Safety and Pharmacokinetics Study of CPL207280 Compound in Healthy Volunteers.

NCT04622111 | Completed Phase 1

• 1 other identifier: 01GPR2019
• Study Type: interventional
• Target: 68
• Locations: 1 country
• Sites: 1

Brief Summary

The planned study is to determine the safety and pharmacokinetic properties of CPL207280 compound after single and multiple (two weeks) administration in healthy volunteers.

Conditions

Healthy Volunteers

Outcome Measures

Primary Outcomes (2)

• 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

Secondary Outcomes (17)

• Cmax - maximum plasma 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

• AUC(0-48) - area under the plasma concentration - time curve from time 0 to 48h 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

  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

  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

  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

Study Arms (3)

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.

Drug: CPL207280

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.

Drug: Placebo

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.

Drug: CPL207280; Drug: Metformin hydrochloride 750 mg

Interventions

CPL207280 DRUG

IMP is a tablet with CPL207280 as an Active Pharmaceutical Ingredient (API).

CPL207280; CPL207280 120 mg + Metformin 750 mg

Placebo DRUG

matching placebo tablet

Placebo

Metformin hydrochloride 750 mg DRUG

IMP is a tablet with Metformin hydrochloride as an Active Pharmaceutical Ingredient (API).

Also known as: Glucophage XR 750 mg

CPL207280 120 mg + Metformin 750 mg

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Caucasian female or male
• Body-mass index (BMI): ≥ 18.5 kg/m² and \< 29.9 kg/m²,
• Physical examination without any clinically relevant abnormality,
• Clinical laboratory results in hematology or renal/hepatic test and clinical laboratory results in other tests without any clinically relevant abnormalities as assessed by Investigator,
• Non-smoker and non-user of tobacco products for at least 3 months before screening,
• Subject able to provide written informed consent after receiving information about the trial,
• Informed Consent Form signed and dated prior to Screening evaluations,
• Ability and willingness to comply with the requirements of the study protocol,
• Volunteer (or his/her partner) of childbearing potential willingness to use acceptable forms of contraception.

You may not qualify if:

• Known allergy, hypersensitivity, intolerance or contraindication to other drugs similar in structure or class to CPL207280 compound, or to any excipients of the formulation,
• Any known significant current or past acute or chronic disease or condition of the: circulatory, respiratory, hematopoietic, endocrine, nervous and musculoskeletal system, alimentary and urinary tracts, allergic disease, genetic or psychiatric disorder that could influence the present general health condition, at the Investigator's discretion,
• A long QT interval analysis syndrome (in the interview) or is under the treatment with antiarrhythmic drugs,
• Current disease of the alimentary tract, liver or kidneys that may influence absorption, distribution and/or elimination of the studied drug, as assessed by the Investigator and documented in the medical history,
• Medical condition that requires administration of other drugs or use of any drug within the 4 weeks preceding the first IMP administration and during the entire study. Drugs commonly used with fast metabolism may be administered and is up to Investigator discretion (i.e. pain killers),
• Participation in other clinical trials, where at least one dose of study drug was administered, within 90 days preceding the screening phase,
• Positive results from pregnancy test in female volunteers,
• Lactation in female volunteers,
• Hypotension or hypertension in medical history,
• Narcotic and alcohol addiction or abuse,
• Positive results of HBsAg, anti-HCV or anti-HIV tests,
• Positive drug screen or alcohol breath tests,
• Subjects who adhere to a special diet (e.g. low calories, vegetarian,etc.).

Sponsors & Collaborators

• Celon Pharma SA: lead
• National Center for Research and Development, Poland: collaborator

Study Sites (1)

BioResearch Group Sp. z o.o.

Kajetany, Nadarzyn, 05-830, Poland

Location

Related Publications (1)

• 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.

  PMID: 34349026 DERIVED

MeSH Terms

Interventions

CPL207280; Metformin

Intervention Hierarchy (Ancestors)

Biguanides; Guanidines; Amidines; Organic Chemicals

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Who Masked: PARTICIPANT, INVESTIGATOR
• Masking Details: Only PART B will be double-blind
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: November 6, 2020
• First Posted: November 9, 2020
• Study Start: May 27, 2020
• Primary Completion: April 1, 2021
• Study Completion: May 5, 2021
• Last Updated: August 18, 2021

Record last verified: 2021-05

Locations

PL (1)