Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
GSK189075 · 11 trials · 5 indications
Data for number of participants who presented one or more adverse events (serious or non serious) was reported. An AE was defined as any untoward medical occurrence (MO) in a participant temporally associated with the use of a medicinal product (MP), whether or not considered related to the MP and can therefore be any unfavourable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with its use. The SAE was any untoward MO that, at any dose, results in death, life threatening, persistent or significant disability/incapacity, results in or prolongs inpatient hospitalization, congenital abnormality or birth defect, that may not be immediately life-threatening or result in death or hospitalization but may jeopardize the participant or may require medical or surgical intervention to prevent one of the other outcomes listed in this definition.
A hypoglycemic event was defined as symptoms of hypoglycemia confirmed by a blood glucose value below normal limits \[less than 3.89 millimoles per liter (mmol/L)\] or 70 milligrams per deciliter (mg/dL). Symptoms of hypoglycemia without confirmed blood glucose values were reported as AEs instead of hypoglycemic events. Number of participants with hypoglycemic events were reported.
SBP and DBP were obtained during each treatment period at the indicated time points. Measurements were made with the participant lying semi-recumbent having rested in this position for at least 10 minute before the initial reading.
Heart rate was obtained during each treatment period at indicated time points. Measurements were made with the participants lying semi-recumbent having rested in this position for at least 10 minutes before the initial reading.
Standard semi-recumbent 12-lead ECG was obtained after the participant rested for a minimum of 10 minutes (If questionable abnormality was noted on the ECG, 2 more measurements were allowed to provide an average of 3 measurements). Number of participants with abnormal ECG were reported.
Clinical Chemistry data for parameters: Alanine Amino Transferase (ALT), Albumin, Alkaline Phosphatase (ALP), Aspartate Amino Transferase (AST), Bicarbonate, Calcium, Chloride, Creatine Kinase, Creatinine, Gamma Glutamyl Transferase (GGT), Glucose, Lactate Dehydrogenase, Magnesium, Phosphorus, Potassium, Total Bilirubin, Sodium, Total protein, triglycerides and urea/BUN was reported. Data for number of participants with abnormal clinical Chemistry data was presented.
Data for abnormal Hematology parameters: Basophils, Eosinophils, Hematocrit, Hemoglobin, Lymphocytes, Mean Corpuscle Hemoglobin (MCH), Mean Corpuscle Volume (MCV), Monocytes, Platelet count, Red Blood Cell (RBC), Reticulocytes, Total Neutrophils, White Blood Cell (WBC) were reported. Data for number of participants with abnormal Hematology were reported.
Urine sample was collected at screening, Day -2 (18:00h) and Day 1 (7:45h) for determination of urine osmolality which was measured in Millimole per kilogram (mmol/kg).
Creatinine clearance was calculated and reported in Milliliters per minute (mL/min) on Day 1 of each period for each collection interval 0-4, 4-8, 8-12, 12-16 and 16-24 hour, as well as the combined intervals of 0-12 and 0-24 hour. For urine measurements, participants were instructed to void within 30 minutes before administration of study medication.
On Day 1, fluid intake, urine volume and number of micturations were recorded over the intervals for each of the following dosing periods: 0-4h, 4-8h, 8-12h, 12-16h and 16-24h. From these measures, fluid balance was calculated over the 24-hour period. Fluid Balance=total fluid intake minus total urine volume. The 0-24h amounts of total Fluid Intake, total urine output, and fluid balance were calculated by adding the amounts collected during these time intervals.
The plasma measurements at specified time points on Day 1 were collected. Derived plasma glucose parameters were presented.
The blood samples were collected at Baseline, Week 4, Week 8 and at Week 12 (or early withdrawal). Baseline was defined as the period immediately preceding treatment with study medication (Week 0). For participants with missing Baseline assessment, the last pre-therapy value prior to the Baseline visit was used as the Baseline value. Change from Baseline was the value at Week 12 minus Baseline value. The primary analysis was performed on the Intent-to-Treat (ITT) Population with Last observation carried forward (LOCF). Adjusted mean is presented as least square (LS) mean.
Fasted blood samples for HbA1c were collected at Baseline and Week 12. Participants were required to fast for at least 8 hours prior to laboratory samples and were told not to take the morning dose of study medication on these visit days and to refrain from eating until instructed to do so by study personnel in the clinic. When the participant had not fasted, the participant was rescheduled to return to the clinic to have a fasted sample taken. Baseline was Week 0. Change from Baseline was calculated by subtracting Baseline values from post-Baseline values. Only those participants with a value at Baseline and at Week 12 (after Last Observation Carried Forward \[LOCF\]) were used for this analysis. Adjusted mean is presented as least square mean.
