A Phase 3, Randomized, Double-Blind,Placebo-Controlled, Multicenter Study to Examine the Effect on Glucose Control (HbA1c) and Safety of rE-4 in Subjects With Type 2 Diabetes Mellitus Treated With Metformin, a Sulfonylurea, or Metformin and Sulfonylurea Combination

This research is a randomized, double-blind,controlled trial. 456 Chinese subjects with Type 2 Diabetes Mellitus will be enrolled in the trial.

Start Date30 Nov 2017

Sponsor / Collaborator

CSPC Zhongqi Pharmaceutical Technology (Tianjin) Co., Ltd.

CTR20160901 / CompletedPhase 1

重组胰高血糖素样肽-1受体激动剂注射液与冻干重组胰高血糖素样肽-1受体激动剂人体药代动力学对比临床试验

[Translation] Comparative clinical trial on the pharmacokinetics of recombinant glucagon-like peptide-1 receptor agonist injection and lyophilized recombinant glucagon-like peptide-1 receptor agonist in humans

主要目的：比较男性健康成年受试者单次皮下注射相同剂量rE-4注射液和冻干rE-4后的药代动力学参数，判断石药集团中奇制药技术（石家庄）有限公司研发的两种制剂是否生物等效。次要目的：评价两种制剂的安全性。

[Translation]

Primary objective: To compare the pharmacokinetic parameters of the same dose of rE-4 injection and lyophilized rE-4 in healthy male adult subjects after a single subcutaneous injection, and to determine whether the two preparations developed by Shijiazhuang Zhongqi Pharmaceutical Technology Co., Ltd. are bioequivalent. Secondary objective: To evaluate the safety of the two preparations.

Start Date23 Dec 2016

Sponsor / Collaborator

CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.

NCT03199261 / CompletedPhase 1

The Pharmacokinetic Comparison and Bioequivalence Evaluation of Two 10-µg Recombinant Exendin-4 Formulations in Chinese Healthy Male Subjects

Evaluation of the pharmacokinetics and safety rE-4 Injection versus rE-4 Freeze-dried Powder in healthy subjects.

Start Date23 Dec 2016

Sponsor / Collaborator

CSPC Zhongqi Pharmaceutical Technology (Tianjin) Co., Ltd.

100 Clinical Results associated with rExenatide-4(CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.)

100 Translational Medicine associated with rExenatide-4(CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.)

100 Patents (Medical) associated with rExenatide-4(CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.)

Literatures (Medical) associated with rExenatide-4(CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.)

01 Jun 2020·Shanghai kou qiang yi xue = Shanghai journal of stomatology

[Effects of Exenatide-4 on proliferation, migration and osteogenic differentiation of human periodontal ligament stem cells].

Article

Author: DU, Ling-Qian ; Ge, Shao-Hua ; Ding, Tian ; Zhang, Rui ; Liang, Qian-Yu

PURPOSETo investigate the effects of exendin-4(EX-4) on proliferation, migration and osteogenic differentiation of human periodontal ligament stem cells(PDLSCs).METHODSPDLSCs were isolated and cultured using limited dilution method in vitro. Colony formation assay, osteogenic and adipogenic differentiation were applied to identify the stem cells. Immunofluorescence staining was used to detect the expression of EX-4 receptor glucagon-like peptide-1 receptor (GLP-1R) on the surface of PDLSCs. PDLSCs were stimulated with 5, 10, 20 or 50 nmol/L EX-4 in vitro. CCK-8, Transwell assay and alkaline phosphatase(ALP) activity assay were used to determine the effects of EX-4 on PDLSCs proliferation, migration and osteogenic differentiation. Quantitative real-time polymerase chain reaction was used to determine the expression of osteogenic related genes ALP, runt-related transcription factor 2(Runx2) and osteocalcin (OCN). The data were analyzed by Graphpad Prims 6.0 software package.RESULTSPDLSCs were successfully isolated and cultivated. GLP-1R positively expressed on the surface of PDLSCs. EX-4 exerted no significant effect on PDLSCs proliferation(P>0.05). EX-4 significantly promoted migration, ALP activity and osteogenic related genes expression of PDLSCs (P<0.05).CONCLUSIONS10 nmol/L EX-4 could promote migration and osteogenic differentiation of PDLSCs.

