diiodohydroxyquinoline / Generic mfg. - LARVOL DELTA

Extra-intestinal Balantidiasis in an 84-year-old Male (ATS 2025) - "tetracycline, metronidazole, and iodoquinol are all available treatments for Balantidiasis. Extra-intestinal Balantidium coli infections are rare and should be considered in cases of unexplained pulmonary symptoms, even in patients without obvious risk factors. Early detection and treatment can lead to a favorable outcome."

Chronic Cough • Chronic Obstructive Pulmonary Disease • Cough • Gastrointestinal Disorder • Immunology • Infectious Disease • Pulmonary Disease • Respiratory Diseases

Delayed Stevens-Johnson syndrome induced by combined administration of carbamazepine and botulinum toxin: A case report. (PubMed, Medicine (Baltimore)) - "In order to prevent severe adverse reactions, patients using carbamazepine in conjunction with other medications should be vigilant for the early symptoms of serious drug rashes."

Journal • Cerebral Hemorrhage • Hematological Disorders • Steven-Johnson Syndrome

Repurposing FDA-approved drugs cetilistat, abiraterone, diiodohydroxyquinoline, bexarotene, and remdesivir as potential inhibitors against RNA dependent RNA polymerase of SARS-CoV-2: A comparative in silico perspective. (PubMed, Inform Med Unlocked) - "Furthermore, to validate the potency of these drugs, we compared them to the antiviral remdesivir, which inhibits RdRp. Our finding indicated that the selected drugs have a high potential to be developed as RdRp inhibitors and, with further validation studies, could serve as potential drugs for the treatment of COVID-19."

FDA event • Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Onchocerciasis Drug Discovery - Evaluation of FDA-Approved Drugs against Onchocerca gutturosa in vitro. (ASTMH 2022) - "Overall, 39 drugs were inactive, while 44 drugs produced moderate activity (50-99% motility and/or MTT reductions), including Amitraz, Broxyquinoline, Cefuroxime sodium, Mangafodipir trisodium, Methenamine, Primaquine phosphate, and Rivastigmine tartrate. However 23 drugs produced good activity (100% motility reductions and significant MTT reductions); these drugs included Atovaquone, Gramicidin, Iodoquinol, Isradipine, Losartan, Nitrofurazone, Oxyquinoline hemisulphate, Rifaximin, Cefaclor, and Pyrantel pamoate. Our results warrant further investigations regarding the possible re-purposing of some of the identified drugs. In addition, the identification of these hits may provide a good starting point for searches for related compounds of possible interest, and/or lead to new chemical synthesis."

FDA event • Preclinical • Infectious Disease

Using a high - throughput, whole - cell hydrogenase assay to identify potential small molecule inhibitors of [NiFe] - hydrogenase. (PubMed, Metallomics) - "Iodoquinol was identified as a potential inhibitor of the nickel biosynthetic pathway of [NiFe] - hydrogenase through a two-step screening process, but further studies with immunoblot assays showed confounding effects dependent on the cell growth phase. This study highlights the significance of considering the growth phenotype for whole - cell based assays overall and its effects on various cellular processes influenced by metal trafficking and homeostasis."

Journal • Infectious Disease

Identifying novel drugs with new modes of action for neglected tropical fungal skin diseases (fungal skinNTDs) using an Open Source Drug discovery approach. (PubMed, Expert Opin Drug Discov) - "From the currently available data, the azoles and iodoquinol were the only compounds with activity against causative agents from the three different fungal skinNTDs...For mycetoma, the fenarimols, aminothiazoles and benzimidazole carbamates are currently being investigated in the MycetOS initiative. To come to a more integrated approach to identify drugs active against all three fungal skinNTDs, compounds made in the MycetOS initiative could also be explored for chromoblastomycosis and sporotrichosis."

Journal • Dermatology • Infectious Disease • Malaria

Experimental Evidence for Diiodohydroxyquinoline-Induced Neurotoxicity: Characterization of Age and Gender as Predisposing Factors. (PubMed, Pharmaceuticals (Basel)) - "Noteworthy, young female rats were more susceptible to DHQ's toxicity than their counterparts. Taken together, these findings confirm previous safety concerns regarding quinoline-associated neurotoxicity and provide an impetus to review risk/benefit balance for their use."

Journal • Mood Disorders • Psychiatry

Clostridioides difficile: Innovations in Target Discovery and Potential for Therapeutic Success. (PubMed, Expert Opin Ther Targets) - "Our review also highlights the therapeutic potential of re-purposing currently available agents such Auranofin, Diiodohydroxyquinoline, Ronidazole, and natural products, for the management of patients with CDI...Considerable progress has been made in the development of new anti-CDI drug candidates. Nevertheless, a greater comprehension of CDI pathogenesis and host-microbe interactions, informed by a systems biology high-throughput interrogation of multidimensional omics and whole structural data, coupled with comparative genomics, is beginning to uncover potential novel therapeutic targets, which can be exploited to plug gaps in the CDI drug discovery pipeline."

Journal • Infectious Disease

Identification of Promising Antifungal Drugs against Scedosporium and Lomentospora Species after Screening of Pathogen Box Library. (PubMed, J Fungi (Basel)) - "SEM revealed morphological alterations and synergism analysis showed that both drugs present positive interactions with voriconazole, fluconazole, and caspofungin. These data suggest that auranofin and iodoquinol are promising compounds to be studied as repurposing approaches against scedosporiosis and lomentosporiosis."

