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Clofazimine

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https://www.readbyqxmd.com/read/28199712/clofazimine-mechanisms-of-action-in-mycobacteria-hiv-and-cancer
#1
William Levis
No abstract text is available yet for this article.
February 12, 2017: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/28158186/a-high-throughput-phenotypic-screen-identifies-clofazimine-as-a-potential-treatment-for-cryptosporidiosis
#2
Melissa S Love, Federico C Beasley, Rajiv S Jumani, Timothy M Wright, Arnab K Chatterjee, Christopher D Huston, Peter G Schultz, Case W McNamara
Cryptosporidiosis has emerged as a leading cause of non-viral diarrhea in children under five years of age in the developing world, yet the current standard of care to treat Cryptosporidium infections, nitazoxanide, demonstrates limited and immune-dependent efficacy. Given the lack of treatments with universal efficacy, drug discovery efforts against cryptosporidiosis are necessary to find therapeutics more efficacious than the standard of care. To date, cryptosporidiosis drug discovery efforts have been limited to a few targeted mechanisms in the parasite and whole cell phenotypic screens against small, focused collections of compounds...
February 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28131606/antimicrobial-susceptibility-and-mic-distribution-of-41-drugs-against-clinical-isolates-from-china-and-reference-strains-of-nontuberculous-mycobacteria
#3
Guilian Li, Hui Pang, Qian Guo, Mingxiang Huang, Yanhong Tan, Chao Li, Jianhao Wei, Yuanzhi Xia, Yi Jiang, Xiuqin Zhao, Haican Liu, Li-Li Zhao, Zhiguang Liu, Donglei Xu, Kanglin Wan
To treat nontuberculous mycobacteria (NTM) infections more optimally, further research pertaining to mycobacterial susceptibility to antimicrobial agents is required. A total of 82 species of NTM reference strains and 23 species of NTM clinical isolates were included. Minimum inhibitory concentrations (MICs) for 41 drugs were determined using the microdilution method in cation-adjusted Mueller-Hinton broth. The results showed that most of the NTM were susceptible to aminoglycosides, quinolones, three macrolides (clarithromycin, azithromycin and roxithromycin), cefmetazole, linezolid and capreomycin...
December 21, 2016: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28122281/anti-cancer-effect-of-clofazimine-as-a-single-agent-and-in-combination-with-cisplatin-on-u266-multiple-myeloma-cell-line
#4
İpek Z Durusu, Hazal H Hüsnügil, Heval Ataş, Ayşenur Biber, Selin Gerekçi, Ezgi A Güleç, Can Özen
Multiple Myeloma (MM) is a malignant neoplasm of bone marrow plasma B cells with high morbidity. Clofazimine (CLF) is an FDA-approved leprostatic, anti-tuberculosis, and anti-inflammatory drug that was previously shown to have growth suppression effect on various cancer types such as hepatocellular, lung, cervix, esophageal, colon, and breast cancer as well as melanoma, neuroblastoma, and leukemia. The objective of this study was to evaluate the anticancer effect and mechanism of CLF on U266 MM cell line. CLF (10μM, 24h) treatment resulted up to 72% growth suppression on a panel of hematological cell lines...
January 16, 2017: Leukemia Research
https://www.readbyqxmd.com/read/28115355/synergistic-interactions-of-mmpl3-inhibitors-with-antitubercular-compounds-in-vitro
#5
Wei Li, Andrea Sanchez-Hidalgo, Victoria Jones, Vinicius Calado Nogueira de Moura, E Jeffrey North, Mary Jackson
A number of inhibitors of the essential Mycobacterium tuberculosis mycolic acid transporter, MmpL3, are currently under development as potential novel antituberculosis agents. Using the checkerboard method to study the interaction profiles of various antituberculosis drugs or experimental compounds with two different chemotypes inhibiting this transporter (indolcarboxamides and adamantyl ureas), we show that MmpL3 inhibitors act synergistically with rifampin, bedaquiline, clofazimine and β-lactams.
January 23, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28079296/elasticity-in-macrophage-synthesized-biocrystals
#6
Elizabeth M Horstman, Rahul K Keswani, Benjamin A Frey, Phillip M Rzeczycki, Vernon LaLone, Jeffery A Bertke, Paul J A Kenis, Gus R Rosania
Supramolecular crystalline assembly constitutes a rational approach to bioengineer intracellular structures. Here, biocrystals of clofazimine (CFZ) that form in vivo within macrophages were measured to have marked curvature. Isolated crystals, however, showed reduced curvature suggesting that intracellular forces bend these drug crystals. Consistent with the ability of biocrystals to elastically deform, the inherent crystal structure of the principal molecular component of the biocrystals-the hydrochloride salt of CFZ (CFZ-HCl)-has a corrugated packing along the (001) face and weak dispersive bonding in multiple directions...
