Delving into the Latest Updates on Nikkomycin Z with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

NIK-Z, Nik Z

+ [1]

Target

Chitin synthase

Mechanism

Chitin synthase inhibitors

Therapeutic Areas

Infectious DiseasesOther Diseases

Active Indication-

Inactive Indication

Coccidioidomycosis

Originator Organization

Valley Fever Solutions, Inc.

Active Organization-

Inactive Organization

Valley Fever Solutions, Inc.

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

RegulationOrphan Drug (US)

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Structure

Molecular FormulaC20H25N5O10

InChIKeyWWJFFVUVFNBJTN-VHDFTHOZSA-N

CAS Registry59456-70-1

The purpose of this study is to determine if nikkomycin Z is safe when administered at different dose levels for 14 days. The study will also determine blood levels and urinary excretion of nikkomycin Z in relation to dose administered. Healthy patients will be eligible to participate and will be allocated to receive nikkomycin Z (various doses) or a placebo.

Start Date01 Oct 2008

Sponsor / Collaborator

University of Arizona

NCT00614666 / TerminatedPhase 1/2IIT

Phase I/II Evaluation of the Safety, Pharmacokinetics, and Preliminary Effectiveness of Nikkomycin Z in the Treatment of Patients With Uncomplicated Coccidioides Pneumonia

The purpose of this study is to determine if nikkomycin Z is safe when administered at different dose levels for 14 days. The study will also determine blood levels and urinary excretion of nikkomycin Z in relation to dose administered. Patients with mild forms of Valley Fever pneumonia will be eligible to participate and will be allocated to receive treatment with nikkomycin Z (various doses) or a placebo. A secondary goal of this study is to evaluate the effectiveness and dose response of nikkomycin Z in an exploratory analysis.

Start Date01 Sep 2007

Sponsor / Collaborator

University of Arizona

100 Clinical Results associated with Nikkomycin Z

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100 Translational Medicine associated with Nikkomycin Z

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100 Patents (Medical) associated with Nikkomycin Z

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316

Literatures (Medical) associated with Nikkomycin Z

03 Oct 2024·Microbiology Spectrum

Evaluation of nikkomycin Z with frequent oral administration in an experimental model of central nervous system coccidioidomycosis

Article

Author: Jaramillo, Rosie ; Larwood, David J. ; Wiederhold, Nathan P. ; Olivo, Marcos ; Patterson, Thomas F. ; Najvar, Laura K.

ABSTRACT We evaluated the in vivo activity of nikkomycin Z against central nervous system coccidioidomycosis. Mice were inoculated intracranially with arthroconidia of Coccidoides immitis , and treatment with nikkomycin Z (50, 100, or 300 mg/kg orally TID) or fluconazole (25 mg/kg orally BID) began 2 days later. Each dose of nikkomycin Z and fluconazole significantly improved survival and reduced brain fungal burden compared with vehicle control. Further studies of nikkomycin Z against coccidioidomycosis are warranted. IMPORTANCECoccidioides species are endemic fungi that are capable of causing disease in patients with various comorbidities, as well as in otherwise healthy individuals. Treatment options for coccidioidomycosis are suboptimal, as azole antifungals may be limited by drug interactions and adverse effects due to interactions with enzymes found in humans and other mammals. Nikkomycin Z is an investigational agent that works against a target specific to the fungal cell wall (chitin), which is not present in the cells of humans or other mammals. In this study, we show that frequent oral administration of nikkomycin Z is effective in an experimental model of central nervous system coccidioidomycosis. Further studies of nikkomycin Z against coccidioidomycosis may be warranted.

27 May 2024·Zeitschrift für Naturforschung C

Controlled delivery of nikkomycin by PEG coated PLGA nanoparticles inhibits chitin synthase to prevent growth of Aspergillus flavus and Aspergillus fumigatus

Article

Author: Ghormade, Vandana ; Mayattu, Kamal

AbstractAspergillosis is one of the most common fungal infections that can threaten individuals with immune compromised condition. Due to the increasing resistance of pathogens to the existing antifungal drugs, it is difficult to tackle such disease conditions. Whereas, nikkomycin is an emerging safe and effective antifungal drug which causes fungal cell wall disruption by inhibiting chitin synthase. Hence, the study aims at the development of nikkomycin loaded PEG coated PLGA nanoparticles for its increased antifungal efficiency and inhibiting Aspergillus infections. The P-PLGA-Nik NPs were synthesized by w/o/w double emulsification method which resulted in a particle size of 208.3 ± 15 nm with a drug loading of 52.97 %. The NPs showed first order diffusion-controlled drug release which was sustained for 24 h. These nanoparticle’s antifungal efficacy was tested using the CLSI – M61 guidelines and the MIC50 defined against Aspergillus flavus and Aspergillus fumigatus was found to be >32 μg/ml which was similar to the nikkomycin MIC. The hyphal tip bursting showed the fungal cell wall disruption. The non-cytotoxic and non-haemolytic nature highlights the drug safety profile.

02 May 2024·Journal of Biomolecular Structure and Dynamics

Analysis of the binding pattern of NIK inhibitors by computational simulation

Article

Author: Tang, Yingkai

NF-kappaB-Inducing Kinase (NIK) is a key kinase in the activation of the NF-κB non-classical signalling pathway, which has been shown to be over-activated in patients with inflammatory diseases, immune disorders and malignancies and solid tumours inducing activation of the NF-κB non-classical signalling pathway. The design of ATP-competitive small molecule inhibitors against NIK has been a hot topic in the last decade, and many efficient NIK inhibitors have been identified. In this work, I aim to unravel the mechanism of NIK inhibition by different representative NIK type I 1/2 kinase inhibitors, using ADME, molecular docking, molecular dynamics simulation, MM-PBSA analysis and 3D-QSAR analysis. This work contributes to the understanding of the efficiency of NIK inhibitor binding by revealing the basis of the efficiency of NIK inhibitors, the difference in binding modes between different inhibitors and the overall effect on NIK.Communicated by Ramaswamy H. Sarma.

100 Deals associated with Nikkomycin Z

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