ArticleThe Prostate2012
Co-administration of piperine and docetaxel results in improved anti-tumor efficacy via inhibition of CYP3A4 activity.
Article in The Prostate, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers, 1 of them a synthesis that pooled it.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
33 citing papers in PubMed, 1 synthesis or guideline pooled it, 117 citations in OpenAlex.
- Phytochemicals in Inhibition of Prostate Cancer: Evidence from Molecular Mechanisms Studies.Biomolecules · 2022Pooled it
- Metabolic Insights into Drug Absorption: Unveiling Piperine's Transformative Bioenhancing Potential.Pharmaceutical research · 2025Review
- Vesicular Carriers for Phytochemical Delivery: A Comprehensive Review of Techniques and Applications.Pharmaceutics · 2025Review
- Therapeutic Potential of Plant- and Marine-Derived Bioactive Compounds in Prostate Cancer: Mechanistic Insights and Translational Applications.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Harnessing the anticancer potential of Piper nigrum: a synergistic approach to chemotherapy enhancement and reduced side effects.Discover oncology · 2025Review
- Metabolic Targets in CRC: The Emerging Role of Cytochrome P450 Inhibitors.Current pharmaceutical design · 2025Review
- Application of Physiologically-Based Pharmacokinetic (PBPK) Model in Drug Development and in Dietary Phytochemicals.Current pharmacology reports · 2025Review
- Molecular Evidence of the Bio-activities of Traditional Home Medicine Ingredients.Current topics in medicinal chemistry · 2025Review
- Role of Cytochrome P450 3A4 in Cancer Drug Resistance: Challenges and Opportunities.Current drug metabolism · 2024Review
- Advanced application of nanotechnology in active constituents of Traditional Chinese Medicines.Journal of nanobiotechnology · 2023Review
- Natural medicinal compounds target signal transduction pathways to overcome ABC drug efflux transporter-mediated multidrug resistance in cancer.Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy · 2023Review
- Piperine Induces Apoptosis and Autophagy in HSC-3 Human Oral Cancer Cells by Regulating PI3K Signaling Pathway.International journal of molecular sciences · 2023Article
- Targeting prostate cancer with docetaxel-loaded peptide 563-conjugated PEtOx-co-PEIAmino acids · 2023Article
- Macrophage Cell Membrane Coating on Piperine-Loaded MIL-100(Fe) Nanoparticles for Breast Cancer Treatment.Journal of functional biomaterials · 2023Article
- Combination Anticancer Therapies Using Selected Phytochemicals.Molecules (Basel, Switzerland) · 2022Review
- Botanical fromEvidence-based complementary and alternative medicine : eCAM · 2021Article
- Prostate cancer: Therapeutic prospect with herbal medicine.Current research in pharmacology and drug discovery · 2021Review
- Review
- Piperine Inhibits TGF-β Signaling Pathways and Disrupts EMT-Related Events in Human Lung Adenocarcinoma Cells.Medicines (Basel, Switzerland) · 2020Article
- Enhanced Bioavailability of Boswellic Acid byFrontiers in pharmacology · 2020Article
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
backgroundDocetaxel is the mainline treatment approved by the FDA for castration-resistant prostate cancer (CRPC) yet its administration only increases median survival by 2-4 months. Docetaxel is metabolized in the liver by hepatic CYP3A4 activity. Piperine, a major plant alkaloid/amide, has been shown to inhibit the CYP3A4 enzymatic activity in a cell-free system. Thus, we investigated whether the co-administration of piperine and docetaxel could increase docetaxel's pharmacokinetic activity in vitro and in vivo.
methodsLiver CYP3A4 enzymatic activity was measured by fluorescence. In vivo docetaxel pharmacokinetic activity was analyzed by liquid chromatography. An in vivo xenograft model of human CRPC was utilized to assess the anti-tumor effect of docetaxel when co-administered with piperine.
resultsInhibition of hepatic CYP3A4 activity resulted in an increased area under the curve, half-life and maximum plasma concentration of docetaxel when compared to docetaxel alone administration. The synergistic administration of piperine and docetaxel significantly improved the anti-tumor efficacy of docetaxel in a xenograft model of human CRPC.
conclusionsDocetaxel is one of the most widely used cytotoxic chemotherapeutic agents and is currently the mainstay treatment for metastatic CRPC. Dietary constituents are important agents modifying drug metabolism and transport. In our studies, dietary consumption of piperine increases the therapeutic efficacy of docetaxel in a xenograft model without inducing more adverse effects on the treated mice.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.