ArticleAntimicrobial agents and chemotherapy2014
The clinical candidate VT-1161 is a highly potent inhibitor of Candida albicans CYP51 but fails to bind the human enzyme.
Article in Antimicrobial agents and chemotherapy, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 87 papers.
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87 citing papers in PubMed, 163 citations in OpenAlex.
- Oteseconazole versus fluconazole for the treatment of severe vulvovaginal candidiasis: a multicenter, randomized, double-blinded, phase 3 trial.Antimicrobial agents and chemotherapy · 2024Trial
- A Randomized Phase 2 Study of VT-1161 for the Treatment of Acute Vulvovaginal Candidiasis.Clinical infectious diseases : an official publication of the Infectious Diseases Society of America · 2021Trial
- WHO Critical Priority Fungi: A Comprehensive Review of Antifungal Resistance, Emerging Therapeutic Strategies, and the Potential of Antifungal Peptides.International journal of molecular sciences · 2026Review
- New and Investigational Treatment Options for Dermatomycosis in the Era of Antifungal Resistance.Journal of fungi (Basel, Switzerland) · 2026Review
- The Upcoming Antifungal Drugs in Clinical Development for the Treatment of Invasive Candidiasis.Infection and drug resistance · 2026Review
- A Comprehensive Overview ofJournal of fungi (Basel, Switzerland) · 2025Review
- Next-generation antifungal drugs: Mechanisms, efficacy, and clinical prospects.Acta pharmaceutica Sinica. B · 2025Review
- CYP51A1 in health and disease: from sterol metabolism to regulated cell death.Cell death discovery · 2025Review
- Exploring Long Arm Amide-Linked Side Chains in the Design of Antifungal Azole Inhibitors of Sterol 14α-Demethylase (CYP51).Journal of medicinal chemistry · 2025Article
- Overcoming antifungal resistance inFrontiers in cellular and infection microbiology · 2025Review
- Baicalein as a potent antifungal agent againstFrontiers in microbiology · 2025Article
- The evolution of antifungal therapy: Traditional agents, current challenges and future perspectives.Current research in microbial sciences · 2025Review
- Epidemiology, pathogenesis, clinical characteristics, and treatment of mucormycosis: a review.Annals of medicine · 2024Review
- Evaluation of Fifteen 5,6-Dihydrotetrazolo[1,5-Journal of fungi (Basel, Switzerland) · 2024Article
- N-substituted-4-(pyridin-4-ylalkyl)piperazine-1-carboxamides and related compounds as Leishmania CYP51 and CYP5122A1 inhibitors.Bioorganic & medicinal chemistry · 2024Article
- Azole Combinations and Multi-Targeting Drugs That Synergistically InhibitJournal of fungi (Basel, Switzerland) · 2024Review
- Ecotoxicity and Mutagenicity Assessment of Novel Antifungal Agents VT-1161 and T-2307.Molecules (Basel, Switzerland) · 2024Article
- Review
- Chiral Fluorescent Antifungal Azole Probes Detect Resistance, Uptake Dynamics, and Subcellular Distribution inJACS Au · 2024Article
- Mucormycosis during COVID-19 era: A retrospective assessment.Infectious medicine · 2024Review
27 more citing papers are in PubMed but not listed here.
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9 authors at 2 institutions in 2 countries.
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Abstract
The binding and cytochrome P45051 (CYP51) inhibition properties of a novel antifungal compound, VT-1161, against purified recombinant Candida albicans CYP51 (ERG11) and Homo sapiens CYP51 were compared with those of clotrimazole, fluconazole, itraconazole, and voriconazole. VT-1161 produced a type II binding spectrum with Candida albicans CYP51, characteristic of heme iron coordination. The binding affinity of VT-1161 for Candida albicans CYP51 was high (dissociation constant [Kd], ≤ 39 nM) and similar to that of the pharmaceutical azole antifungals (Kd, ≤ 50 nM). In stark contrast, VT-1161 at concentrations up to 86 μM did not perturb the spectrum of recombinant human CYP51, whereas all the pharmaceutical azoles bound to human CYP51. In reconstitution assays, VT-1161 inhibited Candida albicans CYP51 activity in a tight-binding fashion with a potency similar to that of the pharmaceutical azoles but failed to inhibit the human enzyme at the highest concentration tested (50 μM). In addition, VT-1161 (MIC = 0.002 μg ml(-1)) had a more pronounced fungal sterol disruption profile (increased levels of methylated sterols and decreased levels of ergosterol) than the known CYP51 inhibitor voriconazole (MIC = 0.004 μg ml(-1)). Furthermore, VT-1161 weakly inhibited human CYP2C9, CYP2C19, and CYP3A4, suggesting a low drug-drug interaction potential. In summary, VT-1161 potently inhibited Candida albicans CYP51 and culture growth but did not inhibit human CYP51, demonstrating a >2,000-fold selectivity. This degree of potency and selectivity strongly supports the potential utility of VT-1161 in the treatment of Candida infections.
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