Fosmanogepix TFA 

Fosmanogepix TFA (APX001 TFA) is an orally active APX001A (HY-18233) prodrug and antifungal agent. Fosmanogepix TFA is effective against Cryptococcus neoformans, Fluconazole (HY-B0101)-resistant C. auris. Fosmanogepix TFA is effective in the treatment of invasive pulmonary aspergillosis and pulmonary murine mucormycosis^[1][2][3][4].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

582.42

C₂₄H₂₂F₃N₄O₈P

Solid

N=C1C(C2=CC(CC3=CC=C(C=C3)COC4=NC=CC=C4)=NO2)=CC=CN1COP(O)(O)=O.O=C(O)C(F)(F)F

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]