MedPath

Lopinavir/r/ Lamivudine/ Abacavir as an Easy to Use Paediatric Formulation

Phase 1
Conditions
HIV
Interventions
Drug: ABC/3TC/LPV/r granules (30/15/40/10 mgs)
Drug: LPV/r Pellets (40/10mgs) plus ABC/3TC (60/30mgs)
Registration Number
NCT03836833
Lead Sponsor
Drugs for Neglected Diseases
Brief Summary

A phase I/II, open label, randomized crossover pharmacokinetic, safety and acceptability study of the Abacavir/Lamivudine/ Lopinavir/Ritonavir (30/15/ 40/10mg ;4-in-1) Fixed-Dose Combination vs. Lopinavir/Ritonavir (40/10mg pellets) plus dual Abacavir/Lamivudine (60/30mg tablets) in HIV infected Children.

The study is intended to support the adoption of the 4-in-1 by healthcare providers and will provide data that may support its registration in certain countries. The study will be carried out in HIV-infected children in Uganda weighing 3 to 25 kg (inclusive) and unable to swallow tablets and will provide supportive clinical data on the pharmacokinetics, safety, tolerability and acceptability of the 4-in-1.

Detailed Description

The primary objective is to estimate the population average exposure to LPV, ABC and 3TC provided by the 4-in-1 formulation in HIV-infected children dosed per WHO weight bands.

The secondary objectives:

* To determine the proportion of children overall, and within each weight band, with a lopinavir C12 \<1.0 mg/L while receiving the 4-in-1 formulation

* To evaluate and compare the safety and tolerability of the 4-in-1 formulation versus a reference treatment regimen.

* To compare the bioavailability of LPV, ABC and 3TC in the 4-in-1 formulation versus a reference treatment regimen.

* To assess post exposure CD4 and viral load

* To assess the factors that contribute to acceptability of the new 4-in-1 formulation.

Recruitment & Eligibility

Status
UNKNOWN
Sex
All
Target Recruitment
50
Inclusion Criteria
  • Children > 4 weeks old and weighing ≥3 and <25 kg at the time of enrolment

  • Past or current documentation of a confirmed diagnosis of HIV infection defined as two positive assays from two different samples. The two results may be in any combination of the following:

  • At any age: HIV-1 DNA PCR positive

  • Documented past HIV-1 RNA viral load > 1,000 copies/mL plasma

  • At any age >18 months of age: HIV-1 antibody reactive on two different rapid tests based on national testing algorithm

  • ARV treatment eligible children with LPV-based treatment indication* as defined by country-specific guidelines or the WHO paediatric treatment guidelines and confirmed by the investigator

  • HIV RNA viral load <1000 copies/mL (suppressed) at the screening visit*

  • Inability to swallow LPV/r tablets

  • Parent or guardian able and willing to provide written informed consent.

  • For lowest weight band (≥3 and ≤ 5.9kgs) ONLY: under treatment for at least 3 weeks but not more than 12 weeks.

    • Does not apply to the youngest children (≥3 and ≤ 5.9kgs)
Exclusion Criteria
  • Planned or concurrent use of NNRTIs, integrase inhibitors, entry inhibitors, or Protease Inhibitors (PIs) other than LPV/r.
  • Treatment failure with proven resistances to PIs.
  • Contraindication to use of PIs
  • Clinical condition requiring the use of a prohibited medication (see section 7.6) in association with LPV/r, ABC/3TC (Refer to section 7.2- 7.3 of the IB)
  • Pulmonary Tuberculosis and any clinically significant disease or finding during screening that, in the investigator's opinion, would compromise participation in this study.
  • Treatment with experimental drugs (except for LPV/r Pellets) for any indication within 30 days prior to study entry
  • Anticipated transfer of care to a non-participating health facility during the study period

