NCT00704119

Study Evaluating the Pharmacokinetic Profile of RhuDex® in a Tablet Formulation

CT 5002 An Open-label, Non-randomized, Monocentric Phase I Study Evaluating the Pharmacokinetic Profile of RhuDex® Using a Tablet Formulation

• Status: Terminated
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 12 (actual)
• Sponsor: MediGene · Industry
• Sex: Male
• Age: 18 Years – 60 Years
• Healthy volunteers: Accepted

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.

Detailed description

This is an open-label, non-randomized, monocentric Phase I study to evaluate the pharmacokinetic profile of single-dosed and repeat-dosed RhuDex® using a tablet formulation as well as to assess the effect of food and the effect with co-administration of a proton pump inhibitor on the bioavailability of RhuDex®. 12 healthy male subjects will receive study medication in 8 different treatment periods in 4 subsequent steps A, B, C and D. Within steps A and B, the subjects will receive different treatments (4 in A and 2 in B), sequentially. There will be a wash-out period of at least 4 days between each of the 8 different treatments/treatment periods of steps A, B, C and D. In Step A, each subject will receive increasing doses of RhuDex® in 4 subsequent treatments. In Step B, each subject will receive 2 different doses of RhuDex® preceded by pantoprazole intake, in 2 subsequent treatments, and in Step C the RhuDex® dosing will be preceded by a standardized high-fat, high-calorie meal. In Step D, RhuDex® will be administered twice daily for 7 days. For assessing the pharmacokinetic profile of RhuDex® in steps A, B and C, blood samples will be collected prior to and at different intervals after RhuDex® administration. In step D, blood samples will be collected on Days 1, 2, 4 and 7. Cmin, Cmax, tmax, t½ term, CL/F, AUC(0-t), and AUC(0-∞) of RhuDex® will be analyzed. Safety will be evaluated by regular observation and documentation of AEs, vital signs, physical examination, ECG, and laboratory parameters.

Conditions

• Pharmacokinetics

Interventions

Type	Name	Description
DRUG	RhuDex®	* Treatment A.1: 31.65 mg RhuDex® once N=12 * Treatment A.2: 63.33 mg RhuDex® once N=12 * Treatment A.3: 126.63 mg RhuDex® once N=12 * Treatment A.4: 253.26 mg RhuDex® once N=12 * Treatment B.1: 31.65 mg RhuDex® once N=12 * Treatment B.2: selected dose of RhuDex® once N=12 * Treatment C: selected dose of RhuDex® once N=12 * Treatment D: selected dose of RhuDex® twice daily for 6 days N=12

Timeline

• Start date: 2008-05-01
• Primary completion: 2008-07-01
• Completion: 2008-08-01
• First posted: 2008-06-24
• Last updated: 2010-03-24

Locations

1 site across 1 country: United Kingdom