This is the phase I study to evaluate the pharmacokinetics and safety of DA-2811 and Forxiga® after a single oral dose in healthy volunteers.
The study will also compare the pharmacokinetics and safety profiles of DA-2811 under fasting and fed states in healthy subjects.

Start Date04 Aug 2020

Sponsor / Collaborator

Dong-A ST Co., Ltd.

100 Clinical Results associated with DA-2811

100 Translational Medicine associated with DA-2811

100 Patents (Medical) associated with DA-2811

Literatures (Medical) associated with DA-2811

01 Jan 2023·Drug design, development and therapy

A Comparison of the Pharmacokinetics and Safety of Dapagliflozin Formate, an Ester Prodrug of Dapagliflozin, to Dapagliflozin Propanediol Monohydrate in Healthy Subjects.

Author: Lee, Sangmi ; Jang, In-Jin ; Kim, Eunjin ; Chung, Jae-Yong ; Kim, Hyun Chul ; Sung, Siyoung

BackgroundDapagliflozin formate (DAP-FOR, DA-2811), an ester prodrug of dapagliflozin, was developed to improve the stability and pharmaceutical manufacturing process of dapagliflozin, a sodium-glucose cotransporter-2 inhibitor.PurposeThis study aimed to evaluate the pharmacokinetics (PKs) and safety of dapagliflozin for DAP-FOR compared to those for dapagliflozin propanediol monohydrate (DAP-PDH, Forxiga) in healthy subjects.MethodsThis was an open-label, randomized, single-dose, two-period, two-sequence crossover study. The subjects received a single dose of DAP-FOR or DAP-PDH 10 mg in each period, with a 7-day washout. Serial blood samples for PK analysis were collected up to 48 hours after a single administration to determine plasma concentrations of DAP-FOR and dapagliflozin. PK parameters were calculated using a non-compartmental method and compared between the two drugs.ResultsIn total, 28 subjects completed the study. DAP-FOR plasma concentrations were not detected in all of the blood sampling time points except for one time point in one subject, and the corresponding DAP-FOR plasma concentration in the subject was close to the lower limit of quantification. The mean plasma concentration-time profiles of dapagliflozin were comparable between the two drugs. The geometric mean ratios and its 90% confidence intervals of the maximum plasma concentration and area under the plasma concentration-time curve of dapagliflozin for DAP-FOR to DAP-PDH were within the conventional bioequivalence range of 0.80-1.25. Both drugs were well-tolerated, with a similar incidence of adverse drug reactions.ConclusionThe rapid conversion of DAP-FOR into dapagliflozin led to the extremely low exposure of DAP-FOR and comparable PK profiles of dapagliflozin between DAP-FOR and DAP-PDH. The safety profiles were also similar between the two drugs. These results suggest that DAP-FOR can be used as an alternative to DAP-PDH.

100 Deals associated with DA-2811

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