RNA-Induced Silencing Complex-Bound Small Interfering RNA Is a
... amount of siRNA in the tissue had no direct effect on tumor growth inhibition; however, it is unclear from these experiments whether siRNA dose and frequency resulted in increased siRNA delivery to the tumor and enhanced target inhibition. Clearly, a comprehensive understanding of the PK and PD of t ...
... amount of siRNA in the tissue had no direct effect on tumor growth inhibition; however, it is unclear from these experiments whether siRNA dose and frequency resulted in increased siRNA delivery to the tumor and enhanced target inhibition. Clearly, a comprehensive understanding of the PK and PD of t ...
The Cytochrome P450 2B6 (CYP2B6) Is the Main Catalyst of
... treatment failure (Marzolini et al., 2001; Langmann et al., 2002), and those with plasma concentrations over 4 mg/l are at increased risk of CNS side effects (Marzolini et al., 2001). Therefore, it appears important to maintain maximum virally suppressive efavirenz concentrations that will prevent t ...
... treatment failure (Marzolini et al., 2001; Langmann et al., 2002), and those with plasma concentrations over 4 mg/l are at increased risk of CNS side effects (Marzolini et al., 2001). Therefore, it appears important to maintain maximum virally suppressive efavirenz concentrations that will prevent t ...
Contributions of CYP3A4, P-glycoprotein, and Serum Protein
... Besides undergoing extensive first-pass metabolism, saquinavir, like several other HIV protease inhibitors, is actively secreted by P-gp (Kim et al., 1998a,b), an ATP-dependent efflux pump located, among other cell types, in the lumenal (apical) membrane of epithelial cells lining the small intestin ...
... Besides undergoing extensive first-pass metabolism, saquinavir, like several other HIV protease inhibitors, is actively secreted by P-gp (Kim et al., 1998a,b), an ATP-dependent efflux pump located, among other cell types, in the lumenal (apical) membrane of epithelial cells lining the small intestin ...
Hepatotoxicity in rats induced by aqueous extract of
... serum ALT or AST levels significantly [31]; the effect of CYP450 level was not taken into account in the previous animal experiments. If the level of CYP450 has an effect on PMR related rat liver injury, a high dose may show a more pronounced effect, and the high dose was adopted in this study. Thir ...
... serum ALT or AST levels significantly [31]; the effect of CYP450 level was not taken into account in the previous animal experiments. If the level of CYP450 has an effect on PMR related rat liver injury, a high dose may show a more pronounced effect, and the high dose was adopted in this study. Thir ...
HIGHLIGHTS OF PRESCRIBING INFORMATION These
... have been reported with the use of nucleoside analogs, including VIREAD, a component of TRUVADA, in combination with other antiretrovirals [see Warnings and Precautions (5.1)]. TRUVADA is not approved for the treatment of chronic hepatitis B virus (HBV) infection and the safety and efficacy of TRUVA ...
... have been reported with the use of nucleoside analogs, including VIREAD, a component of TRUVADA, in combination with other antiretrovirals [see Warnings and Precautions (5.1)]. TRUVADA is not approved for the treatment of chronic hepatitis B virus (HBV) infection and the safety and efficacy of TRUVA ...
Truvada - Gilead Sciences, Inc.
... infection, and the safety and efficacy of TRUVADA have not been established in patients coinfected with HBV and HIV-1. Severe acute exacerbations of hepatitis B have been reported in patients who are coinfected with HBV and HIV-1 and have discontinued TRUVADA. Therefore, hepatic function should be m ...
... infection, and the safety and efficacy of TRUVADA have not been established in patients coinfected with HBV and HIV-1. Severe acute exacerbations of hepatitis B have been reported in patients who are coinfected with HBV and HIV-1 and have discontinued TRUVADA. Therefore, hepatic function should be m ...
Inhibitio¡ of GLutathione S-Õransferases Studies
... residue and the enzyme_bound glutathione herps to rov¡er the pK. of grutathione in the binary enzyme substrate conrplex 1fliu et al. L992). Recently, significant progress in the knowledge of GST has been made, since suitable crystals io. X_ray diffracÈion studies have become avairable (Reinemer et a ...
