Toca FC is an orally administered prodrug, 5-fluorocytosine
(5-FC), which is converted into an anti-cancer drug, 5-fluorouracil (5-FU), when it encounters CD.
Toca FC is an orally administered, extended-release formulation of the prodrug, 5-fluorocytosine
Transfected cytosine deaminase into AT-MSCs in combination with 5-fluorocytosine
can significantly enhance cytotoxicity on target CT-29 tumor cells in vitro.
coli cytosine deaminase (CD), which converts the prodrug 5-fluorocytosine
(5FC) into the active chemotherapeutic agent 5-fluorouracil (5-FU).
In another study, 5-Fluorocytosine
has been introduced as a prodrug.
Drug susceptibility was assessed using FUNGITEST[R] (Sanofi Diagnostics Pasteur) for the analysis of the growth of yeast-like fungi in the presence of six drugs: 5-fluorocytosine
, amphotericin B, miconazole, ketoconazole, itraconazole, and fluconazole used at two concentrations, in modified RPMI 1640 medium, in the presence of a redox indicator.
The genetic basis of resistance to 5-fluorocytosine
in Candida species and Cryptococcus neoformans.
Kim et al., "Dihydropyrimidine dehydrogenase is a prognostic marker for mesenchymal stem cell-mediated cytosine deaminase gene and 5-fluorocytosine
prodrug therapy for the treatment of recurrent gliomas," Theranostics, vol.
Spectral Buffer Signal, width Compound pH ppm SW, ppm Fluphenazine dihydrochloride 1.90 -62 95 Fluoxetine HCl 1.90 -61 95 Fludarabine phosphate 1.90 -52 105 Flurazepam monohydrochloride 1.90 -111 121 -113 5-Fluorocytosine
1.90 -169 175 Fluconazole 1.90 -108 117 -110 Sodium flurbiprofen dihydrate 9.0 -119 125 Transmitter frequency Compound offset O1, ppm Fluphenazine dihydrochloride -68 Fluoxetine HCl -68 Fludarabine phosphate -63 Flurazepam monohydrochloride -95 5-Fluorocytosine
-123 Fluconazole -93 Sodium flurbiprofen dihydrate -98 Table 3: Analytical results for DMSO-[d.sub.6] soluble fluorinated pharmaceuticals.
According to the mechanism of action, there are six classes of antifungal agents: fungal ergosterol synthesis inhibitors (azoles: ketoconazole, fluconazole, and voriconazole), glucan synthesis inhibitors (echinocandins and caspofungin), ergosterol disruptors (polyenes antibiotics: amphotericin B), squalene epoxidase inhibitors (terbinafine and naftifine), chitin synthesis inhibitors (nikkomycin), and nucleic acid synthesis inhibitors (5-fluorocytosine
) (Figure 1) .
Reports have seen success with older antifungal agents including Amphotericin B, Ketoconazole, Miconazole, nystatin, 5-fluorocytosine
, and fluconazole [3, 10, 11].
albicans MCZ 0.064 syn J5 MCZ 0.01 syn 901 MCZ 0.064 syn 103 KCZ 0.066 syn J5 KCZ 0.012 syn 901 KCZ 0.066 syn 103 ICZ 0.063 syn J5 ICZ 0.012 syn 901 ICZ 0.064 syn 103 5-FLU 1.062 indiff J5 5-FLU 0.625 indiff 901 5-FLU 1.062 indiff 103 AMB 1.125 indiff J5 AMB 0.75 indiff 901 AMB 0.75 indiff 103 (a) KCZ, ketoconazole; ICZ, itraconazole; MCZ, miconazole; 5-Fc, 5-fluorocytosine
; AMB, amphotericin B; FRC, Flos Rosae Chinensis; FIC index, fractional inhibitory concentration index; syn, synergism; indiff, indifference.