Australian company Nyrada (ASX:NYR) has announced a preclinical pharmacokinetic study of its lead candidate compounds has found they can cross the blood-brain-barrier (BBB) in the intact uninjured animal brain.
The company said the aim of its 'Brain Injury program' is the development of a therapy to reduce secondary brain damage following head trauma and stroke.
Head trauma (motor vehicle accident, falls, sporting injury) and stroke are leading causes of hospital admissions and long-term rehabilitation service requirements. Nyrada said its 'Brain Injury Program' aims to prevent secondary brain injury by reducing the build-up of calcium ions in brain cells which causes the cells to die.
The company said its first-generation compound, NYX-104, was delivered as a suppository for five days following brain injury in an earlier preclinical proof-of-concept efficacy study in a model of stroke. It said it was found to significantly reduce the injury volume compared to control animals which received placebo.
Nyrada said it has since developed a more potent version of NYX-104, called NYX-242, that blocks calcium ion build-up in cells at three-times greater potency. It has also discovered a new generation of compounds with a different molecular target but considerably greater potency in blocking calcium (lead compound NYX-1010).
In a separate preclinical pharmacokinetic study, Nyrada said it has shown that therapeutic concentrations of both NYX-242 and NYX-1010 can be detected in the healthy animal brain at 30 minutes following a single intravenous dose, confirming both drugs can cross the intact BBB.
The BBB is a protective barrier between the components of the blood and the cells that form the brain tissue, keeping infection at bay in the healthy brain. However, this can pose a major roadblock in the development of drugs for treating brain disorders as a large proportion of drugs cannot cross this barrier and reach the desired target in brain tissue. Some drugs that can cross the BBB get readily removed and cannot accumulate in the brain tissue in sufficient quantity to be effective.
The company said follow-on studies are being undertaken to assess optimal dosing and drug levels in the brain following continuous intravenous administration.
According to CEO James Bonnar,“These latest data are an exciting step forward for Nyrada. Having two potent drug candidates that act on distinctly different targets to limit toxic calcium ion build-up in brain cells is a huge achievement. It provides a solid scientific foundation and greatly de-risks the Brain Injury program. Nyrada is well positioned to becoming a leader in the field of brain injury drug development."