A trial of BIT225 in patients with HIV-1 infection, to study the safety, concentration and distribution in the body, and anti-viral activity of the drug.

Exclusion Criteria27

• Currently has any active AIDS defining illness ( according to the CDC Surveillance Case Definition for HIV Infection, AIDS-Defining Conditions, updated December 5, 2008.
• Patients who are expected to need systemic antiviral therapy at any time during their participation in the study.
• Patients who have received an investigational drug for HIV, HIV vaccine, immunomodulators (e.g., interleukins, interferons, cyclosporine), systemic cytotoxic chemotherapy, or other investigational therapy within 30 days prior to study entry.
• Acute or chronic viral hepatitis as defined by the presence of: 1) anti-HAV IgM Ab (acute hepatitis A), 2) HCV Ab with a detectable HCV RNA by PCR (acute or chronic hepatitis C) or 3) hepatitis B surface antigen or HBV DNA in subjects with isolated HBcAb, defined as negative HBsAg, negative HBsAb and positive HBcAb (acute or chronic hepatitis B).
• History or other evidence of renal disease.
• Abnormal hematological and biochemical parameters within 30 days of Entry (Day 1):
• a. Absolute neutrophil count <1000/mm3
• b. Haemoglobin <12 g/L in females or <13 g/L in males
• c. Platelet count <75,000/mm3
• d. Estimated creatinine clearance < 60 mL/minute. Value will be calculated using the Cockcroft-Gault formula.
• e. Aspartate aminotransferase (AST), alanine aminotransferase (ALT), and alkaline phosphatase >/= 2.5 times upper limit of normal.
• Screening ECG QTc value >/= 450 ms.
• Consumption / administration of prohibited concomitant medication (prescribed, over-the-counter or complementary). This list is not exhaustive and any medication taken from 30 days prior to first dose through to the end of the participation in the study must be permitted by the Biotron Medical Monitor in consultation with the Investigator.
• Active alcohol and/or drug abuse that, in the opinion of the site investigator, would interfere with adherence to study requirements.
• Positive results on urine screen for drugs of abuse (excluding THC) at Screening or Day 1.
• History of immunologically mediated disease (e.g., inflammatory bowel disease, idiopathic thrombocytopenic purpura, lupus erythematosus, autoimmune hemolytic anemia, scleroderma, severe psoriasis, rheumatoid arthritis requiring more than intermittent non-steroidal anti-inflammatory medications for management, etc).
• History of documented or presumed coronary artery disease or cardiovascular disease, or clinically significant arrhythmia.
• History of a severe seizure disorder or current anticonvulsant use.
• Evidence of an active or suspected cancer or a history of malignancy within 2 years.
• History of having received any systemic anti-neoplastic or immunomodulatory treatment (including supraphysiologic doses of steroids and radiation) within 6 months prior to the first dose of study drug or the expectation that such treatment will be needed at any time during the study.
• History of thyroid disease poorly controlled on prescribed medications. Patients with elevated thyroid stimulating hormone concentrations, with elevation of antibodies to thyroid peroxidase and any clinical manifestations of thyroid disease.
• Serious illness requiring systemic treatment and/or hospitalization until subject either completes therapy or is clinically stable on therapy, in the opinion of the site investigator, for at least 7 days prior to study entry.
• Known allergy/sensitivity to any components of study drug or its formulation.
• Current habit of smoking and unable to refrain from smoking during the confinement periods in this trial.
• Difficulty abstaining from grapefruit, star fruit, including grapefruit and star fruit containing products from 7 days prior to the first dose of investigational product until the end of the dosing period.
• Participation in a clinical study with an investigational drug, biologic, or device within 3 months prior to anticipated dose administration.
• Current use of herbal medications or unwillingness to cease use during study participation.