Phase 1
N=12
A Study to Assess the Effect of Ceftobiprole on the PK of Pitavastatin and on Plasma Levels of Coproporphyrin
Drug-drug Interaction Study
Bottom Line
View on ClinicalTrials.gov: NCT06808646 ↗Enrolled (actual)
12
Serious AEs
0.0%
Results posted
Apr 2026
Primary outcome: Primary: Maximum Observed Plasma Concentration (Cmax) of Pitavastatin — 42.79; 33.54 ng/mL
Study Design & Population
- Study type
- Interventional
- Phase
- Phase 1
- Interventions
- pitavastatin (Drug); pitavastatin single dose combined with ceftobiprole (Drug)
- Age
- Adult, Older Adult · 18+ yrs
- Sex
- All
- Sponsor
- Basilea Pharmaceutica
- Primary completion
- Feb 2025
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Maximum Observed Plasma Concentration (Cmax) of Pitavastatin |
42.79; 33.54 | — |
| PRIMARY Area Under the Plasma Concentration-time Curve up to Time (AUC0-t) After Pitavastatin Administration |
100.29; 86.63 | — |
| PRIMARY Area Under the Plasma Concentration-time Curve From Time 0 to Infinity (AUC0-inf) After Pitavastatin Administration |
105.42; 91.59 | — |
| SECONDARY Cmax of Coproporphyrin I (CP-I) |
0.41; 0.42 | — |
| SECONDARY Area Under the Plasma Level-time Curve up to Time 25.5 Hours (AUEC0-25.5h) of CP-I in Plasma |
9.08; 9.27 | — |
| SECONDARY Cmax of Ceftobiprole in Plasma |
26361; 27423 | — |
| SECONDARY Area Under the Plasma Concentration-time Curve up to 8 Hours (AUC0-8h) After IV Ceftobiprole |
104204; 105623 | — |
| SECONDARY Cmax of the Pitavastatin Metabolite Pitavastatin Lactone in Plasma After Pitavastatin Administration |
15.91; 14.39 | — |
| SECONDARY AUC0-t of the Pitavastatin Metabolite Pitavastatin Lactone in Plasma After Pitavastatin Administration |
181.18; 157.11 | — |
| SECONDARY AUC0-inf of of the Pitavastatin Metabolite Pitavastatin Lactone in Plasma After Pitavastatin Administration |
196.73; 171.60 | — |
| SECONDARY Number of Participants Reporting Treatment-emergent Adverse Events (TEAEs) After Administration of Ceftobiprole Without and With a Single Oral Dose of Pitavastatin |
0; 0; 0; 5; 7; 5 | — |
Summary
The goal of this clinical study was to determine the effect of the test drug ceftobiprole (a drug approved for the treatment of bacterial infections) on the elimination of pitavastatin (a drug approved for the treatment of increased levels of cholesterol in blood) from the body. This interaction was investigated by pharmacokinetic (PK) assessments. The clinical study also investigated the safety of ceftobiprole and how well ceftobiprole was tolerated by healthy subjects when it was administered in combination with pitavastatin.
Eligibility Criteria
Main Inclusion Criteria:
- Body mass index: 18.0 to 30.0 kg/m2, inclusive
- Good physical and mental health
- Normal renal function (creatinine clearance ≥ 90 mL/min as determined by the Cockcroft-Gault equation)
- Female participants of childbearing potential were required not be pregnant or lactating and had to agree to use adequate contraception
- Male subjects, if not surgically sterilized, were required to agree to use adequate contraception
- All prescribed medication had to be stopped at least 30 days prior to admission to the clinical research center (an exception was made for hormonal contraceptives)
- All over-the-counter medication, vitamin preparations and other food supplements, or herbal medications (e.g., St. John's wort) had to be stopped at least 14 days prior to admission to the clinical research center
- Ability and willingness to abstain from alcohol from 48 hours (2 days) prior to Screening and admission to the clinical research center
- Ability and willingness to abstain from methylxanthine-containing beverages or food from 48 hours (2 days) prior to admission to the clinical research center
Main Exclusion Criteria:
- History of relevant drug and/or food allergies, particularly to antibiotics.
- Subject received a known potent inhibitor of OATP1B activity within 30 days prior to admission
- Subject received a potential inducer of OATP1B activity within 30 days prior to admission
- Subject had a history of seizures
- Subject had a history of frequent diarrhea
- Smoking more than 5 cigarettes, 1 cigar, or 1 pipe daily; the use of tobacco products in the 48 hours (2 days) prior to admission
- History of alcohol abuse or drug addiction within 12 months prior to Screening.
- Average intake of more than 24 units of alcohol per week
- Positive drug and/or alcohol screen
- Donation or loss of more than 450 mL of blood within 60 days prior to the first pitavastatin administration on Day 1 of the current study. Donation or loss of more than 1.5 liters of blood (for male subjects)/more than 1.0 liters of blood (for female subjects) in the 10 months prior to the first pitavastatin administration on Day 1 of the current study.
Data sourced from ClinicalTrials.gov (NCT06808646). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.