Phase-I Study Evaluating the Pharmacokinetic Profile of RhuDex®

RhuDex® is a novel, orally bioavailable, low molecular weight modulator of co-stimulation of T lymphocytes. RhuDex® binds to the protein CD80 on the surface of antigen-presenting cells and inhibits its interaction with CD28 (but not with CTLA-4) presented by CD4+ T lymphocytes.

Inclusion criteria

• Healthy male subjects between 18 and 60 years at the time of enrollment
• Male volunteers and their partners who are of child-bearing potential must agree to use a double-barrier method of contraception during the study and for 12 weeks after discharge
• BMI between 18.5 and 29.9 kg/m²
• Written informed consent
• Ability to comply with the requirements of the study

Exclusion criteria

• Acute infection at time of enrollment
• History of chronic inflammation, chronic infection, other chronic disease, autoimmune disorders (e.g. diabetes mellitus) or cancer
• Clinical significant abnormal ECG
• Clinical significant abnormal laboratory values (especially in terms of liver or renal insufficiency)
• Clinically significant physical findings
• Major surgery within the last 4 weeks prior to enrollment
• Organ allograft recipient
• Concomitant or planned treatment which would interfere with study results
• Any systemic medical treatment, including over the counter products and dietary supplements such as iodine, fluoride or vitamins, within one week before and during the study course
• Known allergy against any ingredient of the study medication or meglumine
• Participation in an investigational trial within 30 days prior to enrollment
• Systemic intake of immunosuppressive or immunomodulatory medication or vaccination within 30 days prior to enrollment and for the whole study duration
• Blood loss exceeding 450 mL (including blood donations) within 12 weeks prior to enrollment into the study
• Medical history of alcohol or drug abuse or alcohol consumption greater than 21 units per week for males. A unit of alcohol is equivalent to: half a pint of average strength beer (280 mL), a glass (125 mL) of wine or a standard measure (25 mL) of spirits, sherry or port
• A positive alcohol breath test
• A positive urine drug screen
• Regular smokers (more than 20 cigarettes or 5 cigars per day)
• Presence of hepatitis B surface antigen (HBsAG), hepatitis C antibody (HCV Ab) or HIV-1 or HIV-2 antibodies at screening