Novel thyroxine formulations: a further step toward precision medicine
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REVIEW
Novel thyroxine formulations: a further step toward precision medicine Camilla Virili
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Pierpaolo Trimboli
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Marco Centanni
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Received: 3 June 2019 / Accepted: 5 August 2019 © Springer Science+Business Media, LLC, part of Springer Nature 2019
Abstract Levothyroxine (T4) is a critical-dose drug, because little variations in the blood concentration may cause treatment failure as well as iatrogenic thyrotoxicosis. Despite the dose response of this drug being more carefully titrated nowadays, several papers still report that a significant fraction of patients treated with levothyroxine demonstrate a TSH which is not on target. Moreover, some widespread gastrointestinal disorders as well as interfering drugs and foods may cause the “refractoriness” of a significant number of patients to an expected dose of thyroxine. The increasing awareness of the mechanisms interfering with the oral thyroid hormone bioavailability and the body of evidence regarding the complexity of treatment in certain classes of patients prompted pharmaceutical research to identify new hormonal formulations to optimize the performance of this drug. In this brief review, the progression of the scientific knowledge of novel T4 formulations use has been analyzed. Keywords Liquid levothyroxine Softgel thyroxine Thyroxine absorption Thyroxine malabsorption Drugs dissolution Gastrointestinal disorders ●
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Introduction Synthesized in 1927 by Harrington [1] and obtained as sodium salt in 1950 [2], levothyroxine (T4) has subsequently obtained the role of gold standard in the treatment of hypothyroid patients [3]. Prescribed worldwide, it ranks within the top ten most used drugs in western countries [4]. Levothyroxine is a critical-dose drug, since slight variations in blood concentration may result in treatment failure as well as iatrogenic thyrotoxicosis [5]. Therefore, both overand undertreatment have been increasingly recognized in clinical practice and in scientific literature [6, 7], suggesting the need for an individualization of oral T4 treatment. Unfortunately, a daily dose of levothyroxine fitting all patients has been sought without success [3] and different
* Marco Centanni [email protected] 1
Department of Medico-Surgical Sciences and Biotechnologies, “Sapienza” University of Rome, Latina, Italy
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Thyroid Center and Nuclear Medicine, Ente Ospedaliero Cantonale, Bellinzona, Switzerland
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Endocrinology Unit, AUSL Latina, Latina, Italy
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levothyroxine doses are used to treat patients of different ages and with specific clinical conditions [8]. The daily requirement of levothyroxine depends on patients’ lean body mass [9], the leading cause of hypothyroidism and the therapeutic goal [e.g. replacement or TSH suppressive treatment]. Over the last few years, the knowledge of pharmacokinetic features of orally administered levothyroxine has led to a better individualization of treatment with a progressive decrease in administered doses [3]. Despite the fact that the dose response o
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