Study Evaluating the Pharmacokinetic Profile of RhuDex® in a Tablet Formulation
Summary
RhuDex® (code number AV1142742) is a novel, orally bioavailable, low molecular weight modulator of co-stimulation of T lymphocytes. RhuDex® binds to the protein CD80 (also known as B7-1) on the surface of antigen-presenting cells and inhibits its interaction with CD28 (but not with CTLA-4) presented by CD4+ T lymphocytes. RhuDex® is being developed for the treatment of rheumatoid arthritis. To improve oral bioavailability, the study drug has to be co-administered with an alkaline buffer that increases gastric pH values. In previous in vitro and phase I studies, meglumine has been identified as the most effective buffer. Study CT 5002 is designed to evaluate the bioavailability of four increasing doses of RhuDex®, combined with a fixed amount of meglumine using a tablet formulation, under fed and fasted conditions as well as with co-administration of the proton pump inhibitor pantoprazole. Furthermore, dose/plasma concentration proportionality for single dosing and accumulation effects for repeat dosing of RhuDex® will be evaluated.
Timeline
- Start
- 2008-05
- Primary completion
- 2008-07
- Completion
- 2008-08
Outcome
Outcome not reported
Stopped: “Following an SAE, study was put on hold. After performing preclinical follow-up studies, volunteers were no longer available for continuation.”
Drugs
| Evaluation | Drug | Modality | Dose | Route |
|---|---|---|---|---|
| Subject | RhuDex® | Small molecule | 31.65 mg | Oral |
| Subject | RhuDex® | Small molecule | 63.33 mg | Oral |
| Subject | RhuDex® | Small molecule | 126.63 mg | Oral |
| Subject | RhuDex® | Small molecule | 253.26 mg | Oral |
Indications
No indication recorded.