Depending on CYP2D6 metabolizer phenotype, co-administration of eliglustat with CYP2D6 and/or CYP3A inhibitors or CYP3A inducers may alter eliglustat exposure, warrant dosage adjustment or use with caution, or be contraindicated.Current affiliation is Cytokinetics, Inc., South San Francisco, CA.Current affiliation is Gerald Cox Rare Care Consulting, LLC, Needham, MA.We use cookies to help provide and enhance our service and tailor content and ads.



Interestingly, since CYP3A induction was observed in both rat and human hepatocytes, particularly with GW3333, it appears that the N-hydroxyformamide compounds are not species-specific CYP3A inducers like PCN or

2017 Oct;83(10):2242-2248. doi: 10.1111/bcp.13329.

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Arithmetic mean plasma concentration–time profile… Arithmetic mean plasma concentration–time profile of suvorexant following administration of suvorexant alone or… GMRs (90% CI) for suvorexant co-administered with the strong CYP3A inhibitor ketoconazole, the…

Therefore, co-administration of quizartinib with CYP3A inducers may decrease quizartinib exposure.

Quizartinib is metabolized primarily by CYP3A.

2014;29(3):191-202. doi: 10.1515/dmdi-2014-0005.Drugs Today (Barc).

2017 Jul;37(7):659-667. doi: 10.1007/s40261-017-0513-4.J Clin Pharmacol.

Three studies evaluated the effects of paroxetine (strong CYP2D6 inhibitor), ketoconazole (strong CYP3A4 and P-gp inhibitor), and rifampin (strong CYP3A4/P-gp inducer; OATP inhibitor) on the pharmacokinetics of orally administered eliglustat in healthy adults.

Eliglustat is metabolized primarily by CYP2D6 and to a lesser extent by CYP3A4 and is a substrate of P-glycoprotein (P-gp). Cytochrome P-450 CYP3A Inhibitors Accession Number DBCAT000934 (DBCAT003363, DBCAT004051) Description Drugs and compounds which inhibit or antagonize the biosynthesis or actions of CYTOCHROME P-450 CYP3A.

Page 1 of 3 Some Common Substrates, Inhibitors and Inducers of CYP450 Isoenzymes CYP3A group (includes 4, 5, and 7) Substrates Inhibitors Inducers Amiodarone Amlodipine Aripiprazole Atorvastatin Buspirone Ciclosporin By continuing you agree to the Copyright © 2020 Elsevier B.V. or its licensors or contributors. CYP3A inducers; increasing the dose of bosutinib is unlikely to sufficiently compensate for the loss of exposure Cabozantinib Ketoconazole Rifampicin Avoid co-administration of cabozantinib with CYP3A4 inhibitors/inducers (e.g. COVID-19 is an emerging, rapidly evolving situation. Depending on CYP2D6 metabolizer phenotype, co-administration of eliglustat with CYP2D6 and/or CYP3A inhibitors or CYP3A inducers may alter eliglustat exposure, warrant …

This study will assess the effect of a moderate CYP3A inducer efavirenz Co-administration of eliglustat with oral doses of rifampin reduced eliglustat exposure by >85% due to induction of CYP3A4/P-gp by rifampin, while a single intravenous dose of rifampin had no effect on eliglustat, confirming that eliglustat is not an OATP substrate. Wrishko RE, McCrea JB, Yee KL, Liu W, Panebianco D, Mangin E, Chakravarthy M, Martinez-Cantarin MP, Kraft WK.Clin Drug Investig. 2019 May;39(5):453-454. doi: 10.1007/s40261-019-00777-6.Mohamed MF, Jungerwirth S, Asatryan A, Jiang P, Othman AA.Br J Clin Pharmacol. Unable to load your delegates due to an error

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2016 Jan;52(1):29-40. doi: 10.1358/dot.2016.52.1.2439940. Springer

Arithmetic mean plasma concentration–time profile of suvorexant following administration of suvorexant alone or co-administered with GMRs (90% CI) for suvorexant co-administered with the strong CYP3A inhibitor ketoconazole, the moderate CYP3A inhibitor diltiazem, or the strong CYP3A inducer rifampin, versus suvorexant alone, for suvorexant AUC
Clipboard, Search History, and several other advanced features are temporarily unavailable. ScienceDirect ® is a registered trademark of Elsevier B.V.Effects of paroxetine, ketoconazole, and rifampin on the metabolism of eliglustat, an oral substrate reduction therapy for Gaucher disease type 1ScienceDirect ® is a registered trademark of Elsevier B.V. Epub 2017 Jun 19.Yee KL, Khalilieh SG, Sanchez RI, Liu R, Anderson MS, Manthos H, Judge T, Brejda J, Butterton JR.Clin Drug Investig.

A 4.3-fold increase in eliglustat exposure following co-administration of multiple-dose eliglustat and ketoconazole is attributed to inhibition of CYP3A4-mediated metabolism and/or P-gp-mediated transport of eliglustat by ketoconazole. Co-administration of multiple-dose eliglustat and paroxetine (CYP2D6 inhibitor) increased eliglustat exposure.Co-administration of multiple-dose eliglustat and ketoconazole (inhibitor of CYP3A and P-gp) increased eliglustat exposure.Co-administration of eliglustat with oral rifampin (inducer of CYP3A and intestinal P-gp) reduced eliglustat exposure.A single intravenous dose of rifampin had no effect on eliglustat exposure.Eliglustat label contains dose adjustments/contraindications for co-administration with CYP2D6/3A inhibitors or inducers.Eliglustat is an oral glucosylceramide synthase inhibitor indicated for the long-term treatment of adults with Gaucher disease type 1 and CYP2D6 extensive, intermediate, or poor metabolizer phenotypes. 2016 Aug;56(8):1019-27. doi: 10.1002/jcph.693. Unable to load your collection due to an error Cytochrome P-450 CYP3A Inducers Cytochrome P-450 CYP3A Inhibitors Orexin Receptor Antagonists Triazoles suvorexant Diltiazem Ketoconazole Rifampin Grant support T32 GM008562/GM/NIGMS NIH HHS/United States CYP3A inhibitors (%) 21 17 0.99 CYP3A inducers (%) 79 24 0.0001 Serum creatinine (mg/dl) at biopsy 3.5 ± 2.5 2.2 ± 1.5 0.0162 Glomerular filtration rate (ml/min) at biopsy 40 ± 21 69 ± 50 0.0527 Proteinuria (mg/d) at biopsy

Epub 2016 Feb 24.Chiu YY, Ereshefsky L, Preskorn SH, Poola N, Loebel A.Drug Metabol Drug Interact.

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