{
    "abstract": "DBPR108 (prusogliptin) is a novel, orally bioavailable dipeptidyl peptidase-4 (DPP-4) inhibitor. This study investigated the pharmacokinetics and pharmacodynamic characteristics of DBPR108 tablets in patients with type 2 diabetes.\nIn this randomized, parallel-group, open-label, phase I study, Chinese adults with type 2 diabetes, glycated hemoglobin of 7.0-9.5%, and body mass index of 19-35 kg/m\nIn total, 30 patients were randomized with 10 patients in each group. DBPR108 was quickly absorbed with median time to reach the maximum plasma concentration of 1.5-4 h at steady state. Exposure to DBPR108 at steady-state increased dose proportionally with mean maximum steady-state plasma DBPR108 concentration during dosage intervals of 119, 256, and 567 ng/mL in the 50-, 100-, and 200-mg groups, respectively. Accumulation ratio of DBPR108 ranged from 0.85 to 1.3, and steady state was reached after four continuous daily doses. After multiple doses of DBPR108, maximum inhibitory efficacy of DPP-4 increased with higher dose levels ranging from 62.1 to 89.4%. Active glucagon-like peptide-1 levels increased after DBPR108 administration. In addition, six patients experienced treatment-emergent adverse events without leading to treatment interruption or discontinuation.\nDBPR108 was well tolerated in Chinese patients with type 2 diabetes, and both the pharmacokinetic and pharmacodynamic profiles support once-daily dosage regimens of DBPR108 in future studies.\nClinicalTrials.gov (NCT05146869); registered 23 November 2021.",
    "authors": [
        {
            "affiliation": "Clinical Pharmacology Center, Beijing Anzhen Hospital, Capital Medical University, No. 2 Anzhen Road, Chaoyang District, Beijing, 100029, China.",
            "firstname": "Wenfang",
            "initials": "W",
            "lastname": "Liu"
        },
        {
            "affiliation": "Clinical Pharmacology Center, Beijing Anzhen Hospital, Capital Medical University, No. 2 Anzhen Road, Chaoyang District, Beijing, 100029, China.",
            "firstname": "Kexu",
            "initials": "K",
            "lastname": "Yang"
        },
        {
            "affiliation": "Clinical Pharmacology Center, Beijing Anzhen Hospital, Capital Medical University, No. 2 Anzhen Road, Chaoyang District, Beijing, 100029, China.",
            "firstname": "Yang",
            "initials": "Y",
            "lastname": "Lin"
        },
        {
            "affiliation": "Clinical Pharmacology Center, Beijing Anzhen Hospital, Capital Medical University, No. 2 Anzhen Road, Chaoyang District, Beijing, 100029, China.",
            "firstname": "Chunyan",
            "initials": "C",
            "lastname": "Lu"
        },
        {
            "affiliation": "Clinical Pharmacology Center, Beijing Anzhen Hospital, Capital Medical University, No. 2 Anzhen Road, Chaoyang District, Beijing, 100029, China.",
            "firstname": "Jingyi",
            "initials": "J",
            "lastname": "Liu"
        },
        {
            "affiliation": "Clinical Trial Center, The First Affiliated Hospital of Bengbu Medical University, No. 287, Changhuai Road, Bengbu, 233004, China.",
            "firstname": "Huan",
            "initials": "H",
            "lastname": "Zhou"
        },
        {
            "affiliation": "Clinical Division, CSPC Pharmaceutical Group Co., Ltd., Shijiazhuang, China.",
            "firstname": "Juan",
            "initials": "J",
            "lastname": "Wang"
        },
        {
            "affiliation": "Clinical Division, CSPC Pharmaceutical Group Co., Ltd., Shijiazhuang, China.",
            "firstname": "Tianhao",