January 12, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28073970/estimated-generic-prices-for-novel-treatments-for-drug-resistant-tuberculosis
#7
Dzintars Gotham, Joseph Fortunak, Anton Pozniak, Saye Khoo, Graham Cooke, Frederick E Nytko, Andrew Hill
BACKGROUND: The estimated worldwide annual incidence of MDR-TB is 480 000, representing 5% of TB incidence, but 20% of mortality. Multiple drugs have recently been developed or repurposed for the treatment of MDR-TB. Currently, treatment for MDR-TB costs thousands of dollars per course. OBJECTIVES: To estimate generic prices for novel TB drugs that would be achievable given large-scale competitive manufacture. METHODS: Prices for linezolid, moxifloxacin and clofazimine were estimated based on per-kilogram prices of the active pharmaceutical ingredient (API)...
January 10, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28052847/subcellular-partitioning-and-intra-macrophage-selectivity-of-antimicrobial-compounds-against-mycobacterium-tuberculosis
#8
Michael D Schump, Douglas M Fox, Carolyn R Bertozzi, Lee W Riley
The efficacy of antimicrobial drugs against Mycobacterium tuberculosis (Mtb), an intracellular bacterial pathogen, is generally first established by testing compounds against bacteria in axenic culture. However, inside of infected macrophages bacteria encounter an environment which differs substantially from broth culture and are subject to important host-dependent pharmacokinetic phenomena which modulate drug activity. Here we describe how pH dependent partitioning drives asymmetric antimicrobial drug distribution in Mtb infected macrophages...
January 4, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28049171/group-5-drugs-for-multidrug-resistant-tuberculosis-individual-patient-data-meta-analysis
#9
Greg J Fox, Andrea Benedetti, Helen Cox, Won-Jung Koh, Piret Viiklepp, Shama Ahuja, Geoffrey Pasvol, Dick Menzies
The role of so-called "group 5" second-line drugs as a part of antibiotic therapy for multidrug-resistant tuberculosis (MDR-TB) is widely debated. We performed an individual patient data meta-analysis to evaluate the effectiveness of several group 5 drugs including amoxicillin/clavulanic acid, thioacetazone, the macrolide antibiotics, linezolid, clofazimine and terizidone for treatment of patients with MDR-TB.Detailed individual patient data were obtained from 31 published cohort studies of MDR-TB therapy. Pooled treatment outcomes for each group 5 drug were calculated using a random effects meta-analysis...
January 2017: European Respiratory Journal: Official Journal of the European Society for Clinical Respiratory Physiology
https://www.readbyqxmd.com/read/28043638/activity-of-drugs-against-dormant-mycobacterium-tuberculosis
#10
A Iacobino, G Piccaro, F Giannoni, A Mustazzolu, L Fattorini
OBJECTIVE/BACKGROUND: Heterogeneous mixtures of cellular and caseous granulomas coexist in the lungs of tuberculosis (TB) patients, with Mycobacterium tuberculosis (Mtb) existing from actively replicating (AR) to dormant, nonreplicating (NR) stages. Within cellular granulomas, the pH is estimated to be less than 6, whereas in the necrotic centres of hypoxic, cholesterol/triacylglycerol-rich, caseous granulomas, the pH varies between 7.2 and 7.4. To combat TB, we should kill both AR and NR stages of Mtb...
December 2016: International Journal of Mycobacteriology
https://www.readbyqxmd.com/read/28031270/unexpected-high-prevalence-of-resistance-associated-rv0678-variants-in-mdr-tb-patients-without-documented-prior-use-of-clofazimine-or-bedaquiline
#11
Cristina Villellas, Nele Coeck, Conor J Meehan, Nacer Lounis, Bouke de Jong, Leen Rigouts, Koen Andries
OBJECTIVES: Resistance-associated variants (RAVs) in Rv0678, a regulator of the MmpS5-MmpL5 efflux pump, have been shown to lead to increased MICs of bedaquiline (2- to 8- fold) and clofazimine (2- to 4-fold). The prevalence of these Rv0678 RAVs in clinical isolates and their impact on treatment outcomes are important factors to take into account in bedaquiline treatment guidelines. METHODS: Baseline isolates from two bedaquiline MDR-TB clinical trials were sequenced for Rv0678 RAVs and corresponding bedaquiline MICs were determined on 7H11 agar...
