LRRK2, recognized as a crucial drug target in Parkinson's disease, plays a major role in the pathogenesis of the condition. Inhibiting LRRK2 activity has emerged as a promising disease-modifying therapeutic strategy, and several drug candidates have achieved clinical status.
The BT-0267 candidate has an efficient blood-brain barrier penetration while minimized peripheral exposure as well as has a superior overall safety profile. The presented data highlighted the in vivo efficacy of BT-0267 in brain and no visible lung and kidney morphological changes compared to other LRRK2 inhibitorLRRK2 inhibitor candidates. Additionally, BT-0267 has an outstanding cerebrospinal fluid (CSF)/unbound plasma ratio in non-human primates, exhibits a remarkable 1000x selectivity against other kinases, and >500x selectivity against other targets from the safety panel, providing indicators of its best-in-class safety profile.
Dr. Alexei Pushechnikov, Head of Chemistry and CTO at Brenig Therapeutics, remarked, "Achieving an outstanding CSF/plasma ratio for BT-0267 is in line with our rational design strategy to reduce potential lung and kidney toxicity effects in our LRRK2 inhibition program."
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