Saniona announced that it has selected SAN2219 as the first preclinical development candidate from its GABA-A a2/a3 activator program. SAN2219 has demonstrated highly encouraging efficacy in several in vivo seizure models and has the potential to become a valuable therapeutic opportunity for various forms of epilepsy. SAN2219 is a subtype selective activator of GABA-A a2/a3/a5 receptors.

GABA is a neurotransmitter that inhibits signals between nerve cells in the brain. Most forms of epilepsy are caused by an over-excitability in specific neural circuits. By inhibiting the over-excitability in epilepsy, benzodiazepines have proven to be among the most effective treatment principles for control of seizure activity.

Benzodiazepines are non-selective GABA modulators that broadly activate GABA receptors including the GABA-A a1 receptor subtype. Benzodiazepines are often used as rescue medicine in acute epilepsy, and their long-term use is often hampered by the development of tolerance to seizure control, withdrawal symptoms, and adverse events, such as cognitive impairment and sedation. The dose limiting side effects and tolerance development of benzodiazepines are primarily mediated by the GABA-A a1 receptors.

SAN2219 has been designed to selectively modulate GABA-A a2, a3 and a5, resulting in a robust inhibition of seizure activity without the well-known GABA-A a1 mediated side effects of benzodiazepines. The preclinical data supports that SAN2219 may be used for acute and chronic treatment of prevalent epilepsy forms as well as specific epilepsy syndromes.