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
4in1 granulesABC/3TC/LPV/r granules (30/15/40/10 mgs)Abacavir/Lamivudine/ Lopinavir/Ritonavir (30/15/ 40/10mg ;4-in-1) Fixed-Dose Combination in granules formulation administered twice daily for at least 3 weeks, Followed by Lopinavir/Ritonavir (40/10mg pellets) plus dual Abacavir/Lamivudine (60/30mg dispersible tablets) administered twice daily for at least 3 weeks.
4in1 granulesLPV/r Pellets (40/10mgs) plus ABC/3TC (60/30mgs)Abacavir/Lamivudine/ Lopinavir/Ritonavir (30/15/ 40/10mg ;4-in-1) Fixed-Dose Combination in granules formulation administered twice daily for at least 3 weeks, Followed by Lopinavir/Ritonavir (40/10mg pellets) plus dual Abacavir/Lamivudine (60/30mg dispersible tablets) administered twice daily for at least 3 weeks.
LPV/r Pellets Plus ABC/3TCABC/3TC/LPV/r granules (30/15/40/10 mgs)Lopinavir/Ritonavir (40/10mg pellets) plus dual Abacavir/Lamivudine (60/30mg dispersible tablets) administered twice daily for at least 3 weeks. Followed by Abacavir/Lamivudine/ Lopinavir/Ritonavir (30/15/ 40/10mg ;4-in-1) Fixed-Dose Combination in granules formulation administered twice daily for at least 3 weeks
LPV/r Pellets Plus ABC/3TCLPV/r Pellets (40/10mgs) plus ABC/3TC (60/30mgs)Lopinavir/Ritonavir (40/10mg pellets) plus dual Abacavir/Lamivudine (60/30mg dispersible tablets) administered twice daily for at least 3 weeks. Followed by Abacavir/Lamivudine/ Lopinavir/Ritonavir (30/15/ 40/10mg ;4-in-1) Fixed-Dose Combination in granules formulation administered twice daily for at least 3 weeks
Primary Outcome Measures
NameTimeMethod
0 -12 hours Area under the curve plasma concentration versus time for LPV, ABC and 3TC in the 4-in- formulation0-12 hours

0 -12 hours Area under the curve plasma concentration versus time for LPV, ABC and 3TC in the 4-in- formulation

Secondary Outcome Measures
NameTimeMethod
Plasma concentration at 12 hours for LPV in the 4in1 formulation12 hours

Plasma concentration at 12 hours for LPV in the 4in1 formulation

Peak plasma concentration (Cmax) of LPV, ABC and 3TC with the 4-in-1 formulation.3-5 weeks

Plasma concentration maximum of LPV, ABC and 3TC with the 4-in-1 formulation.

Concentration time maximum for LPV, ABC and 3TC with the 4-in-1 formulation.3-5 weeks

Concentration time maximum for LPV, ABC and 3TC with the 4-in-1 formulation.

Clearance function for LPV, ABC and 3TC with the 4-in-1 formulation.3-5 weeks

Clearance function for LPV, ABC and 3TC with the 4-in-1 formulation.

Geometric mean ratio (GMR) of steady state LPV, ABC and 3TC versus time (0-12) in the 4-in-1 formulation versus the reference treatment regimen0 - 12 hours

Geometric mean ratio (GMR) of steady state LPV, ABC and 3TC versus time (0-12) in the 4-in-1 formulation versus the reference treatment regimen.

Area under curve plasma concentration versus time (0-12) in the 4-in-1 formulation versus the reference treatment regimen.0 - 12 hours

Area under curve plasma concentration versus time (0-12) in the 4-in-1 formulation versus the reference treatment regimen.

Geometric mean ratio (GMR) of steady state LPV, ABC and 3TC in the 4-in-1 formulation versus the reference treatment regimen.0 - 12 hours

Geometric mean ratio (GMR) of steady state LPV, ABC and 3TC in the 4-in-1 formulation versus the reference treatment regimen.

Peak plasma concentration in the 4-in-1 formulation versus the reference treatment regimen.3-5 weeks

Peak plasma concentration in the 4-in-1 formulation versus the reference treatment regimen.

Safety: A description of the proportion of children experiencing an Adverse event or Serious Adverse event binomial distribution compared between the two formulations.6-8 weeks

Safety: A description of the proportion of children experiencing an Adverse event or Serious Adverse event binomial distribution compared between the two formulations.

Safety: Summary of the number and percent of subjects with documented Grade 3 or higher adverse events; each summary will be conducted overall and by formulation6-8 weeks

Safety: Summary of the number and percent of subjects with documented Grade 3 or higher adverse events; each summary will be conducted overall and by formulation

Proportion of children with viral load <1000 copies/ml6-8 weeks

Comparison of proportion of children with viral load less than 1000 copies/ml at baseline and at end of the study.

Changes in CD4 counts compared to baseline6-8 week

Changes in CD4 counts compared to baseline

Changes in CD4 percentage compared to baseline6-8 weeks

Changes in CD4 percentage compared to baseline

Acceptability: Description of factors that affect acceptability of the 4 in1 formulation6-8 weeks

Description of factors that affect acceptability of the 4in1 formulation as reported by the caregivers

Trial Locations

Locations (3)

Joint Clinical research Centre

🇺🇬

Kampala, Uganda

Epicentre Mbarara Research Centre

🇺🇬

Mbarara, Uganda

Baylor College of Medicine Children's Foundation Uganda

🇺🇬

Kampala, Uganda

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