Investigation of the effect of food and omeprazole on the relative bioavailability of a single oral dose of 240 mg faldaprevir, a selective inhibitor of HCV NS3/4 protease, in an open-label, randomized, three-way cross-over trial in healthy participants

Wu, Jing; Gießmann, Thomas; Lang, Benjamin; Elgadi, Mabrouk; Huang, Fenglei

doi:10.1111/jphp.12538

Cited by 3 publications

(2 citation statements)

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“…Anti-hepatitis viral infection drugs: Inhibition of hepatitis viral infection can suppress liver inflammation and hepatocyte death to decrease liver injury, resulting in suppression of liver fibrosis. Drugs such as faldaprevir (also known as BI 201335)[ 101 ], ribavirin (HCV treatment)[ 102 ], and peginterferon alfa-2a (HBV treatment)[ 103 , 104 ], have been tested in clinical trials for the treatment of liver fibrosis. In addition, many other drugs have been evaluated or are under clinical trial evaluation against hepatitis viral infection[ 105 - 107 ], such as simeprevir, daclatasvir, and sofosbuvir.…”

Section: Current Treatment Options For Liver Fibrosismentioning

confidence: 99%

Treatment of liver fibrosis: Past, current, and future

Zhang¹,

Liu²,

Yang³

2023

World J Hepatol

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Liver fibrosis accompanies the progression of chronic liver diseases independent of etiologies, such as hepatitis viral infection, alcohol consumption, and metabolic-associated fatty liver disease. It is commonly associated with liver injury, inflammation, and cell death. Liver fibrosis is characterized by abnormal accumulation of extracellular matrix components that are expressed by liver myofibroblasts such as collagens and alpha-smooth actin proteins. Activated hepatic stellate cells contribute to the major population of myofibroblasts. Many treatments for liver fibrosis have been investigated in clinical trials, including dietary supplementation ( e.g. , vitamin C), biological treatment ( e.g. , simtuzumab), drug ( e.g. , pegbelfermin and natural herbs), genetic regulation ( e.g. , non-coding RNAs), and transplantation of stem cells ( e.g. , hematopoietic stem cells). However, none of these treatments has been approved by Food and Drug Administration. The treatment efficacy can be evaluated by histological staining methods, imaging methods, and serum biomarkers, as well as fibrosis scoring systems, such as fibrosis-4 index, aspartate aminotransferase to platelet ratio, and non-alcoholic fatty liver disease fibrosis score. Furthermore, the reverse of liver fibrosis is slowly and frequently impossible for advanced fibrosis or cirrhosis. To avoid the life-threatening stage of liver fibrosis, anti-fibrotic treatments, especially for combined behavior prevention, biological treatment, drugs or herb medicines, and dietary regulation are needed. This review summarizes the past studies and current and future treatments for liver fibrosis.

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Section: Current Treatment Options For Liver Fibrosismentioning

confidence: 99%

Treatment of liver fibrosis: Past, current, and future

Zhang¹,

Liu²,

Yang³

2023

World J Hepatol

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“…In HCV‐infected patients, when FDV dose was increased from 120 to 240 mg, exposure increased approximately five to seven times (Boehringer Ingelheim data on file). Food has no clinically relevant effects on FDV absorption . The mean elimination half‐life of FDV in healthy volunteers and HCV‐infected adult patients was approximately 20–30 hr ; therefore, FDV is given once daily in all treatment regimens for HCV infection.…”

mentioning

confidence: 99%

Pharmacokinetic Interaction between Faldaprevir and Cyclosporine or Tacrolimus in Healthy Volunteers: A Prospective, Open‐Label, Fixed‐Sequence, Crossover Study

Huang

Voelk

Trampisch

et al. 2018

Basic Clin Pharma Tox

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Faldaprevir (FDV) is a potent, orally administered inhibitor of hepatitis C virus. In this single-centre, open-label, fixed-sequence, crossover study of 32 healthy adult male and female volunteers, subjects received either a single dose of cyclosporine (CsA) 50 mg (N = 16) or tacrolimus (TAC) 0.5 mg (N = 16), followed by a washout of at least 14 days. Each subject then received a loading dose of FDV 240 mg followed by 120 mg FDV once daily for 6 days. FDV 120 mg was then co-administered with an additional single dose of CsA (50 mg) or TAC (0.5 mg), followed by an additional 6 days of FDV 120 mg once daily. Intensive blood sampling was performed to assess the PK interaction potential. Assessment of relative BA indicated that exposure to CsA co-administered with FDV was similar to CsA alone. However, the AUC and C of FDV were increased by 23% and 41%, respectively, when FDV was co-administered with CsA. Exposure to TAC was slightly increased (AUC increased by 27%, no change in C ) when TAC was co-administered with FDV. In contrast, exposure to FDV co-administered with TAC was similar to FDV alone. No unexpected safety findings arose from the trial. The limitations of the study (use of single, low dose of TAC and CsA, and only healthy volunteers in the trial) are discussed.

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Drug-Nutrition Interactions in Infectious Diseases

Boullata

2020

Nutrition and Infectious Diseases

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Investigation of the effect of food and omeprazole on the relative bioavailability of a single oral dose of 240 mg faldaprevir, a selective inhibitor of HCV NS3/4 protease, in an open-label, randomized, three-way cross-over trial in healthy participants

Abstract: Administration of a single dose of 240 mg faldaprevir after high-fat breakfast led to a modest, clinically irrelevant increase in faldaprevir exposure, while coadministration of omeprazole did not influence faldaprevir exposure.

Cited by 3 publications

References 22 publications

Treatment of liver fibrosis: Past, current, and future

Treatment of liver fibrosis: Past, current, and future

Pharmacokinetic Interaction between Faldaprevir and Cyclosporine or Tacrolimus in Healthy Volunteers: A Prospective, Open‐Label, Fixed‐Sequence, Crossover Study

Drug-Nutrition Interactions in Infectious Diseases

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