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Candida and parasitic infection: Helminths, trichomoniasis, lice, scabies, and malaria
Published in Hung N. Winn, Frank A. Chervenak, Roberto Romero, Clinical Maternal-Fetal Medicine Online, 2021
Niclosamide, a salicylanilide, inhibits oxidative phosphor-ylation in the cestode mitochondria, killing the worm on contact. Niclosamide has been shown to have no teratogenic effect in rat and rabbit studies (45). No human malformations have been reported (pregnancy category B). The drug is poorly absorbed, but no information is available on niclosamide levels in breastmilk or on its ability to cross the placenta. There are inadequate data to assure the safety of uninterrupted breastfeeding following niclosamide therapy. Since single-dose therapy is used, temporary interruption (24 hours) of breastfeeding with disposal of milk can accommodate this therapy.
The Evaluation of Photo Allergic Contact Sensitizers in Humans
Published in Francis N. Marzulli, Howard I. Maibach, Dermatotoxicology Methods: The Laboratory Worker’s Vade Mecum, 2019
Some photocontact sensitizers are also capable of inducing ordinary contact allergy. The halogenated salicylanilides and certain sunscreens (e.g., PABA) are examples. Contact sensitization developed in 6 of 25 subjects exposed to TCSA in the photomaxi mi zati on test, while in another 6 a combined contact and photocontact sensitivity was suspected on the basis of a marked accentuation of the patch test reactions by UVA (Kaidbey and Kligman, 1980). Similar observations were made with DBS and bithionol, although they were far less active. It should be pointed out, however, that the photomaximization test is not designed to assess contact sensitization. Repeated exposures to the chemical and UV during induction may lead to the formation of photoproducts, which can themselves be sensitizing. UV may also alter local reactivity and cellular responses by its well-known effects on lymphoid cells. Nonetheless, the halogenated salicylanilides appear to be strong sensitizers in humans (Marzulli and Maibach, 1973). There is, however, no apparent relation between photocontact potential and ordinary contact sensitization. Thus the substituted coumarins, which are potent photosensitizers, are weak or poor contact allergens in the maximization test in humans (Opdyke, 1976, 1981). No instances of contact sensitization have been reported with musk ambrette, either clinically or in the maximization test.
Photoallergy
Published in Henry W. Lim, Nicholas A. Soter, Clinical Photomedicine, 2018
Cross-reactivity among many of the above antibacterial agents and other related chemicals has been reported. A list of salicylanilide-related antibacterials is provided in Table 3.
Development and validation of HPLC method for simultaneous estimation of erlotinib and niclosamide from liposomes optimized by screening design
Published in Journal of Liposome Research, 2023
Amruta Prabhakar Padakanti, Sachin Dattaram Pawar, Pramod Kumar, Naveen Chella
Erlotinib hydrochloride (ERL) is a broad-spectrum anticancer molecule that potently and selectively inhibits the tyrosine kinase enzyme in the epidermal growth factor receptor (EGFR). ERL monotherapy was approved clinically by USFDA in 2016 as first-line therapy for advanced non-small cell lung cancer (Ricciardi et al. 2011). However, major therapeutic failure is associated with erlotinib within 8–12 months of treatment by the development of acquired EGFR resistance (Nguyen et al.2009; Tang et al. 2013). Studies manifested that erlotinib HCl in combination with niclosamide represses the erlotinib resistance in various cancer like non-small cell lung cancer (Li et al. 2013), head and neck cancer (Li et al. 2013), and colon cancer (Shi et al. 2017). Niclosamide (NCM) is a salicylanilide derivative approved by US FDA in 1982 to treat tapeworm infections (Chen et al. 2018). Despite its clinical use as an anthelmintic drug, several studies exhibited it as a multi-functional repurposing drug with potential activity against various complicated diseases (Li et al. 2014). NCM has received more attention as a promising drug for different cancer therapy as it can control or inhibit multiple cell-signaling networks (Kadri et al. 2018).
Recent advances and future perspectives in the pharmacological treatment of Candida auris infections
Published in Expert Review of Clinical Pharmacology, 2021
Daniele R. Giacobbe, Laura Magnasco, Chiara Sepulcri, Malgorzata Mikulska, Philipp Koehler, Oliver A. Cornely, Matteo Bassetti
Some other agents have shown preliminary anti-C. auris activity in vitro. For example, the halogenated salicylanilide N1-(3,5-dichlorophenyl)-5-chloro-2-hydroxybenzamide (TCSA: Tri-Chloro-Salicyanilide) was individuated from a chemical library of 678 small molecules preselected for their bioactivity against S. cerevisiae and was investigated against the hyphal growth of one strain of C. auris and nine strains of C. albicans [117]. TCSA showed a good anti-biofilm activity against C. auris at low concentrations (1 μM). The proposed mechanism of action involves perturbation of the fungal mitochondrial protein import machinery[117].
Efflux in Gram-negative bacteria: what are the latest opportunities for drug discovery?
Published in Expert Opinion on Drug Discovery, 2023
Teresa Gil-Gil, Pablo Laborda, Luz Edith Ochoa-Sánchez, José Luis Martínez, Sara Hernando-Amado
Gram-negative bacteria possess innate resistance to clinically approved salicylanilide compounds, such as niclosamide, oxyclozanide, closantel, and rafoxanide, which are PMF-disrupting compounds that might potentiate the activity of diverse antibiotics through the disruption of the efflux. These compounds cross the outer membrane but are expelled from the cell via PMF-dependent mediated efflux. Then, when efflux is inhibited, or the membrane is disrupted via compounds such as colistin, salicylanilides uncouple the electron transport chain, dissipate the PMF, increase oxygen consumption, and decrease ATP production [120].