Bioequivalence Study of Tofacitinib 10 mg Film-Coated Tablets in Healthy Volunteers

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What is this study about?

The study involves healthy volunteers and evaluates two oral tablets that contain the medication Tofacitinib, one marketed as XELJANZ. The aim is to show that the test tablet and the marketed tablet deliver the drug to the body in the same way, a concept known as bioequivalence, meaning they are expected to work similarly and be equally safe.

Participants will take a single dose of one tablet while fasting, then after a short break will take the other tablet under the same conditions. Blood samples will be collected to measure how much drug appears in the bloodstream, including the highest level reached (Cmax), the overall exposure over time (AUC), the time to reach the highest level (tmax), and how quickly the drug level falls (half‑life). Throughout the study, volunteers will be observed for any side effects or abnormal lab results, and vital signs will be checked regularly.

1 enrollment and consent

after joining the study you will sign a consent form that explains what will happen during the trial and confirms that you agree to participate.

your personal information will be recorded and you will be assigned a unique study number.

2 randomization to treatment sequence

the study team will assign you to one of two possible sequences: test tablet first then reference tablet, or reference tablet first then test tablet.

the assignment is done randomly so that the order is not predictable.

3 fasting before the first dose

you must not eat or drink anything except water for at least ten hours before taking the study medication.

this fasting period ensures that food does not affect how the medicine is absorbed.

4 first single dose administration

under supervision you will swallow one 10 mg film‑coated tablet of the assigned product (test or reference) with a small amount of water.

the tablet is taken orally and is the only medication given during this period.

5 post‑dose blood sampling

after the dose you will remain at the clinic for a series of blood draws that may last up to 24 hours.

the samples are collected at several time points to measure the amount of tofacitinib in your blood.

the exact timing of each draw is scheduled by the study staff.

6 monitoring for safety

during the blood‑sampling period you will be observed for any signs of discomfort, side effects, or abnormal laboratory results.

any adverse event, which means an unwanted medical occurrence, will be recorded and evaluated.

7 washout period

after the first dosing period you will have a washout interval during which no study medication is taken.

the length of this interval is defined by the study protocol to allow the first dose to leave your body completely before the next dose.

8 fasting before the second dose

similar to the first period, you must fast for at least ten hours before receiving the second tablet.

no food or drink, except water, is allowed during this time.

9 second single dose administration

you will take the other tablet (if you received the test tablet first, you now receive the reference tablet, and vice versa).

the dose is again one 10 mg film‑coated tablet taken orally with water.

10 second post‑dose blood sampling

the same series of blood draws as in step 5 will be performed after the second dose.

these samples allow comparison of how the two tablets are absorbed and processed by your body.

11 final safety assessment and study completion

after the second sampling period you will undergo a final check for any adverse events or abnormal test results.

once the study staff confirm that all required procedures are finished, your participation in the trial ends.

Who Can Join the Study?

Free written informed consent must be given before any study procedures; this means signing a document after understanding what will happen in the trial.
Must be a non‑smoker or have stopped using tobacco or nicotine products for at least 3 months before the screening visit.
Must be willing to follow all study procedures and any restrictions that are part of the trial.
Women are eligible if they either cannot become pregnant (non‑childbearing potential) or, if they can become pregnant, they agree to use an approved contraceptive method from at least 4 weeks before the first dose until at least 4 weeks after the last dose.
Must be between 18 and 55 years old (inclusive) at the time of signing the consent.
Must have a body mass index (BMI) between 18.5 and 30.0 kg/m²; BMI is a calculation that compares weight to height to assess whether weight is in a healthy range.
Must have no clinically relevant diseases noted in the medical history.
Must have no clinically relevant abnormalities found during the physical examination.
Must have a normal 12‑lead ECG, which is a test that records the heart’s electrical activity.
Must have normal results on standard clinical laboratory tests (blood and urine checks).
Must have a negative result from the IGRA test, a blood test that screens for certain tuberculosis infections.
Must test negative for anti‑HIV antibodies, Hepatitis B surface antigen, and anti‑Hepatitis C antibodies, which are tests for HIV, Hepatitis B, and Hepatitis C infections.

Who Cannot Join the Study?

