A study of the safety of 3 months treatment with BIT225 and Combination Antiretroviral Therapy (cART), in patients with Human Immunodeficiency Virus-1 (HIV-1), compared to cART alone, including measurement of the concentration of BIT225 in the blood and antiviral activity.

Exclusion Criteria32

• Currently have any active AIDS defining illness (according to the CDC Surveillance Case Definition for HIV infection, AIDS-Defining Conditions, revised April 11, 2014, Appendix 1).
• Patients who have received an investigational drug for HIV-1, HIV-1 vaccine, immunomodulators (e.g. interleukins, interferons, cyclosporine), systemic cytotoxic chemotherapy, or other investigational therapy within 45 days prior to study entry (Day 1).
• 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)
• Confirmed or suspected active TB disease (confirmation determined by chest X-ray and if necessary, sputum smear)
• History or other evidence of clinically significant renal disease.
• Pregnancy or breast feeding, male partners of pregnant females.
• Abnormal haematological and biochemical parameters within 45 days of Entry (Day 1):
• a. Absolute neutrophil count <1000/mm3
• b. Haemoglobin <12 g/dL in females or 13 g/dL in males
• c. Platelet count <150,000/mm3
• d. International normalised ratio (INR) >1.5
• e. Aspartate aminotransferase (AST), alanine aminotransferase (ALT), and alkaline phosphatase >/=2.5 times upper limit of normal
• f. Total bilirubin > 1.5 times the normal reference range
• g. Creatinine > 1.5 mg/dL
• Estimated creatinine clearance < 60 mL/minute at Screening. Value will be calculated using the Cockcroft-Gault formula.
• Screening ECG QTcB value >/=450 ms.
• The consumption / administration of concomitant medication (prescribed, over-the-counter or complementary) at the time of the Screening visit listed in Appendix 4. 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 approved by the Biotron Medical Monitor in consultation with the Investigator.
• Active drug or alcohol use or dependence that, in the opinion of the site Investigator, would interfere with adherence to study requirements.
• A positive result on urine screen for drugs of abuse at Screening or Day 1 which in the opinion of the Investigator should preclude them from participation in the study.
• Any prior suicide attempt.
• History of immunologically mediated disease (e.g., inflammatory bowel disease, idiopathic thrombocytopenic purpura, lupus erythematosus, autoimmune haemolytic anaemia, 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, 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 of the study.
• 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.
• Active thyroid disease (use of thyroid hormone replacement therapy permitted by TSH or free T4 must be in normal range.)
• Serious illness requiring systemic treatment and/or hospitalization until the participant either completes therapy or is clinically stable on therapy, in the opinion of the site Investigator, or at least 7 days prior to study entry.
• Known allergy/sensitivity or any hypersensitivity to components of study drug or its formulation.
• Unable to refrain from smoking during the PK evaluation periods of the trial, if enrolled in the PK sub-study.
• Difficulty abstaining from grapefruit, starfruit, and pomelo including, products containing these fruit, 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.