Poster Presentations: American Diabetes Association 81st Scientific Sessions 2021


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DA-1241 is a small, novel, chemically synthesized, potent molecule, and a selective agonist for GPR119. It has been reported that GPR119 stimulates glucose-dependent insulin secretion in the pancreatic beta cells which makes GPR119 a promising drug target for controlling glucose levels with little to no risk of hypoglycemia. Data from pre-clinical studies showed that DA-1241 efficiently lowered both blood glucose and lipid levels simultaneously. These data suggest that DA-1241 has enhanced intrinsic efficacy in glycemic control compared to other GPR119 investigational drugs; DA-1241 may therefore have therapeutic potential for patients with T2DM and dyslipidemia.

Part 1 of Phase 1b Multiple Ascending Dose (MAD) Study:

Part 1 of this study showed that DA-1241 is well-tolerated in healthy volunteers. It also generated a favorable pharmacokinetic profile. Part 2 extends the safety, tolerability, pharmacokinetic, and pharmacodynamic assessment of DA-1241 to T2DM patients.

Part 2 of Phase 1b Multiple Ascending Dose (MAD) Study:

Key findings from the study in T2DM subjects:

  • Doses tested were generally safe and well tolerated. The most frequent TEAEs were mild GI side effects (nausea, diarrhea, abdominal pain), all resolved spontaneously.
  • Multiple parameters from continuous glucose monitoring (CGM), trended towards improvement for all DA-1241 doses; especially time spent at BG < 180 mg/dL and glucose AUE0-24h.
  • After 8-week treatment, HbA1c trended towards improvement across dosing groups, as did body weight.
  • Secretion of GIP, GLP-1 and PYY were increased at day 56 in DA-1241-treated groups, consistent with the mechanism of action of DA-1241.


  • This phase 1b study in T2DM showed favorable safety, tolerability, and PK profiles of DA-1241 administered daily over a period of 56 days, compared to placebo or sitagliptin in the target population of subjects with T2DM on metformin monotherapy.
  • Biomarkers and PD data support the hypothesized mechanism of action and showed favorable efficacy data trends.
  • Data presented here supports further progressing the DA-1241 clinical development program.


Mi-Kyung Kim, DaeYoung Lee, Jiyoon Jeong, Bridgette Franey, Michael Grimm, Marcus Hompesch