PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 35168517-2 2022 PQ is metabolized by CYP3A4, mainly regulated by pregnane X receptor (PXR). piperaquine 0-2 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-27 34602032-7 2021 RESULTS: Serum biochemical levels (ALT and BUN) increased significantly (P < 0.05) in mice after three-day oral doses of PQ (> 200 mg/kg/day), indicating hepatotoxicity and nephrotoxicity of PQ at a high dose. piperaquine 121-123 glutamic pyruvic transaminase, soluble Mus musculus 35-38 34602032-7 2021 RESULTS: Serum biochemical levels (ALT and BUN) increased significantly (P < 0.05) in mice after three-day oral doses of PQ (> 200 mg/kg/day), indicating hepatotoxicity and nephrotoxicity of PQ at a high dose. piperaquine 191-193 glutamic pyruvic transaminase, soluble Mus musculus 35-38 34602032-12 2021 The mRNA levels of targets in NF-kappaB and p53 pathways could be up-regulated by 2-30-fold in mice by PQ or M1. piperaquine 103-105 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 30-39 34602032-12 2021 The mRNA levels of targets in NF-kappaB and p53 pathways could be up-regulated by 2-30-fold in mice by PQ or M1. piperaquine 103-105 transformation related protein 53, pseudogene Mus musculus 44-47 34602032-14 2021 The hepatotoxicity of PQ and its N-oxidation metabolite was partly mediated by NF-kappaB inflammatory pathway and p53 apoptosis pathway. piperaquine 22-24 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 79-88 34602032-14 2021 The hepatotoxicity of PQ and its N-oxidation metabolite was partly mediated by NF-kappaB inflammatory pathway and p53 apoptosis pathway. piperaquine 22-24 transformation related protein 53, pseudogene Mus musculus 114-117 35168517-2 2022 PQ is metabolized by CYP3A4, mainly regulated by pregnane X receptor (PXR). piperaquine 0-2 nuclear receptor subfamily 1 group I member 2 Homo sapiens 49-68 35168517-2 2022 PQ is metabolized by CYP3A4, mainly regulated by pregnane X receptor (PXR). piperaquine 0-2 nuclear receptor subfamily 1 group I member 2 Homo sapiens 70-73 35168517-4 2022 OBJECTIVES: The effect of PXR (8055C>T) polymorphism on the pharmacokinetic profiles of PQ was investigated. piperaquine 88-90 nuclear receptor subfamily 1 group I member 2 Homo sapiens 26-29 35168517-12 2022 CONCLUSIONS: Both CYP3A4 and CYP3A5 were involved in PQ clearance. piperaquine 53-55 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 18-24 35168517-12 2022 CONCLUSIONS: Both CYP3A4 and CYP3A5 were involved in PQ clearance. piperaquine 53-55 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 29-35 35168517-14 2022 There might be a low risk of variable exposures to PQ in malaria patients carrying mutated PXR (8055C>T) genes, which deserves further study especially in a larger sample size. piperaquine 51-53 nuclear receptor subfamily 1 group I member 2 Homo sapiens 91-94 33674271-0 2021 Metabolic Retroversion of Piperaquine (PQ) via Hepatic CYP-mediated N-oxidation and Reduction: not an Important Contributor to the Prolonged Elimination of PQ. piperaquine 26-37 peptidylprolyl isomerase G Homo sapiens 55-58 33674271-0 2021 Metabolic Retroversion of Piperaquine (PQ) via Hepatic CYP-mediated N-oxidation and Reduction: not an Important Contributor to the Prolonged Elimination of PQ. piperaquine 39-41 peptidylprolyl isomerase G Homo sapiens 55-58 33674271-1 2021 As a partner antimalarial with an extremely long elimination half-life (~30 days), piperaquine (PQ) is mainly metabolized into a pharmacologically active N-oxide metabolite (PN1) in humans. piperaquine 83-94 serpin family E member 2 Homo sapiens 174-177 33674271-1 2021 As a partner antimalarial with an extremely long elimination half-life (~30 days), piperaquine (PQ) is mainly metabolized into a pharmacologically active N-oxide metabolite (PN1) in humans. piperaquine 96-98 serpin family E member 2 Homo sapiens 174-177 33674271-3 2021 The results showed that interconversion existed for PQ and its metabolite PN1. piperaquine 52-54 serpin family E member 2 Homo sapiens 74-77 33674271-4 2021 The N-oxidation of PQ to PN1 was mainly mediated by CYP3A4, and PN1 can rapidly reduce back to PQ via CYP/FMO enzymes. piperaquine 19-21 serpin family E member 2 Homo sapiens 25-28 33674271-4 2021 The N-oxidation of PQ to PN1 was mainly mediated by CYP3A4, and PN1 can rapidly reduce back to PQ via CYP/FMO enzymes. piperaquine 19-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-58 33674271-4 2021 The N-oxidation of PQ to PN1 was mainly mediated by CYP3A4, and PN1 can rapidly reduce back to PQ via CYP/FMO enzymes. piperaquine 19-21 serpin family E member 2 Homo sapiens 64-67 33674271-4 2021 The N-oxidation of PQ to PN1 was mainly mediated by CYP3A4, and PN1 can rapidly reduce back to PQ via CYP/FMO enzymes. piperaquine 19-21 peptidylprolyl isomerase G Homo sapiens 52-55 33674271-4 2021 The N-oxidation of PQ to PN1 was mainly mediated by CYP3A4, and PN1 can rapidly reduce back to PQ via CYP/FMO enzymes. piperaquine 95-97 serpin family E member 2 Homo sapiens 25-28 33674271-4 2021 The N-oxidation of PQ to PN1 was mainly mediated by CYP3A4, and PN1 can rapidly reduce back to PQ via CYP/FMO enzymes. piperaquine 95-97 serpin family E member 2 Homo sapiens 64-67 33674271-7 2021 After an oral dose of PQ (or PN1) to mice, the parent form predominated in the blood circulation, and PN1 (or PQ) was detected as a major metabolite. piperaquine 22-24 5'-nucleotidase, cytosolic III Mus musculus 29-32 33674271-7 2021 