The assessment of global changes in fibrillar collagens and to the larger extent e.g., ECM induced upon inhibitor treatment has largely been lacking for the currently available LOX family inhibitors. We therefore undertook a quantitative pharmacodynamics approach to characterize the global alterations in the ECM composition and organization upon targeting LOX with LXG6403 using state-of-the-art ECM-targeted proteomics coupled with mass spectrometry imaging