- |||||||||| Olorofim (orotomide) / F2G
Preclinical, Journal: Olorofim effectively eradicates dermatophytes in vitro and in vivo. (Pubmed Central) - Dec 16, 2021 Following one week of daily topical administration of olorofim, similar to the clotrimazole group, the skin lesions were resolved and normal hair growth patterns appeared. In light of the in vitro and in vivo activity of olorofim against dermatophytes, this novel agent may be considered as a treatment of choice, against dermatophytosis.
- |||||||||| Review, Journal: Advances in anti-fungal therapies. (Pubmed Central) - Oct 28, 2021
These include VT-1161 and VT-1598, modified azoles with a tetrazole metal-binding group; the echinocandin rezafugin; the novel β-1,3-d-glucan synthase inhibitor ibrexafungerp; fosmanogepix, a novel anti-fungal targeting Gwt1; the arylamidine T-2307; the dihydroorotate inhibitor olorofim; and the cyclic hexapeptide ASP2397. The available data including spectrum of activity, toxicity and stage of clinical development will be discussed for each of these so clinicians are aware of promising anti-fungal agents with a strong likelihood of clinical availability in the next 5-7 years.
- |||||||||| rezafungin IV (CD101 IV) / Cidara Therap, Mundipharma
Journal: How urgent is the need for new antifungals? (Pubmed Central) - Oct 2, 2021 They also go on to describe the new antifungal agents that are in the clinical stage of development and how they might be best utilized in patient care in the future.Expert opinion: The antifungal drug development pipeline has responded to a growing need for new agents to effectively treat fungal disease without concomitant toxicity or issues with drug tolerance. Olorofim (F901318), ibrexafungerp (SCY-078), fosmanogepix (APX001), rezafungin (CD101), oteseconazole (VT-1161), encochleated amphotericin B (MAT2203), nikkomycin Z (NikZ) and ATI-2307 are all in the clinical stage of development and offer great promise in offering clinicians better agents to treat these difficult infections.
- |||||||||| Olorofim (orotomide) / F2G
Preclinical, Journal: In vivo efficacy of olorofim against systemic scedosporiosis and lomentosporiosis. (Pubmed Central) - Sep 24, 2021 Furthermore, histopathology of kidneys revealed no or only few lesions with hyphal elements in the olorofim-treated mice, while numerous fungal hyphae were present in control mice. These results indicate olorofim to be a promising therapeutic agent for systemic scedosporiosis/lomentosporiosis, a devastating emerging fungal infection difficult to treat with currently available antifungals.
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Journal: Madurella mycetomatis, the main causative agent of eumycetoma, is highly susceptible to olorofim. (Pubmed Central) - Jun 26, 2021 The potent in vitro activity of olorofim against drug-resistant dermatophytes and opportunistic moulds is promising, warranting evaluation of the clinical utility of olorofim. We demonstrated olorofim has potent in vitro activity against M. mycetomatis and should be further evaluated in vivo as a treatment option for this disease.
- |||||||||| Olorofim (orotomide) / F2G
Journal: Antifungal susceptibility profiles of olorofim (formerly F901318), and currently available systemic antifungals against mold and yeast phases of Talaromyces marneffei. (Pubmed Central) - Jun 22, 2021 In vitro antifungal susceptibility of 32 clinical and environmental Talaromyces marneffei isolates recovered from southern China was performed against olorofim and 7 other systemic antifungals including: amphotericin B, 5-flucytosine, posaconazole, voriconazole, caspofungin and terbinafine using the CLSI methodology. In comparison, olorofim was the most active antifungal agent against both mold and yeast phases of all tested Talaromyces marneffei isolates, exhibiting an MIC range, MIC, and MIC of 0.0005-0.002 μg/ml, 0.0005 μg/ml, and 0.0005 μg/ml, respectively.
- |||||||||| Olorofim (orotomide) / F2G, ibrexafungerp (SCY-078) / Scynexis, fosmanogepix (APX001) / Amplyx Pharma
Review, Journal: Investigational Agents for the Treatment of Resistant Yeasts and Molds. (Pubmed Central) - Jun 3, 2021 Ibrexafungerp, olorofim, oteseconazole, and fosmanogepix possess novel mechanisms of actions with potent activity against MDR fungi. Successful clinical development is neither easy nor guaranteed; thus, perpetual efforts to discover new antifungals are needed.
- |||||||||| Olorofim (orotomide) / F2G
[VIRTUAL] Tissue distribution of (14C)-olorofim following intravenous dosing in the rat () - May 20, 2021 - Abstract #ECCMID2021ECCMID_3454; Importantly, the tissue distribution data show that drug-related material penetrates the blood brain barrier and thus may have the potential to treat serious CNS fungal infections in man . Similarly, brain penetration has been previously observed in the mouse, where LC-MS assay results have shown mean olorofim brain:plasma ratios of approximately 1:1 after oral dosing and 1:6 after IV dosing.
- |||||||||| Olorofim (orotomide) / F2G, arylamidine (T-2307) / Fujifilm Holdings, fosmanogepix (APX001) / Amplyx Pharma
Journal: Innovative therapies for invasive fungal infections in preclinical and clinical development. (Pubmed Central) - Feb 3, 2021 It is imperative to expand the pipeline of antifungals to tackle emerging fungal resistance against conventional antimycotic drugs, toxicity and drug-drug interactions. This unmet medical need should not be underappreciated.
- |||||||||| Olorofim (orotomide) / F2G
Trial completion, Trial completion date, Trial primary completion date: A Biopharmaceutics Study to Assess the Pharmacokinetics of Single Oral and IV Doses of Olorofim (clinicaltrials.gov) - Jan 7, 2021 P1, N=24, Completed, While overall mortality was high, combination antifungal treatment, and in particular combination therapy with voriconazole plus terbinafine may be associated with improved treatment outcomes compared with other antifungal regimens for the treatment of invasive L. prolificans infections. Recruiting --> Completed | Trial completion date: Dec 2023 --> Sep 2020 | Trial primary completion date: Jan 2023 --> Sep 2020
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