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

Phase 1
Completed
Conditions
HIV Infection
Interventions
Registration Number
NCT02191657
Lead Sponsor
ApoPharma
Brief Summary

The purpose of this study was to examine the safety, efficacy, and pharmacokinetics of different dosages of deferiprone in subjects with or without HIV infection.

Detailed Description

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

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
26
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.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Cohort 2DeferiproneSubjects in this arm were healthy volunteers who received a dose of 50 mg/kg deferiprone three times a day for a total daily dosage of 150 mg/kg
Cohort 3DeferiproneSubjects in this arm were asymptomatic HIV-infected individuals who received a dose of 50 mg/kg deferiprone three times a day for a total daily dosage of 150 mg/kg.
Cohort 1DeferiproneSubjects in this arm were asymptomatic HIV-infected individuals who received a dose of 33 mg/kg deferiprone three times a day for a total daily dosage of 99 mg/kg
Primary Outcome Measures
NameTimeMethod
Occurrence of adverse events following repeated oral doses of deferiprone in asymptomatic HIV-infected subjects and healthy volunteers9 weeks (from receipt of first dose until 8 weeks after the last dose)

Collection of adverse events, including abnormal findings in physical examination, vital signs, 12-lead ECG, 24-hour Holter ECG, and laboratory variables (hematology, clinical chemistry, and urinalysis)

Measurement of viral load following repeated oral doses of deferiprone in asymptomatic HIV-infected subjects and healthy volunteers9 weeks (pre-dose until 8 weeks after last dose)

Measurement of HIV RNA load for the assessment of antiretroviral activity

Cluster of differentiation 4 (CD4) count and p24 antigen status following repeated oral doses of deferiprone in asymptomatic HIV-infected subjects and healthy volunteers1 week (pre-dose to day of last dose)

Measurement of CD4 count and p24 antigen status for assessment of antiviral activity

Secondary Outcome Measures
NameTimeMethod
T1/2 of deferiprone and deferiprone 3-O-glucuronide24-hour interval

Determination of T1/2 of deferiprone and its metabolite following a dose of deferiprone in asymptomatic HIV-infected subjects and healthy volunteers

Cmax of deferiprone and deferiprone 3-O-glucuronide24-hour interval

Determination of Cmax following a dose of deferiprone in asymptomatic HIV-infected subjects and healthy volunteers

Tmax of deferiprone and deferiprone 3-O-glucuronide24-hour interval

Determination of Tmax of deferiprone and its metabolite following a dose of deferiprone in asymptomatic HIV-infected subjects and healthy volunteers

Area under the curve (AUC) 0-infinity of deferiprone and deferiprone 3-O-glucuronide24-hour interval

Determination of AUC 0-infinity of deferiprone and its metabolite following a dose of deferiprone in asymptomatic HIV-infected subjects and healthy volunteers

Trial Locations

Locations (1)

PAREXEL International

🇿🇦

Bloemfontein,, South Africa

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