| Identification | Back Directory | [Name]
Vipadenant | [CAS]
442908-10-3 | [Synonyms]
V 2006
BIIB 014
CEB 4520
VER 11135
Vipadenant
VER-ADO 49
VER-A 00049
VER-A 00-11
Vipadenant(BIIB 014)
5-BROMO-4-(METHYLSULFANYL)-1H-PYRROLO[2,3-B]PYRIDINE
3-[(4-Amino-3-methylphenyl)methyl]-7-(2-furanyl)-3H-1,2,3-triazolo[4,5-d]pyrimidin-5-amine | [Molecular Formula]
C16H15N7O | [MDL Number]
MFCD12024697 | [MOL File]
442908-10-3.mol | [Molecular Weight]
321.34 |
| Chemical Properties | Back Directory | [Melting point ]
245.3-246.1 °C | [Boiling point ]
668.5±65.0 °C(Predicted) | [density ]
1.56±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:37.0(Max Conc. mg/mL);115.14(Max Conc. mM) | [form ]
A crystalline solid | [pka]
4.27±0.30(Predicted) | [color ]
Light yellow to yellow |
| Questions And Answer | Back Directory | [Description]
Vipadenant (also known as BIIB014) is a potent, selective oral adenosine A2A receptor antagonist under development for the treatment of Parkinson’s disease. It has successfully completed phase I clinical studies. It might also be a potential adjunctive therapy reagent for cancer treatment. It was found that it has certain potentials to disrupt an immunosuppressive mechanism of tumour protection, generating improved efficacy for immunotherapies of certain cancers when used in combination with other drugs.
| [References]
http://www.medkoo.com/products/8047
Shook, B. C., and P. F. Jackson. "Adenosine A(2A) Receptor Antagonists and Parkinson's Disease. " Acs Chemical Neuroscience2.10(2011):555-67.
Brooks, D. J., et al. "An open-label, positron emission tomography study to assess adenosine A2A brain receptor occupancy of vipadenant (BIIB014) at steady-state levels in healthy male volunteers." Clinical Neuropharmacology 33.2(2010):55.
http://www.vernalis.com/nce-pipeline/oncology/v2006
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| Hazard Information | Back Directory | [Uses]
Vipadenant is a potent, selective and orally available adenosine A2A receptor antagonist under development for for Parkinson''s disease. Vipadenant demonstrates strong oral activity in commonly used models of Parkinson''s disease. Vipadenant has shown excellent preclinical pharmacokinetics and has successfully completed phase I clinical studies. | [in vivo]
Vipadenant (0.3-30 mg/kg) produces a dose-dependent reduction in catalepsy. Vipadenant (10 mg/kg) does not produce any statistically significant dyskinetic episodes in 6-OHDA-lesioned rats during a 19-day dosing regimen[1]. In the mouse and rat haloperidol-induced hypolocomotion models, vipadenant has a minimum effective dose of 0.1 and 1 mg/kg, respectively. Vipadenant (3 and 10 mg/kg, p.o.) is able to increase contralateral rotations in 6-OHDA lesioned rats[2]. |
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