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Study to Compare the Pharmacokinetics of Mycophenolate Mofetil Metabolites From Four Tablet Formulations in Healthy Participants

Phase 1
Completed
Conditions
Healthy Volunteers
Interventions
Drug: Renodapt
Drug: Mycept
Drug: Cellmune
Registration Number
NCT02981290
Lead Sponsor
Hoffmann-La Roche
Brief Summary

This is a single center, randomized, open label, 4-treatment, 4-period, 4-sequence, 4-way crossover study to compare the pharmacokinetics of mycophenolate mofetil (MMF) metabolites from 4 tablet formulations in healthy participants.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
32
Inclusion Criteria

A body mass index (BMI) between 18 and 32 kilogram per meter square (kg/m^2)

Exclusion Criteria
  • Any evidence of clinically significant allergic, renal, cardiac, bronchopulmonary, vascular, gastro-intestinal, neurological, metabolic or immunodeficiency disorders, cancer, hepatitis or cirrhosis
  • Any evidence of gall bladder surgery, surgery of the gastro-intestinal tract or any other medical condition considered likely to affect drug absorption
  • Any major illness within 2 months prior to first dosing or febrile illness within 14 days prior to first dosing
  • Any known history of clinically significant allergic reactions or drug hypersensitivity, especially hypersensitivity to MMF or mycophenolic acid (MPA)
  • Any other ongoing concomitant disease or condition that could interfere with, or the treatment of which might interfere with, the conduct of the study, or that would, in the opinion of the investigator, pose an unacceptable risk to the participants
  • Any prescribed or over-the-counter (OTC) medication, herbal medicine or dietary aid taken within 2 weeks before the first study drug dosing or within six times the elimination half-life of the medication before the first study drug dosing

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Renodapt Then Mycept Then Cellmune Then CellCeptCellmuneParticipants will receive Renodapt in first treatment period (each treatment period= 3 days) followed by Mycept in second treatment period then Cellmune in third treatment period and CellCept in fourth treatment period. A washout period of 7 days will be separating each treatment period.
Mycept Then CellCept Then Renodapt Then CellmuneRenodaptParticipants will receive Mycept in first treatment period (each treatment period= 3 days) followed by CellCept in second treatment period then Renodapt in third treatment period and Cellmune in fourth treatment period. A washout period of 7 days will be separating each treatment period.
Cellmune Then Renodapt Then CellCept Then MyceptRenodaptParticipants will receive Cellmune in first treatment period (each treatment period= 3 days) followed by Renodapt in second treatment period then CellCept in third treatment period and Mycept in fourth treatment period. A washout period of 7 days will be separating each treatment period.
Mycept Then CellCept Then Renodapt Then CellmuneMyceptParticipants will receive Mycept in first treatment period (each treatment period= 3 days) followed by CellCept in second treatment period then Renodapt in third treatment period and Cellmune in fourth treatment period. A washout period of 7 days will be separating each treatment period.
Mycept Then CellCept Then Renodapt Then CellmuneCellmuneParticipants will receive Mycept in first treatment period (each treatment period= 3 days) followed by CellCept in second treatment period then Renodapt in third treatment period and Cellmune in fourth treatment period. A washout period of 7 days will be separating each treatment period.
Renodapt Then Mycept Then Cellmune Then CellCeptRenodaptParticipants will receive Renodapt in first treatment period (each treatment period= 3 days) followed by Mycept in second treatment period then Cellmune in third treatment period and CellCept in fourth treatment period. A washout period of 7 days will be separating each treatment period.
Renodapt Then Mycept Then Cellmune Then CellCeptMyceptParticipants will receive Renodapt in first treatment period (each treatment period= 3 days) followed by Mycept in second treatment period then Cellmune in third treatment period and CellCept in fourth treatment period. A washout period of 7 days will be separating each treatment period.
CellCept Then Cellmune Then Mycept Then RenodaptCellmuneParticipants will receive CellCept in first treatment period (each treatment period= 3 days) followed by Cellmune in second treatment period then Mycept in third treatment period and Renodapt in fourth treatment period. A washout period of 7 days will be separating each treatment period.
Cellmune Then Renodapt Then CellCept Then MyceptMyceptParticipants will receive Cellmune in first treatment period (each treatment period= 3 days) followed by Renodapt in second treatment period then CellCept in third treatment period and Mycept in fourth treatment period. A washout period of 7 days will be separating each treatment period.
Cellmune Then Renodapt Then CellCept Then MyceptCellmuneParticipants will receive Cellmune in first treatment period (each treatment period= 3 days) followed by Renodapt in second treatment period then CellCept in third treatment period and Mycept in fourth treatment period. A washout period of 7 days will be separating each treatment period.
CellCept Then Cellmune Then Mycept Then RenodaptRenodaptParticipants will receive CellCept in first treatment period (each treatment period= 3 days) followed by Cellmune in second treatment period then Mycept in third treatment period and Renodapt in fourth treatment period. A washout period of 7 days will be separating each treatment period.
CellCept Then Cellmune Then Mycept Then RenodaptMyceptParticipants will receive CellCept in first treatment period (each treatment period= 3 days) followed by Cellmune in second treatment period then Mycept in third treatment period and Renodapt in fourth treatment period. A washout period of 7 days will be separating each treatment period.
Renodapt Then Mycept Then Cellmune Then CellCeptCellCeptParticipants will receive Renodapt in first treatment period (each treatment period= 3 days) followed by Mycept in second treatment period then Cellmune in third treatment period and CellCept in fourth treatment period. A washout period of 7 days will be separating each treatment period.
Mycept Then CellCept Then Renodapt Then CellmuneCellCeptParticipants will receive Mycept in first treatment period (each treatment period= 3 days) followed by CellCept in second treatment period then Renodapt in third treatment period and Cellmune in fourth treatment period. A washout period of 7 days will be separating each treatment period.
Cellmune Then Renodapt Then CellCept Then MyceptCellCeptParticipants will receive Cellmune in first treatment period (each treatment period= 3 days) followed by Renodapt in second treatment period then CellCept in third treatment period and Mycept in fourth treatment period. A washout period of 7 days will be separating each treatment period.
CellCept Then Cellmune Then Mycept Then RenodaptCellCeptParticipants will receive CellCept in first treatment period (each treatment period= 3 days) followed by Cellmune in second treatment period then Mycept in third treatment period and Renodapt in fourth treatment period. A washout period of 7 days will be separating each treatment period.
Primary Outcome Measures
NameTimeMethod
Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0-inf)] of MPAPredose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of MPAPredose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
Maximum Observed Plasma Concentration (Cmax) of MPAPredose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
Time to Reach Maximum Observed Plasma Concentration (Tmax) of MPAPredose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
Absorption Lag Time (Tlag) of MPAPredose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
Plasma Terminal Half-Life (t1/2) of MPAPredose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
Apparent Oral Clearance (CL/F) of MPAPredose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
Secondary Outcome Measures
NameTimeMethod
Apparent Oral Volume of Distribution (V/F) of MPAPredose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
AUC (0-inf) of the Glucuronide Metabolite of MPA (MPAG)Predose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
AUClast of MPAGPredose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
Cmax of MPAGPredose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
Tmax of MPAGPredose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
Tlag of MPAGPredose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
t1/2 of MPAGPredose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
CL/F of MPAGPredose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
V/F of MPAGPredose (0.5 hours), and 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 16, 24, 36, 48 hours post dose on Day 1
Percentage of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)Baseline up to 9 weeks

Trial Locations

Locations (1)

Christchurch Clinical Studies Trust

🇳🇿

Christchurch, New Zealand

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