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Healthy SubjectsPhase 1NCT04468425

Tofacitinib Citrate Topical Gel 3.2% FDA BA Bridging Study

A Phase 1 study testing Tofacitinib Citrate in people with Healthy Subjects, run by TWi Biotechnology, Inc. at 1 site in Canada.

Completed

Finished. The study has ended and is not enrolling. Results may be posted on the official record.

Official record
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Trial summary

This is a Phase 1, single center, open-label, fixed sequence, two-period pharmacokinetic (PK) study to evaluate the safety and relative systemic bioavailability of topical and oral tofacitinib formulations in approximately 14 healthy subjects. Read more about this study

Who is it for?
Ages 18 to 60 yearsHealthy volunteers can take part
Conditions the study is for
Healthy Subjects
What is being tested?
Tofacitinib Citrate
Type of treatment
Pill or oral medicine
Could I receive a placebo?
No, everyone receives an active treatment
How many people
20 participants
Where
1 siteCanada
Study dates
14 Oct 2020to 21 Dec 2020
Phase
Phase 1
Are there results?
None posted in the registry

Key requirements

Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.

  • Ages 18 to 60 years
  • All sexes
  • Healthy volunteers accepted
  • Adult

Who may be able to join

  • Male or female, smoker (no more than 25 cigarettes or equivalent daily) or non-smoker, ≥18 and ≤60 years of age, with BMI >18.5 and <30.0 kg/m2 and body weight ≥50.0 kg for males and ≥45.0 kg for females.
  • Healthy as defined by:
  • The absence of clinically significant illness. Subjects vomiting within 24 hours pre dose will be carefully evaluated for upcoming illness/disease. Inclusion pre dosing is at the discretion of the Investigator;
  • The absence of clinically significant history of dermatological, neurological, endocrine, cardiovascular, respiratory, hematological, immunological, psychiatric, gastrointestinal, renal, hepatic, and metabolic disease.
  • Females of childbearing potential who are sexually active with a male partner must be willing to use one of the following acceptable contraceptive methods throughout the study and for 30 days after the last study drug administration:
  • Intra-uterine contraceptive device without hormone release system placed at least 4 weeks prior to study drug administration;
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  • Male condom with intravaginally applied spermicide started at least 21 days prior to study drug administration;
  • Sterile male partner (vasectomized since at least 6 months).
  • Absence of excessive body hair at the topical application site, or willing to have excess body hair removed prior to dosing.
  • Capable of consent.

