Epalex is developing EP102 for the acute treatment of migraine headache pain and migraine-related symptoms. EP102 is an oral dosage form that can achieve circulating levels of a drug substance that has been approved by the FDA for a different indication. Until now, this drug could be administered only intravenously in an emergency room or inpatient setting.
The mechanism of action of EP102 differs from that of other products currently marketed for the acute treatment of migraine. EP102 is thought to impact migraine by modulating the inhibitory action of the neurotransmitter gamma aminobutyric acid (GABAA) on GABAA receptors and may be involved in the inhibition of the neurologic process of cortical spreading depression, a possible cause of migraine and migraine aura.
Epalex recently completed a Phase 1a, randomized, placebo-controlled, double-blind ascending-dose study of EP102 in 99 healthy male and female adults. This study established a well-characterized pharmacokinetic and safety profile, exhibiting good safety-tolerability of EP102.
A proof-of-concept study is currently underway using EP102 in adult women and men experiencing moderate to severe migraine.
Epalex’s proprietary, patent-pending delivery technology improves the bioavailability of the active compound in EP102 by substantially increasing the peak concentration (Cmax) and area under the curve (AUC) compared to a standard tablet.
Epalex is developing EP103 for the control of seizure disorders resistant to available therapies. EP103 is an oral formulation that can deliver therapeutic levels of an FDA-approved drug that has shown activity in controlling seizures in off-label use in people with epilepsy and exhibits a dose-related effect in animal seizure models. Until now, this drug could be administered only intravenously in an emergency room or inpatient setting.
Epalex has shown that the active moiety in EP103 delays seizure onset in chemically induced seizures in rodents. Separate groups of rats received a continuous IV infusion of placebo (n=6) or one of three different dose levels (n=3-4) of the active moiety of EP103 throughout the experiment. Pentylenetetrazole (PTZ), a GABAA receptor antagonist commonly used to produce seizure activity, was infused IV at a constant rate. Time until first onset of seizure activity (myoclonic jerks) and time until onset of a clonic seizure was recorded. The active moiety of EP103 displayed a dose-related delay (up to four-fold) in the onset of seizure activity that was statistically significant, p<0.001, 2-tailed.
