Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Autoimmune disease

Multiple sclerosis (MS)

Protein kinase Cb (PRKCB)

Mouse studies suggest PRKCB inhibitors could help treat MS. PRKCB can induce hyperpermeability of the blood brain barrier (BBB). In an experimental autoimmune encephalomyelitis (EAE) mouse model of relapsed-remitting MS, the PRKCB inhibitor enzastaurin decreased migration of proinflammatory T cells across the BBB and decreased demyelination of spinal cord neurons compared with vehicle. Next steps could include testing the long-term efficacy and safety of PRKCB inhibitors in the EAE models.
Eli Lilly and Co.'s Arxxant ruboxistaurin (LY333531), a synthetic PRKCB inhibitor, is under review to treat diabetic retinopathy. In May, the pharma discontinued development of enzastaurin (LY317615) after the synthetic inhibitor of PRKCB and protein kinase B (PKB; PKBA; AKT; AKT1) missed the primary endpoint in a Phase III trial to treat relapsed or refractory diffuse large B cell lymphoma (DLBCL).

SciBX 6(36); doi:10.1038/scibx.2013.986
Published online Sept. 19, 2013

Unpatented; unlicensed

Lanz, T.V. et al. Proc. Natl. Acad. Sci. USA; published online Aug. 19, 2013;
doi:10.1073/pnas.1302569110
Contact: Michael Platten, German Cancer Research Center,
Heidelberg, Germany
e-mail:

michael.platten@med.uni-heidelberg.de