December 28, 2016: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/28007559/macrophage-mediated-clofazimine-sequestration-is-accompanied-by-a-shift-in-host-energy-metabolism
#12
Julie Trexel, Gi S Yoon, Rahul K Keswani, Cora McHugh, Larisa Yeomans, Victor Vitvitsky, Ruma Banerjee, Sudha Sud, Yihan Sun, Gus R Rosania, Kathleen A Stringer
Prolonged (8 weeks) oral administration of clofazimine results in a profound pharmacodynamic response- bioaccumulation in macrophages (including Kupffer cells) as intracellular crystal-like drug inclusions (CLDIs) with an associated increase in interleukin-1 receptor antagonist production. Notably, CLDI formation in Kupffer cells concomitantly occurs with the formation of macrophage-centric granulomas. Accordingly, we sought to understand the impact of these events on host metabolism using (1)H-nuclear magnetic resonance metabolomics...
December 19, 2016: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27993848/mycobacterium-tuberculosis-is-selectively-killed-by-rifampin-and-rifapentine-in-hypoxia-at-neutral-ph
#13
Angelo Iacobino, Giovanni Piccaro, Federico Giannoni, Alessandro Mustazzolu, Lanfranco Fattorini
The activity of rifampin, rifapentine, bedaquiline, PA-824, clofazimine, nitazoxanide, isoniazid, amikacin, moxifloxacin, niclosamide, thioridazine and pyrazinamide was tested against nonreplicating (dormant) Mycobacterium tuberculosis under conditions of hypoxia at pH 5.8 and 7.3 mimicking environments of cellular granulomas and caseous granulomas, respectively. At pH 5.8, several drugs killed dormant bacilli, with the best being rifampin and rifapentine. At pH 7.3, only rifampin and rifapentine efficiently killed dormant bacilli while all other drugs showed little activity...
December 19, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27983790/multifunctional-polymer-ligand-interface-cdznses-zns-quantum-dot-cy3-labeled-protein-pairs-as-sensitive-fret-sensors
#14
Hong Yu Yang, Yan Fu, Moon-Sun Jang, Yi Li, Jung Hee Lee, Heeyeop Chae, Doo Sung Lee
High-quality CdZnSeS/ZnS alloyed core/thick-shell quantum dots (QDs) as energy donors were first exploited in Förster resonance energy transfer (FRET) applications. A highly efficient ligand-exchange method was used to prepare low toxicity, high quantum yield, stabile, and biocompatible CdZnSeS/ZnS QDs densely capped with multifunctional polymer ligands containing dihydrolipoic acid (DHLA). The resulting QDs can be applied to construct QDs-based Förster resonance energy transfer (FRET) systems by their high affinity interaction with dye cyanine 3 (Cy3)-labeled human serum albumin (HSA)...
December 28, 2016: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/27927925/emergence-of-mmpt5-variants-during-bedaquiline-treatment-of-mycobacterium-intracellulare-lung-disease
#15
David C Alexander, Ravikiran Vasireddy, Sruthi Vasireddy, Julie V Philley, Barbara A Brown-Elliott, Benjamin J Perry, David E Griffith, Jeana L Benwill, Andrew D S Cameron, Richard J Wallace
Bedaquiline (BDQ), a diarylquinoline antibiotic that targets ATP synthase, is effective for the treatment of Mycobacterium tuberculosis infections that no longer respond to conventional drugs. While investigating the off-label use of BDQ as salvage therapy, seven of 13 patients with Mycobacterium intracellulare lung disease had an initial microbiological response and then relapsed. Whole-genome comparison of pretreatment and relapse isolates of M. intracellulare uncovered mutations in a previously uncharacterized locus, mmpT5 Preliminary analysis suggested similarities between mmpT5 and the mmpR5 locus, which is associated with low-level BDQ resistance in M...
February 2017: Journal of Clinical Microbiology
https://www.readbyqxmd.com/read/27878107/imaging-the-nadh-nad-homeostasis-for-understanding-the-metabolic-response-of-mycobacterium-to-physiologically-relevant-stresses
#16
Shabir A Bhat, Iram K Iqbal, Ashwani Kumar
The NADH:NAD(+) ratio is the primary indicator of the metabolic state of bacteria. NAD(H) homeostasis is critical for Mycobacterium tuberculosis (Mtb) survival and is thus considered an important drug target, but the spatio-temporal measurements of NAD(H) remain a challenge. Genetically encoded fluorescent biosensors of the NADH:NAD(+) ratios were recently described, paving the way for investigations of the metabolic state of pathogens during infection. Here we have adapted the genetically encoded biosensor Peredox for measurement of the metabolic state of Mtb in vitro and during infection of macrophage cells...
