Novexatin
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Novexatin

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Novexatin is a novel antifungal peptide specifically designed for the topical treatment of onychomycosis.

Category
Peptide APIs
Catalog number
BAT-009113
CAS number
942577-31-3
Molecular Formula
C42H84N28O7
Molecular Weight
1093.32
IUPAC Name
2-[3-[(2S,5S,8S,11S,14S,17S,20S)-5,8,11,14,17,20-hexakis[3-(diaminomethylideneamino)propyl]-3,6,9,12,15,18,21-heptaoxo-1,4,7,10,13,16,19-heptazacyclohenicos-2-yl]propyl]guanidine
Synonyms
NP-213; NP213; NP 213
Appearance
Solid Powder
Purity
>98%
Density
1.61±0.1 g/cm3(Predicted)
Sequence
cyclo[Arg-Arg-Arg-Arg-Arg-Arg-Arg]
Storage
Store at -20°C
Solubility
Soluble in DMSO
InChI
InChI=1S/C42H84N28O7/c43-36(44)57-15-1-8-22-29(71)65-24(10-3-17-59-38(47)48)31(73)67-26(12-5-19-61-40(51)52)33(75)69-28(14-7-21-63-42(55)56)35(77)70-27(13-6-20-62-41(53)54)34(76)68-25(11-4-18-60-39(49)50)32(74)66-23(30(72)64-22)9-2-16-58-37(45)46/h22-28H,1-21H2,(H,64,72)(H,65,71)(H,66,74)(H,67,73)(H,68,76)(H,69,75)(H,70,77)(H4,43,44,57)(H4,45,46,58)(H4,47,48,59)(H4,49,50,60)(H4,51,52,61)(H4,53,54,62)(H4,55,56,63)/t22-,23-,24-,25-,26-,27-,28-/m0/s1
InChI Key
NVZLKNHDHPPJHL-RMIXPHLWSA-N
Canonical SMILES
C(CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCN=C(N)N)CCCN=C(N)N)CCCN=C(N)N)CCCN=C(N)N)CCCN=C(N)N)CCCN=C(N)N)CN=C(N)N
1. Sequential and Structural Aspects of Antifungal Peptides from Animals, Bacteria and Fungi Based on Bioinformatics Tools
Neelabh, Karuna Singh, Jyoti Rani Probiotics Antimicrob Proteins. 2016 Jun;8(2):85-101. doi: 10.1007/s12602-016-9212-3.
Emerging drug resistance varieties and hyper-virulent strains of microorganisms have compelled the scientific fraternity to develop more potent and less harmful therapeutics. Antimicrobial peptides could be one of such therapeutics. This review is an attempt to explore antifungal peptides naturally produced by prokaryotes as well as eukaryotes. They are components of innate immune system providing first line of defence against microbial attacks, especially in eukaryotes. The present article concentrates on types, structures, sources and mode of action of gene-encoded antifungal peptides such as mammalian defensins, protegrins, tritrpticins, histatins, lactoferricins, antifungal peptides derived from birds, amphibians, insects, fungi, bacteria and their synthetic analogues such as pexiganan, omiganan, echinocandins and Novexatin. In silico drug designing, a major revolution in the area of therapeutics, facilitates drug development by exploiting different bioinformatics tools. With this view, bioinformatics tools were used to visualize the structural details of antifungal peptides and to predict their level of similarity. Current practices and recent developments in this area have also been discussed briefly.
2. NP213 (Novexatin®): A unique therapy candidate for onychomycosis with a differentiated safety and efficacy profile
Derry K Mercer, Jennifer C Robertson, Lorna Miller, Colin S Stewart, Deborah A O'Neil Med Mycol. 2020 Nov 10;58(8):1064-1072. doi: 10.1093/mmy/myaa015.
NP213 (Novexatin®) is a novel antifungal peptide specifically designed for the topical treatment of onychomycosis. NP213 was designed using host defense peptides (HDP), essential components of the innate immune response to infection, as a template. NP213 is a water-soluble cyclic fungicidal peptide that effectively penetrates human nail. NP213 demonstrated a promising preclinical and clinical safety profile, with no evidence of systemic exposure following topical application to the skin and nails. NP213 was efficacious in two phase IIa human trials with 43.3% of patients having no fungi detectable by culture of fragments from NP213-treated nails after 180 days in the first study and likewise 56.5% of patients were culture negative for dermatophytes after 360 days in the second phase IIa study. In both trials, NP213 was applied daily for only 28 days in marked contrast to other topical onychomycosis treatments that require application for up to 52 weeks. Patient reported outcomes from the phase IIa studies were positive with participants recording an improved appearance of their nails after only 14 days of application. All fungi identified in these studies were Trichophyton spp. NP213 (Novexatin®) is a promising, highly differentiated peptide-based candidate for the topical treatment of onychomycosis, addressing the infectious cause and cosmetic issues of this very common condition.
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