Phase 1
Completed N=28
A Study To Describe The Effect Of Impaired Hepatic Function Of The Pharmacokinetics Of Palbociclib
Healthy, Hepatic Insufficiency
Source: ClinicalTrials.gov NCT02334800 ↗
Enrolled (actual)
28
Serious AEs
3.6%
Results posted
Jan 2018
Primary outcomePrimary: Area Under the Concentration-Time Curve From Time 0 Extrapolated to Infinite Time (AUCinf) — 1031; 758.9; 1189; 1378 nanogram*hour/milliliter (ng*hr/mL)
Summary
This is a phase 1 study to describe the plasma pharmacokinetics of a single oral 75mg dose of palbociclib administered to healthy volunteers, and subjects with mild, moderate, and severely impaired hepatic function.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Area Under the Concentration-Time Curve From Time 0 Extrapolated to Infinite Time (AUCinf) |
1031; 758.9; 1189; 1378 | — |
| PRIMARY Maximum Plasma Concentration (Cmax) |
28.64; 27.20; 33.72; 37.20 | — |
| SECONDARY Unbound AUCinf (AUCinf,u) |
196.6; 163.2; 264.1; 347.8 | — |
| SECONDARY Area Under the Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) |
973.3; 708.6; 1125; 1311 | — |
| SECONDARY Unbound AUClast (AUClast,u) |
185.5; 152.4; 250.3; 331.0 | — |
| SECONDARY Apparent Clearance After Oral Dose(CL/F) |
72.64; 98.84; 63.15; 54.42 | — |
| SECONDARY Unbound CL/F (CLu/F) |
381.3; 459.2; 283.8; 215.8 | — |
| SECONDARY Unbound Cmax (Cmax,u) |
5.456; 5.858; 7.501; 9.399 | — |
| SECONDARY Fraction of Unbound Drug in Plasma (fu) |
0.1910; 0.2157; 0.2236; 0.2546 | — |
| SECONDARY Terminal Half-Life (t1/2) |
25.84; 27.23; 35.03; 33.84 | — |
| SECONDARY Time for Cmax (Tmax) |
8.00; 6.00; 6.00; 6.00 | — |
| SECONDARY Apparent Volunm of Distribution After Oral Dose (Vz/F) |
2679; 3814; 3168; 2627 | — |
| SECONDARY Unbound Vz/F (Vz,u/F) |
14060; 17730; 14260; 10410 | — |
| SECONDARY Number of Participants With Treatment Emergent Adverse Events |
2; 0; 2; 1 | — |
| SECONDARY Number of Participants With Treatment Emergent Serious Adverse Events |
0; 0; 1; 0 | — |
| SECONDARY Number of Participants With Laboratory Test Abnormalities (Without Regard to Baseline Abnormality) |
6; 6; 5; 7 | — |
| SECONDARY Number of Participants With Physical Examination Test Abnormalities (Change From Prior Visit) |
0; 0; 2; 0 | — |
| SECONDARY Number of Participants With Post Baseline Vital Signs Values Meeting Categorical Summarization Criteria |
0; 1; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Post Baseline Electrocardiogram Values Meeting Categorical Summarization Criteria (Maximum Absolute Values) |
0; 0; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Post Baseline Electrocardiogram Values Meeting Categorical Summarization Criteria (Maximum Increase From Baseline) |
0; 0; 0; 0; 0; 0 | — |
| SECONDARY Number of Participants With Concomitant Medications |
0; 3; 7; 7 | — |
Eligibility Criteria
Inclusion Criteria
- Body Mass Index (BMI) of 18 to 40 kg/m2; and a total body weight >50 kg (110 lbs)
- Evidence of a personally signed and dated informed consent document indicating that the subject has been informed of all pertinent aspects of the study
- Subjects who are willing and able to comply with all scheduled visits, treatment plan, laboratory tests, and other study procedures
Exclusion Criteria
- Any condition possibly affecting drug absorption (eg, gastrectomy)
- A positive urine drug screen
- Pregnant female subjects; breastfeeding female subjects; female subjects of childbearing potential; male subjects with partners currently pregnant; male subjects of childbearing potential who are unwilling or unable to use a highly effective method of contraception for the duration of the study and for 90 days after the last dose of investigational product
- History of sensitivity to heparin or heparin-induced thrombocytopenia
- Blood donation of approximately 1 pint (500 mL) or more within 56 days prior to dosing
- Unwilling or unable to comply with the Lifestyle Guidelines described in this protocol
- Use of tobacco or nicotine products in excess of 5 cigarettes per day (or equivalent)
- History of sensitivity to palbociclib
Data sourced from ClinicalTrials.gov (NCT02334800). 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. Informational only — not medical advice.