Background and Aim: DA-1241 is a novel small molecule selective GPR119 agonist. In preclinical studies DA-1241 enhanced insulin and GLP-1 secretion, reduced glucose excursions, lowered blood glucose and improved dyslipidaemia. The primary objective of Part 1 of this study was to assess the safety and tolerability of multiple once daily oral doses of DA-1241 compared to placebo in HV. Secondary objective was to estimate the plasma PK characteristics. Methods: Part 1 was a double blind placebo-controlled, single-center study of DA-1241 in HV. Three sequential cohorts of HV (n=8/cohort) were blinded and randomized (3:1) to receive DA-1241: 50, 100 or 200 mg (n=6/cohort) or placebo (n=2/cohort), as single daily oral doses for 28 days. Safety data reviews and dose escalation decisions between cohorts took place after all subjects of an ongoing cohort had completed procedures through day 14. Results: Overall 24 male subjects participated in Part 1 (Age 38.4 ± 10.7, BMI 26.0 ± 2.7). All doses tested were safe and well tolerated. There were no SAEs and no discontinuations due to AE. All TEAE’s were mild with no obvious dose relation and resolved spontaneously. The day 28 Cmax and AUC0-tau PK parameters showed dose proportional characteristics across the tested dose range, with Cmax (50mg: 464.9 ± 284.1; 100mg: 569.3 ± 173.2; 200mg: 1653.2 ± 615.4 ng/mL) and AUC0-tau (50mg: 5168.4 ± 1651.2; 100mg: 7620.0 ± 1837.7; 200mg: 19167 ± 9088.8 h*ng/mL). Tmax was reached at 2.9 ± 1.8; 2.3 ± 1.2 and 1.9 ± 0.6 hours respectively with a t1/2 of 590 ± 370; 368 ± 355 and 537 ± 395 hours, values for 50, 100, and 200 mg doses respectively. Conclusion: Data from this phase 1b study in HV confirmed a favorable safety, tolerability and PK profile of DA-1241, and supported a progression of the clinical development program into patients. Disclosure M. Kim: Employee; Self; Dong-A ST Co. Ltd. D. Lee: Employee; Self; Dong-A ST Co. Ltd. J. Jeong: Employee; Self; Dong-A ST Co. Ltd. M. Grimm: None. B. B. Franey: None. M. Hompesch: Other Relationship; Self; Wiley, Stock/Shareholder; Self; ProSciento, Inc.