更新于：2024-11-04
Phenomix Corp.
更新于：2024-11-04
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A Phase 3, Randomized, Double-Blind, Active-Controlled, Multi-Center Extension Study to Evaluate Safety and Efficacy of Dutogliptin in Subjects With Type 2 Diabetes Mellitus on a Background Medication of Metformin
A Phase III, Multicenter, Double-blind, Active-Controlled, 52 Week Extension Study to Evaluate the Safety and Efficacy of Dutogliptin in Patients With Type 2 Diabetes Mellitus Receiving Background Treatment With Glimepiride Alone or in Combination With Metformin or With Pioglitazone Alone
A Randomized, Double-Blind, Placebo- and Sitagliptin-Controlled, Multi-Center Study to Evaluate Safety and Efficacy of Dutogliptin in Type 2 Diabetes Mellitus Subjects With Moderate and Severe Renal Impairment Including Subjects on Hemodialysis
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2012-02-01Antiviral therapy4区 · 医学
Pharmacokinetics and Antiviral Activity of Phx1766, a Novel HCV Protease Inhibitor, Using An Accelerated Phase I Study Design
4区 · 医学
Article
作者: Reesink, Hendrik W ; Boyea, Teresa ; Li, Xin ; Weegink, Christine J ; Hotho, Daphne M ; de Bruijne, Joep ; Molenkamp, Richard ; Janssen, Harry LA ; Campbell, David ; de Knegt, Robert J ; Li, Jianke ; O'Farrell, A Marie ; van Vliet, Andre ; van de Wetering de Rooij, Jeroen ; Bracken, Michele ; Guler, Hans-Peter ; Schinkel, Janke
Background:
PHX1766 is a novel HCV NS3/4 protease inhibitor with robust potency and high selectivity in replicon studies (50% maximal effective concentration 8 nM). Two clinical trials investigated the safety, tolerability, pharmacokinetics and antiviral activity of PHX1766 in healthy volunteers (HV) and chronic hepatitis C patients, by use of a dose-adaptive overlapping clinical trial design.
Methods:
Two randomized, double-blind, placebo-controlled clinical trials were conducted. Single doses of PHX1766 or placebo were administered to 25 HV and six HCV genotype 1-infected patients (50 mg once daily –1,000 mg once daily, 250 mg twice daily and 100 mg of a new formulation of PHX1766 once daily). Multiple doses of PHX1766 or placebo were administered to 32 HV and seven HCV genotype 1-infected patients (50 mg once daily –800 mg twice daily).
Results:
Oral administration of PHX1766 was safe and well tolerated at all dose levels with rapid absorption (time at which concentration maximum is reached of 1–4 h) and with mean terminal half-lives of 4–23 h. Multiple doses of PHX1766 800 mg twice daily in HCV patients produced an area under the plasma concentration–time curve from time of drug administration to the last time point with a measurable concentration after dosing accumulation ratio of 2.3. The mean maximal observed HCV RNA decline was 0.6 log10 IU/ml in the first 24 h in the single-dose protocol and 1.5 log10 IU/ml after 6 days of PHX1766 dosing.
Conclusions:
An overlapping, dose-adaptive single-dose and multiple-dose escalating design in HV and HCV-infected patients proved to be highly efficient in identifying a therapeutic dose. Although in vitro replicon studies indicated a robust HCV RNA viral decline of PHX1766, the study in HCV patients demonstrated only modest viral load reduction.
2010-08-01Current medical research and opinion4区 · 医学
Evaluation of the potential for pharmacokinetic and pharmacodynamic interactions between dutogliptin, a novel DPP4 inhibitor, and metformin, in type 2 diabetic patients
4区 · 医学
Article
作者: Hans-Peter Guler ; Julie M Cherrington ; Jianke Li ; Teresa Boyea ; Kirsti Klemm ; A Marie O'Farrell ; Sherwyn Schwartz
OBJECTIVE:
Dutogliptin is a novel, orally available, potent, and selective DPP4 inhibitor that improves glycemic control in type 2 diabetic patients. The objective of this study was to evaluate the potential pharmacokinetic and pharmacodynamic interactions, as well as the tolerability, of dutogliptin and metformin alone and in combination in type 2 diabetic patients.
METHODS:
This was a single-center, randomized, open-label, 3-way, crossover study in type 2 diabetic patients. All patients received three treatment regimens, each of 5 days duration in order to reach steady state: 400 mg once daily of dutogliptin (the anticipated clinical dose); 1000 mg metformin twice daily (maximum effective clinical dose); and concomitant administration of 400 mg dutogliptin once daily and 1000 mg metformin twice daily.