... residue and the enzyme_bound glutathione herps to rov¡er the pK. of grutathione in the binary enzyme substrate conrplex 1fliu et al. L992). Recently, significant progress in the knowledge of GST has been made, since suitable crystals io. X_ray diffracÈion studies have become avairable (Reinemer et a ...
67Dihydroxybergamottin Contributes to the Grapefruit
... grapefruit juice– drug interactions. The 2 most abundant furanocoumarins present in the juice are bergamottin and 6',7'-dihydroxybergamottin (DHB). Bergamottin is the “parent” furanocoumarin and has been shown to be both a reversible and a mechanism-based inhibitor of CYP3A4.5,6 DHB, as its name imp ...
... grapefruit juice– drug interactions. The 2 most abundant furanocoumarins present in the juice are bergamottin and 6',7'-dihydroxybergamottin (DHB). Bergamottin is the “parent” furanocoumarin and has been shown to be both a reversible and a mechanism-based inhibitor of CYP3A4.5,6 DHB, as its name imp ...
Australian public assessment report for Dolutegravir (as sodium)
... antiretroviral therapy (ART), INIs block the action of the integrase (IN) viral enzyme required for HIV replication. Two INIs, raltegravir (RAL) and elvitegravir (EVG), have proved effective and have been approved for use in combination with other ART. However, new therapies continue to be required ...
... antiretroviral therapy (ART), INIs block the action of the integrase (IN) viral enzyme required for HIV replication. Two INIs, raltegravir (RAL) and elvitegravir (EVG), have proved effective and have been approved for use in combination with other ART. However, new therapies continue to be required ...
EFFECTS OF POMEGRANATE JUICE ON HUMAN CYTOCHROME
... pomegranate juice. Therefore, to confirm this hypothesis, the effects of pomegranate juice on the absorption of carbamazepine were tested. The absorption of carbamazepine from various parts of the rat intestine was examined in the presence or absence of pomegranate juice by the in situ closed loop t ...
... pomegranate juice. Therefore, to confirm this hypothesis, the effects of pomegranate juice on the absorption of carbamazepine were tested. The absorption of carbamazepine from various parts of the rat intestine was examined in the presence or absence of pomegranate juice by the in situ closed loop t ...
Thalidomide: The Tragedy of Birth Defects and the Effective
... because of the hold on its approval by Dr Frances Kelsey of the U.S. Food and Drug Administration, who was recognized by President John F. Kennedy as a recipient of the Gold Medal Award for Distinguished Civilian Service. Dr Kelsey’s decision to hold the approval of thalidomide was not because of th ...
... because of the hold on its approval by Dr Frances Kelsey of the U.S. Food and Drug Administration, who was recognized by President John F. Kennedy as a recipient of the Gold Medal Award for Distinguished Civilian Service. Dr Kelsey’s decision to hold the approval of thalidomide was not because of th ...
EPAR - Assessment Report - Variation - EMA
... 2. Scientific discussion 2.1. Introduction Product profile Eviplera contains the active substances emtricitabine (FTC) 200 mg, rilpivirine (RPV) 25 mg, and tenofovir disoproxil (as fumarate) (TDF) 245 mg. In the European Union, Eviplera is indicated for the treatment of human immunodeficiency virus ...
... 2. Scientific discussion 2.1. Introduction Product profile Eviplera contains the active substances emtricitabine (FTC) 200 mg, rilpivirine (RPV) 25 mg, and tenofovir disoproxil (as fumarate) (TDF) 245 mg. In the European Union, Eviplera is indicated for the treatment of human immunodeficiency virus ...
Amphotericin B as a mycolic acid specific targeting agent in tuberculosis
... Fig. 2.5 H-numbering of AmB derivative II ................................................................37 Fig. 2.6 Schematic representation of the formation of INH-TPA................................39 Fig. 2.7 Structure of the INH-TPA (left) and the INH-TPA-INH (right). ...................39 Fig ...
