Efinaconazole
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MedKoo CAT#: 314247

CAS#: 164650-44-6

Description: Efinaconazole is a triazole antifungal. It is approved for use in Canada and the USA as a 10% topical solution for the treatment of onychomycosis (fungal infection of the nail). Efinaconazole acts as a 14α-demethylase inhibitor. Efinaconazole inhibits fungal lanosterol 14α-demethylase involved in the biosynthesis of ergosterol, a constituent of fungal cell membranes. Efinaconazole has been shown to be active against isolates of the following microorganisms, both in vitro and in clinical infections. Efinaconazole exhibits in vitro minimum inhibitory concentrations (MICs) of 0.06 μg/mL or less against most ( ≥ 90%) isolates of the following microorganisms: Trichophyton rubrum; Trichophyton mentagrophytes.


Price and Availability

Size Price Shipping out time Quantity
50mg USD 150 2 weeks
100mg USD 250 2 weeks
200mg USD 450 2 weeks
500mg USD 950 2 weeks
1g USD 1650 2 weeks
2g USD 2450 2 weeks
5g USD 4250 2 weeks
10g USD 5650 2 weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-20. Prices are subject to change without notice.

Efinaconazole, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 314247
Name: Efinaconazole
CAS#: 164650-44-6
Chemical Formula: C18H22F2N4O
Exact Mass: 348.1762
Molecular Weight: 348.39
Elemental Analysis: C, 62.05; H, 6.36; F, 10.91; N, 16.08; O, 4.59


Synonym: KP103; KP-103; KP 103; CTK5J2975; AGJ95634; KB145948; Efinaconazole; trade name: Jublia.

IUPAC/Chemical Name: (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol

InChi Key: NFEZZTICAUWDHU-RDTXWAMCSA-N

InChi Code: InChI=1S/C18H22F2N4O/c1-13-5-7-23(8-6-13)14(2)18(25,10-24-12-21-11-22-24)16-4-3-15(19)9-17(16)20/h3-4,9,11-12,14,25H,1,5-8,10H2,2H3/t14-,18-/m1/s1

SMILES Code: C[C@@H](N1CCC(CC1)=C)[C@@](O)(C2=CC=C(F)C=C2F)CN3N=CN=C3


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO.

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


References

1: Pollak RA. Efinaconazole topical solution, 10% the development of a new topical treatment for toenail onychomycosis. J Am Podiatr Med Assoc. 2014 Nov;104(6):568-73. doi: 10.7547/8750-7315-104.6.568. PubMed PMID: 25514267.

2: Tosti A, Elewski BE. Treatment of onychomycosis with efinaconazole 10% topical solution and quality of life. J Clin Aesthet Dermatol. 2014 Nov;7(11):25-30. PubMed PMID: 25489379; PubMed Central PMCID: PMC4255695.

3: Gupta AK, Simpson FC, Abramovits W, Scheinfeld N. Efinaconazole 10% nail solution: a post-FDA approval update. Skinmed. 2014 Jul-Aug;12(4):235-7. PubMed PMID: 25335353.

4: Zeichner JA, Stein Gold L, Korotzer A. Penetration of ((14)C)-Efinaconazole Topical Solution, 10%, Does Not Appear to be Influenced by Nail Polish. J Clin Aesthet Dermatol. 2014 Sep;7(9):34-6. PubMed PMID: 25276275; PubMed Central PMCID: PMC4174918.

5: Joseph WS, Vlahovic TC, Pillai R, Olin JT. Efinaconazole 10% solution in the treatment of onychomycosis of the toenails. J Am Podiatr Med Assoc. 2014 Sep-Oct;104(5):479-85. doi: 10.7547/0003-0538-104.5.479. PubMed PMID: 25275736.

6: Efinaconazole topical solution (Jublia) for onychomycosis. Med Lett Drugs Ther. 2014 Sep 15;56(1451):88-9. PubMed PMID: 25211303.

7: Jo W, Glynn M, Nejishima H, Sanada H, Minowa K, Calvarese B, Senda H, Pillai R, Mutter L. Nonclinical safety assessment of Efinaconazole Solution (10%) for onychomycosis treatment. Regul Toxicol Pharmacol. 2014 Oct;70(1):242-53. doi: 10.1016/j.yrtph.2014.07.012. Epub 2014 Jul 16. PubMed PMID: 25038564.

8: Gupta AK, Elewski BE, Sugarman JL, Ieda C, Kawabata H, Kang R, Pillai R, Olin JT, Watanabe S. The efficacy and safety of efinaconazole 10% solution for treatment of mild to moderate onychomycosis: a pooled analysis of two phase 3 randomized trials. J Drugs Dermatol. 2014 Jul;13(7):815-20. PubMed PMID: 25007364.

9: Iwata A, Watanabe Y, Kumagai N, Katafuchi-Nagashima M, Sugiura K, Pillai R, Tatsumi Y. In vitro and in vivo assessment of dermatophyte acquired resistance to efinaconazole, a novel triazole antifungal. Antimicrob Agents Chemother. 2014 Aug;58(8):4920-2. doi: 10.1128/AAC.02703-13. Epub 2014 May 27. PubMed PMID: 24867968; PubMed Central PMCID: PMC4136074.

10: Gupta AK, Simpson FC. Efinaconazole (Jublia) for the treatment of onychomycosis. Expert Rev Anti Infect Ther. 2014 Jul;12(7):743-52. doi: 10.1586/14787210.2014.919852. Epub 2014 May 22. PubMed PMID: 24850511.