Phase 1
Completed N=16
A Target Occupancy Study With Ritlecitinib.
Healthy
Source: ClinicalTrials.gov NCT05128058 ↗
Enrolled (actual)
16
Serious AEs
0.0%
Results posted
Nov 2023
Primary outcomePrimary: Percent Target Occupancy for JAK3 — 0.00; 0.00; 72.41; 28.74 percentage of occupancy
Summary
This is a phase 1, open label, two-arm study to assess target occupancy and functional inhibition of JAK3 and TEC kinases by Ritlecitinib in healthy adult participants
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Percent Target Occupancy for JAK3 |
0.00; 0.00; 72.41; 28.74; 12.28; 64.14 | — |
| PRIMARY Percent Target Occupancy for BTK |
0.00; 0.00; 98.45; 99.57; 96.83; 99.37 | — |
| PRIMARY Percent Target Occupancy for ITK |
0.00; 0.00; 94.40; 97.03; 67.77; 97.06 | — |
| PRIMARY Percent Target Occupancy for TXK |
0.00; 0.00; 100.00; 100.00; 44.97; 100.00 | — |
| PRIMARY Percent Target Occupancy for TEC |
0.00; 0.00; 96.50; 100.0; 94.60; 99.42 | — |
| PRIMARY Percent Target Occupancy for BMX |
0.00; 0.00; 67.51; 99.13; 85.26; 92.53 | — |
| SECONDARY Maximum Observed Plasma Concentration (Cmax) of Ritlecitinib |
297.1; 1275 | — |
| SECONDARY Time to Reach Maximum Observed Plasma Concentration (Tmax) of Ritlecitinib |
1.00; 1.00 | — |
| SECONDARY Last Quantifiable Plasma Concentration (Clast) of Ritlecitinib |
4.812; 4.036 | — |
| SECONDARY Average Plasma Concentration From Time 0 to 24 Hours (Cav) of Ritlecitinib |
28.42; 144.9 | — |
| SECONDARY Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of Ritlecitinib |
651.4; 3382 | — |
| SECONDARY Area Under the Curve From Time 0 to 24 Hours (AUC24) of Ritlecitinib |
681.8; 3475 | — |
| SECONDARY Number of Participants With All-Causality and Treatment-Related Treatment-Emergent Adverse Events (TEAEs) |
3; 2; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Treatment-Emergent Adverse Events by Severity |
3; 2; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Laboratory Abnormalities Without Regard to Baseline Abnormality |
0; 2; 1; 1; 1; 0 | — |
| SECONDARY Number of Participants With Pre-defined Criteria for Vital Signs |
0; 0; 0; 0; 0; 0 | — |
Eligibility Criteria
Inclusion Criteria
Participants are eligible to be included in the study only if all the following criteria apply:
- Participants who are willing and able to comply with all scheduled visits, treatment plan, laboratory tests, lifestyle considerations, and other study procedures.
- Male and female participants who are overtly healthy as determined by medical evaluation including medical history, physical examination including BP and pulse rate measurement, 12-lead ECG, or clinical and laboratory tests.
- BMI of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lb).
Exclusion Criteria
Participants are excluded from the study if any of the following criteria apply:
- Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurological, or allergic disease (including drug allergies, but excluding untreated, asymptomatic, seasonal allergies at the time of dosing).
- Infection with HIV, hepatitis B or hepatitis C viruses
- Have evidence of untreated or inadequately treated active or latent Mycobacterium TB infection
- Known active or history of recurrent bacterial, viral, fungal, mycobacterial or other infections.
- Have received only one of the 2 required doses of COVID-19 vaccine.
- Participants have a known present or a history of malignancy other than a successfully treated or excised non metastatic basal cell or squamous cell cancer of the skin or cervical carcinoma in situ.
Data sourced from ClinicalTrials.gov (NCT05128058). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.