A Phase 1, Randomized, Single-Center Study to Investigate the Safety, Tolerability and Pharmacokinetics of Single and Multiple Doses of R289 in Healthy Subjects.
- Conditions
- Autoimmune disorder10003816
- Registration Number
- NL-OMON55213
- Lead Sponsor
- Rigel Pharmaceuticals, Inc.
- Brief Summary
Not available
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- Completed
- Sex
- Not specified
- Target Recruitment
- 78
Subjects must be able and willing to give written informed consent.
Subjects must be at least 18 years at Screening and maximum 65 years old on
date of first dose with a body mass index (BMI) of 19.0-30.0 kg/m2, inclusive
at Screening.
Female subjects must be post-menopausal or surgically sterile with negative
serum pregnancy test at Screening and a negative urine pregnancy test at
admission.
Male subjects must be willing to use adequate contraception, and to refrain
from sperm donation, from the time of dosing until 90 days after the last dose
of study drug.
Subjects must be healthy as determined by pre-study medical history, physical
examination and 12-lead ECG.
The subject has a clinically relevant history or presence of respiratory,
gastrointestinal, renal, hepatic, hematological, lymphatic, neurological,
cardiovascular, psychiatric, musculoskeletal, immunological, dermatological,
connective tissue diseases or disorders.
The subject has a clinically relevant surgical history, including
cholecystectomy.
The subject has a history of relevant atopy.
The subject has a history of relevant drug hypersensitivity.
The subject has a history of hypertension or a blood pressure of >140 mmHg
systolic or >90 mmHg diastolic at Screening.
Study & Design
- Study Type
- Interventional
- Study Design
- Not specified
- Primary Outcome Measures
Name Time Method <p>Part 1<br /><br>Safety and tolerability parameters include: physical examination, AEs, clinical<br /><br>laboratory values, vital signs, and 12-lead ECG.<br /><br>Part 2 and Part 4 (Optional)<br /><br>Safety and tolerability parameters include: physical examination, AEs, clinical<br /><br>laboratory values, vital signs, and 12-lead ECG.<br /><br>Part 3<br /><br>Pharmacokinetic parameters for R289 and its active and secondary metabolites<br /><br>R835 and R466 include: Cmax, tmax, t1/2, AUC0-t, AUC0-inf, AUC0-tau,<br /><br>%AUCextrap, CL/F (R835 only), Vz/F (R835 only), and MR (R466/R835).<br /><br>Safety and tolerability parameters include: physical examination, AEs, clinical<br /><br>laboratory values, vital signs, and 12-lead ECG.</p><br>
- Secondary Outcome Measures
Name Time Method <p>Part 1<br /><br>Pharmacokinetic parameters for R289 and its active and secondary metabolites<br /><br>R835 and R466 include: Cmax, tmax, t1/2, AUC0-t, AUC0-inf, AUC0-tau, AUCextrap,<br /><br>CL/F (R289 only), Vz/F (R289 only), and MR in fasted and fed status.<br /><br><br /><br>Part 2 and Part 4 (Optional)<br /><br>Pharmacokinetic parameters for R289 and its active and secondary metabolites<br /><br>R835 and R466 include: Cmax, tmax, t1/2, AUC0-t, AUC0-inf, AUC0-tau,<br /><br>%AUCextrap, CL/F (Day 1; R835 only), CLss/F (Day 14; R835 only), Vz/F (Day 1;<br /><br>R835 only), Vss/F (Day 14; R835 only), Cssavg (Day 14), AR, MR (R466/R835).</p><br>