Pharmacokinetic Study of Oral Marimastat (PKL-021) and Heparin Sodium in Healthy Adult Subjects

1 1 1 1

What is this study about?

The study is being done with healthy adult volunteers, not people who have a specific illness. The investigational medication is a tablet taken by mouth that contains the active ingredient marimastat, which is identified in the trial by the code name PKL-021. A standard intravenous solution of heparin sodium may also be given as part of routine procedures during the study.

The purpose of the trial is to determine the pharmacokinetic profile of the drug, meaning how it is absorbed, distributed, broken down, and cleared from the body, and to see if taking it with food changes any of these processes. Participants will first receive a single dose of the tablet, then after a short break will take the same dose each day for several days. Some doses will be taken with a meal and others on an empty stomach. Throughout the study, blood samples will be collected at several time points to measure drug levels, and safety checks will be performed to monitor how participants feel.

1 initial study visit

you arrive at the study site and read the information about the trial. you sign the consent form to confirm that you understand the procedures.

basic health information is recorded, including your medical history and current medications.

2 baseline assessments

vital signs such as blood pressure, heart rate, and temperature are measured.

blood and urine samples are taken to confirm that you are healthy and meet the study criteria.

3 single oral dose of <b>PKL-021</b>

you swallow one tablet containing 400 mg of marimastat (the active ingredient of PKL-021) with a glass of water.

the tablet is taken by mouth (oral use) and no other medication is taken at the same time.

4 blood sampling after single dose

over the next several hours, small blood samples are drawn at scheduled times to measure how the drug is absorbed, distributed, metabolized, and eliminated from your body.

5 single oral dose with food

on a separate visit you take another 400 mg tablet of PKL-021 after eating a standardized meal.

blood samples are collected in the same way as after the fasting dose to see how food affects the drug’s behavior.

6 multiple oral dosing

you receive the same 400 mg tablet of PKL-021 once each day for a series of consecutive days as defined by the study protocol.

blood is drawn each day after the dose to track the drug’s levels during repeated administration.

7 background intravenous heparin

during the periods when blood is drawn, a low‑concentration solution of heparin sodium (2.4 IU/ml) may be administered intravenously to prevent the blood from clotting.

the heparin is given as an injection (intravenous use) and is not intended as a treatment for you.

8 final safety evaluation

after the last dose, vital signs are checked again and final blood tests are performed.

any side effects or discomfort you experienced during the study are recorded.

Who Can Join the Study?

Be a healthy male or a female who is not pregnant and not breast‑feeding, and be between 18 and 55 years old on the day you sign the consent form.
Do not smoke, or if you used to smoke, you must have stopped at least 6 months before the first dose.
Have a Body Mass Index (BMI) – a measure of weight compared to height – that is between 18.5 and 30.0 kg/m² on the screening day.
Be able to stay in the study for its entire duration and provide written informed consent (a signed agreement that you understand the study and agree to take part).
Be in good health, as shown by your medical history, a physical exam, and normal vital signs (heart rate, blood pressure, and body temperature) and a 12‑lead ECG (a test that records the heart’s electrical activity). Small differences that are not important to your health are allowed.
Have all lab test results (blood work, urine tests, etc.) within the normal range, with only minor, non‑significant differences permitted.
If you are a female who could become pregnant, you must use a highly effective method of birth control for the whole study; male participants must also use birth control during the study.
Be able to speak and understand Czech fluently.

Who Cannot Join the Study?

Having any acute (sudden) or chronic (long‑lasting) illness that could affect the study drug’s safety, how the body handles it (pharmacokinetics), or the results, including problems with muscles, bones, or joints.
Giving or losing at least 500 mL of blood within the past 90 days, or donating plasma or platelets within 14 days before the first dose.
Losing 50–499 mL of blood within the past 30 days before the first dose.
Getting a tattoo, body piercing, or any skin‑penetrating cosmetic procedure within 90 days before screening, unless the doctor decides it will not affect the study.
Testing positive for illegal drugs in a urine test at screening or check‑in.
Testing positive for alcohol on a breath test at screening or check‑in.
Testing positive for nicotine (cotinine) in a urine test at screening.
For women: having a positive pregnancy blood test at screening, a positive urine pregnancy test at check‑in, being breast‑feeding, or not having a pregnancy test result.
Having a body temperature outside the normal range of 35.7 °C to 36.9 °C at screening or check‑in.
Having a sitting blood pressure after 5 minutes of rest that is below 90 mmHg or above 140 mmHg (systolic) or below 60 mmHg or above 90 mmHg (diastolic), or a heart rate outside 50–100 beats per minute during screening.
Having any significant abnormal lab result, including a positive test for hepatitis B surface antigen (HBsAg), hepatitis C virus (HCV), or HIV during screening.
Having a history of serious allergic reactions to any similar product or its inactive ingredients, especially severe reactions like swelling of the face or throat (angioedema).
Having anemia, which means low hemoglobin (below 120 g/L for women or 130 g/L for men) at screening.
Having taken part in another clinical study within the past 30 days.
Having current or past liver disease with abnormal liver blood tests such as high ALT, AST, GGT, bilirubin, low albumin, or abnormal clotting time (prothrombin time).
Having any acute or chronic disease, including problems with the musculoskeletal system (muscles, bones, joints).
Having a history of high blood sugar (hyperglycaemia) or sugar in the urine (glycosuria).
Having current or past thyroid gland disease or thyroid hormone levels outside the normal range, unless the doctor decides it is not important.
Having a mental health condition that would make it difficult to cooperate with the study team.
Abusing drugs, alcohol (40 g or more per day for men, 20 g or more per day for women of pure ethanol), or solvents.
Being unable to avoid foods and drinks that contain methylxanthine (such as coffee, tea, cocoa, cola, energy drinks, chocolate) from 48 hours before each dose until the last blood draw of each study period.
Having a significant illness within 28 days before the first dose, including major surgery.
Taking any over‑the‑counter medicines, vitamins, herbal products (e.g., Saint John’s Wort), or food supplements within 14 days before the first dose.
Taking any prescription medicines within 28 days before the first dose, except for stable hormonal birth control or hormone replacement that has not changed dose for at least 90 days.
Using drugs that are toxic to organs or that strongly affect liver metabolism within 90 days before the first dose.

Where you can join this trial?

Verified and Recommended Sites

No sites found in this category

Verified Sites

No sites found in this category

Other Sites

Site Name	City	Country	Status
Qhtvdziheheqogsk ssrnod	Prague	Czechia

Trial status

Country	Status	Recruitment Start
Czechia	Not recruiting	16.10.2023

Trial locations

Investigated Drugs:

Heparin Sodium

PKL-021 is an oral tablet that contains the active ingredient marimastat. In this study the drug is being given to healthy volunteers to see how it is absorbed, distributed, broken down, and eliminated by the body. The researchers are also checking whether eating food changes how much of the medicine gets into the bloodstream. The purpose is to understand the drug’s behavior when taken once and when taken repeatedly.

Heparin Léčiva Injekční roztok is a solution that contains heparin sodium, a medication that helps prevent blood clots. In this trial it is used as a background treatment, meaning it may be given to participants for safety reasons or as part of standard medical care while the test drug is being studied. It is administered through an IV (intravenous) line.

Trial ID:

2023-506633-30-00

Trial Phase:

Human Pharmacology (Phase I) – Other

Other Trials to Consider

#1 Clinical Trials Search in Europe

Pharmacokinetic Study of Oral Marimastat (PKL-021) and Heparin Sodium in Healthy Adult Subjects

What is this study about?

Who Can Join the Study?

Who Cannot Join the Study?