, Volume 73, Issue 17, pp 1977–1983 | Cite as

Efinaconazole: First Global Approval

  • Trina Patel
  • Sohita Dhillon
R&D Insight Report


A non-lacquer 10 % topical solution of efinaconazole, developed by Valeant Pharmaceuticals International, received its first global approval in Canada in October 2013 for the treatment of onychomycosis. The product is under regulatory review in the US and Japan. The mechanism of anti-fungal activity of efinaconazole, a small-molecule triazole compound, appears to be similar to that of other anti-fungal triazoles, namely ergosterol synthesis inhibition. In particular, it appears to inhibit 14α demethylase, an enzyme involved in the conversion of lanosterol to ergosterol, resulting in secondary degenerative changes. This article summarizes the milestones in the development of efinaconazole leading to this first approval for onychomycosis.


Terbinafine Tinea Pedis Ciclopirox Mycological Cure Topical Solution 
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  1. 1.
    Alley MR, Baker SJ, Beutner KR, et al. Recent progress on the topical therapy of onychomycosis. Expert Opin Investig Drugs. 2007;16(2):157–67.PubMedCrossRefGoogle Scholar
  2. 2.
    Tchernev G, Penev PK, Nenoff P, et al. Onychomycosis: modern diagnostic and treatment approaches. Wien Med Wochenschr. 2013;163(1–2):1–12.PubMedCrossRefGoogle Scholar
  3. 3.
    Gupta AK, Paquet M, Simpson FC. Therapies for the treatment of onychomycosis. Clin Dermatol. 2013;31(5):544–54.PubMedCrossRefGoogle Scholar
  4. 4.
    Jarratt M, Siu WJ, Yamakawa E, et al. Safety and pharmacokinetics of efinaconazole 10 % solution in healthy volunteers and patients with severe onychomycosis. J Drugs Dermatol. 2013;12(9):1010–6.PubMedGoogle Scholar
  5. 5.
    Rich P. Topical treatment of onychomycosis with efinaconazole solution 10 %. Cutis. 2013;91(6):305–7.PubMedGoogle Scholar
  6. 6.
    Valeant Pharmaceuticals International Inc. Valeant Pharmaceuticals announces approval of Jublia® for the treatment of onychomycosis in Canada [media release]. 3 Oct 2013.
  7. 7.
    Valeant Pharmaceuticals International Inc. Valeant pharmaceuticals announces receipt of U.S. FDA complete response letter for efinaconazole [media release]. 28 May 2013.
  8. 8.
    Kaken Pharmaceutical Co. Ltd. R&D pipeline. 2013. Accessed 22 Oct 2013.
  9. 9.
    Valeant Pharmaceuticals International Inc. Valeant pharmaceuticals provides efinconazole update [media release]. 2 May 2013.
  10. 10.
    Valeant Pharmaceuticals International Inc. Valeant pharmaceuticals announces award in Anacor dispute [media release]. 18 Oct 2013.
  11. 11.
    Valeant Pharmaceuticals Inc. Valeant Pharmaceuticals announces settlement agreement with Anacor [media release]. 28 Oct 2013.
  12. 12.
    Kaken P. Kaken pharmaceutical to license its antifungal compound KP-103 to Dow Pharmaceutical Sciences [media release]. 11 May 2006.
  13. 13.
    Valeant Pharmaceuticals International Inc. Valeant Pharmaceuticals completes acquisition of Dow Pharmaceutical Sciences Inc [media release]. 2 Jan 2009.
  14. 14.
    Tatsumi Y, Nagashima M, Shibanushi T, et al. Mechanism of action of efinaconazole, a novel triazole antifungal agent. Antimicrob Agents Chemother. 2013;57(5):2405–9.PubMedCrossRefGoogle Scholar
  15. 15.
    Bhatt V, Sarpotdar P, Pillai R, et al. Development of an optimal formulation for efinaconazole a novel antifungal agent for the treatment of onychomycosis by topical application [abstract no. P6541]. J Am Acad Dermatol. 2013;68(4 Suppl 1):AB104.Google Scholar
  16. 16.
    Tatsumi Y, Yokoo M, Arika T. In vitro antifungal activity of KP-103, a novel triazole derivative, and its therapeutic efficacy against experimental plantar tinea pedis and cutaneous candidiasis in guinea pigs. Antimicrob Agents Chemother. 2001;45(5):1493–9.PubMedCrossRefGoogle Scholar
  17. 17.
    Tatsumi Y, Yokoo M, Senda H. Therapeutic efficacy of topically applied KP-103 against experimental tinea unguium in guinea pigs in comparison with amorolfine and terbinafine. Antimicrob Agents Chemother. 2002;46(12):3797–801.PubMedCrossRefGoogle Scholar
  18. 18.
    Jo Siu WJ, Tatsumi Y, Senda H, et al. Comparison of in vitro antifungal activities of efinaconazole and currently available antifungal agents against a variety of pathogenic fungi associated with onychomycosis. Antimicrob Agents Chemother. 2013;57(4):1610–6.PubMedCrossRefGoogle Scholar
  19. 19.
    Sugiura K, Hosaka S, Sugimoto N, et al. Efinaconazole’s nail penetration and fungicidal activity may contribute to its therapeutic efficacy as a topical treatment for onychomycosis [abstract no. 1151]. J Invest Dermatol. 2013;133(Suppl 1):S195.Google Scholar
  20. 20.
    Del Rosso JQ, Reece B, Smith K, et al. Efinaconazole 10 % solution: a new topical treatment for onychomycosis: contact sensitization and skin irritation potential. J Clin Aesthet Dermatol. 2013;6(3):20–4.PubMedGoogle Scholar
  21. 21.
    Glynn M, Nejishima H, Sanada H, et al. Efinaconazole 10 % solution: nonclinical safety supports topical use in onychomycosis [abstract no. P6552]. J Am Acad Dermatol. 2013;68(4 Suppl 1):AB105.Google Scholar
  22. 22.
    Jo W, Glynn M, Minowa K, et al. Efinaconazole: developmental and reproductive toxicity potential [abstract no. P712]. Int J Toxicol. 2013;32(1):82–3.Google Scholar
  23. 23.
    Jo Siu W, Mutter L, Aoyama A, et al. In vitro CYP inhibition and induction assessments of efinaconazole coupled with low clinical systemic exposure suggest low DDI potential in topical onychomycosis [abstract no. 1140]. J Invest Dermatol. 2013;133 Suppl 1:S193.Google Scholar
  24. 24.
    Elewski BE, Rich P, Pollak R, et al. Efinaconazole 10 % solution in the treatment of toenail onychomycosis: two phase III multicenter, randomized, double-blind studies. J Am Acad Dermatol. 2013;68(4):600–8.PubMedCrossRefGoogle Scholar
  25. 25.
    Tschen EH, Bucko AD, Oizumi N, et al. Efinaconazole solution in the treatment of toenail onychomycosis: a phase 2, multicenter, randomized, double-blind study. J Drugs Dermatol. 2013;12(2):186–92.PubMedGoogle Scholar

Copyright information

© Springer International Publishing Switzerland 2013

Authors and Affiliations

  1. 1.Adis R & D InsightNorth ShoreNew Zealand
  2. 2.AdisAucklandNew Zealand

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