After an oral dose of PQ (or PN1) to mice, the parent form predominated in the blood circulation, and PN1 (or PQ) was detected as a major metabolite. piperaquine 22-24 5'-nucleotidase, cytosolic III Mus musculus 102-105 29304859-2 2018 Based on in vitro data, a two-way pharmacokinetic interaction was hypothesized for KAF156 use in combination with piperaquine (PPQ) as both drugs are CYP3A4 substrates and inhibitors. piperaquine 114-125 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 150-156 29304859-2 2018 Based on in vitro data, a two-way pharmacokinetic interaction was hypothesized for KAF156 use in combination with piperaquine (PPQ) as both drugs are CYP3A4 substrates and inhibitors. piperaquine 127-130 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 150-156 25845867-3 2015 A two-way pharmacokinetic interaction was hypothesized for KAE609 and PPQ, as both drugs are CYP3A4 substrates and inhibitors. piperaquine 70-73 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 93-99 17967917-11 2008 Although PQ has a longer t 1/2 beta than CQ, its prompt distribution and lack of active metabolite may limit its posttreatment malaria-suppressive properties. piperaquine 9-11 interleukin 1 receptor like 1 Homo sapiens 25-35 33344893-7 2020 Analysis revealed drug-drug interactions unique to specific genetic backgrounds, including antagonism between piperaquine and pyronaridine associated with gene amplification of plasmepsin II/III, two aspartic proteases that localize to the parasite digestive vacuole. piperaquine 110-121 plasmepsin ii/iii None 177-194 32928233-4 2020 Multiple copies of the plasmepsin II/III (pm2/3) genes, located on chromosome 14, have been shown to be associated with PPQ resistance. piperaquine 120-123 KDEL endoplasmic reticulum protein retention receptor 1 Homo sapiens 42-47 30169629-3 2019 Piperaquine was separated from the internal standard mefloquine on a reversed-phase C18 column, with the mobile phase consisting of a mixture of acetonitrile and 0.1% trichloroacetic acid (in water) (15:85, v:v) running at a flow rate of 1.0 mL/min. piperaquine 0-11 Bardet-Biedl syndrome 9 Homo sapiens 84-87 29352982-0 2018 Inhibition of CYP3A by Antimalarial Piperaquine and Its Metabolites in Human Liver Microsomes With IVIV Extrapolation. piperaquine 36-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-19 29352982-1 2018 The potential of the antimalarial piperaquine and its metabolites to inhibit CYP3A was investigated in pooled human liver microsomes. piperaquine 34-45 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 77-82 29352982-3 2018 Piperaquine was found to be a reversible, potent inhibitor of CYP3A with the following parameter estimates (%CV): IC50 = 0.76 muM (29), Ki = 0.68 muM (29). piperaquine 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-67 26695060-0 2015 Plasmodium falciparum dihydroartemisinin-piperaquine failures in Cambodia are associated with mutant K13 parasites presenting high survival rates in novel piperaquine in vitro assays: retrospective and prospective investigations. piperaquine 41-52 keratin 13 Homo sapiens 101-104 26695060-11 2015 Combined ex vivo PSA and K13 genotyping provides a convenient monitor for both artemisinin and piperaquine resistance where dihydroartemisinin-piperaquine is used. piperaquine 95-106 keratin 13 Homo sapiens 25-28 25311421-13 2014 Two of the new piperaquine phosphate related substances, imp-2 and imp-6, were identified and characterized as 4-hydroxy-7-chloro-quinoline and a piperaquine oxygenate with a piperazine ring of nitrogen oxide in bulk drug and oxidation sample, respectively. piperaquine 15-26 inositol monophosphatase 2 Homo sapiens 57-62 22671777-0 2012 In vitro metabolism of piperaquine is primarily mediated by CYP3A4. piperaquine 23-34 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-66 22671777-4 2012 Concentrations of PQ were measured after incubation with both human liver microsomes (HLMs) and expressed cytochrome P450 enzymes (P450s). piperaquine 18-20 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 117-121 22671777-8 2012 Using a mixture of recombinant P450 enzymes, turnover for PQ metabolism was estimated as 0.0099 min(-1); recombinant CYP3A4 had a higher metabolic rate (0.017 min(-1)) than recombinant CYP2C8 (p < .0001). piperaquine 58-60 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 31-35 22671777-8 2012 Using a mixture of recombinant P450 enzymes, turnover for PQ metabolism was estimated as 0.0099 min(-1); recombinant CYP3A4 had a higher metabolic rate (0.017 min(-1)) than recombinant CYP2C8 (p < .0001). piperaquine 58-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 117-123 22671777-8 2012 Using a mixture of recombinant P450 enzymes, turnover for PQ metabolism was estimated as 0.0099 min(-1); recombinant CYP3A4 had a higher metabolic rate (0.017 min(-1)) than recombinant CYP2C8 (p < .0001). piperaquine 58-60 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 185-191 22671777-9 2012 Inhibition of CYP3A4-mediated PQ loss was greatest using the selective inhibitor ketoconazole (9.1 +- 3.5% loss with ketoconazole vs 60.7 +- 5.9% with no inhibitor, p < .0001). piperaquine 30-32 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-20 22671777-10 2012 In summary, the extent of inhibition of in vitro metabolism with ketoconazole (83%) denotes that PQ appears to be primarily catalyzed by CYP3A4. piperaquine 97-99 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 137-143