Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
| Name | Class |
|---|---|
| National Center for Research and Development, Poland | OTHER |
Not provided
Not provided
Not provided
Not provided
The planned study is to determine the safety and pharmacokinetic properties of CPL207280 compound after single and multiple (two weeks) administration in healthy volunteers.
This is to be one-centre, single ascending dose and double-blind multiple ascending dose two part study of CPL207280 compound in healthy volunteers. PART A is a single dose, open-label part with CPL207280 compound administered with dose escalation between cohorts.Additionaly assessing the effect of food and effect of metformin on bioavailability of CPL207280 is to be done in additional cohort. PART B is a multiple, double-blind part with CPL207280 compound administered for 14 days with dose escalation between cohorts. Participants in this part are to be randomized to receive Investigational Medicinal Product (IMP) or placebo in 3:1 ratio. Safety and pharmacokinetic properties of CPL207280 compound is to be determined following different doses in single oral IMP administration in PART A and different doses of IMP administered orally for two weeks in PART B.
Not provided
Not provided
Not provided
Not provided
Not provided
| Label | Type | Description | Intervention Names |
|---|---|---|---|
| CPL207280 | Experimental | PART A: 8 cohorts are to receive single dose of IMP.Each participant is to take single dose of IMP. There is to be dose escalation between cohorts. PART B: 4 cohorts are to receive multiple dose of IMP. Each participant is to take IMP once daily for 14 days. There is to be dose escalation between cohorts. |
|
| Placebo | Placebo Comparator | PART B: 2 Participants from each of 4 cohorts (total of 8 participants) are to receive masking placebo tablet once daily for 14 days. There is to be dose escalation between cohorts. Participants are to be randomized within cohorts. |
|
| CPL207280 120 mg + Metformin 750 mg | Experimental | 1 cohort (total of 12 participants) are to receive single dose of IMP in fed and fasted state, IMP with metformin and metformin alone to assess the effect of food and metformin on bioavailability of CPL207280. There is to be one week wash-out between four treatments periods for this cohort. |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| CPL207280 | Drug | IMP is a tablet with CPL207280 as an Active Pharmaceutical Ingredient (API). |
|
| Measure | Description | Time Frame |
|---|---|---|
| Determination of maximum tolerated dose (MTD) or administration of the maximum dose provided in the protocol after single and multiple oral administration of IMP. | MTD is defined as the highest dose for which no more than 1 of the 6 treated volunteers (less than 1/3) exhibits dose limiting toxicity (DLT). | up to 48 hours after single administration of IMP in PART A and up to 48 hours after the last IMP administration in PART B |
| Safety and tolerability of IMP after single and multiple oral administration | Participants during hospitalization are to be closely observed to assure maximal safety and to collect occurrence of all adverse event. To follow-up on all study participants telephone calls with a request for information regarding their health condition are to be made. | up to 14 days in PART A and up to 28 days in PART B of the study |
| Measure | Description | Time Frame |
|---|---|---|
| Cmax - maximum plasma concentration | The maximum concentration of the CPL207280 compound in plasma after IMP administration, obtained directly from the measured concentrations. | up to 48 hours after administration of IMP in PART A and up to 24 hours after the IMP administration determined on Day 1, 8 in PART B and up to 48 hours after the last IMP administration on Day 14 in PART B |
Not provided
Inclusion Criteria:
Exclusion Criteria:
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| BioResearch Group Sp. z o.o. | Kajetany | Nadarzyn | 05-830 | Poland |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 34349026 | Derived | Bazydlo-Guzenda K, Buda P, Matloka M, Mach M, Stelmach F, Dzida R, Smuga D, Hucz-Kalitowska J, Teska-Kaminska M, Vialichka V, Dubiel K, Kaminska B, Wieczorek M, Pieczykolan J. CPL207280, a Novel G Protein-Coupled Receptor 40/Free Fatty Acid Receptor 1-Specific Agonist, Shows a Favorable Safety Profile and Exerts Antidiabetic Effects in Type 2 Diabetic Animals. Mol Pharmacol. 2021 Oct;100(4):335-347. doi: 10.1124/molpharm.121.000260. Epub 2021 Aug 4. |
Not provided
Not provided
Not provided
| ID | Term |
|---|---|
| C000721547 | CPL207280 |
| D008687 | Metformin |
| ID | Term |
|---|---|
| D001645 | Biguanides |
| D006146 | Guanidines |
| D000578 | Amidines |
| D009930 | Organic Chemicals |
Not provided
Not provided
Not provided
Not provided
Not provided
Only PART B will be double-blind
| Placebo | Drug | matching placebo tablet |
|
| Metformin hydrochloride 750 mg | Drug | IMP is a tablet with Metformin hydrochloride as an Active Pharmaceutical Ingredient (API). |
