Fosmanogepix TFA (APX001 TFA) is an orally active APX001A prodrug and antifungal agent. Fosmanogepix TFA is effective against Cryptococcus neoformans, Fluconazole -resistant C. auris. Fosmanogepix TFA is effective in the treatment of invasive pulmonary aspergillosis and pulmonary murine mucormycosis [1] [2] [3] [4].
In Vivo, Fosmanogepix (390 mg/kg; p.o.; three times daily; 7 days) TFA reduces the fungal burden in a mouse model of cryptococcal meningitis[1]. Fosmanogepix (78-264 mg/kg; p.o.; once or twice daily; 3-7 days) TFA significantly increases the median survival time and 21-day survival rate of immunosuppressed mice with invasive pulmonary aspergillosis (IPA) infection, and reduces the pulmonary fungal burden by up to 7.64 log10 conidial equivalent/g[2]. Fosmanogepix (104-260 mg/kg; i.p.; three/two times daily; 7 days) TFA exerts protective effects against *Candida auris* invasive candidiasis in mouse models[3]. Fosmanogepix (52-104 mg/kg; p.o.; once daily; 7 days) TFA significantly improves the survival rate of neutropenic mice with pulmonary mucormycosis caused by Rhizopus arrhizus var. delemar 99-880[4].
References:
[1]. Shaw KJ, et al. In Vitro and In Vivo Evaluation of APX001A/APX001 and Other Gwt1 Inhibitors against Cryptococcus. Antimicrob Agents Chemother. 2018 Jul 27;62(8):e00523-18.
[2]. Gebremariam T, et al. APX001 Is Effective in the Treatment of Murine Invasive Pulmonary Aspergillosis. Antimicrob Agents Chemother. 2019;63(2):e01713-18. Published 2019 Jan 29.
[3]. Wiederhold NP, et al. Efficacy of Delayed Therapy with Fosmanogepix (APX001) in a Murine Model of Candida auris Invasive Candidiasis. Antimicrob Agents Chemother. 2019;63(11):e01120-19. Published 2019 Oct 22.
[4]. Gebremariam T, et al. Fosmanogepix (APX001) Is Effective in the Treatment of Pulmonary Murine Mucormycosis Due to Rhizopus arrhizus. Antimicrob Agents Chemother. 2020;64(6):e00178-20. Published 2020 May 21.
In Vivo, Fosmanogepix (390 mg/kg; p.o.; three times daily; 7 days) TFA reduces the fungal burden in a mouse model of cryptococcal meningitis[1]. Fosmanogepix (78-264 mg/kg; p.o.; once or twice daily; 3-7 days) TFA significantly increases the median survival time and 21-day survival rate of immunosuppressed mice with invasive pulmonary aspergillosis (IPA) infection, and reduces the pulmonary fungal burden by up to 7.64 log10 conidial equivalent/g[2]. Fosmanogepix (104-260 mg/kg; i.p.; three/two times daily; 7 days) TFA exerts protective effects against *Candida auris* invasive candidiasis in mouse models[3]. Fosmanogepix (52-104 mg/kg; p.o.; once daily; 7 days) TFA significantly improves the survival rate of neutropenic mice with pulmonary mucormycosis caused by Rhizopus arrhizus var. delemar 99-880[4].
References:
[1]. Shaw KJ, et al. In Vitro and In Vivo Evaluation of APX001A/APX001 and Other Gwt1 Inhibitors against Cryptococcus. Antimicrob Agents Chemother. 2018 Jul 27;62(8):e00523-18.
[2]. Gebremariam T, et al. APX001 Is Effective in the Treatment of Murine Invasive Pulmonary Aspergillosis. Antimicrob Agents Chemother. 2019;63(2):e01713-18. Published 2019 Jan 29.
[3]. Wiederhold NP, et al. Efficacy of Delayed Therapy with Fosmanogepix (APX001) in a Murine Model of Candida auris Invasive Candidiasis. Antimicrob Agents Chemother. 2019;63(11):e01120-19. Published 2019 Oct 22.
[4]. Gebremariam T, et al. Fosmanogepix (APX001) Is Effective in the Treatment of Pulmonary Murine Mucormycosis Due to Rhizopus arrhizus. Antimicrob Agents Chemother. 2020;64(6):e00178-20. Published 2020 May 21.