Genetic polymorphisms of <i>ABCB1</i> (P-glycoprotein) as a covariate influencing daptomycin pharmacokinetics: a population analysis in patients with bone and joint infection

Bricca, Romain; Goutelle, Sylvain; Roux, Sandrine; Gagnieu, Marie‐Claude; Becker, Agathe; Conrad, Anne; Valour, Florent; Laurent, François; Triffault-Fillit, Claire; Chidiac, Christian; Ferry, Tristan; Perpoint, Thomas; Boibieux, A.; Biron, F.; Miailhes, Patrick; Ader, Florence; Bosch, Alexie; Daoud, Fatiha; Lippman, Johanna; Braun, E.; Lustig, Sébastien; Servien, Elvire; Gaillard, Romain; Schneider, Antoine; Gunst, Stanislas; Batailler, Cécile; Michel-Henry, Fessy; Herry, Yannick; Viste, Anthony; Chaudier, Philippe; Courtin, Cyril; Louboutin, Lucie; Martres, Sébastien; Trouillet, Franck; Barrey, Cédric; Jouanneau, Emmanuel; Jacquesson, Timothée; Mojallal, Ali; Braye, F.; Boucher, F.; Shipkov, Hristo; Château, J.; Céruse, Philippe; Fuchsmann, Carine; Gleizal, A.; Aubrun, Frédéric; Dziadzko, Mikhail; Macabéo, Caroline; Rasigade, Jean-Philippe; Beraut, Laetitia; Dupieux, Céline; Kolenda, Camille; Josse, Jérôme; Craighero, Fabien; Boussel, Loîc; Pialat, Jean‐Baptiste; Morelec, I.; Janier, Marc; Giammarile, Francesco; Tod, Michel; Mabrut, Eugénie

doi:10.1093/jac/dky541

Cited by 11 publications

(8 citation statements)

References 34 publications

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“…In two studies, clearance has been shown to be 20-44% lower for female subjects than for male subjects. [56,80,81] However, in some other studies, difference of clearance between genders was not significant. [82,101] It may be hypothesized that gender could be a better descriptor of the influence of body size on the clearance of daptomycin, but this requires further investigation.…”

Section: Gendermentioning

confidence: 72%

“…[55] In patients (n=81) with bone and joint infection, the volume of distribution of daptomycin was reported to be 25% lower in individuals having the CGC/CGC haplotype for pgp compared with any other haplotype, which, according to the authors, could be due to a greater efflux of certain tissues. [56] However, in another study conducted on 12 healthy volunteers, neither rifampicin administration nor pgp single nucleotide polymorphism were associated with significant differences in daptomycin disposition. [57] Distribution within cells.…”

Section: Distributionmentioning

confidence: 95%

“…[82,101] It may be hypothesized that gender could be a better descriptor of the influence of body size on the clearance of daptomycin, but this requires further investigation. [56].…”

Section: Gendermentioning

confidence: 99%

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Clinical Pharmacokinetics of Daptomycin

Grégoire¹,

Chauzy²,

Buyck³

et al. 2020

Clin Pharmacokinet

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Due to the low level of resistance observed with daptomycin, this antibiotic has an important place in the treatment of severe Gram-positive infections. It is the first in class of the group of calcium-dependent, membrane binding lipopeptide. It is a cyclic peptide constituted of 13 amino acids and a n-decanoyl fatty acid chain. The antibacterial action of daptomycin requires its complexation with calcium.Daptomycin is not absorbed from the gastrointestinal tract and needs to be administered parenterally. The distribution of daptomycin is limited (volume of distribution of 0.1 L/kg in healthy volunteers) due to its negative charge at physiological pH and its high binding to plasma proteins (about 90%). Its elimination is mainly renal, with about 50% of the dose excreted unchanged in the urine, justifying dosage adjustment for patients with renal insufficiency. Pharmacokinetics of daptomycin is altered under certain pathophysiological conditions, resulting in high inter-individual variability. As a result, therapeutic drug monitoring (TDM) of daptomycin may be of interest for certain patients such as intensive care unit (ICU) patients, patients with renal or hepatic insufficiency, dialysis patients, obese patients or children. A target for the ratio of the area under the curve to the minimum inhibitory concentration (AUC/MIC) greater than 666 is usually recommended for clinical efficacy, whereas in order to limit the risk of undesirable muscular effects the residual concentration (Cmin) should not exceed 24.3 mg/L.

