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Effects of GABAA Receptor Modulation by AP-325 on Insulin Secretion in Patients with Type 2 Diabetes

Phase 2
Completed
Conditions
Type2 Diabetes
Interventions
Drug: Placebo matching AP-325
Registration Number
NCT05160272
Lead Sponsor
The Deutsche Diabetes Forschungsgesellschaft e.V.
Brief Summary

The aim of this single-center, prospective, randomized, double-blind, placebo-controlled, 2-arm parallel-group interventional study is to investigate the effect of 4-week treatment with AP-325 on C-peptide release as measure of insulin secretion compared to placebo in type 2 diabetes (T2D) patients.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
38
Inclusion Criteria
  • Diagnosis of T2D
  • Age between 25 and 75 years
  • HbA1c ≥6.5 and ≤9.5 %
  • BMI ≤ 45 kg/m2
  • Treatment-naive or stable antihyperglycemic therapy with metformin, α-glucosidase-inhibitor and/or SGLT2 inhibitor
  • Ability to give consent
Exclusion Criteria
  • Acute infections (hsCRP > 5mg/dl, body temperature >37.5°C)
  • Insulin therapy or treatment with sulfonylureas, glinides, GLP-1 receptor agonists, thiazolidinediones; current treatment with DPP-4 inhibitors or during the 4 weeks prior to baseline examination
  • Uncontrolled hyperglycemia, e.g. fasting blood glucose >240 mg/dl
  • Heart rate <50 or >100 beats per minute; systolic blood pressure <100 or >160 mmHg; diastolic blood pressure <50 or >100 mmHg; uncontrolled hypertension
  • Creatinine clearance <60 ml/min (eGFR by MDRD formula)
  • Severe chronic illnesses, such as congestive heart failure (NYHA III/IV), liver insufficiency (Child-Pugh Class B/C), history of acute coronary syndrome, stroke
  • Anemia (Hb <12 g/l for men, Hb <11 g/l for women)
  • Participation in another intervention study within 2 months before the examination
  • Hypersensitivity against AP-325, placebo or other ingredients of IMP
  • Immunocompromising diseases
  • Immunomodulatory drugs (e.g. oral cortisone preparations, biologicals)
  • Thyroid diseases with an unstable metabolic state (change in L-thyroxine dose within the past 6 weeks, TSH and fT4 outside the normal range)
  • Planned pregnancy, pregnant or lactating women, positive pregnancy test, and woman of childbearing potential not using two adequate methods of contraception, including a barrier method and a highly efficacious non-barrier method
  • Past (≤ 5 years) or current history of psychiatric disorders, including psychiatric depression
  • HIV, hepatitis B or C disease
  • Previous / current alcohol and / or drug abuse
  • Malignant cancer
  • BIA and MR-incompatible metal or magnetic implants, devices or objects inside of or on the body, claustrophobia
  • Treatment with the following drug groups or agents:

Anticoagulant drugs (exception: acetylsalicylic acid 100 mg/day), dihydropyridines (e.g. nifedipine, amlodipine), azilsartan, losartan and irbesartan, celecoxib; if applicable, other drugs that are predominantly metabolized by CYP2C9

  • Inhibitors or inducers of CYP2C9, CYP3A4, such as amiodarone, verapamil, rifampicin
  • Poor CYP2C9 metabolizer

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Placebo TreatmentPlacebo matching AP-325Placebo matching AP-325 film-coated tablet, once daily
AP-325 TreatmentAP-325AP-325, film-coated tablet, 50mg once daily
Primary Outcome Measures
NameTimeMethod
Circulating C-peptide by iAUC of C-peptide during an IVGTT4 weeks

Change in circulating C-peptide levels from baseline to end of intervention measured by iAUC of C-peptide during an IVGTT until 60th minute (second phase) with AP-325 compared to placebo

Secondary Outcome Measures
NameTimeMethod
iAUC of circulating insulin (AIR) (first 10 min)4 weeks

Change in iAUC of circulating insulin (AIR) during an IVGTT in the first 10 minutes from baseline to end of treatment

iAUC of C-peptide level (overall)4 weeks

Change in C-peptide level during an IVGTT from baseline to end of treatment

disposition index (DI)4 weeks

Change in the disposition index (DI) through Minimal Model during an IVGTT from baseline to end of treatment

Ctrough-ss (Day 28) and the change from baseline to Day 284 weeks

Change in relationship between Ctrough-ss (Day 28) and the change from baseline to Day 28 in primary and secondary endpoints

fructosamine levels III4 weeks

Change in fasting blood glucose from baseline to end of treatment

Plasma concentrations of AP-3254 weeks

Change in Plasma concentrations of AP-325 at 1 hour post-dose on Days 1 and 28; pre-dose on Days 4 and 28. Accumulation of Ctrough from Day 4 to Day 28

Basal insulin level4 weeks

Change in basal insulin level from baseline to end of treatment

C-peptide level4 weeks

Change in C-peptide level from baseline to end of treatment

Glucose level4 weeks

Change in glucose level from baseline to end of treatment

iAUC of glucose level (overall)4 weeks

Change in iAUC of glucose level during an IVGTT from baseline to end of treatment

fructosamine levels4 weeks

Change in 1.5-Anhydroglucitol glucose from baseline to end of treatment

iAUC of circulating insulin (overall)4 weeks

Change in iAUC of circulating insulin during an IVGTT from baseline to end of treatment

iAUC of C-peptide (first 10 min)4 weeks

Change in iAUC of C-peptide during an IVGTT in the first 10 minutes from baseline to end of treatment

iAUC of glucose (first 10 min)4 weeks

Change in iAUC of glucose during an IVGTT in the first 10 minutes from baseline to end of treatment

insulin secretion rate (ISR)4 weeks

Change in insulin secretion rate (ISR) during an IVGTT from baseline to end of treatment

fructosamine levels II4 weeks

Change in fructosamine level from baseline to end of treatment

peak insulin response4 weeks

Change in peak insulin response during an IVGTT from baseline to end of treatment

Trial Locations

Locations (1)

German Diabetes Center

🇩🇪

Duesseldorf, NRW, Germany

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