Literature DB >> 26714164

Influence of tumour burden on trastuzumab pharmacokinetics in HER2 positive non-metastatic breast cancer.

Guillemette Bernadou1,2, Mario Campone3, Jean-Louis Merlin4,5,6, Valérie Gouilleux-Gruart1,7, Thomas Bachelot8, François Lokiec9, Keyvan Rezai9, Monica Arnedos10, Véronique Diéras10, Marta Jimenez11, Gilles Paintaud1,12, David Ternant1,12.   

Abstract

AIMS: Trastuzumab, an antibody binding to epidermal growth factor receptor-2 (HER2), has been approved to treat HER2-positive breast cancer in different settings. This study aimed at evaluating the influence of tumour size on trastuzumab pharmacokinetics (PK) in non-metastatic breast cancer patients treated with short term pre-operative trastuzumab.
METHODS: Trastuzumab PK data were obtained from a multicentre, randomized and comparative study. This antibody was administered pre-operatively to patients with localized HER2-positive breast cancer as a single 4 mg kg(-1) loading dose followed by 5 weekly 2 mg kg(-1) doses. Trastuzumab concentrations were measured repeatedly using an ELISA technique. Tumour size was evaluated at baseline using breast echography. Trastuzumab pharmacokinetics were studied using a population approach and a two compartment model. The influence of tumour burden on trastuzumab pharmacokinetics was quantified as a covariate.
RESULTS: A total of 784 trastuzumab concentrations were available from the 79 eligible patients. Estimated parameters (interindiviual standard deviation) were central volume of distribution =2.1 l (23%), peripheral volume of distribution =1.3 l (38%), intercompartment clearance =0.36 l day(-1) , with an elimination half-life of 11.8 days. Typical clearance was 0.22 l day(-1) (19%) and its value was increased with tumour size. In patients with the highest tumour size, trastuzumab clearance was 50% [18%-92%] higher than in patients with the lowest tumour size.
CONCLUSIONS: In non-metastatic breast cancer patients, trastuzumab clearance increases with tumour size. The elimination half-life of trastuzumab was shorter in the present population of patients than in metastatic breast cancer patients previously studied.
© 2015 The British Pharmacological Society.

Entities:  

Keywords:  breast cancer; pharmacokinetics; population PK modelling; trastuzumab

Mesh:

Substances:

Year:  2016        PMID: 26714164      PMCID: PMC4834606          DOI: 10.1111/bcp.12875

Source DB:  PubMed          Journal:  Br J Clin Pharmacol        ISSN: 0306-5251            Impact factor:   4.335


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