[CAS NO. 441785-25-7] Besifovir
PRODUCTS SPECIFICATIONS [441785-25-7]
DESCRIPTION [441785-25-7]
Overview
| MDL | MFCD09834071 |
|---|---|
| Molecular Weight | 299.22 |
| Molecular Formula | C10H14N5O4P |
| SMILES | NC1=NC=C2N=CN(CC3(OCP(O)(O)=O)CC3)C2=N1 |
Summary
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 T max s 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 t 1/2 ranged from 2.5 to 3.3 h [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01937806 | IlDong Pharmaceutical Co Ltd |
Chronic Hepatitis B
|
October 2013 | Phase 3 |
| NCT02792088 | IlDong Pharmaceutical Co Ltd |
Chronic Hepatitis B
|
July 2015 | Phase 3 |
| NCT03604016 | IlDong Pharmaceutical Co Ltd |
Hepatitis B
|
September 23, 2018 | Phase 4 |
| NCT04249908 | IlDong Pharmaceutical Co Ltd |
Renal Impairment
|
February 13, 2020 | Phase 1 |
| NCT04202536 | IlDong Pharmaceutical Co Ltd |
Hepatitis B|Besifovir Dipivoxil Maleate|Tenofovir Disoproxil Fumarate
|
May 29, 2019 | Phase 4 |
| NCT03885778 | IlDong Pharmaceutical Co Ltd |
Food Effect|Health Subjects
|
January 13, 2019 | Phase 4 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 835.51 mM ; Need ultrasonic)
H 2 O : ≥ 100 mg/mL ( 334.20 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.3420 mL | 16.7101 mL | 33.4202 mL |
| 5 mM | 0.6684 mL | 3.3420 mL | 6.6840 mL |
| 10 mM | 0.3342 mL | 1.6710 mL | 3.3420 mL |
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.
- [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.
- [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.
Synonyms