2016: Frontiers in Cellular and Infection Microbiology
https://www.readbyqxmd.com/read/27854508/new-repurposed-drugs-for-pediatric-multidrug-resistant-tuberculosis-practice-based-recommendations
#17
Elizabeth P Harausz, Anthony J Garcia-Prats, James A Seddon, H Simon Schaaf, Anneke C Hesseling, Jay Achar, Jonathan Bernheimer, Andrea Cruz, Lia D'Ambrosio, Anne Detjen, Stephen M Graham, Jennifer Hughes, Sylvie Jonckheere, Ben J Marais, Giovanni Battista Migliori, Lindsay McKenna, Alena Skrahina, Marina Tadolini, Peyton Wilson, Jennifer Furin
It is estimated that 33,000 children develop multidrug-resistant tuberculosis (MDR-TB) each year. In spite of these numbers, children and adolescents have limited access to the new and repurposed MDR-TB drugs. There is also little clinical guidance for the use of these drugs and for the shorter MDR-TB regimen in the pediatric population. This is despite the fact that these drugs and regimens are associated with improved interim outcomes and acceptable safety profiles in adults. This review fills a gap in the pediatric MDR-TB literature by providing practice-based recommendations for the use of the new (delamanid and bedaquiline) and repurposed (linezolid and clofazimine) MDR-TB drugs and the new shorter MDR-TB regimen in children and adolescents...
November 17, 2016: American Journal of Respiratory and Critical Care Medicine
https://www.readbyqxmd.com/read/27816662/applicability-of-the-shorter-bangladesh-regimen-in-high-mdr-tb-settings
#18
Giovanni Sotgiu, Simon Tiberi, Rosella Centis, Lia D'Ambrosio, Zhenia Fuentes, Alimuddin Zumla, Giovanni Battista Migliori
In spite of the recent introduction of two new drugs (delamanid and bedaquiline) and a few repurposed compounds to treat multidrug-resistant and extensively drug-resistant tuberculosis (MDR- and XDR-TB), clinicians are facing increasing problems in designing effective regimens in severe cases. Recently a 9 to 12-month regimen (known as Bangladesh regimen) proved to be effective in treating MDR-TB cases. It included an initial phase of 4 to 6 months of kanamycin, moxifloxacin, prothionamide, clofazimine, pyrazinamide, high dose isoniazid and ethambutol followed by 5 months of moxifloxacin, clofazimine, pyrazinamide and ethambutol...
November 2, 2016: International Journal of Infectious Diseases: IJID
https://www.readbyqxmd.com/read/27800519/clofazimine-enteropathy-a-rare-and-underrecognized-complication-of-mycobacterial-therapy
#19
Winnie Szeto, Monica T Garcia-Buitrago, Lilian Abbo, Joseph D Rosenblatt, Baharak Moshiree, Michele I Morris
Clofazimine-induced crystal-storing histiocytosis is a rare complication of treatment previously reported in dermatology literature as a complication of leprosy therapy. We report a case of disseminated Mycobacterium abscessus requiring treatment with high-dose oral clofazimine resulting in enteropathy in a patient who presented with abdominal pain, malnutrition, and melena.
September 2016: Open Forum Infectious Diseases
https://www.readbyqxmd.com/read/27798208/mechanisms-of-action-and-therapeutic-efficacies-of-the-lipophilic-antimycobacterial-agents-clofazimine-and-bedaquiline
#20
REVIEW
Moloko C Cholo, Maborwa T Mothiba, Bernard Fourie, Ronald Anderson
Drug-resistant (DR)-TB is the major challenge confronting the global TB control programme, necessitating treatment with second-line anti-TB drugs, often with limited therapeutic efficacy. This scenario has resulted in the inclusion of Group 5 antibiotics in various therapeutic regimens, two of which promise to impact significantly on the outcome of the therapy of DR-TB. These are the 're-purposed' riminophenazine, clofazimine, and the recently approved diarylquinoline, bedaquiline. Although they differ structurally, both of these lipophilic agents possess cationic amphiphilic properties that enable them to target and inactivate essential ion transporters in the outer membrane of Mycobacterium tuberculosis...
October 20, 2016: Journal of Antimicrobial Chemotherapy
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