Study to Investigate the Safety, Tolerability and Pharmacokinetics of AD 452 [(+)-Mefloquine] Compared With Racemic Mefloquine

NCT ID: NCT00931697

Last Updated: 2010-08-03

Study Results

Results pending

The study team has not published outcome measurements, participant flow, or safety data for this trial yet. Check back later for updates.

Basic Information

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Recruitment Status

COMPLETED

Clinical Phase

PHASE1

Total Enrollment

46 participants

Study Classification

INTERVENTIONAL

Study Start Date

2009-06-30

Study Completion Date

2009-11-30

Brief Summary

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Mefloquine is a quinolinemethanol antimalarial that is effective as therapy and prophylaxis for all species of malaria infecting humans, including multi-drug resistant Plasmodium falciparum. The marketed anti-malaria drug consists of two enantiomers of mefloquine.

Mefloquine's clinical utility has been impaired by its association with neuropsychiatric side effects. The pharmacological basis of mefloquine's side effects is not known but two of the most reported hypotheses relate to its action on (i) the adenosine receptor and (ii) its effect on the cholinesterase enzyme. For both of these mechanisms, there is a significant stereoselective activity of the two enantiomers. In vitro studies show that the (-) isomer is 50-100 fold more potent towards adenosine receptors compared with the (+) isomer. In addition, (-)-mefloquine has considerably more anti-cholinesterase activity. It has therefore been hypothesised that (+)-mefloquine may have a better central nervous system (CNS) safety profile compared with either the racemate or (-)-mefloquine.

This study is a randomized, ascending dose, double-blind, active and placebo-controlled, parallel group study in healthy male and female volunteers designed to investigate this hypothesis and to describe the comparative pharmacokinetics of the racemate and the single enantiomer.

Detailed Description

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Conditions

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Healthy Subjects

Study Design

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Allocation Method

RANDOMIZED

Intervention Model

PARALLEL

Primary Study Purpose

TREATMENT

Blinding Strategy

TRIPLE

Participants Caregivers Investigators

Study Groups

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AD 452 (+) mefloquine

Group Type EXPERIMENTAL

AD 452 (+) mefloquine

Intervention Type DRUG

Single dose delivered as over-encapsulated tablet at ascending doses

Racemic mefloquine

Group Type ACTIVE_COMPARATOR

Racemic Mefloquine

Intervention Type DRUG

Single dose delivered as over-encapsulated tablet at ascending dose

Placebo

Group Type PLACEBO_COMPARATOR

Placebo

Intervention Type DRUG

Over-encapsulated placebo to maintain blinding

Interventions

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AD 452 (+) mefloquine

Single dose delivered as over-encapsulated tablet at ascending doses

Intervention Type DRUG

Racemic Mefloquine

Single dose delivered as over-encapsulated tablet at ascending dose

Intervention Type DRUG

Placebo

Over-encapsulated placebo to maintain blinding

Intervention Type DRUG

Eligibility Criteria

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Inclusion Criteria

* A BMI of between 19 and 28
* Negative urine drugs of abuse and breath alcohol test
* Willing to use double barrier contraception for 13 weeks after administration of study drug

Exclusion Criteria

* Pregnant or lactating females
* Existence of any surgical or medical condition which, in the judgement of the Principal Investigator, might interfere with the absorption and disposition of the drug or with the aim of the study including clinically significant lactose intolerance
* Receipt of prescription medication within 21 days of the first study day or over the counter medication (with the exception of multi-vitamins or paracetamol) within 1 week before the planned dosing date without prior approval
* Definite or suspected personal or family history of adverse drug reaction or hypersensitivity to drugs with a chemical structure similar to AD 452
* Participation in a clinical study within the previous 12 weeks
* A history of sensitivity to antimalarial or related compounds
* Definite or suspected personal or family history of adverse drug reaction or hypersensitivity to drugs with a chemical structure similar to AD 452
* Active depression or a recent history of depression or generalised anxiety disorder
* Any personal history of psychosis or schizophrenia or other major psychiatric disorders or convulsions
* Previous exposure to racemic mefloquine
Minimum Eligible Age

18 Years

Maximum Eligible Age

50 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

Yes

Sponsors

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Medicines for Malaria Venture

OTHER

Sponsor Role collaborator

Treague Ltd

INDUSTRY

Sponsor Role lead

Responsible Party

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Treague Ltd

Principal Investigators

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Robert Tansley, MBBS

Role: STUDY_DIRECTOR

Treague Ltd

Locations

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LCG Bioscience

Cambridge, Cambridgeshire, United Kingdom

Site Status

Countries

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United Kingdom

Other Identifiers

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P-AD452-023

Identifier Type: -

Identifier Source: org_study_id

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