GLPG-0259 / J&J - LARVOL DELTA

Extracellular vesicles derived from monomeric α-synuclein-treated microglia ameliorate neuroinflammation by delivery of miRNAs targeting PRAK. (PubMed, Neurosci Lett) - "The specific PRAK inhibitor GLPG0259 could mitigate microglial activation insulted by oligomeric α-synuclein...These results suggest that PRAK serves as an intersection in microglial activation when challenged with conformationally different α-synuclein. EVs derived from microglia treated with monomeric α-synuclein promote anti-inflammatory microglia by delivering miRNAs that target PRAK into recipient microglia."

Journal • CNS Disorders • Inflammation • Movement Disorders • Parkinson's Disease

The TLK1-MK5 Axis Regulates Motility, Invasion, and Metastasis of Prostate Cancer Cells. (PubMed, Cancers (Basel)) - "PC3, a highly metastatic cell line when assayed in xenografts, was further tested in a tail-vein injection/lung metastasis model, and we showed that, following inoculation, treatment with GLPG0259 (MK5 specific inhibitor) or J54 (TLK1 inhibitor) resulted in the lung tumor nodules being greatly diminished in number, and for J54, also in size. Our data support that the TLK1-MK5 axis is functionally involved in driving PCa cell metastasis and clinical aggressiveness; hence, disruption of this axis may inhibit the metastatic capacity of PCa."

Journal • Genito-urinary Cancer • Lung Cancer • Oncology • Prostate Cancer • Solid Tumor • TLK1

Targeting ERK3/MK5 complex for treatment of obesity and diabetes. (PubMed, Biochem Biophys Res Commun) - "Finally, we show that the expression of ERK3 and MK5 correlates with the degree of obesity and that ERK3/MK5 complex regulates energy dissipation in human adipocytes. Altogether, we demonstrate that ERK3/MK5 complex can be targeted in vivo to preserve metabolic health and combat obesity and diabetes."

Journal • Diabetes • Genetic Disorders • Metabolic Disorders • Obesity

Charles River Laboratories to acquire Galapagos’ Argenta and BioFocus service operations for up to €134 million (Galapagos Press Release) - "Galapagos NV...announces the signing of a definitive agreement to sell the BioFocus and Argenta service division operations to Charles River Laboratories International, Inc...for a total consideration of up to €134 million. The transaction is subject to customary closing conditions and is expected to close early in the second quarter of 2014."; Proceeds will be used for Galapagos’ pipeline progress.

Anticipated M & A • Financing • Immunology • Inflammatory Bowel Disease • Psoriasis • Rheumatoid Arthritis

A twelve-week exploratory phase II trial of GLPG0259 versus placebo in patients with active rheumatoid arthritis and inadequate response to methotrexate (ACR/ARHP 2011) - P2, N=200; The interim analysis, involving 12 weeks of treatment with 50mg GLPG0259 or placebo in patients with active RA and insufficient response to MTX, did not show any clinical benefit from GLPG0259; Part B of the trial will not be initiated

P2 data • Rheumatoid Arthritis