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Phase 4 Completed N=31 Other

Genetics and HIV-1 Protease Inhibitors

Source: ClinicalTrials.gov NCT01388543 ↗
Enrolled (actual)
31
Serious AEs
0.0%
Results posted
Nov 2019
Primary outcomePrimary: Day 7 Atazanavir Oral Clearance — .25; .18 L/h/kg
◆ Published Evidence
Established
49citations · ~3 / year
Atazanavir pharmacokinetics in genetically determined CYP3A5 expressors versus non-expressors.
The Journal of antimicrobial chemotherapy · 2009 · Open access · High-confidence link

Summary

This study evaluated the blood levels of atazanavir according to a genetic makeup for CYP3A5 (cytochrome P450 3A5, an enzyme that metabolizes atazanavir). The hypothesis was that people with a slow-metabolizing genotype would have higher blood levels of atazanavir compared to people with the normal metabolizing genotype.

Linked Publications (3)

  • Atazanavir pharmacokinetics in genetically determined CYP3A5 expressors versus non-expressors.
    The Journal of antimicrobial chemotherapy · 2009 · 49 citations · Open access · High-confidence link
  • A population pharmacokinetic-pharmacogenetic analysis of atazanavir.
    AIDS research and human retroviruses · 2012 · 41 citations · High-confidence link
  • Atazanavir metabolism according to CYP3A5 status: an in vitro-in vivo assessment.
    Drug metabolism and disposition: the biological fate of chemicals · 2011 · 29 citations · Open access · High-confidence link

Outcome Measures

OutcomeResultp-value
PRIMARY
Day 7 Atazanavir Oral Clearance
.25; .18

Eligibility Criteria

Inclusion Criteria

  • Age 18 to 55 years
  • Negative HIV screening antibody test
  • CYP3A5 expressor status, race, and sex fit an enrollment opening.

Exclusion Criteria

  • Pregnant or breast-feeding
  • Medical history of
  • hepatitis B or C,
  • autoimmune disease,
  • active malignancy,
  • kidney disease including nephrolithiasis
  • Organ dysfunction manifested by
  • liver transaminases or
  • serum creatinine >1.25 times the upper limit of normal, or
  • any comprehensive metabolic test (except asymptomatic unconjugated hyperbilirubinemia), blood count, or lipid value > Grade I according to Division of AIDS (DAIDS) adverse drug event grading system (appendix).
  • Medical history of arrhythmias (including atrial fibrillation, atrioventricular block, and/or pacemaker)
  • Any QT interval abnormalities or other congenital arrhythmia syndromes on ECG or
  • Any ECG abnormality that in the opinion of the investigators would preclude entry into the study.
  • Medical history of any serious heart condition including:
  • congestive heart failure,
  • myopathies,
  • coronary artery disease, or
  • unexplained syncope.
  • Medical history of bleeding disorders (i.e., hemophilia)
  • Hyperlipidemia
  • Any prescription, herbal, recreational, or over-the-counter medication contraindicated with ritonavir or atazanavir including:
  • substrates/inhibitors/inducers of CYP3A/P-gp,
  • cardio-active medication, or
  • medications that alter the acid in the stomach. The study investigators will review each concurrent medication on a case-by-case basis.
  • Inability to refrain from grapefruit or grapefruit juice during the study.
  • Investigational drugs within the last 30 days.
  • Active alcohol / recreational drug abuse,
  • Inability to give informed consent.
  • A body mass index below 18.5 or above 34.
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT01388543) and the linked publication. Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.

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