MedPath

Safety and Tolerability of Chlorquine in Addition to Anti-tuberculosis Therapy

Phase 1
Recruiting
Conditions
Tuberculosis Infection
Interventions
Drug: Nivaquine ® (Chloroquine)
Registration Number
NCT05443178
Lead Sponsor
University of Zurich
Brief Summary

In vitro and in vivo data show promising results of adjunctive use of Chloroquine to standard tuberculosis therapy as Chloroquine enhances animicrobial effectiveness against intracellular MTB. To date, no safety data of the concurrent use of both treatments is availble. In a phase I trial, the investigators aim to evaluate safety and tolerability of the concurrent use of Chloroquine and standard anti-TB drug in healthy volunteers.

Detailed Description

Even though tuberculosis (TB) remains one of the top 10 causes of death worldwide in 2019, there exists a gap in development of new diagnostics and treatments. There is a substantial need for new TB regimens, which would ideally be shorter, more tolerable and more efficient in eradicating all subpopulations of mycobacterium tuberculosis (MTB). In this regard, a promising TB drug pipeline emerges through re-use of marketed non TB-drugs, re-engineering of existing anti-TB compounds and discovery of new compounds. In vitro data showed that Chloroquine (CQ) inhibits an efflux pump expressed on macrophages. Inhibition of this pump increases intracellular concentration of Isoniazid and Pyrazinamide and enhances antimicrobial effectiveness against intracellular MTB. Recently published in vivo mouse model data confirmed the positive effect of CQ combined with the standard anti-TB therapy.

In line with global attempts to enhance effectiveness and shorten TB therapy, the investigators propose to evaluate this combination in a clinical setting. The absence of clinical study data showing safety and tolerability of CQ administered with first-line anti-TB drugs in humans shows the need for the research team to conduct this study. the investigators hypothesize that additional CQ to standard 4-drug anti-TB therapy is safe and increases the efficacy against intracellular MTB, leading to a pronounced reduction of the intracellularly hiding bacteria and overall to an accelerated reduction of bacterial load. The major advantages of this new combination with CQ and the 4-drug anti-TB therapy are, that all substances are long-term approved, commercially available drugs and that effective CQ concentrations are well achievable in humans.

Primary objective of the study is to investigate the safety and tolerability of a combination of standard doses of Nivaquine® (Chloroquine) with standard doses of Rimstar® (4-drug anti-TB therapy) in healthy volunteers.

Secondary objective of the study is to assess drug concentration of the new combination (Nivaquine® and Rimstar®) in healthy volunteers over time.

Recruitment & Eligibility

Status
RECRUITING
Sex
All
Target Recruitment
16
Inclusion Criteria

Not provided

Exclusion Criteria

Not provided

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Cohort 1Nivaquine ® (Chloroquine)100 mg Nivaquine and 4 Tabl Rimstar peroral once daily before breakfast for 14 days
Cohort 2Nivaquine ® (Chloroquine)200 mg Chloroquine and 4 Tabl Rimstar peroral once daily before breakfast for 14 days
Cohort 3Nivaquine ® (Chloroquine)300 mg Chloroquine and 4 Tabl Rimstar peroral once daily before breakfast for 14 days
Dose extension groupNivaquine ® (Chloroquine)Dose escalation: XX mg Chloroquine (depending on results) and 4 Tabl Rimstar peroral once daily before breakfast for 14 days
Primary Outcome Measures
NameTimeMethod
Safety Laboratory samples Panel 5.1day 1

Total Bilirubin (umol/l)

Vital Signs 3.2day 7

temperature (°C)

Vital Signs 3.3day 14

temperature (°C)

Physicial examination 1.1day 14

Heart auscultation (normal/abnormal)

Physicial examination 2.2day 30

lung auscultation (normal, abnormal)

Physicial examination 3.1day 14

abdominal examination (normal, abnormal)

Physicial examination 3.2day 30

abdominal examination (normal, abnormal)

Physicial examination 4.1day 14

lymph node palpation (normal, abnormal)

Vital Signs 3.1day 1

temperature (°C)

Vital Signs 3.5day 30

temperature (°C)

Safety Laboratory samples Panel 1.1day 1

Sodium (mmol/l)

Safety Laboratory samples Panel 1.3day 14

Sodium (mmol/l)

