Medicinal Chemistry Expertise

Parkinson’s Disease

Parkinson’s Disease

Califia Bio, Inc. has been awarded a Michael J. Fox Foundation Research grant to investigate the efficacy of CLFB-1134 in animal models of Parkinson’s Disease.

  • Califia Bio has been invited to present positive results of this grant funded research at the Michael J. Fox Foundation’s Parkinson’s Disease Therapeutics Conference, in New York City, November 3, 2015.
  • HAND (HIV-Associated Neurocognitive Disorders) and Parkinson’s Dementia have similar underlying pathologies involving dopaminergic pathways and synaptodendritic damage.
  • Our very selective MLK3 inhibitor CLFB-1134 has now shown efficacy in both animal models of Parkinson’s Disease and HAND.

Previously, inhibitors of mixed lineage kinase 3 (MLK3) showed great promise for treatment of Parkinson’s disease in pre-clinical models, but interest in this area halted when a non-selective inhibitor (CEP-1347) failed in Phase II clinical trials. We have investigated the poor target specificity and poor ability of CEP-1347 to penetrate the blood-brain barrier1 and have developed new compounds with much higher selectivity for MLK3 and much improved ability to achieve high concentrations in the brain.

 

We are seeking partners to develop and commercialize orally active, brain penetrant and highly selective MLK3 inhibitor compounds for potential treatments for Parkinson’s Disease, Post- Operative Cognitive Dysfunction (POCD) and HIV-Associated Neurocognitive Disorders.

 

(1) Goodfellow VS, Loweth CJ, Ravula SB, Wiemann T, Nguyen T, Xu Y, Todd DE, Sheppard D, Pollack S, Polesskaya O, Marker DF, Dewhurst S, Gelbard HA. Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. J Med Chem. 2013 56 8032-48.