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Albaconazole
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Christina C. Chang, Monica A. Slavin
Albaconazole is undergoing clinical development. A phase II, single-blind, dose-finding trial (NCT00199264) comparing five doses of albaconazole (10, 40, 80, 160, and 320 mg) versus fluconazole for the treatment of acute, nonrecurrent candidal vulvovaginitis in 64 women has been completed. This suggested that a single dose of albaconazole 40 mg was more efficacious than fluconazole (Bartroli and Uriach, 2005). A phase Ib trial using albaconazole for the treatment of moccasin-type tinea pedis is currently underway (NCT00509275) (Steifel Laboratories, 2008). There are no current phase III studies.
Oral antifungal therapies for toenail onychomycosis: a systematic review with network meta-analysis toenail mycosis: network meta-analysis
Published in Journal of Dermatological Treatment, 2022
Maria L. D. Fávero, Aline F. Bonetti, Eric L. Domingos, Fernanda S. Tonin, Roberto Pontarolo
The second-generation azoles have broad-spectrum antifungal activity, both for superficial and invasive infections, acting as reversible inhibitors of the sterol enzyme of P450 cytochrome (67). Albaconazole has good pharmacokinetic and bioavailability properties with a long half-life that allows for weekly dosing schedules (15,68). This has the potential to improve patient compliance to treatment, particularly with long courses therapies. The effects of albaconazole are dose-dependent, as demonstrated in our network meta-analysis, where higher cure rates were obtained with higher doses of albaconazole. Concerning safety, we found that albaconazole was more prone to causing gastrointestinal events, such as nausea and diarrhea. However, it seems that this drug is well-tolerated, with treatment-related adverse events occurring in less than 3% of patients, all with mild-moderated severity (15). Posaconazole at 200 and 400 mg is significantly associated with complete cure in long-term treatments (over 48 weeks) when compared to terbinafine (35); however, higher doses were more related to discontinuation due adverse events, which may prevent its broad use in practice.
Synthesis of novel pyrroles and fused pyrroles as antifungal and antibacterial agents
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Rania Helmy Abd El-Hameed, Amira Ibrahim Sayed, Shima Mahmoud Ali, Mohamed A. Mosa, Zainab M. Khoder, Samar Said Fatahala
Another major cause of OIs and the consequent fatality is the fungal pathogens. The most common opportunistic fungi include Candida species, Aspergillus species, and Fusarium species5. Candida species, was a major cause of morbidity and mortality worldwide over the past few decades6. Aspergillus fumigatus (A. fumigatus) is a saprophyte that has become the most prevalent airborne fungal pathogen7. A. fumigatus causes severe and usually fatal invasive aspergillosis in immuno-compromised hosts in developed countries7. The members of Fusarium oxysporum (F. oxysporum) complex, (FOSC) are soil borne pathogens that cause diseases to a broad range of important crops with a number of them having the ability to cause human diseases that can be fatal8. Because fungi are eukaryotes, they have similarities with mammalian cells making it difficult to design a drug with selective toxicity9. The first antifungal drug discovered was amphotericin B10 followed by flucytosine11, later on two imidazole derivatives, clotrimazole and miconazole, were extensively used in treatment of fungal infections12–15. Triazole derivative, fluconazole, is an antifungal agent with low toxicity and high antifungal activity16. Resistance of some fungi against imidazole is now becoming a serious clinical problem17, several azole-related adverse drug effects (ADEs) are now considered such as hepatotoxicity and cardiac effects. In order to enrich the antifungal activity and/or diminish antifungal ADEs, new derivatives were synthesised containing other heterocycles instead of imidazole and 1,2,4-triazole, such as indole, 1,2,3-triazoles14,18–20. Voriconazole is a clinically important triazoles antifungal containing fluoropyrimidine13,20. Using quinazoline ring instead of a triazole ring results in albaconazole with higher in vitro activity than fluconazole21. Itraconazole with piperazinyl phenyl side chain showed remarkable in vitro antifungal activity against several pathogenic fungi16, as shown in Figure 1.