Septerna is a clinical-stage biotech developing oral small molecule drugs targeting G protein-coupled receptors (GPCRs), the most historically productive drug target class, responsible for roughly one-third of all FDA-approved drugs. The core technology — the Native Complex Platform — reconstitutes functional GPCR proteins in a lab setting, enabling structure-based drug design and computational screening to be applied to GPCR targets at scale. Septerna has three wholly-owned pipeline programs: SEP-479, an oral PTH1R agonist for hypoparathyroidism targeting Phase 1 in early 2026; SEP-631, an oral MRGPRX2 inhibitor for chronic spontaneous urticaria (CSU) that completed Phase 1 with positive results and is headed for Phase 2b in late 2026; and a TSHR inhibitor for Graves' disease still in preclinical development. A key selling point across all three programs is oral delivery, versus the injectable standard of care in each indication. Septerna is pre-revenue on its own pipeline, but in May 2025 it signed a global collaboration with Novo Nordisk to develop oral small molecule drugs targeting metabolic disease GPCRs, including the GLP-1, GIP, and glucagon receptors. Novo paid a $195M upfront payment, reimburses 100% of R&D costs under the collaboration, and Septerna is eligible for up to ~$498M in milestones per program plus royalties. The Novo deal funds near-term operations while Septerna advances its wholly-owned endocrinology and immunology programs toward clinical proof-of-concept.
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