Comment on: Pharmacokinetics, Pharmacodynamics, and Safety of the Novel Calcimimetic Agent Evocalcet in Healthy Japanese Subjects: First-in-Human Phase I Study
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Cinacalcet hydrochloride (Sensipar®) has been approved for the treatment of secondary hyperparathyroidism (SHPT) in chronic kidney disease (CKD) patients [1, 2]. Due to the efficient targeting of calcium sensory receptors present in parathyroid glands, the pharmacodynamic activity elicited by cinacalcet directly leads to the lowering of serum parathyroid hormone (PTH) and reduced serum levels of both calcium and phosphorous . Despite beneficial effects of cinacalcet therapy in CKD patients pertaining to delayed onset of cardiovascular events, gastrointestinal tolerability issues such as nausea and vomiting have been reported [1, 2, 3]. Another drawback of cinacalcet therapy is with regards to cinacalcet being a perpetrator drug for cytochrome P450 (CYP) 2D6 and a victim drug especially for CYP3A4 [4, 5, 6]. In other words, the CYP profile of cinacalcet suggests that it may precipitate the occurrence of potential drug–drug interactions of substrates and inhibitors of CYP2D6 (i.e....
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No funding was received to prepare this letter.
Conflict of Interest
The author has no conflict of interest to declare in the contents of the manuscript, which was solely prepared to exchange clinical pharmacology-related thoughts on a topic of considerable interest.
- 1.Sensipar® (cinacalcet) tablets. Highlights of prescribing information. Amgen, initial approval 2004. https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/021688s017lbl.pdf. Accessed 8 Oct 2018.
- 10.Narushima K, Maeda H, Shiramoto M, Endo Y, Ohtsuka S, Nakamura H, et al. Assessment of CYP-mediated drug interactions for evocalcet, a new calcimimetic agent, based on in vitro investigations and a cocktail study in humans. Clin Transl Sci. 2018. https://doi.org/10.1111/cts.12588.CrossRefPubMedGoogle Scholar