01 Dec 2017·Clinical Drug InvestigationQ4 · MEDICINE

Pharmacokinetics and Preliminary Pharmacodynamics of Single- and Multiple-dose Lyophilized Recombinant Glucagon-like Peptide-1 Receptor Agonist (rE-4) in Chinese Patients with Type 2 Diabetes Mellitus

Q4 · MEDICINE

Article

Author: Zhu, Lixia ; Chen, Yingli ; Cui, Yimin ; Ji, Linong ; Xu, Ling ; Wang, Qian ; Lou, Kun ; Xu, Bingfeng ; Fang, Yi ; Wang, Yitong ; Zhao, Xia ; Guo, Xiaohui

BACKGROUND AND OBJECTIVESRecombinant glucagon-like peptide-1 receptor agonist (rE-4) is a glucagon-like peptide-1 receptor agonist, which has the same amino acid sequence to exenatide, except for the C-terminal deamidated. This study assessed the pharmacokinetics and preliminary pharmacodynamics of rE-4, following single and multiple subcutaneous injections in Chinese patients with type 2 diabetes mellitus (T2DM).DESIGN AND METHODSIn the randomized, open-label study, Chinese patients with T2DM (n = 36) were randomly assigned to three groups of rE-4 (n = 12), rE-4 with metformin (n = 12) and exenatide (n = 12, as the control group) for 12 weeks. rE-4 and exenatide were administered by subcutaneous injection in the abdomen, and metformin was given by oral administration. Patients received rE-4 or exenatide 5 μg twice a day for the first 4 weeks and adjusted the dose of rE-4 or exenatide to 10 μg twice a day at day 29 for the following 8 weeks, if their glycated albumin (GA) values were still greater than 17%. We evaluated pharmacokinetic parameters of rE-4 and exenatide, fasting plasma glucose (FPG), 2-h postprandial blood glucose (PG2 h), glycosylated hemoglobin (HbA1c) and body weight at designated time points.RESULTSThirty-six patients were enrolled, and 29 subjects finished the study. rE-4 was absorbed quickly with a median peak-reaching time (t _max) of 0.8-1.5 h and eliminated rapidly with a median terminal half-life (t _1/2z) of 1.6-1.9 h. The exposure of rE-4 increased in an approximately dose-proportional method without accumulation. rE-4 10 μg twice a day could reduce FPG (~2.29 mmol/L), PG2 h (~6.00 mmol/L), HbA1c (~1.19%) and body weight (~0.48 kg) from baseline to 12 weeks, with no statistical significance compared with exenatide (FPG: ~1.88 mmol/L; PG2 h: ~6.66 mmol/L; HbA1c: ~1.13%; body weight: ~0.47 kg) and rE-4 with metformin (FPG: ~2.33 mmol/L; PG2 h: ~6.51 mmol/L; HbA1c: ~0.84%; body weight: ~1.16 kg) (p > 0.05).CONCLUSIONSrE-4 twice a day has a pharmacokinetic profile similar to exenatide and rE-4 with metformin after single and multiple doses in Chinese patients with T2DM. Also, rE-4 could improve glycemic control effectively. CLINICALTRIALS.GOV IDENTIFIERNCT01342042.

01 Aug 2017·Int. Journal of Clinical Pharmacology and TherapeuticsQ4 · MEDICINE

Population pharmacokinetics of lyophilized recombinant glucagon-like peptide-1 receptor agonist (recombinant exendin-4, rE-4) in Chinese patients with type 2 diabetes mellitus

Q4 · MEDICINE

Article

Author: Guo, Wei ; Wang, Chen ; Zhang, Min-Jie ; Fang, Yi ; Wang, Qian ; Wang, Yi-Tong ; Ji, Li-Nong ; Zang, Yan-Nan ; Zheng, Qing-Shan

OBJECTIVETo investigate the population pharmacokinetics of lyophilized recombinant glucagon-like peptide-1 receptor agonist (rE-4) in Chinese patients with type 2 diabetes mellitus (T2DM) for plasma concentration estimation and individualized treatment.METHODSTwelve patients with T2DM were enrolled to receive subcutaneous injections of rE-4 at 5 µg twice daily for 84 days. Administration dosage was adjusted from 5 µg to 10 µg twice daily at day 29 in case of glycated albumin (GA) ≥ 17%. The population pharmacokinetic model was developed in the nonlinear mixed-effects modeling software NONMEM.RESULTSThe data were best described by a two-compartment model with first-order absorption and elimination. The outcome parameters were as follows: apparent clearance (CL/F) 6.67 L/h, apparent distribution volume of central compartment (V_c/F) 19.4 L, absorption rate constant (K_a) 1.39 h^-1, apparent distribution volume of peripheral compartment (V_p/F) 22.6 L, intercompartmental clearance (Q/F) 1.28 L/h. The interindividual variabilities for CL/F, V_c/F, K_a, and Q/F were 64.4%, 57.7%, 45.5%, and 153.3%, respectively. The intra-individual variability of proportional error model was 41.7%. No covariate was screened out that showed significant influence on the model parameters.CONCLUSIONSThe established two-compartment model with first-order absorption and elimination successfully described the pharmacokinetic characteristics of rE-4 in Chinese patients with T2DM. .

100 Deals associated with rExenatide-4(CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.)

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	Phase 3	CN	CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co., Ltd.	27 Nov 2017

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