A Phase 1 study to assess the bioavailability and pharmacokinetics of a 600 mg immediate release tablet formulation of lefamulin when administered to fed and fasted healthy subjects in comparison to an intravenous formulation and a capsule formulation.
This is a single center, single cohort, open label, randomized, four- period cross-over study with healthy subjects receiving a single dose of lefamulin at four study sessions at least 4 days apart. Lefamulin will be taken: 1) as 600 mg IR tablet orally in the fasted state; 2) as 600 mg API in capsule (3 x 200 mg capsules) orally in the fasted state; 3) as 150 mg i.v. infusion in 250 mL citrate buffered saline over 1 h; 4) as 600 mg IR tablet orally one hour after breakfast. The order will be randomized. A total of 20 healthy subjects will be enrolled in the study. The same subjects will take part in all study sessions. After each study session, the Safety Monitoring Team will review the safety and tolerance data before the commencement of the subsequent session.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Masking
NONE
Enrollment
20
Lefamulin administered iv or orally in the fasted state and orally in the fed state
Quotient Clinical
Nottingham, United Kingdom
The area under the concentration time curve (AUC) of an intravenous and oral formulation of lefamulin in the fasting state
Time frame: 36 hours
The area under the concentration time curve (AUC) of a tablet and capsule formulation of lefamulin in the fasting state
Time frame: 36 hours
The area under the concentration time curve (AUC) of a 600 mg IR tablet of lefamulin in the fed state
Time frame: 36 hours
Assessment of the safety and tolerability of lefamulin when administered, as single doses orally and i.v. to healthy subjects aged 18 to 55 years (adverse events, laboratory assessments, vital signs and electrocardiograms)
Assessment of safety and tolerability by recording adverse events, laboratory assessments, vital signs and electrocardiograms
Time frame: 36 hours
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