ALS-8176
ALS-8176 Basic information
- Product Name:
- ALS-8176
- Synonyms:
-
- ALS-8176
- 4'-chloromethyl-2'-deoxy-3',5'-di-O-isobutyryl-2'-fluorocytidine
- ALS-008176
- Lumicitabine
- 4-Amino-1-{5-chloro-2,5-dideoxy-2-fluoro-3-O-isobutyryl-4-[(isobutyryloxy)methyl]-a-L-lyxofuranosyl}-2(1H)-pyrimidinone
- LUMICITABINE;ALS8176;ALS 8176
- ALS-8176 (Lumicitabine
- Lumicitabine (ALS-8176)
- CAS:
- 1445385-02-3
- MF:
- C18H25ClFN3O6
- MW:
- 433.86
- Mol File:
- 1445385-02-3.mol
ALS-8176 Chemical Properties
- Boiling point:
- 533.5±60.0 °C(Predicted)
- Density
- 1.43±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 50 mg/mL (115.24 mM)
- form
- Solid
- pka
- 4.26±0.10(Predicted)
- color
- White to off-white
ALS-8176 Usage And Synthesis
Uses
Lumicitabine (ALS-008176) is an inhibitor of the respiratory syncytial virus (RSV) polymerase.
in vivo
Lumicitabine demonstrates excellent anti-RSV efficacy and safety in a phase 2 clinical RSV challenge study. It exhibits good oral bioavailability and a high level of 2c-TP in vivo. Lumicitabine has excellent stability profiles in formulations (>24 h storage stability in 0.5% methylcellulose aqueous formulation at rt) and simulats gastric and intestinal fluids (half-life >2 h). Its solubility is adequate to support oral administration in solutions with relatively low percentage of organic solvent and in aqueous suspensions. High levels of NMP and NTP are obtained following oral administration of Lumicitabine to monkeys[2]. In an adult human challenge study, Lumicitabine has shown efficacy against RSV infection[1].
References
[1] DeVincenzo JP, et al. Activity of Oral ALS-008176 in a Respiratory Syncytial Virus Challenge Study. N Engl J Med. 2015 Nov 19;373(21):2048-58. DOI:10.1056/NEJMoa1413275
[2] Wang G, et al. Discovery of 4'-chloromethyl-2'-deoxy-3',5'-di-O-isobutyryl-2'-fluorocytidine (ALS-8176), a first-in-class RSV polymerase inhibitor for treatment of human respiratory syncytial virus infection. J Med Chem. 2015 Feb 26;58(4):1862-78. DOI:10.1021/jm5017279
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