Stability of Sirolimus and Everolimus Measured by Immunoassay Techniques in Whole Blood Samples from Kidney Transplant Patients

Capone, Domênico; Gentile, Antonio; Polichetti, Giuliano; Federico, Stefano; Sabbatini, Massimo; Acampora, Antonio; Basile, Vincenzo S.; Pieri, Maria; Tarantino, Giovanni

doi:10.1177/039463200802100206

Cited by 13 publications

(5 citation statements)

References 15 publications

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“…Blood samples were frozen at −80°C for 1 month prior to analysis, which might have adversely affected measurement of the rapamycin concentration in those samples. Results of other studies 24,25 indicate that the rapamycin concentration is not substantially affected in blood samples stored frozen at −80°C for 90 days and subsequently thawed. Therefore, we do not believe that blood sample storage prior to analysis significantly affected measurement of blood rapamycin concentration in the present study.…”

Section: Discussionmentioning

confidence: 79%

Pharmacokinetics of orally administered low-dose rapamycin in healthy dogs

Larson

Allstadt

Fan

et al. 2016

ajvr

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Objective To determine the pharmacokinetics of orally administered rapamycin in healthy dogs. Animals 5 healthy purpose-bred hounds. Procedures The study consisted of 2 experiments. In experiment 1, each dog received rapamycin (0.1 mg/kg, PO) once; blood samples were obtained immediately before and at 0.5, 1, 2, 4, 6, 12, 24, 48, and 72 hours after administration. In experiment 2, each dog received (0.1 mg/kg, PO) once daily for 5 days; blood samples were obtained immediately before and at 3, 6, 24, 27, 30, 48, 51, 54, 72, 75, 78, 96, 96.5, 97, 98, 100, 102, 108, 120, 144, and 168 hours after the first dose. Blood rapamycin concentration was determined by a validated liquid chromatography-tandem mass spectrometry assay. Pharmacokinetic parameters were determined by compartmental and non-compartmental analyses. Results Mean ± SD blood rapamycin terminal half-life, area under the concentration-time curve from 0 to 48 hours after dosing, and maximum concentration were 38.7 ± 12.7 h, 140 ± 23.9 ng•h/mL, and 8.39 ± 1.73 ng/mL, respectively, for experiment 1, and 99.5 ± 89.5 h, 126 ± 27.1 ng•h/mL, and 5.49 ± 1.99 ng/mL, respectively, for experiment 2. Pharmacokinetic parameters for rapamycin after administration of 5 daily doses differed significantly from those after administration of 1 dose. Conclusions and Clinical Relevance Results indicated that oral administration of low-dose (0.1 mg/kg) rapamycin to healthy dogs achieved blood concentrations measured in ng/mL. The optimal dose and administration frequency of rapamcyin required to achieve therapeutic effects in tumor-bearing dogs, as well as toxicity after chronic dosing, needs to be determined.

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Section: Discussionmentioning

confidence: 79%

Pharmacokinetics of orally administered low-dose rapamycin in healthy dogs

Larson

Allstadt

Fan

et al. 2016

ajvr

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“…Transport of the sample is performed after immediate freezing post-sampling (<4 h). 13 Because these pre-analytical recommendations were followed for this patient, an analytical error was not suspected.…”

Section: Discussionmentioning

confidence: 99%

Advantages of everolimus therapeutic drug monitoring in oncology when drug–drug interaction is suspected: A case report

Strobbe

Pannier

Sakji

et al. 2020

J Oncol Pharm Pract

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Introduction Drug interactions involving everolimus are fairly well known because of its common use, primarily as an immunosuppressant. Several recommendations regarding therapeutic drug monitoring are also available for the use of everolimus-based immunosuppression regimens. However, everolimus use in oncology differs substantially, particularly because of the high doses involved. Therapeutic drug monitoring, although sometimes necessary, is not recommended as a routine in oncology. Thus, it was deemed inapplicable due to the lack of clear recommendations. Case report Here, we present a case where a patient was prescribed everolimus for renal cell carcinoma. The patient benefitted from a pharmaceutical consultation prior to treatment initiation, and a drug interaction with verapamil was suspected. Management and outcome: Therapeutic drug monitoring of everolimus was proposed. Based on the everolimus values reported in the literature, trough plasma concentration in the patient was greatly increased. The patient was then diagnosed with grade 4 oral mucositis, thereby requiring temporary suspension of everolimus treatment. Management of adverse effects was performed through multiple medicated mouthwashes. Discussion Therapeutic drug monitoring for everolimus is important for potential drug interactions or the occurrence of severe adverse events. In such cases, dose adjustments should be managed according to everolimus plasma concentrations. Clear oncological recommendations regarding plasma everolimus thresholds are required for a successful follow-up of the patient’s condition and to ensure adequate response to treatment.

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“…The Yukon Choice PC – Elite Coronary Stent System is a balloon-expandable sirolimus-eluting coronary stent with a micro porous surface and a fully biodegradable abluminal polymer, mounted on a low-profile rapid-exchange delivery system provided in a temperature-controlled packaging. 10 …”

Section: Methodsmentioning

confidence: 99%