Safety Laboratory samples Panel 2.2day 7

Potassium (mmol/l)

Safety Laboratory samples Panel 3.1day 1

Calcium (mmol/l)

Safety Laboratory samples Panel 4.1day 1

Creatinine (umol/l)

Physicial examination 1.2day 30

Heart auscultation (normal/abnormal)

Physicial examination 2.1day 14

lung auscultation (normal, abnormal)

Physicial examination 4.2day 30

lymph node palpation (normal, abnormal)

Physicial examination 5.1day 14

reflex testing (normal, abnormal)

Physicial examination 5.2day 30

reflex testing (normal, abnormal)

Physicial examination 6.2day 30

test vibration sense with tuning fork (mallelor left and right X/8)

Vital Signs 1.3day 14

heart rate (beats/min)

Vital Signs 1.4day 15

heart rate (beats/min)

Vital Signs 1.5day 30

heart rate (beats/min)

Vital Signs 2.1day 1

blood pressure (mmHg)

Vital Signs 2.2day 7

blood pressure (mmHg)

Vital Signs 2.4day 15

blood pressure (mmHg)

Vital Signs 2.5day 30

blood pressure (mmHg)

Vital Signs 3.4day 15

temperature (°C)

Safety Laboratory samples Panel 1.2day 7

Sodium (mmol/l)

Physicial examination 6.1day 14

test vibration sense with tuning fork (mallelor left and right X/8)

Vital Signs 1.1day 1

heart rate (beats/min)

Vital Signs 1.2day 7

heart rate (beats/min)

Vital Signs 2.3day 14

blood pressure (mmHg)

Safety Laboratory samples Panel 1.4day 30

Sodium (mmol/l)

Safety Laboratory samples Panel 2.3day 14

Potassium (mmol/l)

Safety Laboratory samples Panel 2.4day 30

Potassium (mmol/l)

Safety Laboratory samples Panel 3.2day 7

Calcium (mmol/l)

Safety Laboratory samples Panel 3.3day 14

Calcium (mmol/l)

Safety Laboratory samples Panel 3.4day 30

Calcium (mmol/l)

Safety Laboratory samples Panel 4.2day 7

Creatinine (umol/l)

Safety Laboratory samples Panel 4.3day 14

Creatinine (umol/l)

Safety Laboratory samples Panel 4.4day 30

Creatinine (umol/l)

Safety Laboratory samples Panel 5.3day 14

Total Bilirubin (umol/l)

Safety Laboratory samples Panel 5.4day 30

Total Bilirubin (umol/l)

Safety Laboratory samples Panel 5.2day 7

Total Bilirubin (umol/l)

Safety Laboratory samples Panel 7.1day 1

Glucose (mmol/l)

Safety Laboratory samples Panel 8.4day 30

CRP (mg/l)

Safety Laboratory samples Panel 10.4day 30

Platlets (G/l)

Safety Laboratory samples Panel 12.2day 30

Blood pregnancy test (Blood beta-hCG)

Urinanalysis 1.3day 14

Dipstick: protein negative/+/++/+++

Urinanalysis 2.2day 7

Dipstick: white blood cells negative/+/++/+++

Urinanalysis 2.3day 14

Dipstick: white blood cells negative/+/++/+++

Urinanalysis 2.4day 30

Dipstick: white blood cells negative/+/++/+++

Urinanalysis 3.1day 1

Dipstick: red blood cells negative/+/++/+++

Urinanalysis 3.2day 7

Dipstick: red blood cells negative/+/++/+++

Safety Laboratory samples Panel 2.1day 1

Potassium (mmol/l)

Safety Laboratory samples Panel 6.3day 14

ALT (U/l)

Safety Laboratory samples Panel 6.4day 30

ALT (U/l)

Safety Laboratory samples Panel 7.2day 7

Glucose (mmol/l)

Safety Laboratory samples Panel 7.3day 14

Glucose (mmol/l)

Safety Laboratory samples Panel 7.4day 30

Glucose (mmol/l)

Safety Laboratory samples Panel 8.2day 7

CRP (mg/l)

Safety Laboratory samples Panel 10.1day 1

Platlets (G/l)

Safety Laboratory samples Panel 11.3day 14

White blood cell (G/l)

Safety Laboratory samples Panel 6.1day 1

ALT (U/l)

Safety Laboratory samples Panel 6.2day 7

ALT (U/l)