RESULTS:
Co-administration of dutogliptin and metformin did not alter the pharmacokinetics of either agent. The geometric mean ratio, GMR (dutogliptin + metformin/dutogliptin) of the area under the plasma concentration-time curve (AUC(0-24h)) at steady state was 0.91 (90% CI: 0.79-1.06; p = 0.29); the GMR of the maximum plasma concentrations (C(max)) was 0.95 (90% CI: 0.76-1.19; p = 0.70); the time to maximum plasma concentrations (T(max)) was essentially the same for dutogliptin with or without metformin. The GMR (dutogliptin + metformin/metformin) of AUC(0-12h) at steady state was 0.99 (90% CI: 0.84-1.17; p = 0.93); the GMR of C(max) was 0.91 (90% CI: 0.79-1.04; p = 0.18); T(max) was comparable for metformin with or without dutogliptin. Metformin added to dutogliptin had no effect on plasma DPP4 inhibition. All three treatment regimens were well tolerated.
CONCLUSIONS:
In this small, multiple dose study, the steady state pharmacokinetics of either dutogliptin or metformin were not altered by co-administration of the two agents. Dutogliptin and metformin were well tolerated either alone or in combination and co-administered metformin did not alter the ex vivo DPP4 inhibition by dutogliptin. There is no need to consider pharmacokinetic and pharmacodynamic interactions when determining the dosage of either agent for co-administration. A phase 3 clinical trial is underway to provide more definitive data on the safety and efficacy of dutogliptin administered on a background of metformin treatment.
2010-04-01Diabetes, obesity & metabolism2区 · 医学
Dutogliptin, a selective DPP4 inhibitor, improves glycaemic control in patients with type 2 diabetes: a 12‐week, double‐blind, randomized, placebo‐controlled, multicentre trial
2区 · 医学
Article
作者: H.‐P. Guler ; A. M. O’Farrell ; H. M. R. Pattzi ; J. Li ; J. M. Cherrington ; C. Bennett ; M. Alpizar ; S. Pitale
Aim: To determine efficacy and tolerability of dutogliptin, a dipeptidyl peptidase 4 (DPP4) inhibitor, in patients with type 2 diabetes mellitus.Methods: This was a 12‐week, multicentre, randomized, double‐blind, placebo‐controlled trial in 423 patients with type 2 diabetes with suboptimal metabolic control. Following a 2‐week single‐blind placebo run‐in, patients aged 18–75 years with a body mass index of 25–48 kg/m2 and baseline HbA1c of 7.3–11.0% were randomized 2:2:1 to receive once‐daily oral therapy with either dutogliptin (400 or 200 mg) or placebo on a background medication of either metformin alone, a thiazolidinedione (TZD) alone or a combination of metformin plus a TZD.Results: Average HbA1c at baseline was 8.4%. Administration of dutogliptin 400 and 200 mg for 12 weeks decreased HbA1c by −0.52% (p < 0.001) and −0.35% (p = 0.006), respectively (placebo‐corrected values), with absolute changes in HbA1c for the 400 mg, 200 mg and placebo groups of −0.82, −0.64 and −0.3%, respectively. The proportion of patients achieving an HbA1c < 7% was 27, 21 and 12% at dutogliptin doses of 400 and 200 mg or placebo, respectively (p = 0.008 for comparison of 400 mg vs. placebo). Fasting plasma glucose (FPG) levels were significantly reduced in both active treatment groups compared to placebo: the placebo‐corrected difference was −1.00 mmol/l (p < 0.001) for the 400 mg group and −0.88 mmol/l (p = 0.003) for the 200 mg group. Dutogliptin caused significantly greater reductions in postprandial glucose AUC 0–2h in both the 400 and 200 mg groups (placebo corrected values −2.58 mmol/l/h, p < 0.001 and −1.63 mmol/l/h, p = 0.032, respectively). In general, patients tolerated the study drug well. There were minor, not clinically meaningful differences in adverse events (AEs) between dutogliptin‐treated patients and placebo controls, and 60% of all reported AEs were mild. Vital signs and body weight were stable, and routine safety laboratory parameters did not change compared with placebo. Trough ex vivo DPP4 inhibition at the end of the 12‐week treatment period was 80 and 70%, at the 400 and 200 mg doses of dutogliptin, respectively.Conclusions: Dutogliptin treatment for 12 weeks improved glycaemic control in patients with type 2 diabetes who were on a background medication of metformin, a TZD or metformin plus a TZD. Tolerability was favourable for both doses tested. The 400 mg dose of dutogliptin resulted in larger changes of HbA1c and FPG and more subjects reached an HbA1c target of < 7% than the 200 mg dose.
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