The study investigated the pharmacokinetics, safety, and tolerability of cadazolid in subjects with severe Clostridium difficile diarrhea (CDAD) and whether this influenced the quantity of cadazolid absorbed into the systemic circulation.
Study Type
INTERVENTIONAL
Allocation
NA
Masking
NONE
Enrollment
6
Cadazolid was provided as dry powder for oral suspension (Amber glass bottles of 60 mL). The powder was reconstituted with tap water by a pharmacist immediately prior to dispensing to subjects.
Clinical Hospital for Infective Disease
Zagreb, Croatia
Maximum plasma concentration (Cmax) of cadazolid
Blood samples for pharmacokinetic analysis taken immediately prior to dosing with cadazolid, and at 0.5, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours after dosing. Cmax was calculated on the basis of the blood sampling time points.
Time frame: 144 hours
Time to reach maximum plasma concentration (tmax) of cadazolid
Blood samples for pharmacokinetic analysis taken immediately prior to dosing with cadazolid, and at 0.5, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours after dosing. tmax was calculated on the basis of the blood sampling time points.
Time frame: 144 hours
Area under the plasma concentration-time curve (AUC(0-144h)) of cadazolid
Blood samples for pharmacokinetic analysis taken immediately prior to dosing with cadazolid, and at 0.5, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, and 144 hours after dosing. AUC(0-144) was calculated according to the linear trapezoidal rule using the measured concentration-time values above the limit of quantification.
Time frame: 144 hours
Unchanged cadazolid in urine up to Day 7
Urine was collected into standard-weight polyethylene containers over the following time intervals: 0-12 h, 12-24 h, 24-36 h, 36-48 h, 48-72 h, 72-96 h, 96-120 h, and 120-144 h. The concentration of cadazolid was determined using validated liquid chromatography-tandem mass spectrometry assays. The amount of drug excreted in the urine was obtained by multiplying the concentration of drug by the volume of matrix collected.
Time frame: 144 hours
Unchanged cadazolid in faeces up to Day 7
Faeces were collected in pre-weighed polypropylene boxes. The concentration of cadazolid was determined using validated liquid chromatography-tandem mass spectrometry assays. The amount of drug excreted in the faeces was obtained by multiplying the concentration of drug by the volume of matrix collected.
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Time frame: 144 hours
Change from baseline up to Day 7 in systolic blood pressure (SBP)
Blood pressure (systolic and diastolic) and pulse rate were measured using an automatic oscillometric device, always on the leading arm (i.e., leading arm = writing arm). Measurements were recorded in the supine position after the subject had rested for a 5-minute period.
Time frame: 144 hours
Change from baseline up to Day 7 in diastolic blood pressure (DBP)
Blood pressure (systolic and diastolic) and pulse rate were measured using an automatic oscillometric device, always on the leading arm (i.e., leading arm = writing arm). Measurements were recorded in the supine position after the subject had rested for a 5-minute period.
Time frame: 144 hours
Change from baseline up to Day 7 in pulse rate
Blood pressure (systolic and diastolic) and pulse rate were measured using an automatic oscillometric device, always on the leading arm (i.e., leading arm = writing arm). Measurements were recorded in the supine position after the subject had rested for a 5-minute period.
Time frame: 144 hours
Change from baseline to Day 7 in body weight
Body weight was measured using the same weighing scales.
Time frame: 144 hours
Change from baseline up to Day 7 in heart rate
Heart rate was determined from standard 12-lead electrocardiographs (ECGs) recorded in the supine position, after a 5-minute period of resting.
Time frame: 144 hours
Change from baseline up to Day 7 in PQ interval (time interval from the beginning of the P wave to the beginning of the QRS complex)
PQ interval was determined from standard 12-lead ECGs recorded in the supine position, after a 5-minute period of resting.
Time frame: 144 hours
Change from baseline up to Day 7 in QRS duration (time interval from the beginning of the Q wave to the end of the S wave)
QRS duration was determined from standard 12-lead ECGs recorded in the supine position, after a 5-minute period of resting.
Time frame: 144 hours
Change from baseline up to Day 7 in QT (time interval from beginning of the Q wave until end of the T wave)
QT interval was determined from standard 12-lead ECGs recorded in the supine position, after a 5-minute period of resting.
Time frame: 144 hours
Change from baseline up to Day 7 in QT interval according to Bazett's correction (QTcB)
QTcB interval was determined from standard 12-lead ECGs recorded in the supine position, after a 5-minute period of resting. The QTcB interval is the QT interval (interval from beginning of the Q wave until end of the T wave) corrected for heart rate with Bazett's formula (QTcB = QT/RR\^0.5 where RR is 60/heart rate)
Time frame: 144 hours
Change from baseline up to Day 7 in QT interval according to Fridericia's correction (QTcF)
QTcF interval was determined from standard 12-lead ECGs recorded in the supine position, after a 5-minute period of resting. The QTcF interval is the QT interval (interval from beginning of the Q wave until end of the T wave) corrected for heart rate with Fridericia's formula (QTcB = QT/RR\^0.33 where RR is 60/heart rate)
Time frame: 144 hours
Frequency of treatment-emergent ECG abnormalities from up to Day 7
Treatment-emergent abnormalities were determined from standard 12-lead ECGs recorded in the supine position, after a 5-minute period of resting. An ECG abnormality was considered treatment-emergent if it was not present during the screening period and/or at time of pre-dose assessment.
Time frame: 144 hours