Safety Laboratory samples Panel 8.1day 1

CRP (mg/l)

Safety Laboratory samples Panel 9.1day 1

Haemoglobin (g/l)

Safety Laboratory samples Panel 9.2day 7

Haemoglobin (g/l)

Safety Laboratory samples Panel 9.3day 14

Haemoglobin (g/l)

Safety Laboratory samples Panel 9.4day 30

Haemoglobin (g/l)

Safety Laboratory samples Panel 10.2day 7

Platlets (G/l)

Safety Laboratory samples Panel 10.3day 14

Platlets (G/l)

Safety Laboratory samples Panel 11.1day 1

White blood cell (G/l)

Safety Laboratory samples Panel 11.2day 7

White blood cell (G/l)

Safety ophtalmological examination 1.2day 30

Refraction both sides (+/-)

Safety ophtalmological examination 1.5day 30

Color sense test according to Panel D-15 bilateral (normal/abnormal)

Occurence of adverse events and serious adverse events 1.1day 1

according to GCP Guideline

Occurence of adverse events and serious adverse events 1.2day 7

according to GCP Guideline

Occurence of adverse events and serious adverse events 1.3day 14

according to GCP Guideline

Occurence of adverse events and serious adverse events 1.4day 15

according to GCP Guideline

Occurence of adverse events and serious adverse events 1.5day 30

according to GCP Guideline

Occurence of adverse events and serious adverse events 1.6day 256

according to GCP Guideline

Safety Laboratory samples Panel 8.3day 14

CRP (mg/l)

Safety Laboratory samples Panel 11.4day 30

White blood cell (G/l)

Urinanalysis 1.1day 1

Dipstick: protein negative/+/++/+++

Urinanalysis 2.1day 1

Dipstick: white blood cells negative/+/++/+++

Safety Laboratory samples Panel 12.1day 7

Blood pregnancy test (Blood beta-hCG)

Urinanalysis 1.2day 7

Dipstick: protein negative/+/++/+++

Urinanalysis 1.4day 30

Dipstick: protein negative/+/++/+++

Urinanalysis 3.3day 14

Dipstick: red blood cells negative/+/++/+++

Urinanalysis 3.4day 30

Dipstick: red blood cells negative/+/++/+++

Urinanalysis 4.1day 1

Dipstick: Glucose negative/+/++/+++

Urinanalysis 4.2day 7

Dipstick: Glucose negative/+/++/+++

Urinanalysis 4.3day 14

Dipstick: Glucose negative/+/++/+++

Urinanalysis 4.4day 30

Dipstick: Glucose negative/+/++/+++

Safety 12 lead ECG 1.1day 7

Rate/min

Safety 12 lead ECG 1.230

Rate/min

Safety 12 lead ECG 2.1day 7

Rhythm (regular/irregular)

Safety 12 lead ECG 2.2day 30

Rhythm (regular/irregular)

Safety 12 lead ECG 3.1day 7

PQ interval (ms)

Safety 12 lead ECG 3.3day 30

PQ interval (ms)

Safety 12 lead ECG 4.1day 7

QRS interval (ms)

Safety 12 lead ECG 4.2day 30

QRS interval (ms)

Safety 12 lead ECG 5.1day 7

ST Segment (normal/elevation/depression)

Safety 12 lead ECG 5.2day 30

ST Segment (normal/elevation/depression)

Safety ophtalmological examination 1.1day 30

Slit lamp examaniation both sides (normal/abnormal)

Safety ophtalmological examination 1.3day 30

Biomicroscopy of the central fundus both sides(normal/abnormal)

Safety ophtalmological examination 1.4day 30

Applanation tonometry and stereoscopic papilla evaluation bilateral (normal/abnormal), Color sense test according to Panel D-15 right and left side (normal/abnormal)

Secondary Outcome Measures
NameTimeMethod
Drug concentration over time measured by the pharmacokineticsday 14 prior to dosing (-15 until -5 minutes) and 1, 2, 4, 6 and 24 hours after dosing

drug concentration (mg/l) of Rifampicin, Isoniazid, 25-O-Desacetylrifampicin, Ethambutol, Pyrazinamide, Chloroquine, Desethylchloroquine

Trial Locations

Locations (1)

Clinical Trial Center

🇨🇭

Zurich, Switzerland

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