Universität zu Köln

Hoenigl, Martin ORCID: 0000-0002-1653-2824, Sprute, Rosanne ORCID: 0000-0003-2457-6437, Egger, Matthias ORCID: 0000-0002-7795-4406, Arastehfar, Amir ORCID: 0000-0002-4361-4841, Cornely, Oliver A., Krause, Robert, Lass-Florl, Cornelia ORCID: 0000-0002-2946-7785, Prattes, Juergen, Spec, Andrej, Thompson, George R., III, Wiederhold, Nathan and Jenks, Jeffrey D. (2021). The Antifungal Pipeline: Fosmanogepix, Ibrexafungerp, Olorofim, Opelconazole, and Rezafungin. Drugs, 81 (15). S. 1703 - 1730. NORTHCOTE: ADIS INT LTD. ISSN 1179-1950

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Abstract

The epidemiology of invasive fungal infections is changing, with new populations at risk and the emergence of resistance caused by the selective pressure from increased usage of antifungal agents in prophylaxis, empiric therapy, and agriculture. Limited antifungal therapeutic options are further challenged by drug-drug interactions, toxicity, and constraints in administration routes. Despite the need for more antifungal drug options, no new classes of antifungal drugs have become available over the last 2 decades, and only one single new agent from a known antifungal class has been approved in the last decade. Nevertheless, there is hope on the horizon, with a number of new antifungal classes in late-stage clinical development. In this review, we describe the mechanisms of drug resistance employed by fungi and extensively discuss the most promising drugs in development, including fosmanogepix (a novel Gwt1 enzyme inhibitor), ibrexafungerp (a first-in-class triterpenoid), olorofim (a novel dihyroorotate dehydrogenase enzyme inhibitor), opelconazole (a novel triazole optimized for inhalation), and rezafungin (an echinocandin designed to be dosed once weekly). We focus on the mechanism of action and pharmacokinetics, as well as the spectrum of activity and stages of clinical development. We also highlight the potential future role of these drugs and unmet needs.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Hoenigl, Martin UNSPECIFIED orcid.org/0000-0002-1653-2824 UNSPECIFIED Sprute, Rosanne UNSPECIFIED orcid.org/0000-0003-2457-6437 UNSPECIFIED Egger, Matthias UNSPECIFIED orcid.org/0000-0002-7795-4406 UNSPECIFIED Arastehfar, Amir UNSPECIFIED orcid.org/0000-0002-4361-4841 UNSPECIFIED Cornely, Oliver A. UNSPECIFIED UNSPECIFIED UNSPECIFIED Krause, Robert UNSPECIFIED UNSPECIFIED UNSPECIFIED Lass-Florl, Cornelia UNSPECIFIED orcid.org/0000-0002-2946-7785 UNSPECIFIED Prattes, Juergen UNSPECIFIED UNSPECIFIED UNSPECIFIED Spec, Andrej UNSPECIFIED UNSPECIFIED UNSPECIFIED Thompson, George R., III UNSPECIFIED UNSPECIFIED UNSPECIFIED Wiederhold, Nathan UNSPECIFIED UNSPECIFIED UNSPECIFIED Jenks, Jeffrey D. UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-600358
DOI:	10.1007/s40265-021-01611-0
Journal or Publication Title:	Drugs
Volume:	81
Number:	15
Page Range:	S. 1703 - 1730
Date:	2021
Publisher:	ADIS INT LTD
Place of Publication:	NORTHCOTE
ISSN:	1179-1950
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language IN-VITRO ACTIVITY; BROAD-SPECTRUM ANTIFUNGAL; VULVO-VAGINAL CANDIDIASIS; INVASIVE FUNGAL-INFECTIONS; LONG-ACTING ECHINOCANDIN; CRYPTOCOCCUS-NEOFORMANS; FILAMENTOUS FUNGI; ASPERGILLUS SPP.; FLUCONAZOLE RESISTANCE; ORAL IBREXAFUNGERP Multiple languages Pharmacology & Pharmacy; Toxicology Multiple languages
URI:	http://kups.ub.uni-koeln.de/id/eprint/60035