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16E3-2-1 is a neutralizing monoclonal antibody developed by the Novartis Institutes for BioMedical Research that targets Gremlin-1 (GREM1). Gremlin-1 is a secreted glycoprotein and a known antagonist of the bone morphogenetic protein (BMP) signaling pathway. In pulmonary arterial hypertension (PAH), GREM1 expression is significantly upregulated in the lungs, which suppresses BMP signaling and promotes pulmonary vascular remodeling and right ventricular hypertrophy. By binding to and neutralizing GREM1, the antibody restores BMP pathway activity and has demonstrated the ability to reduce vascular remodeling and disease progression in preclinical mouse models of chronic hypoxia-induced PAH. Although preclinical data published in 2013 established GREM1 as a viable therapeutic target, this specific antibody does not appear to have advanced into human clinical trials.
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