2016
1
Targeted (biological) therapy
in ophthalmology
Department of Pharmacology, Faculty of Medicine, Masaryk University in Brno
Indications:
• neovascular (Wet) Age-Related Macular Degeneration (AMD)
• macular edema following Retinal Vein Occlusion (RVO)
• diabetic macular edema (DME) and diabetic retinopathy
• neovascular glaucoma
Pathogenesis:
- dysregulated neovascularisation -> irreversible damage (blindness)
- newly formed blood vessels formed from retinal blood vessels cause
ocular vitreous hemorrhage -> conversion to retinal detachment
The use of targeted/biological
therapy in ophthalmology
2016
2
(pegaptanib, vertepofin )
The use of targeted/biological
therapy in ophthalmology
2016
3
• pegaptanib - synthetic oligonucleotide
• inactivation of the extracellular vascular endothelial growth
factor (VEGF165), specific binding
• VEGF165 is responsible for angiogenesis, increased vascular permeability
and other inflammatory changes that play a role in the wet form of AMD
• I: therapy of the wet form of AMD
• CI: eye infection, allergy
• intravitreal drug administration: 0,3 mg pegaptanib (i.e. 90
microliters) (9x per year)
• aseptic conditions, with a local anaesthetic and an ATB
The use of targeted/biological
therapy in ophthalmology
The use of targeted/biological
therapy in ophthalmology
• verteporfin - synthetic benzoporphyrin derivative
• photosensitizer for photodynamic therapy to eliminate abnormal
blood vessels in the eye (blockage and local damage to the
endothelium)
• accumulation in the abnormal blood vessels
• production of highly reactive oxygen radicals when stimulated by
nonthermal red light (wavelength of 689nm) in the presence of
oxygen
• I: therapy of the wet form of macular degeneration (AMD)
– also for the therapy of secondary subfoveolar chorioidal
neovascularisation in pathologic myopia
• aflibercept - recombinant fusion protein composed of the
extracellular domen of the human (vascular endothelial growth factor)
VEGF receptor 1+ 2 fusioned with the Fc fragment of the human Ig G1
• as a false soluble "decoy“ receptor it binds to the VEGF-A and PlGF
(placental growth factor) with high affinity, thus it blocks the angiogenic
effect of the VEGR
• I: intravitreal administration in the wet form of AMD in adults
– also for the therapy of diabetic macular edema (DME)
– vision impairment caused by the chorioidal neovascularisation in
pathologic myopia
– vision impairment caused by the macular edeme after retinal vein
oclusion
• CI: allergy, eye infections
The use of targeted/biological
therapy in ophthalmology