Bevasiranib
Bevasiranib is a siRNA that targets and silences VEGF-A. Bevasiranib activates the RNA-induced silencing complex to degrade VEGF-A mRNA, mediates TLR3-related inhibition of choroidal neovascularization, and triggers RNA interference-mediated gene silencing through endogenous eukaryotic RNAi mechanisms. After intravitreal injection, Bevasiranib distributes to various ocular tissues and resists degradation by intraocular nucleases, reducing choroidal neovascularization area and alleviating vascular leakage. Bevasiranib can be used in research related to macular degeneration.
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- No. CAS: 959961-96-7
- Peso molecular:13345.07
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Almacenamiento:
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Actividad biológica
Descripciòn
In Vivo
Bevasiranib (70-350 µg; intravitreal injection; 3 doses) reduces CNV area by more than 50% in a dose-dependent manner and alleviates vascular leakage in a laser-induced CNV monkey model[1].
Bevasiranib (0.5-2 mg; intravitreal injection; single dose) achieves extensive ocular distribution in rabbits and results in substantial accumulation of the intact compound in the retinal pigment epithelium-Bruch's membrane complex[1].
Bevasiranib (0.5-2.0 mg/eye; intravitreal administration; single bolus dose) achieves broad ocular distribution and substantial and sustained uptake in the retina in Dutch Belted rabbits[2].
Bevasiranib (2 mg/eye; intravitreal; single bolus dose) delivers intact siRNA to multiple ocular tissues, including the retina and RPE, in male Dutch Belted rabbits, with RPE levels ranging from 423 ng to 2696 ng per eye[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cynomolgus monkeys (laser photocoagulation-induced CNV model)[1]
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Dosage:70 µg; 150 µg; 350 µg
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Administration:intravitreal injection; three doses
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Result:Significantly inhibited the growth of the neovascular area compared to control animals for all three doses.
Reduced CNV area by greater than 50% relative to the control group.
Reduced vascular leakage as determined by fluorescein angiograms significantly in a dose-dependent manner.
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Animal Model:Dutch-Belted rabbits (both male and female; approximately 5 months of age; body weight 1.9-2.9 kg)[2]
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Dosage:0.5, 2.0 mg/eye
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Administration:intravitreal; single bolus dose; 50 µl/eye, both eyes treated
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Result:Achieved broad ocular distribution in Dutch Belted rabbits, with substantial and sustained uptake in the retina, reaching retinal drug concentrations of 370 µg-eq/g (0.5 mg/eye dose) and 683 µg-eq/g (2.0 mg/eye dose) in male rabbits, with vitreous elimination T1/2 of 30 h and 52 h, respectively.
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Animal Model:Dutch-Belted rabbits (male; body weight 2.0-2.4 kg)[2]
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Dosage:2 mg/eye
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Administration:intravitreal; single bolus dose; 50 µl/eye, 5 eyes treated across 3 animals
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Result:Detected intact Bevasiranib in aqueous fluid, vitreous fluid, iris, ciliary body, RPE, choroid and retina at 24 h after intravitreal injection; showed the highest substance levels in vitreous fluid which exceeded upper limit of quantification in 4 out of 5 tested eyes, and intact compound was absent in lens tissue for 4 out of 5 eyes. Measured low absolute mass and low percentage of administered dose for intact Bevasiranib in RPE, iris, aqueous fluid, retina and choroid tissue samples.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 959961-96-7
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Peso molecular 13345.07
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SMILES
[Bevasiranib]
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Garba AO, et al. Bevasiranib for the treatment of wet, age-related macular degeneration. Ophthalmology and eye diseases. 2010;2:75-83. [Content Brief]
[2]. Dejneka NS, et al. Ocular biodistribution of bevasiranib following a single intravitreal injection to rabbit eyes. Molecular vision. 2008 May 28;14:997-1005. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Bevasiranib Related Classifications
HY-153484 Related Classifications
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