Known allergy to the study drug or any of its inactive ingredients.
History of frequent infections.
Lived or traveled to areas where tuberculosis or certain fungal infections are common within the last 3 months, or have a condition that makes infections more likely.
History of blood clots (such as deep‑vein clot, lung clot, or artery clot) or risk factors for clotting (like inherited clotting disorders or autoimmune diseases that increase clot risk).
History of serious heart problems such as a heart attack (myocardial infarction) or stroke.
History of any cancer (malignancy).
Family history of sudden death before age 40.
Resting blood pressure (systolic or diastolic) outside the normal range.
Low hemoglobin (the protein in red blood cells that carries oxygen) below normal.
Low neutrophil count (a type of white blood cell that fights infection) below normal.
Low lymphocyte count (another white‑blood‑cell type) below normal.
Known severe allergy to any other medication.
Liver enzymes (ALT or AST) higher than normal, indicating possible liver issues.
Kidney function (creatinine clearance) below normal, measured by a specific calculation.
Total cholesterol higher than the normal upper limit.
Positive IGRA test (a blood test for tuberculosis infection).
Positive test for illegal drugs, nicotine (cotinine), or alcohol.
Planned receipt of live or weakened vaccines during the study or within two months after it.
Received a long‑acting injection or implant of any drug in the past 6 months.
Drinks more than 14 alcoholic drinks per week (men) or more than 7 per week (women) in the past 6 months.
Consumes more than about 500 mg of caffeine each day (found in coffee, tea, cola, chocolate, etc.).
Participated in another clinical trial in the past 2 months.
Has rare inherited problems with processing certain sugars (galactose intolerance, lactose deficiency, or glucose‑galactose malabsorption).
Participated in more than two clinical trials in the past 12 months.
Donated blood or lost a large amount of blood (≥ 450 mL) or had plasma exchange in the past 2 months.
Cannot fast or follows a special diet (e.g., lactose‑free, vegan, low‑fat, low‑salt) that would interfere with the study meals.
Veins in both arms unsuitable for drawing blood or giving an IV.
Difficulty swallowing pills or capsules.
If able to become pregnant, a positive pregnancy test (blood).
If female, is currently breast‑feeding.
Any other condition that the investigator believes makes participation unsafe.
Recent illness, condition, or treatment that could put the person at risk or affect how the drug is processed.
Use of prescription or over‑the‑counter medicines (including vitamins, supplements, herbs such as St John’s Wort) in the past 2 weeks unless the investigator says they are safe.
Any gastrointestinal, kidney or liver disease or surgery (such as ulcer, inflammatory bowel disease, pancreatitis, gallbladder removal, stomach removal) that could change how the drug works or affect safety.
Consumption of pineapple, Seville oranges, pomelo, pomegranate, starfruit, or grapefruit (fresh, canned, or frozen) in the past week.
Use of medicines that strongly block or increase the activity of the enzyme CYP3A4 (examples include ketoconazole, itraconazole, erythromycin, clarithromycin, barbiturates, phenytoin, carbamazepine, rifampicin, etc.) in the past 4 weeks.
History of gastrointestinal perforation or diverticulitis.
History of diabetes mellitus.
Active or past tuberculosis.
Current infection, even if it is localized to one area of the body.
History of a serious or opportunistic infection.

Where you can join this trial?

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Site Name	City	Country	Status
Bsrsdvaxvniz Iufxcnwydnci E Dichnglmjrigxnf Eb Sddgv Lawo	Porto	Portugal

Trial status

Country	Status	Recruitment Start
Portugal	Not recruiting	10.01.2024

Trial locations

Investigated Drugs:

Tofacitinib

Tofacitinib is an oral tablet that contains the active ingredient tofacitinib. In this study it is the test product, meaning it is a version being examined to see if it works the same way as the approved brand. Participants take the tablet by mouth after fasting, and the researchers measure how much of the drug gets into the bloodstream and how quickly it is cleared. The goal is to show that this test tablet behaves in the same way as the reference product.

XELJANZ is the brand-name oral tablet that also contains tofacitinib. It is used in the trial as the comparator, or reference, product because it is already approved and known to be effective. Like the test tablet, it is taken by mouth under fasting conditions, and its absorption and clearance are measured. Comparing the test tablet to XELJANZ helps determine if the new version is bioequivalent, meaning it provides the same amount of medication to the body.

Trial ID:

2023-504516-15-00

Protocol code:

BLCL-TOF-EU-01

Trial Phase:

Human Pharmacology (Phase I) – Bioequivalence Study

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Bioequivalence Study of Tofacitinib 10 mg Film-Coated Tablets in Healthy Volunteers

What is this study about?

Who Can Join the Study?

Who Cannot Join the Study?