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ANPA-0073 is a novel, orally available small molecule that acts as a G-protein biased agonist of the apelin receptor (also known as APJ or APLNR). It was designed to have an increased half-life and fewer side effects compared to native apelin peptides, particularly by reducing β-arrestin signaling and subsequent receptor internalization. This bias aims to improve safety and tolerability for long-term administration. The drug is being developed primarily for pulmonary arterial hypertension (PAH), with additional development in idiopathic pulmonary fibrosis (IPF) and selective weight loss/obesity. In first-in-human studies, ANPA-0073 demonstrated good safety and tolerability profiles in healthy volunteers, with only mild transient adverse events reported[1][2][6]. The drug is administered orally in capsule form[2][8].
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