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Pharmacokinetic Parameters of Innovative Valganciclovir Versus Generic Valganciclovir

Not Applicable
Completed
Conditions
Kidney Transplantation
Cytomegalovirus Infections
Pharmacokinetics
Therapeutic Equivalency
Interventions
Registration Number
NCT03631316
Lead Sponsor
Luis Eduardo Morales Buenrostro
Brief Summary

Cytomegalovirus (CMV) is the most common opportunistic viral pathogen in solid organ transplant receptors (SOTR). In Mexico, the experience using generic immunosuppressants have been demonstrated a wide variation in the pharmacokinetic parameters between generic and innovative formulation, resulting in a suboptimal absorption of the drug and reaching infratherapeutic trough levels in blood. In this study the investigators will compare the pharmacokinetic parameters of innovative and generic valganciclovir in renal transplant recipients.

Detailed Description

Cytomegalovirus (CMV) is the most common opportunistic viral pathogen in solid organ transplant receptors (SOTR). In the absence of prophylaxis, the frequency of CMV disease in high-risk recipients (R- / D +) is 60% and 20% for intermediate-risk patients (R + / D + or -). For universal prophylaxis, the antivirals most commonly used are valganciclovir (valGCV) and IV ganciclovir. ValGCV, a prodrug of ganciclovir, has a bioavailability of 60%, which represents more than 10 times that those obtained with ganciclovir.

Pharmacokinetic studies of Valganciclovir in SOTR have been demonstrated that insufficient doses can diminish its clinical efficacy and the development of viral resistance, while excessive doses can increase its toxicity.

The risk of viremia may be associated with ineffective plasma doses, as described by Wiltshire et al., where values of the area under the curve (AUC) between 40 and 50 μg/h/ml were associated with a lower incidence of viremia, while lower AUC values are associated with an increase 8 times more for viral replication rates. As a result, pharmacokinetic studies in SOTR guide the investigators in continuing with the research of their clinical impact.

A generic drug before their release to the market needs to show that is bioequivalent with the innovative drug, assuming that it has the same therapeutic effects.

The studies for demonstrate bioequivalence are carried out in controlled conditions with healthy participants, different of SOTR characteristics as: age, gender, race, comorbidities and concomitant medication. In addition, the excipients used in generic drug are different from those of the innovative drug, so the properties of the formulation can be modified (particle size or half-life), therefore, the efficacy and drug safety.

The primary outcome will be compare the pharmacokinetic parameters of the innovative versus generic formulation of valGCV in renal transplant recipients.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
8
Inclusion Criteria
  • Signed consent form for the study
  • Age between 18 and 70 years
  • Kidney transplant recipients who are stable during their follow-up
  • Kidney transplant recipients between day 31 and 90 post-transplant surgery
  • Kidney transplant recipients under prophylaxis with valganciclovir
Exclusion Criteria
  • Participants who can not stay 12 hours at the hospital for taking the blood samples.
  • Participants with an acute rejection event
  • Participants with active cytomegalovirus disease
  • Participants with measurements of pharmacokinetic parameters with a single formulation without comparator
  • Participants that withdraw their informed consent

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Innovative valganciclovirInnovative ValganciclovirThe same participant will receive innovative drug valcyte (roche), 450 mg tablets, total dosage 900 mg daily during 4 days.
Generic valganciclovirGeneric ValganciclovirParticipants will receive generic formulation (Pisa) of valganciclovir, 450 mg tablets, total dosage 900 mg daily for 4 days.
Primary Outcome Measures
NameTimeMethod
Area Under the Curve, AUC (ng/h/mL)At day 4 of treatment

AUC (ngh/mL) in both drugs (innovative and generic)

Secondary Outcome Measures
NameTimeMethod
Maximum serum concentration, Cmax (ng/mL)At day 4 of treatment

Cmax (ng/mL) in both drugs (innovative and generic)

Initial concentration, C0 (ng/mL)At day 4 of treatment

C0 (ng/mL) in both drugs (innovative and generic)

Total clearance of the drug, CL/F (L/h)At day 4 of treatment

CL/F (L/h), in both drugs (innovative and generic)

Distribution volume, Vd/F (L/h)At day 4 of treatment

Vd/F (L/h), in both drugs (innovative and generic)

Trial Locations

Locations (1)

Instituto Nacional de Ciencias Medicas y Nutricion Salvador Zubiran

🇲🇽

Mexico City, Mexico

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