|
|
| AUC(0-48) - area under the plasma concentration - time curve from time 0 to 48h after IMP administration | The AUC(0-48) is a measure of total plasma exposure to the drug from time point zero to 48 hours after IMP administration | up to 48 hours after administration of IMP in PART A and after the IMP administration determined on Day 14 in PART B |
| AUC(0-24) - area under the plasma concentration - time curve from time 0 to 24h after IMP administration | The AUC(0-24) is a measure of total plasma exposure to the drug from time point zero to 24 hours after IMP | up to 24 hours after administration of IMP in PART A and up to 24 hours after the IMP administration determined on Day 1 and 8 in PART B |
| AUC(0-inf) - area under the plasma concentration - time curve from time 0 to infinity time | The AUC(0-inf) is a measure of total plasma exposure to the drug from time point zero extrapolated to infinity. | up to 48 hours after administration of IMP in PART A and up to 24 hours after the IMP administration determined on Day 1, 8 in PART B and up to 48 hours after the last IMP administration on Day 14 in PART B |
| Tmax - time to reach maximum concentration | The Tmax is time to reach the maximum plasma concentration (Cmax), obtained directly from the actual sampling times. | up to 48 hours after administration of IMP in PART A and up to 24 hours after the IMP administration determined on Day 1, 8 in PART B and up to 48 hours after the last IMP administration on Day 14 in PART B |
| Kel - terminal elimination rate constant | Kel is to be estimated via linear regression of time versus log of concentration. | up to 48 hours after administration of IMP in PART A and up to 24 hours after the IMP administration determined on Day 1, 8 in PART B and up to 48 hours after the last IMP administration on Day 14 in PART B |
| T1/2 - The plasma elimination half-life | T1/2 is to be calculated as 0.693/Kel. | up to 48 hours after administration of IMP in PART A and up to 24 hours after the IMP administration determined on Day 1, 8 in PART B and up to 48 hours after the last IMP administration on Day 14 in PART B |
| C (1,t) - CPL207280 concentration | The concentration of CPL207280 on day t before product administration. | Determined on Day 2, 3, 4, 5, 6, 7, 9, 10, 11, 12 and 13 in PART B |
| C (Tmax, t) - CPL207280 concentration | The concentration on day t measured on time Tmax which was calculated in PART A of the study. | Determined on Day 2, 3, 4, 5, 6, 7, 9, 10, 11, 12 and 13 in PART B |
| Glucose AUEC -area under the effect-time curve after IMP administration | The AUEC is a measure of total glucose concentration from time point zero to 6 hours after IMP | up to 6 hours after administration of IMP in PART A and up to 6 hours after the IMP administration determined on Day 1, 8,14 in PART B |
| Insulin AUEC -area under the effect-time curve after IMP administration | The AUEC is a measure of total insulin concentration from time point zero to 6 hours after IMP | up to 6 hours after administration of IMP in PART A and up to 6 hours after the IMP administration determined on Day 1, 8,14 in PART B |
| Proinsulin AUEC -area under the effect-time curve after IMP administration | The AUEC is a measure of total proinsulin concentration from time point zero to 6 hours after IMP | up to 6 hours after administration of IMP in PART A and up to 6 hours after the IMP administration determined on Day 1, 8,14 in PART B |
| C-peptide AUEC -area under the effect-time curve after IMP administration | The AUEC is a measure of total c-peptide concentration from time point zero to 6 hours after IMP | up to 6 hours after administration of IMP in PART A and up to 6 hours after the IMP administration determined on Day 1, 8,14 in PART B |
| Glucagon AUEC -area under the effect-time curve after IMP administration | The AUEC is a measure of total glucagon concentration from time point zero to 6 hours after IMP | up to 6 hours after administration of IMP in PART A and up to 6 hours after the IMP administration determined on Day 1, 8,14 in PART B |
| AUC(0-tau, t)- area under the curve of plasma concentration vs time, from time point zero up to the time of 24h in day t | AUC(0-tau, t) will be calculated according to the linear trapezoidal rule | up to 24 hours after administration of IMP in PART A and up to 24 hours after the IMP administration determined on Day 1, 8 and 14 in PART B |
| Cav,t, averate IMP concentration on day t | Cav,t, will be calculated as AUC(0-tau, t)/24h. | up to 24 hours after administration of IMP in PART A and up to 24 hours after the IMP administration determined on Day 1, 8 and 14 in PART B |
| Fluctuation | Fluctuation will be calcilated as a difference between C(Tmax,t) and C(1,t) relative to the Cav,t, calculated as (C(Tmax,t)-C(1,t))/Cav,t x 100%. | up to 24 hours after administration of IMP in PART A and up to 24 hours after the IMP administration determined on Day 1, 8 and 14 in PART B |