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Population Pharmacokinetics of Palbociclib in a Real-World Situation

Laboratoire de Pharmacologie Clinique et Toxicologie, CHU Besançon, 25000 Besançon, France
INSERM, EFS BFC, UMR1098, RIGHT, Interactions Greffon-Hôte-Tumeur/Ingénierie Cellulaire et Génique, University of Bourgogne Franche-Comté, 25000 Besançon, France
Oncology Department, Centre Georges-François Leclerc, 21000 Dijon, France
INSERM U1231, University of Burgundy Franche-Comté, 21000 Dijon, France
Pharmacy Department, Centre Georges-François Leclerc, 21000 Dijon, France
Author to whom correspondence should be addressed.
Academic Editor: Thomas Efferth
Pharmaceuticals 2021, 14(3), 181;
Received: 8 January 2021 / Revised: 4 February 2021 / Accepted: 19 February 2021 / Published: 24 February 2021
Palbociclib is an oral cyclin-dependent kinase inhibitor that is used in combination with aromatase inhibitors in the treatment of postmenopausal women with metastatic breast cancer. Its metabolism profile is associated with an important interpatient variability. We performed a population pharmacokinetics study of palbociclib in women routinely followed in a cancer center. One hundred and fifty-one samples were analyzed. The sampling times after administration ranged from 0.9 to 75 h and the samples were taken between 1 and 21 days after the beginning of the palbociclib cycle. Palbociclib was determined using a validated mass spectrometry method. The best model that described the concentrations was a one-compartment model with first-order absorption and an absorption lag time. Interindividual variability could only be estimated on the clearance and the first-order absorption. Creatinine clearance was found to be a significant covariate for the apparent clearance. No significant covariates could be observed with the first-order absorption. First-order absorption and absorption lag times were difficult to assess because of the constraints linked to the real-world setting due to the small number of samples used during the absorption process. However, palbociclib apparent clearance was satisfactorily estimated. Population pharmacokinetics (POP PK) with palbociclib could help to optimize dosing. View Full-Text
Keywords: palbociclib; population pharmacokinetics; real-world situation palbociclib; population pharmacokinetics; real-world situation
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MDPI and ACS Style

Royer, B.; Kaderbhaï, C.; Fumet, J.-D.; Hennequin, A.; Desmoulins, I.; Ladoire, S.; Ayati, S.; Mayeur, D.; Ilie, S.; Schmitt, A. Population Pharmacokinetics of Palbociclib in a Real-World Situation. Pharmaceuticals 2021, 14, 181.

AMA Style

Royer B, Kaderbhaï C, Fumet J-D, Hennequin A, Desmoulins I, Ladoire S, Ayati S, Mayeur D, Ilie S, Schmitt A. Population Pharmacokinetics of Palbociclib in a Real-World Situation. Pharmaceuticals. 2021; 14(3):181.

Chicago/Turabian Style

Royer, Bernard, Courèche Kaderbhaï, Jean-David Fumet, Audrey Hennequin, Isabelle Desmoulins, Sylvain Ladoire, Siavoshe Ayati, Didier Mayeur, Sivia Ilie, and Antonin Schmitt. 2021. "Population Pharmacokinetics of Palbociclib in a Real-World Situation" Pharmaceuticals 14, no. 3: 181.

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