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 the third quarter of 2025, marking a major step toward bringing this novel therapy to patients with obesity, type 2 diabetes and metabolic dysfunction.
"MolecuLern integrates AI-driven molecular design, wet lab validation and proprietary structural modelling to identify innovative small molecules for challenging drug targets,” Vankayalapati added. “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."
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