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| Clinical data | |
|---|---|
| Trade names | Eucapil |
| Other names | Fluridil; BP-766 |
| Routes of administration | Topical[1][2][3][4][5] |
| Drug class | Nonsteroidal antiandrogen |
| ATC code |
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| Identifiers | |
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| CAS Number | |
| PubChemCID | |
| ChemSpider | |
| UNII | |
| ECHA InfoCard | 100.245.367 |
| Chemical and physical data | |
| Formula | C13H11F6N3O5 |
| Molar mass | 403.237 g·mol−1 |
| 3D model (JSmol) | |
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Topilutamide, known more commonly asfluridil and sold under the brand nameEucapil, is anantiandrogen medication which is used in the treatment ofpattern hair loss in men and women.[6][1][2][3][4][5] It is used as atopical medication and is applied to thescalp.[1][2][3][4][5] Topilutamide belongs to a class of molecules known as perfluoroacylamido-arylpropanamides.[6]
Topilutamide is anonsteroidal antiandrogen (NSAA), or anantagonist of theandrogen receptor (AR), thebiological target ofandrogens liketestosterone anddihydrotestosterone (DHT).[1][2][3][4][5]
Topilutamide was introduced for medical use in 2003.[7] It is marketed only in theCzech Republic andSlovakia.[8] The patent for Topilutamide expired in 2020.[6]
Topilutamide is used as atopical medication in the treatment ofpattern hair loss in men and women.[1][2][3][4][5] Topilutamide is approved for cosmetic use in Europe but has not receivedFDA approval nor approval by theEMA for the treatment ofandrogenetic alopecia.[8]Finasteride andMinoxidil are currently the only treatments approved for the treatment of this condition.[2]
Under the brand name Eucapil, topilutamide is available as a 2% topicalformulation intended for application to thescalp.[4]
Topilutamide is anantagonist of the AR, thebiological target ofandrogens liketestosterone 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 asbicalutamide andhydroxyflutamide, but more research is required to validate these findings.[6]
| Compound | 3 μM | 10 μM |
|---|---|---|
| BP-766 (Topilutamide) | 41 ± 5 | 95.9 ± 6 |
| BP-521 | 62 ± 7 | 100 |
| BP-34 | 3 ± 4 | 2 ± 2 |
| Bicalutamide | 3 ± 3 | 11 ± 3 |
| Hydroxyflutamide | 2 ± 6 | 6 ± 7 |
Topilutamide is atopical medication and is applied to thescalp.[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 decomposehydrolytically to BP-34 and their correspondingperfluorocarboxylic acid.[6] In the case of topilutamide, that perfluorocarboxylic acid istrifluoroacetic 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]
Topilutamide is anonsteroidal compound and is closely related to other NSAAs such asflutamide andbicalutamide.[7]
Topilutamide was introduced for medical use in 2003.[7]
Topilutamide is thegeneric name of the drug and itsINNTooltip International Nonproprietary Name.[9][10][11] It is also known more commonly asfluridil.[6] Topilutamide is also known by its former developmental code nameBP-766.[6]
Topilutamide is marketed by Interpharma Praha under the brand name Eucapil.[7][3]
Topilutamide is available only inEurope in theCzech Republic andSlovakia.[8]
Fluridil was developed as a topical antiandrogen, suitable for the treatment of hyperandrogenic skin syndromes. The cosmetic product Eucapil® containing 2% fluridil in isopropanol was tested in women with AGA in a 9-month open study. [...] In a clinical study conducted at our facility, fluridil in solution (Eucapil®, Interpharma Praha, Czech Republic) has been shown to be effective and safe in the treatment of men with androgenetic alopecia (30, 31).