Targeting DUX4 by Myocyte-Selective siRNA Conjugate to Treat FSHD


Topic:

Translational Research

Poster Number: 435 O

Author(s):

David Strochlic, PhD, Souffle Therapeutics, Jordan Chambers, Souffle Therapeutics, Olga Sergeeva, Souffle Therapeutics, Tanvi Saxena, Souffle Therapeutics, Megan Minnix, Souffle Therapeutics, Joseph Sapiente, Souffle Therapeutics, Eun Sung Suh, Souffle Therapeutics, David Murison, Souffle Therapeutics, Travis Ness, Souffle Therapeutics, Isabel Klink, Souffle Therapeutics, Thomas Pires, Souffle Therapeutics, Beau Morrison, Souffle Therapeutics, Linda Zhang, Souffle Therapeutics, Ingrid Rankin, Souffle Therapeutics, Dylan Hoots, Souffle Therapeutics, John Yoon, Souffle Therapeutics, Peiru Chen, Souffle Therapeutics, Chanis Harpin, Souffle Therapeutics, Xiao Guo, Souffle Therapeutics, Joseph D’Amico, Souffle Therapeutics, Elissa Hobert, Souffle Therapeutics, Ellen Rohde, Souffle Therapeutics, Jesse Milling, Souffle Therapeutics, Ying Xu, Souffle Therapeutics, Lorenzo Benatuil, Souffle Therapeutics, Roman Bogorad, Souffle Therapeutics, Timofei Zatsepin, Souffle Therapeutics, Vadim Dudkin, Souffle Therapeutics

Facioscapulohumeral muscular dystrophy (FSHD) is a severe muscle wasting disease caused by the aberrant expression of DUX4. Activation of DUX4 in skeletal muscle triggers a cascade of transcriptional changes, ultimately leading to myocyte cell death. Genetic silencing of DUX4 represents a promising disease modifying therapy for FSHD.

Soufflé Therapeutics has leveraged a propriety discovery platform to enable muscle-selective functional delivery of genetic therapeutics. This receptor-mediated delivery pathway offers a differentiated selectivity and safety profile compared to other approaches. Our proprietary antibody to the myocyte receptor was used to generate antibody-siRNA conjugates that can be administered intravenously or subcutaneously. In mouse, a single administration achieves both potent (IC50 <0.05 mg/kg) and sustained silencing of target transcripts in striated muscle, while sparing off-target tissues. This muscle-specific delivery has been confirmed in non-human primates. SFL-0821 is a covalent conjugate comprised of Soufflé’s proprietary myocyte-targeting antibody and an siRNA that is highly specific for the human DUX4 transcript. We administered SFL-0821 into Acta-MCM;FLExDUX4 mice, which express tamoxifen-inducible human DUX4 and show FSHD-like pathophysiology upon induction. A single intravenous administration of SFL-0821 resulted in potent and dose-dependent silencing of DUX4 mRNA (>80%) in skeletal muscle that persisted for 3 months. Immunohistochemical analysis revealed a substantial reduction of nuclear DUX4 protein expression, consistent with an observed downregulation of DUX4-regulated transcripts. Knockdown of DUX4 was associated with increased muscle mass and improved muscle function in tamoxifen-induced mice. Our non-clinical data support the potential of SFL-0821 as a novel therapeutic to help people living with FSHD and we are planning to initiate a clinical trial in 2026.