Biolexis Therapeutics Unlocks a New Frontier in GLP-1 Receptor Activation

CryoEM Confirms a First-in-Class Allosteric Binding Mode, Validating MolecuLern™ AI-Driven Discovery

LEHI, Utah, March 14, 2025 /PRNewswire/ -- Biolexis Therapeutics has achieved a transformative milestone in metabolic drug discovery with the successful resolution of the cryo-electron microscopy (cryoEM) structure of BLX-7006, its first-in-class oral small-molecule GLP-1 receptor agonist. This breakthrough confirms a completely novel allosteric activation mechanism for the GLP-1 receptor, distinct from any previously known approaches.

The cryoEM structural confirmation validates the predictive power of MolecuLern, Biolexis' AI-enabled drug discovery platform. MolecuLern identified BLX-7006 as a novel small molecule capable of allosterically modulating GLP-1 receptor activity. Unlike many oral small-molecule GLP-1 therapies being developed—whose compounds are almost exclusively modified analogs of existing molecules such as Pfizer's Danuglipron and Eli Lilly's Orforglipron—BLX-7006 is a brand-new chemotype with an entirely unique binding mode.

"The cryoEM structural confirmation of BLX-7006 provides definitive proof that we have discovered a new way to activate the GLP-1 receptor allosterically," said Dr. Hariprasad Vankayalapati, Chief Scientific Officer of Biolexis Therapeutics. "This isn't just an incremental improvement on existing compounds—it's a new mechanism enabled by our AI-driven approach to drug discovery. With superior metabolic stability and a more efficient synthesis process, BLX-7006 represents a breakthrough in the quest for next-generation, oral GLP-1 therapies."

Biolexis is actively completing the toxicology and manufacturing studies necessary to support human clinical testing of BLX-7006. With these critical studies underway, the company plans to initiate first-in-human trials in Q3 2025, marking a major step toward bringing this novel therapy to patients with obesity, type 2 diabetes, and metabolic dysfunction.

Asked to provide additional details on Biolexis' AI drug discovery platform, Vankayalapati stated, "MolecuLern integrates AI-driven molecular design, wet lab validation, and proprietary structural modeling to identify innovative small molecules for challenging drug targets. The successful cryoEM validation of BLX-7006's novel binding mode underscores the ability of MolecuLern to accurately predict molecular interactions and accelerate the discovery of first-in-class therapeutics."

About Biolexis Therapeutics

Biolexis Therapeutics is a biopharmaceutical company pioneering the discovery and development of next-generation metabolic drugs to address chronic diseases such as obesity and type 2 diabetes. Its proprietary AI-enabled drug discovery platform, MolecuLern, drives the rapid identification of novel small-molecule therapies, delivering superior efficacy and safety profiles. With a commitment to scientific excellence and patient-centered innovation, Biolexis is redefining the future of metabolic medicine.

For more information, visit biolexistx.com.

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SOURCE Biolexis Therapeutics Inc