| Arm | Type | Description |
|---|---|---|
| Arm a | EXPERIMENTAL | GSK189075 |
| Arm b | PLACEBO_COMPARATOR | Placebo |
| GSK189075 | EXPERIMENTAL | Participants will receive GSK189075 for 12 weeks |
| Placebo | PLACEBO_COMPARATOR | Participants will receive GSK189075 matching Placebo for 12 weeks |
| Arm 1 | EXPERIMENTAL | GSK189075 |
| Arm 2 | PLACEBO_COMPARATOR | Placebo |
| Arm 3 | OTHER | pioglitazone (active control) |
| Subjects receiving treatment sequence 1 | EXPERIMENTAL | Eligible subjects will receive treatment A in period 1, treatment B in period 2 and treatment C in period 3. A= Bupropion SR + GSK189075 placebo, B= Bupropion SR placebo + GSK189075 and C= Bupropion SR + GSK189075 |
| Subjects receiving treatment sequence 2 | EXPERIMENTAL | Eligible subjects will receive treatment B in period 1, treatment C in period 2 and treatment A in period 3. A= Bupropion SR + GSK189075 placebo, B= Bupropion SR placebo + GSK189075 and C= Bupropion SR + GSK189075 |
| Subjects receiving treatment sequence 3 | EXPERIMENTAL | Eligible subjects will receive treatment C in period 1, treatment A in period 2 and treatment B in period 3. A= Bupropion SR + GSK189075 placebo, B= Bupropion SR placebo + GSK189075 and C= Bupropion SR + GSK189075 |
| Subjects receiving treatment sequence 4 | EXPERIMENTAL | Eligible subjects will receive treatment A in period 1, treatment C in period 2 and treatment B in period 3. A= Bupropion SR + GSK189075 placebo, B= Bupropion SR placebo + GSK189075 and C= Bupropion SR + GSK189075 |
| Subjects receiving treatment sequence 5 | EXPERIMENTAL | Eligible subjects will receive treatment B in period 1, treatment A in period 2 and treatment C in period 3. A= Bupropion SR + GSK189075 placebo, B= Bupropion SR placebo + GSK189075 and C= Bupropion SR + GSK189075 |
| Subjects receiving treatment sequence 6 | EXPERIMENTAL | Eligible subjects will receive treatment A in period 1, treatment C in period 2 and treatment B in period 3. A= Bupropion SR + GSK189075 placebo, B= Bupropion SR placebo + GSK189075 and C= Bupropion SR + GSK189075 |
| Subjects receiving treatment P | PLACEBO_COMPARATOR | Eligible subjects will receive placebo twice daily along with metformin twice daily for 13 days. |
| Subjects receiving treatment A | EXPERIMENTAL | Eligible subjects will receive GSK189075 500 milligrams twice daily along with metformin twice daily for 13 days. |
| Subjects receiving treatment B | EXPERIMENTAL | Eligible subjects will receive GSK189075 750 milligrams twice daily along with metformin twice daily for 13 days. |
| Mild renal impairmnent | OTHER | - |
| moderate renal impairment | OTHER | - |
| Normal renal function | OTHER | - |
| Brevicon | OTHER | Oral contraceptive used to determine pharmacokinetics when given with GSK189075 to look for interaction. |
| Name | Type | Description |
|---|---|---|
| GSK189075 | DRUG | investigational drug |
| placebo | DRUG | placebo comparator |
| pioglitazone | DRUG | Active Control |
| GSK189075 oral tablets | DRUG | - |
| GW869682 oral tablets | DRUG | - |
| Bupropion | DRUG | Bupropion will be available as sustained release film-coated tablets with a dose of 150 milligrams administered orally. |
| Metformin | DRUG | Metformin will be available as an immediate release oral tablet with dosing strengths of 500 milligrams and 850 milligrams. |
| Brevicon | DRUG | Given with GSK189075 to determine if GSK189075 exerts an effect on GSK189075 PK. |
| metformin tablets | DRUG | - |
Inclusion Criteria: * Adult male/female, 18 to 55 years old * Diagnosis of type 1 diabetes mellitus for at least 6 months; and using a continuous insulin pump * Willing and able to follow all study-related instructions provided by the site staff. * Willing to provide signed informed consent. Exclu...
GSK189075 is an investigational small molecule being developed for the treatment of Type 2 Diabetes Mellitus. It is also being studied in patients with Type 1 Diabetes Mellitus. The drug is in Phase 2 clinical development and is being evaluated for its effects on blood sugar control in diabetic patients.
GSK189075 is being developed by GSK plc, a global pharmaceutical company listed on the stock exchange under the ticker symbol GSK. The company is conducting clinical trials to evaluate the safety and efficacy of this investigational drug for the treatment of diabetes mellitus.
GSK189075 is currently in Phase 2 clinical development. It has completed five clinical trials with a total enrollment of 706 participants. All five trials have been completed, and no active trials are currently ongoing for this investigational drug.
GSK189075 has been studied in five completed clinical trials, including NCT00376038, NCT00501462, NCT00504816, and NCT00532610. These trials evaluated drug interactions with metformin, blood levels in patients with normal and reduced kidney function, effects on oral contraceptive pharmacokinetics, and effects on heart rhythm compared to placebo and moxifloxacin.
GSK189075 is not FDA approved. It is an investigational drug currently in Phase 2 clinical development for the treatment of Type 2 Diabetes Mellitus. The drug has completed several Phase 1 trials, but it has not yet received regulatory approval from the FDA or any other health authority.
The specific molecular target and mechanism of action for GSK189075 have not been disclosed in available clinical trial information. The drug is being studied for its ability to manage blood glucose levels in patients with Type 2 Diabetes Mellitus, but its precise pharmacological action remains under investigation.