Verseon Reveals Preclinical Data on Novel Drug Candidates to Treat Diabetic Macular Edema
June 26 2017 - 9:08AM
Business Wire
- Candidates show good pharmacokinetic
properties for topical ophthalmic dosing.
- In preclinical testing, the candidates
demonstrated reduced leakage into the retina and shorter mean
circulation times – suggesting a slowing of the disease
progression.
- Some of the candidates may be suitable
for oral dosing.
Verseon presented preclinical data on multiple novel drug
candidates for the treatment of diabetic macular edema (DME) at the
2017 BIO International Conference in San
Diego, last week. Diabetic macular edema is the leading
cause of blindness in the diabetic population according to the
National Institutes of Health.1
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Left to right: normal vision; blurred
vision due to DME; floating spots (hemorrhages) due to advanced
diabetic retinopathy. Photos courtesy of the National Eye
Institute, National Institutes of Health. (Photo: Business
Wire)
Verseon is developing plasma kallikrein inhibitors that target a
validated disease pathway2 and treat an underlying cause of DME.
The current standard of care comprises monthly injections into the
eye and laser treatments, which are associated with side effects
such as inflammation, infections, and cataracts.3 To avoid these
unwanted effects, Verseon is designing its inhibitors for eye-drop
or oral delivery.
Studies estimate that one in three people living with diabetes
for more than 20 years may develop DME.4 Chronically high blood
sugar associated with diabetes can weaken the blood vessels in the
eye, leading to fluid leaking into the retina (edema). Over time,
fluid may accumulate in the macula, the central region of the
retina (see illustration), resulting in swelling, blurred vision,
and eventually central vision loss (see photos).i If current trends
continue, researchers estimate that about one in three US adults
could be suffering from diabetes by 2050,5 leading to a sharp
increase in the number of people affected by DME.
Recent research suggests that the serine protease plasma
kallikrein may be a promising new target for the treatment of
DME.ii The level and activity of plasma kallikrein are both known
to be upregulated in the eyes of DME patients. This results in the
activation of inflammatory pathways and vasodilation in the retina,
leading to edema. By inhibiting plasma kallikrein, Verseon’s drug
candidates target the direct cause of downstream inflammation
caused by this hyperactivity and can potentially lower leakage into
the retina.
“We are designing several series of compounds in parallel,
covering both topical and oral delivery,” said Dr. David Kita,
Verseon’s Vice President of R&D, who presented preclinical data
on the Company’s drug candidates at the recent BIO 2017 conference.
“This includes preclinical experiments to test whether our drugs
reach the back of the eye when applied as eye drops.”
“At BIO, we presented pharmacokinetic data for two series of
compounds, which reach good exposure in the relevant tissues of the
eye when administered topically,” he said. “In addition, some other
drug candidates show high oral bioavailability, indicating that
they may be suitable for oral dosing.”
Dr. Kita also presented an in-vivo efficacy study with systemic
dosing. In this experiment, Verseon’s compounds demonstrated
reduced leakage into the retina and shorter mean circulation times,
both of which suggest a slowing of the disease progression.
The series of kallikrein inhibitors presented at the BIO
conference are novel chemical entities discovered and developed by
Verseon’s scientists using the Company’s platform. DME is Verseon’s
second therapeutic area, following their anticoagulation program,
which has produced multiple novel direct thrombin inhibitors with
low bleeding risk.
About Verseon
Verseon (AIM: VSN) employs its proprietary, computational drug
discovery platform to develop novel therapeutics that are unlikely
to be found using conventional methods. The company has three drug
programs in anticoagulation, diabetic macular edema, and
oncology._______________________________1 “Managing diabetic
macular edema”
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3158878/2 Bhat, M.,
Pouliot, M., Couture, R., and Vaucher, E. (2014) The
Kallikrein-Kinin System in Diabetic Retinopathy. Prog. Drug Res.
pp. 111–143.3 Facts about diabetic macular oedema – Moorfields Eye
Hospital
http://www.moorfields.nhs.uk/sites/default/files/diabetic-macular-oedema.pdf4
Klein, R., et al. The Wisconsin Epidemiologic Study of Diabetic
Retinopathy. Ophthalmology, Volume 91, Issue 12, 1464 - 14745
Boyle, J. P., Thompson, T. J., Gregg, E. W., Barker, L. E., &
Williamson, D. F. (2010). Projection of the year 2050 burden of
diabetes in the US adult population: dynamic modeling of incidence,
mortality, and prediabetes prevalence. Population Health
Metrics, 8, 29. http://doi.org/10.1186/1478-7954-8-29
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Vane Percy & RobertsSimon Vane
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