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GNE-7915 is a highly potent, selective, and brain-penetrable leucine-rich repeat kinase2 (LRRK2) inhibitor, with Ki and IC50 of 1 nM and 9 nM, respectively.

GEN-7915 is extensive inhibitor across 187 screened kinases, except TTK kinase. In an extended profile across 392 kinases, GNE-7915 only bound to 10 enzymes to a significant extent (>50% probe displaced at 100 nM). GNE-7915 and its progenitors are the first selective LRRK2 inhibitors to penetrating the brain barrier. [1]

GEN-7915 has been shown to induce dephosphorylation of LRRK2 in the brain of transgenic mice. GNE-7915 is not reported to cause cellular or genetic toxicity, and has progressed into preclinical studies in cynomolgus monkeys [3]. The use of in silico modelling, extensive in vitro assays and resource-efficient in vivo techniques to produce GNE-7915, reflects a trend towards the concerted optimisation of potency, selectivity and pharmacokinetic properties in early-stage drug development [1]. GNE-7915 can inhibit TNFαand CXCL10 at higher concentrations (≥ 3 μM) in both WT and LRRK2 KO experiments [2].

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