Czech Republic and Slovakia.[8] The patent for Topilutamide expired in 2020.[6]
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Medical uses
Topilutamide is used as a topical medication in the treatment of pattern hair loss in men and women.[1][2][3][4][5] Topilutamide is approved for cosmetic use in Europe but has not received FDA approval nor approval by the EMA for the treatment of androgenetic alopecia.[8] Finasteride and Minoxidil are currently the only treatments approved for the treatment of this condition.[2]
Available forms
Under the brand name Eucapil, topilutamide is available as a 2% topical formulation intended for application to the scalp.[4]
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Pharmacology
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Pharmacodynamics
Topilutamide is an antagonist of the AR, the biological target of androgens like testosterone and DHT.[1][2][3][4][5] Fluridil binds to the androgen receptor with approximately a 9-15-fold higher affinity than more primitive NSAAs such as bicalutamide and hydroxyflutamide, but more research is required to validate these findings.[6]
Pharmacokinetics
Topilutamide is a topical medication and is applied to the scalp.[1][2][3][4][5] Topilutamide degrades in human serum at 37 °C with a half-life of approximately 6 hours and is undetectable after 48 hours.[6] Perfluoroacylamido-arylpropanamides decompose hydrolytically to BP-34 and their corresponding perfluorocarboxylic acid.[6] In the case of topilutamide, that perfluorocarboxylic acid is trifluoroacetic acid.[6] The two metabolites of topilutamide namely BP-34 and trifluoroacetic acid were undetectable in human serum (below the detection limit of 5 ng/mL) along with the parent compound topilutamide, in human studies.[6] BP-34 was shown to be devoid of anti-androgenic activity.[6]
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Chemistry
Topilutamide is a nonsteroidal compound and is closely related to other NSAAs such as flutamide and bicalutamide.[7]
History
Topilutamide was introduced for medical use in 2003.[7]
Society and culture
Generic names
Topilutamide is the generic name of the drug and its INN.[9][10][11] It is also known more commonly as fluridil.[6] Topilutamide is also known by its former developmental code name BP-766.[6]
Brand names
Topilutamide is marketed by Interpharma Praha under the brand name Eucapil.[7][3]
Availability
Topilutamide is available only in Europe in the Czech Republic and Slovakia.[8]
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See also
References
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