Glaucoma is a sight-threatening disease caused by elevated intraocular pressure. Over time, this elevated pressure leads to degeneration of cells of the optic nerve, slowly worsening vision. Near by 2.3 million Americans age 40 and older have been diagnosed with the disease. With over 30 million glaucoma prescriptions in 2013. According to the World Health Organization, it is the second leading cause of blindness worldwide. It is a chronic condition tat cannot be prevented or reversed, and therefore requires life-long monitoring.
Prostaglandin analog ophthalmic drops lower intraocular pressure, managing the progression of the disease. However, since glaucoma affects a primarily elderly population, many of those afflicted with the disease have difficulty complying with the required dosing regimen or being able to self-administer eye drops. In fact, it has been reported that <50% of glaucoma patients at 6 months administer ophthalmic drops as directed. Poor adherence to prescription regimens is of great concern to healthcare practitioners since consequences of non-compliance can lead to costly and invasive surgeries, vision impairment, or blindness. Prostaglandin analog intracanalicular plugs may help manage the issues of non-compliance by vastly reducing dosing frequency.
All existing medications are given by topical drops:
Poor compliance (<30%)
Low residence time (<15min)
Low bioavailability (<5%)
Not so effective during night
> 50% of Glaucoma patients need a combination of drugs
More drugs = Even less patient compliance
No breakthrough, new drug or drug delivery in 20 years
The fact that Glaucoma remains a leading cause of blindness, despite the availability of 5 different classes of IOP-lowering topical medications, suggests a great need for improved treatment options
Second product :
EXP-LP-TM Sustained Release Latanoprost & Timolol
First product EXP-LP:
Sustained Release Latanoprost
Eximore is tailoring sustained-release prostaglandin analogs for the treatment of glaucoma and ocular hypertension. Inserted non-invasively through the punctum, the sustained release plug resides within the canaliculus, delivering latanoprost to the ocular surface for up to 60 days, to reduce or eliminate the need for daily dosing. After therapy is completed, the plug is removed easily by the ophthalmologist when the patient comes for routine eye check.
The intracanalicular plugs are visible under normal lighting conditions. In a recent pre-clinical study (see figure below), Eximore demonstrated a robust IOP reduction at three months with a single plug, demonstrating efficacy of the latanoprost plugs for the treatment of ocular hypertension and glaucoma. Results are comparable to use of topical prostaglandin (Latanoprost) ophthalmic drops. No adverse effects occurred, including no increase in hyperemia, and animals were comfortable overall.
EXP-LP is in FIM (first in man) clinical development for glaucoma and ocular hypertension.
EXP-LP-TM is a combination of an ophthalmic prostaglandin drug (Latanoprost) and an ophthalmic beta-blocking drug (Timolol) , both of which lower the pressure within the eye in different ways. The prostaglandin drug works by increasing the natural outflow of fluid from inside the eye. The betablocking drug works by decreasing the fluid production in the eye. Eximore demonstrated in-vitro sustain release of latanoprost and timolol for a month with a single plug.
Sustained Release Latanoporst
Preclinical Study Results
Normotensive dog model.
Unilateral implantation of plug.
Implantation went well, no need to anesthetize.
IOP and Miosis checked daily (miosis is the reduction of pupil size, a known effect of latanoprost in dog)
Results so far indicate strong efficacy of
~7-10mmHg IOP reduction (40-70%),
when plug in place.
EXP-LP Comparison to Xalatan Topical Drops
* Plugs did not retain for the duration of the study and were replaced with new when fell