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Septerna Announces Dosing of the First Participants in Phase 1 Clinical Trial of SEP-631

Septerna, Inc. (SEPN) | August 21, 2025

By Hannah Lewis

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Septerna, Inc. announced the dosing of the first participants in its Phase 1 clinical trial of SEP-631, a small molecule MRGPRX2 negative allosteric modulator.

The trial aims to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of SEP-631 in healthy volunteers.

SEP-631 is being developed for the treatment of mast cell-driven diseases, including chronic spontaneous urticaria.

Phase 1 Clinical Trial Initiated

Septerna initiated the Phase 1 clinical trial of SEP-631 to assess its safety and efficacy in healthy volunteers.

Treatment for Mast Cell-Driven Diseases

SEP-631 is a potential treatment for mast cell-driven diseases, offering a convenient oral option for patients with chronic spontaneous urticaria.

Targeting MRGPRX2

SEP-631 aims to inhibit mast cell activation by selectively blocking the MRGPRX2 receptor, which plays a crucial role in mast cell degranulation.

  • The Phase 1 trial targets mast cell-driven diseases, addressing unmet medical needs and providing hope for patients with inadequate symptom relief from current therapies.
  • SEP-631's mechanism of action involves modulating G protein-coupled receptors (GPCRs), offering a novel approach to treating chronic spontaneous urticaria and related conditions.

The initiation of the Phase 1 trial for SEP-631 marks a significant milestone in Septerna's drug development efforts, reflecting the company's commitment to pioneering GPCR drug discovery for improved patient outcomes.