Who cannot join

  • Presence of any clinically significant abnormality at physical examination, clinically significant abnormal laboratory assessment or positive test for hepatitis B, hepatitis C, or HIV found during medical screening.
  • Positive urine drug screen or alcohol breath test at screening.
  • History of allergic reactions to tofacitinib or other related drugs, or to any excipient in the formulation.
  • Positive pregnancy test at screening.
  • Clinically significant ECG abnormalities or vital sign abnormalities (systolic blood pressure lower than 90 or over 140 mmHg, diastolic blood pressure lower than 50 or over 90 mmHg, or heart rate less than 50 or over 100 bpm) at screening.
  • History of significant alcohol abuse within 1 year prior to screening or regular use of alcohol within 6 months prior to the screening visit (more than 14 units of alcohol per week [1 unit = 150 mL of wine, 360 mL of beer, or 45 mL of 40% alcohol]).
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  • History of significant drug abuse within 1 year prior to screening or use of soft drugs (such as marijuana) within 3 months prior to the screening visit or hard drugs (such as cocaine, phencyclidine [PCP], crack, opioid derivatives including heroin, and amphetamine derivatives) within 1 year prior to screening.
  • Participation in a clinical research study involving the administration of an investigational or marketed drug or device within 30 days prior to the first dosing, administration of a biological product in the context of a clinical research study within 90 days prior to the first dosing, or concomitant participation in an investigational study involving no drug or device administration.
  • Use of medications for the timeframes specified below, with the exception of medications exempted by the Investigator on a case-by-case basis because they are judged unlikely to affect the pharmacokinetic profile of the study drug or subject safety e.g. topical drug products without significant systemic absorption (not including topical drug products administered to the gel application site):
  • Prescription medications within 14 days prior to the first dosing;
  • Over-the-counter products and natural health products (including herbal remedies, homeopathic and traditional medicines, probiotics, food supplements such as vitamins, minerals, amino acids, essential fatty acids, and protein supplements used in sports) within 7 days prior to the first dosing, with the exception of the occasional use of acetaminophen (up to 2 g daily);
  • Depot injection or implant of any drug within 3 months prior to the first dosing;
  • Any drugs known to induce or inhibit hepatic drug metabolism via the CYP3A4 and CYP2C19 enzymes within 30 days prior to first dose;
  • Examples of inducers for CYP3A4 include barbiturates, carbamazepine, phenytoin, glucocorticoids, St. John's wort, etc.
  • Examples of inhibitors for CYP3A4 include HIV antivirals, clarithromycin, ciprofloxacin, gestodene, etc.
  • Examples of inducers for CYP2C19 include carbamazepine, norethindrone, prednisone, rifampicin, etc.
  • Examples of inhibitors for CYP2C19 include proton pump inhibitors, fluoxetine, ketoconazole, etc.
  • Donation of plasma within 7 days prior to dosing. Donation or loss of blood (excluding volume drawn at screening) of 50 mL to 499 mL of blood within 30 days, or more than 499 mL within 56 days prior to the first dosing.
  • Breast-feeding subject.
  • History of active tuberculosis or exposure to endemic areas within 8 weeks prior to QuantiFERON®-TB testing performed at screening.
  • Positive QuantiFERON®-TB indicating possible tuberculosis infection.
  • Immunization with a live attenuated vaccine within 1 month prior to dosing or planned vaccination during the course of the study.
  • History of clinically significant opportunistic infection e.g. invasive candidiasis or pneumocystis pneumonia.
  • Serious local infection e.g. cellulitis, abscess, or systemic infection e.g. septicemia, within 3 months prior to screening.
  • Presence of fever (body temperature >37.6 °C) e.g. a fever associated with a symptomatic viral or bacterial infection, within 2 weeks prior to the first dosing.
  • Presence of sunburn at the gel application site, or excessive exposure to ultraviolet light such as sunlight or a tanning lamp, or recent use of laser at the gel application areas that would prevent a safe application of the gel formulation as judged by the Investigator, within 7 days before the gel application.
  • Presence of tattoos or significant skin aberrations at the gel application site, which in the opinion of the investigator, would interfere with the ability to perform an accurate dermal reaction assessment.
  • Any reason that, in the opinion of the Investigator, would prevent the subject from participating in the study.

Trial locations and contacts

1 site in 1 country.

Canada1 site

  • Syneos Health Facility

    Québec

Other trials in Canada

About this study

Official title: Open-label, Fixed-sequence, Two-period Comparative Bioavailability Study of Tofacitinib From Repeated Topical Applications of Tofacitinib Citrate Topical Gel 3.2% to Single Oral Administration of Xeljanz 5 mg Tablet in Healthy Subjects

This is a Phase 1, single center, open-label, fixed sequence, two-period pharmacokinetic (PK) study to evaluate the safety and relative systemic bioavailability of topical and oral tofacitinib formulations in approximately 14 healthy subjects. Participants will receive a single oral dose of tofacitinib 5 mg tablet in Period 1 of the study followed by a 7-day washout period. In Period 2, participants will receive repeat administration of Tofacitinib Citrate Topical Gel 3.2% BID for 14 days.

Being tested
Tofacitinib Citrate

What participants receive

What participants receive. In a randomised study each person is assigned to one group by chance.