            "initials": "T",
            "lastname": "Zhang"
        },
        {
            "affiliation": "Clinical Division, CSPC Pharmaceutical Group Co., Ltd., Shijiazhuang, China.",
            "firstname": "Lingli",
            "initials": "L",
            "lastname": "Yao"
        },
        {
            "affiliation": "Clinical Division, CSPC Pharmaceutical Group Co., Ltd., Shijiazhuang, China.",
            "firstname": "Huanhuan",
            "initials": "H",
            "lastname": "Qi"
        },
        {
            "affiliation": "Clinical Division, CSPC Pharmaceutical Group Co., Ltd., Shijiazhuang, China.",
            "firstname": "Xiaofang",
            "initials": "X",
            "lastname": "Zhang"
        },
        {
            "affiliation": "Clinical Division, CSPC Pharmaceutical Group Co., Ltd., Shijiazhuang, China.",
            "firstname": "Rui",
            "initials": "R",
            "lastname": "Jia"
        },
        {
            "affiliation": "Clinical Trial Center, The First Affiliated Hospital of Bengbu Medical University, No. 287, Changhuai Road, Bengbu, 233004, China. 158169847@qq.com.",
            "firstname": "Xiaoli",
            "initials": "X",
            "lastname": "Li"
        },
        {
            "affiliation": "Clinical Pharmacology Center, Beijing Anzhen Hospital, Capital Medical University, No. 2 Anzhen Road, Chaoyang District, Beijing, 100029, China. jingshan@anzhengcp.com.",
            "firstname": "Shan",
            "initials": "S",
            "lastname": "Jing"
        }
    ],
    "conclusions": null,
    "copyrights": "\u00a9 2025. The Author(s).",
    "doi": "10.1007/s40262-025-01501-8\n10.1080/07853890510037400\n10.2147/dddt.S37647\n10.2337/dci18-0033\n10.2337/dci22-0034\n10.4239/wjd.v13.i2.85\n10.1016/j.lanwpc.2022.100509\n10.1016/j.diabres.2020.108095\n10.1016/j.bmc.2021.116354\n10.1161/circresaha.118.312673\n10.2337/dc15-1707\n10.1111/j.1463-1326.2011.01458.x\n10.2337/dc12-0706\n10.1016/j.lfs.2021.119574\n10.1016/j.bmcl.2010.04.124\n10.2174/0113892002288120240221111336\n10.3389/fendo.2024.1359407\n10.5414/cp201902\n10.1111/j.1365-2125.2011.03937.x\n10.1111/j.1463-1326.2009.01046.x\n10.1007/s00228-016-2175-1\n10.1111/jdi.12538",
    "journal": "Clinical pharmacokinetics",
    "keywords": [],
    "methods": null,
    "publication_date": "2025-04-19",
    "pubmed_id": "40252162\n16179267\n35211246\n35789825\n32112790\n34428715\n29436388\n27659407\n21672124\n23033241\n33961850\n20483603\n38454771\n38529396\n23782587\n21651615\n19476474\n27999883\n27182005",
    "results": "In total, 30 patients were randomized with 10 patients in each group. DBPR108 was quickly absorbed with median time to reach the maximum plasma concentration of 1.5-4 h at steady state. Exposure to DBPR108 at steady-state increased dose proportionally with mean maximum steady-state plasma DBPR108 concentration during dosage intervals of 119, 256, and 567 ng/mL in the 50-, 100-, and 200-mg groups, respectively. Accumulation ratio of DBPR108 ranged from 0.85 to 1.3, and steady state was reached after four continuous daily doses. After multiple doses of DBPR108, maximum inhibitory efficacy of DPP-4 increased with higher dose levels ranging from 62.1 to 89.4%. Active glucagon-like peptide-1 levels increased after DBPR108 administration. In addition, six patients experienced treatment-emergent adverse events without leading to treatment interruption or discontinuation.",
    "title": "Pharmacokinetics and Pharmacodynamics of Prusogliptin (DBPR108), a Once-Daily Dipeptidyl Peptidase-4 Inhibitor, in Patients with Type 2 Diabetes.",
    "xml": "<Element 'PubmedArticle' at 0x78850432b880>"
}