LX2761 is an orally-delivered small molecule compound for the treatment of diabetes which is currently in Phase 1 clinical trials. LX2761 is an internally generated compound and is designed to inhibit SGLT1 locally in the gastrointestinal tract without any significant inhibition of SGLT2 in the kidney.  

In preclinical studies, LX2761 delayed and reduced intestinal glucose absorption and reduced postprandial glucose, the level of blood glucose after a meal, while increasing plasma levels of GLP-1, consistent with inhibition of intestinal SGLT1.  In addition, LX2761 was minimally absorbed into the systemic circulation, resulting in little effect on urinary glucose excretion, indicating that LX2761 was restricted to the gastrointestinal tract.  The initial Phase 1 clinical trial of LX2761 is planned as a double-blind, randomized, placebo-controlled, ascending single dose study in both healthy volunteers and people with type 2 diabetes.  The study is designed to evaluate the safety and tolerability of LX2761.  Lexicon has granted Sanofi certain rights of first negotiation with respect to the future development and commercialization of LX2761.


LX9211 is an orally-administered small molecule for the treatment of neuropathic pain.  In preclinical studies, LX9211 has shown robust efficacy in models of neuropathic pain and is well-tolerated at and above efficacious doses in animals.  LX9211 was jointly developed by us and Bristol-Myers Squibb Company as part of our neuroscience drug discovery alliance.  LX9211 is in Phase 1 clinical trials.

In November 2016, we obtained exclusive research, development and commercialization rights to LX9211 in Lexicon has acquired the rights to LX9211 under an amendment to the neuroscience alliance, pursuant to which we agreed to pay Bristol-Myers Squibb development and regulatory milestones starting with the commencement of the first Phase 2 clinical trial in the first indication.  We have agreed to pay additional development and regulatory milestones for each of the second and third indications, if applicable.  Finally, we have agreed to pay royalties on worldwide net sales of small molecules related to the alliance that act through the target of LX9211 as well as certain sales performance milestones. Additional small molecule compounds acting through the same target as LX9211 are also included in the exclusive arrangement.