| Description | Fosaprepitant dimeglumine (MK-0517) is the dimeglumine salt form of fosaprepitant, the water-soluble, N-phosphorylated prodrug of aprepitant, with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent binds selectively to the human substance P/neurokinin 1 (NK1) receptors in the central nervous system (CNS). This inhibits receptor binding of the endogenous substance P and prevents substance P-induced emesis. |
| In vitro | Fosaprepitant (MK-0517，L-758,298) 可作为 aprepitant 的磷酸酯前药。Aprepitant 是一种选择性物质P（NK-1受体）拮抗剂，用于与皮质类固醇和5-HT 3受体拮抗剂组合治疗，预防急性及延迟的化疗引起的恶心和呕吐。[1] |
| In vivo | Fosaprepitant通过静脉注射后，由于广泛存在的磷酸酶的作用，在30分钟内转化为aprepitant。Fosaprepitant在150 mg（1 mg/ml）剂量下具有良好的耐受性，而Fosaprepitant 115 mg在其AUC上与aprepitant 125 mg生物等效。Fosaprepitant 115 mg已作为3天口服aprepitant方案第1天的替代方案提交FDA审批，其中第2天和第3天采用口服aprepitant。[1] |
| Synonyms | 福沙匹坦二甲葡胺, L785298, 福沙吡坦二甲葡胺, MK-0517, Fosaprepitant dimeglumine salt |
| molecular weight | 1004.83 |
| Molecular formula | C37H56F7N6O16P |
| CAS | 265121-04-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 185 mg/mL (184.1 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: 124 mg/mL (123.4 mM) |
| References | 1. Navari RM. Expert Opin Investig Drugs, 2007, 16(12), 1977-1985. |