| Identification | Back Directory | [Name]
PHOSPHONIC ACID, [[[1-[(2-AMINO-9H-PURIN-9-YL)METHYL]CYCLOPROPYL]OXY]METHYL]- (9CI) | [CAS]
441785-25-7 | [Synonyms]
Besifovir
Besifovir(b)
Besifovir (LB8033)
[1-[(2-aminopurin-9-yl)methyl]cyclopropyl]oxymethylphosphonic acid
[1-[(2-amino-9-purinyl)methyl]cyclopropyl]oxymethylphosphonic acid
(1-((2-Amino-9H-purin-9-yl)methyl)cyclopropoxy)methylphosphonic acid
[[[1-[(2-Amino-9H-purin-9-yl)methyl]cyclopropyl]oxy]methyl]phosphonic acid
PHOSPHONIC ACID, [[[1-[(2-AMINO-9H-PURIN-9-YL)METHYL]CYCLOPROPYL]OXY]METHYL]-
P-[[[1-[(2-amino-9H-purin-9-yl)methyl]cyclopropyl]oxy]methyl]-Phosphonic acid
Phosphonic acid, P-[[[1-[(2-amino-9H-purin-9-yl)methyl]cyclopropyl]oxy]methyl]-
PHOSPHONIC ACID, [[[1-[(2-AMINO-9H-PURIN-9-YL)METHYL]CYCLOPROPYL]OXY]METHYL]- (9CI) | [Molecular Formula]
C10H14N5O4P | [MDL Number]
MFCD09834071 | [MOL File]
441785-25-7.mol | [Molecular Weight]
299.22 |
| Chemical Properties | Back Directory | [Boiling point ]
668.4±65.0 °C(Predicted) | [density ]
1.94±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 250 mg/mL (835.51 mM) | [form ]
Solid | [pka]
2.44±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Besifovir (LB80331), a parent agent converted by LB80380 (HY-19447A), further metabolizes to its active form, LB80317 (HY-106235). Besifovir is an orally active, novel antiviral agent against hepatitis B virus (HBV)[1][2]. | [in vivo]
The prodrug, LB80380, is rapidly absorbed after oral administration (30, 60, 120, 240 mg) and is converted to its parent drug, Besifovir (LB80331) (LB80380 was not detected in plasma). The median Tmaxs of LB80331 ranged from 1.0 to 2.0 h postdosing. Thereafter, the plasma LB80331 concentration declined in a monoexponential manner, and the mean values of t1/2 ranged from 2.5 to 3.3 h[2]. | [References]
[1] Jung JA, et al. Pharmacokinetic comparison of the maleate and free base formulations of LB80380, a novel nucleotide analog, in healthy male volunteers. Int J Clin Pharmacol Ther. 2012 Sep;50(9):657-64. DOI:10.5414/cp201716
[2] Yuen MF, et al. A randomized placebo-controlled, dose-finding study of oral LB80380 in HBeAg-positive patients with chronic hepatitis B. Antivir Ther. 2006;11(8):977-83. PMID:17302367
[3] Lung-Yi Mak, et al. Pharmacokinetic evaluation of besifovir for the treatment of HBV infection. Expert Opin Drug Metab Toxicol. 2018 Jan;14(1):101-106. DOI:10.1080/17425255.2018.1417983 |
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T&W GROUP
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Bide Pharmatech Ltd.
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