  • Tofacitinib CitrateDrug

    Period 1: Xelijanz® 5 mg tablet (tofacitinib citrate) for single oral dosing. Period 2: Tofacitinib Citrate Topical Gel 3.2% for repeat topical dosing BID for 14 days.

Study groups in NCT04468425
Study groupRoleWhat they receive
Pharmacokinetic StudyExperimentalPeriod 1 (Day 1) and 2 (Day 8 - Day 21) separated by 7-day washout period. Period 1: A single 5 mg tofacitinib tablet will be administered orally on Day 1. Period 2: Repeat dosing of Tofacitinib Citrate Topical Gel 3.2% to approximately 10% BSA in the morning of Day 8 and twice daily from Day 9 to Day 20 with the last dose in the morning of Day 21.
Receives: Drug: Tofacitinib Citrate

What is being measured

The primary outcome is the main question the study is designed to answer.

  1. Maximum Plasma Concentration [Cmax] of tofacitinib from single oral dosing in Period 1

    Measured: Day 1

  2. Area Under Curve [AUC] of tofacitinib from single oral dosing in Period 1

    Measured: Day 1

  3. Maximum Plasma Concentration [Cmax] of tofacitinib from repeat topical dosing in Period 2

    Measured: Day 8

  4. Area Under Curve [AUC] of tofacitinib from repeat topical dosing in Period 2

    Measured: Day 8

  5. Maximum Plasma Concentration [Cmax] of tofacitinib from repeat topical dosing in Period 2

    Measured: Day 21

  6. Area Under Curve [AUC] of tofacitinib from repeat topical dosing in Period 2

    Measured: Day 21

  7. Safety and tolerability of Tofacitinib Citrate Topical Gel 3.2% as assessed by treatment-emergent adverse events and Dermal Reaction Scoring, respectively.

    Measured: Day 24

Timeline

From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.

  1. First posted13 Jul 2020
  2. Study start14 Oct 2020
  3. Primary completion21 Dec 2020
  4. Study completion21 Dec 2020

Resources

More details

For doctors and researchers: how the study is designed, who runs it, and its registry IDs.

Study design
Study type
Interventional
Phase
Phase 1
Primary purpose
Other
Allocation
Not applicable
Intervention model
Sequential
Masking
None (open label)
Enrolment
20 participants (actual)
IDs, dates and publications
ClinicalTrials.gov ID
NCT04468425
Sponsor's protocol ID
AC-1101-PK-001
Status last verified
Oct 2026
First submitted
7 Jul 2020
Last updated
15 Oct 2026
Results posted
No
FDA-regulated drug
Yes
FDA-regulated device
No
Individual data sharing
No

Questions about this trial

What is this clinical trial studying?

A Phase 1 study testing Tofacitinib Citrate in people with Healthy Subjects, run by TWi Biotechnology, Inc. at 1 site in Canada.

The full registered description is in the About this study section and the official record.

Who may be eligible to take part?

The sponsor lists 10 inclusion and 28 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.

Is this clinical trial currently recruiting?

The record says: finished, as of the sponsor's last update on 15 Oct 2026. Status can change between updates, so confirm with the study contact before making plans.

Where is the study taking place?

The record lists 1 site in Canada. Whether a site is taking part right now should be confirmed with that site. See every site.

What are the possible benefits and risks?

They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.

What does this phase mean?

Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.

Not every study follows the same path, and some studies (observational studies, device studies) have no phase.

Are results available for this study?

The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.

How can a doctor refer a patient or contact the research team?

The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.

What does the primary outcome measure?

Maximum Plasma Concentration [Cmax] of tofacitinib from single oral dosing in Period 1 (time frame: Day 1). The study lists 7 primary outcomes in all. It is what the study was designed to measure, not a finding.

Where can I read the original study information?

On the ClinicalTrials.gov record for NCT04468425.

Does a listing mean the treatment is approved or proven to work?

No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.

How often is this information updated?

AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 15 Oct 2026.

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