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Section: Gendermentioning

confidence: 72%

Section: Distributionmentioning

confidence: 95%

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Clinical Pharmacokinetics of Daptomycin

Grégoire¹,

Chauzy²,

Buyck³

et al. 2020

Clin Pharmacokinet

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“…Based on in‐vitro studies, rivoceranib is a substrate for P‐gp but not a not a substrate for BCRP, OATP1B1, OATP1B3, and OCT1 (data not shown). Previous studies have shown that P‐gp polymorphism can influence drug disposition [16–18]. Further studies are needed to investigate the cause of high variability.…”

Section: Discussionmentioning

confidence: 99%

Absence of ethnic difference on single‐dose pharmacokinetics of rivoceranib between healthy male Caucasian, Japanese, and Chinese subjects

Sachar¹,

Park²,

Pesco-Koplowitz

et al. 2020

Fundamemntal Clinical Pharma

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Rivoceranib (known in China as apatinib) is a selective vascular endothelial growth factor receptor‐2 (VEGFR‐2) tyrosine kinase inhibitor which inhibits angiogenesis in solid tumors. The aim of study was to evaluate potential pharmacokinetic (PK) differences between the Caucasian, Japanese, and Chinese populations. An open‐label, single‐dose, parallel‐design PK study of rivoceranib was conducted in Caucasian, Japanese, and Chinese subjects. A total of 18 healthy males were recruited to each group (54 total), and 201 mg rivoceranib tablets (as 250 mg rivoceranib mesylate) were administered orally to subjects. Plasma samples were collected, and rivoceranib plasma concentration was determined using LC‐MS/MS. For PK analysis, non‐compartmental and compartmental analyses were performed. Intrinsic factors (CYP2C19 and CYP3A4 genotype) were also examined. Non‐compartmental analysis showed no significant difference in AUC0–t, AUC0–∞, Cmax, tmax, and t1⁄2. Apparent clearance and volume of distribution were different across the three populations; however, the extent of this difference does not require dose modification. For compartmental modeling, a two‐compartment model was used to fit the plasma concentrations. No significant difference was observed in absorption, elimination, and intercompartmental transfer rate constants among the three groups. The present study shows no major ethnic PK differences between Caucasian, Japanese, and Chinese populations.

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“…For E. faecium , the PD target was a free drug 24‐hour AUC/MIC value of 12.9 . As the rate of protein binding in humans (91%) was similar to that reported in mice (90%), we can assume that the exposure targets identified in the mouse model are valid in humans . After correction for 91% protein binding, this led to the following total drug 24‐hour AUC/MIC ≥ 143 for E. faecium .…”

Section: Methodsmentioning

confidence: 66%

Pharmacokinetic/Pharmacodynamic Analysis of Daptomycin Against Staphylococcus aureus and Enterococcus faecium in Pediatric Patients by Monte Carlo Simulation

Wei

Zhao

et al. 2020

The Journal of Clinical Pharma

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The objective of this study was to evaluate the efficacy of various daptomycin dosing regimens against Staphylococcus aureus and Enterococcus faecium in pediatric patients with proven/suspected gram-positive infection. Monte Carlo simulations (MCSs) were conducted using pharmacokinetic (PK) parameters and pharmacodynamic (PD) data to determine the probabilities of target attainment and cumulative fractions of response in terms of area under the concentration curve/minimum inhibition concentration (MIC) targets of daptomycin. According to the results of the MCSs, currently approved pediatric dosage regimens were sufficient against Staphylococcus aureus with MIC ࣘ 0.5 μg/mL for all pediatric patients, but poor when MIC ࣙ 1 μg/mL except for adolescents (12-17 years) who need a dosage of ࣙ10 mg/kg/day at MIC = 1 μg/mL. For Enterococcus faecium with MIC ࣘ 4 μg/mL, the recommended dosage of 8-12 mg/kg/day in adults was enough for adolescents, but not subjected to younger pediatric patients. Furthermore, based on MIC distributions obtained from the European Committee on Antimicrobial Susceptibility Testing, the approved high-dose regimen should be recommended for infants aged 3-12 months, children (2-11 years), and adolescents to achieve better clinical efficacy against methicillin-resistant Staphylococcus aureus. In addition, the dosage of 8-12 mg/kg/day was powerful against Enterococcus faecium for adolescents; however, only the highest dosage of 12 mg/kg/day was effective for infants aged 3-12 months and children. All the simulated regimens were not optimal for infants aged 13-24 months. These PK/PD-based simulations rationalize and optimize the dosage regimens of daptomycin against Staphylococcus aureus and Enterococcus faecium in pediatric patients.

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Genetic polymorphisms of ABCB1 (P-glycoprotein) as a covariate influencing daptomycin pharmacokinetics: a population analysis in patients with bone and joint infection

Cited by 11 publications

References 34 publications

Clinical Pharmacokinetics of Daptomycin

Clinical Pharmacokinetics of Daptomycin

Absence of ethnic difference on single‐dose pharmacokinetics of rivoceranib between healthy male Caucasian, Japanese, and Chinese subjects

Pharmacokinetic/Pharmacodynamic Analysis of Daptomycin Against Staphylococcus aureus and Enterococcus faecium in Pediatric Patients by Monte Carlo Simulation

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