Science

Science

NeuroTherapeutics Pharma has identified drug candidates that act through a new mechanism of action, modulating a novel therapeutic target within a well-validated inhibitory neuronal pathway. These molecules modulate a specific subset of GABAA receptors while having no activity at classic, post-synaptic GABA receptors.

A novel mechanism for pain, epilepsy,
and neurological conditions

Further, they preferentially enhance inhibition at times of abnormal neuronal excitability. By acting during such states, and only in specific regions of the brain, NTP compounds have repeatedly shown significant efficacy in a range of in vivo models of disease pathology, coupled with a consistent lack of the sedative and cognitive side effects which are typically observed with classic GABAergic drug mechanisms.

Extensive molecular pharmacology studies have demonstrated both selectivity for specific GABAA receptors, as well as preferential activity at times when receptor function is aberrant. These effects seen at the target are consistent with data that demonstrate increased inhibitory drive in hippocampal brain slice models of epilepsy and spinal cord preparations from animals with neuropathic pain conditions. NTP drug candidates demonstrated a wide breadth of activity across animal models of neurological disorders including epilepsy, neuropathic, inflammatory and acute pain, anxiety, and migraine. This mechanism may also provide therapeutic potential in other psychiatric disorders.

Compounds that increase inhibition by acting on specific regions of the brain, and preferentially at times of abnormal neuronal excitability, potentially represent a significant advancement in therapy. NTP’s novel mechanism increases inhibition in a new way and represents a new class of potential therapy for neurologic disorders.