Autoimmune disorder
Conditions
Interventions
R289 as 20 mg capsules or tablet
Sponsors
Rigel Pharmaceuticals, Inc.
Eligibility
Age
18 Years to 64 Years
Inclusion criteria
Inclusion criteria: 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.
Exclusion criteria
Exclusion criteria: 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.
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Part 1 Safety and tolerability parameters include: physical examination, AEs, clinical laboratory values, vital signs, and 12-lead ECG. Part 2 and Part 4 (Optional) Safety and tolerability parameters include: physical examination, AEs, clinical laboratory values, vital signs, and 12-lead ECG. Part 3 Pharmacokinetic parameters for R289 and its active and secondary metabolites R835 and R466 include: Cmax, tmax, t1/2, AUC0-t, AUC0-inf, AUC0-tau, %AUCextrap, CL/F (R835 only), Vz/F (R835 only), and MR (R466/R835). Safety and tolerability parameters include: physical examination, AEs, clinical laboratory values, vital signs, and 12-lead ECG. | — |
Secondary
| Measure | Time frame |
|---|---|
| Part 1 Pharmacokinetic parameters for R289 and its active and secondary metabolites R835 and R466 include: Cmax, tmax, t1/2, AUC0-t, AUC0-inf, AUC0-tau, AUCextrap, CL/F (R289 only), Vz/F (R289 only), and MR in fasted and fed status. Part 2 and Part 4 (Optional) Pharmacokinetic parameters for R289 and its active and secondary metabolites R835 and R466 include: Cmax, tmax, t1/2, AUC0-t, AUC0-inf, AUC0-tau, %AUCextrap, CL/F (Day 1; R835 only), CLss/F (Day 14; R835 only), Vz/F (Day 1; R835 only), Vss/F (Day 14; R835 only), Cssavg (Day 14), AR, MR (R466/R835). | — |
Countries
Netherlands
Outcome results
None listed