Antiretroviral Activity and Pharmacokinetics of Deferiprone in Healthy Volunteers and Asymptomatic HIV-infected Subjects

Three cohorts were enrolled: two of individuals who were asymptomatically infected with HIV and one of healthy volunteers. Dosages were as follows:

• Cohort 1 (asymptomatic HIV infected subjects): 33 mg/kg deferiprone three times daily for a total of 99 mg/kg/day
• Cohort 2 (healthy volunteers): 50 mg/kg deferiprone three times daily for a total of 150 mg/kg/day
• Cohort 3 (asymptomatic HIV infected subjects): 50 mg/kg deferiprone three times daily for a total of 150 mg/kg/day

Inclusion criteria

• Male or female aged ≥18 years and ≤ 60 years.
• Absolute neutrophil count (ANC) of >1000/mm3 for African black population and ≥ 1600/mm3 for all other races.
• For Cohort 2: HIV-negative
• For Cohorts 1 and 3: HIV-1 positive; CD4 count of at least 300/mm3; HIV-1 RNA copies (viral load) >10 000 copies/mL serum; and current physical health stable and not requiring antiretroviral treatment
• For Cohorts 1 and 3: Chest x-ray showing absence of active infectious diseases (such as tuberculosis, viral or atypical bacteria or parasitic infection).

Exclusion criteria

• Presence of any severe concomitant disease.
• History of or current, recurrent or recent (4 weeks) febrile disease.
• History of opportunistic infections, neoplasm or AIDS-defining conditions.
• Inability to discontinue any medication from screening onwards, or for at least 2 weeks before the first admission; in particular any antiviral or therapy with immunosuppressive activity.
• Significant liver impairment: aspartate aminotransferase (AST), alanine aminotransferase (ALT) ≥ 2.5 times the upper normal limit.
• Significant kidney impairment: serum creatinine ≥ two times the upper normal limit.
• Any concomitant disorder or resultant therapy likely to have interfered with subject compliance or with study procedures.
• Known hypersensitivity to any of the test materials or related compounds.
• Positive test for Hepatitis B and/or C antibodies.
• A history of multiple and/or severe allergies to drugs or foods or a history of anaphylactic reactions.
• History of seizures or epilepsy.