Journal • Infectious Disease

Inhibitory activity of FDA-approved drugs cetilistat, abiraterone, diiodohydroxyquinoline, bexarotene, remdesivir, and hydroxychloroquine on COVID-19 main protease and human ACE2 receptor: A comparative in silico approach. (PubMed, Inform Med Unlocked) - "The MD simulation results demonstrated that these drugs interact to stabilize the systems, allowing them to be used as effective inhibitors of these proteins. Meanwhile, bexarotene, abiraterone, cetilistat, and diiodohydroxyquinoline's systemic effects should be further investigated in suitable ex vivo human organ culture or organoids, animal models, or clinical trials."

FDA event • Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Transforming iodoquinol into broad spectrum anti-tumor leads: Repurposing to modulate redox homeostasis. (PubMed, Bioorg Chem) - "Additionally, an anti-angiogenic effect was evident with compound 5 as supported by the decreased expression of VEGF. Interesting binding modes within NQO-1 active site had been identified and confirmed by both molecular docking and dymanic experiments."

IO biomarker • Journal • Oncology • BCL2 • CASP3 • CDK1 • NQO1 • TP53

Balantioides coli. (PubMed, Res Vet Sci) - "Efective treatments include tetracycline, iodoquinol and 5-nitroimidazole compounds (metronidazole, secnidazole). The main effective individual preventive measure is the use of disinfected water for drinking and other uses. Adequate water supply infrastructures, proper disposal of wastewater and animal faeces, and regular monitoring programs on farms will help limit transmission."

Journal • Review

Identification of two potential inhibitors of Sporothrix brasiliensis and Sporothrix schenckii in the Pathogen Box collection. (PubMed, PLoS One) - "Sporotrichosis treatment remains restricted to a few options, itraconazole being the first choice for human and animal therapy. Scanning electron microscopy and flow cytometry analyses revealed that MMV102872 and iodoquinol induced changes in cell morphology, membrane integrity, and the presence of neutral lipids, impairing fungal survival. Our results indicate that MMV102872 and iodoquinol are promising molecules for use as scaffolds for the development of new antifungal agents."

Journal • Dermatology • Infectious Disease • Malaria

Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening system. (PubMed, Pharmacol Res) - "A few clinically approved drugs, such as remdesivir, chloroquine, hydroxychloroquine, nafamostat, camostat, and ivermectin, exhibited anti-SARS-CoV-2 activity in vitro and/or in a small number of patients. Bexarotene demonstrated the highest Cmax:EC ratio (1.69) which was higher than those of chloroquine, hydroxychloroquine, and ivermectin. These results demonstrated the efficacy of the two-tier screening system and identified potential COVID-19 treatments which can achieve effective levels if given by inhalation or systemically depending on their pharmacokinetics."

FDA event • Journal • Infectious Disease • Novel Coronavirus Disease • Oncology

A screening of the MMV Pathogen Box® reveals new potential antifungal drugs against the etiologic agents of chromoblastomycosis. (PubMed, PLoS One) - "The analysis of potential synergism of these compounds with itraconazole and terbinafine was performed by the checkerboard method. Toxicity analysis revealed that MMV021013 showed high selectivity indices (SI ≥ 10) against the fungi tested. In summary, auranofin, iodoquinol, and MMV021013 were identified as promising compounds to be tested in CBM models of infection."

Journal • Dermatology

Repurposing the antiamoebic drug diiodohydroxyquinoline for treatment of Clostridioides difficile infections. (PubMed, Antimicrob Agents Chemother) - "In a time-kill assay, DIHQ was superior to vancomycin and metronidazole, reducing a high bacterial inoculum by 3-log within six hours. Additionally, DIHQ did not inhibit growth of key species that compose the host intestinal microbiota, such as Bacteroides, Bifidobacterium and Lactobacillus spp. Collectively, our results indicate that DIHQ is a promising anticlostridial drug that warrants further investigation as a new therapeutic for CDIs."

Journal • APP

Repositionable Compounds with Antifungal Activity against Multidrug Resistant Candida auris Identified in the Medicines for Malaria Venture's Pathogen Box. (PubMed, J Fungi (Basel)) - "Both drugs possess broad spectrum of activity against Candida spp., including multiple strains of the emergent C. auris, and may constitute promising repositionable options for the development of novel therapeutics for the treatment of candidiasis."

Journal

Flavonoids as a Natural Treatment Against Entamoeba histolytica. (PubMed, Front Cell Infect Microbiol) - "...Usually, intestinal amebiasis and ALA are treated with synthetic chemical compounds (iodoquinol, paromomycin, diloxanide furoate, and nitroimidazoles). Metronidazole is the most common treatment for amebiasis...Interestingly, it was found that these natural compounds can induce morphological changes in the amebas, such as chromatin condensation and cytoskeletal protein re-organization, as well as the upregulation and downregulation of fructose-1,6-bisphosphate aldolase, glyceraldehyde-phosphate dehydrogenase, and pyruvate:ferredoxin oxidoreductase (enzymes of the glycolytic pathway). Although the specific molecular targets, bioavailability, route of administration, and doses of some of these natural compounds need to be determined, flavonoids represent a very promising and innocuous strategy that should be considered for use against E. histolytica in the era of microbial drug resistance."

Journal • Review