... Fig. 2.5 H-numbering of AmB derivative II ................................................................37 Fig. 2.6 Schematic representation of the formation of INH-TPA................................39 Fig. 2.7 Structure of the INH-TPA (left) and the INH-TPA-INH (right). ...................39 Fig ...
BAX 855, a PEGylated rFVIII product with prolonged half-life
... A longer acting recombinant FVIII is expected to serve patients’ demand for a more convenient prophylactic therapy. We have developed BAX 855, a PEGylated form of Baxter’s rFVIII product ADVATETM based on the ADVATETM manufacturing process. The conjugation process for preparing BAX 855 uses a novel ...
... A longer acting recombinant FVIII is expected to serve patients’ demand for a more convenient prophylactic therapy. We have developed BAX 855, a PEGylated form of Baxter’s rFVIII product ADVATETM based on the ADVATETM manufacturing process. The conjugation process for preparing BAX 855 uses a novel ...
The Proton Pump Inhibitor, Omeprazole, but Not Lansoprazole or
... ylline, and tacrine (Angiolillo et al., 2011; Wallace and Sharkey, 2011; MTDI database, http://www.druginteractioninfo.org). The inhibitory DDIs listed above have been attributed, at least in part, to inhibition of CYP2C19 by omeprazole. However, clinically relevant DDIs with omeprazole are generall ...
... ylline, and tacrine (Angiolillo et al., 2011; Wallace and Sharkey, 2011; MTDI database, http://www.druginteractioninfo.org). The inhibitory DDIs listed above have been attributed, at least in part, to inhibition of CYP2C19 by omeprazole. However, clinically relevant DDIs with omeprazole are generall ...
Tetracyclines in malaria | Malaria Journal | Full Text
... anti-malarial drugs has gradually limited the number of potential malaria therapeutics available to clinicians. In this context, doxycycline, a synthetically derived tetracycline, constitutes an interesting alternative for malaria treatment and prophylaxis. Doxycycline is a slow-acting blood schizon ...
... anti-malarial drugs has gradually limited the number of potential malaria therapeutics available to clinicians. In this context, doxycycline, a synthetically derived tetracycline, constitutes an interesting alternative for malaria treatment and prophylaxis. Doxycycline is a slow-acting blood schizon ...
Duloxetine Inhibits Effects of MDMA (``Ecstasy``) In Vitro and in
... humans. Duloxetine was used because it is the most potent and selective dual SERT and NET inhibitor, although it also inhibits the DAT with 10- to 100-fold lower potency compared with the SERT and NET [13,14]. MDMA is mainly metabolized to 3,4dihydroxymethamphetamine (HHMA) by cytochrome P450 (CYP) ...
... humans. Duloxetine was used because it is the most potent and selective dual SERT and NET inhibitor, although it also inhibits the DAT with 10- to 100-fold lower potency compared with the SERT and NET [13,14]. MDMA is mainly metabolized to 3,4dihydroxymethamphetamine (HHMA) by cytochrome P450 (CYP) ...
PDF - Pharmacological Reviews
... C. Extension of mass-action law to multiple drug-effect systems . . . . . . . . . . . . . . . . . . . . . . . . . . . . 1. The multiple drug-effect equation . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 2. The combination index theorem and plot . ...
... C. Extension of mass-action law to multiple drug-effect systems . . . . . . . . . . . . . . . . . . . . . . . . . . . . 1. The multiple drug-effect equation . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 2. The combination index theorem and plot . ...
Lopinavir/Ritonavir
... attenuated by a high first-pass hepatic metabolism. The low-dose ritonavir coadministered with lopinavir inhibits metabolic inactivation of lopinavir and acts only as its pharmacokinetic enhancer. Therefore, the antiretroviral activity of coformulated lopinavir/ritonavir 400/100mg twice daily is der ...
... attenuated by a high first-pass hepatic metabolism. The low-dose ritonavir coadministered with lopinavir inhibits metabolic inactivation of lopinavir and acts only as its pharmacokinetic enhancer. Therefore, the antiretroviral activity of coformulated lopinavir/ritonavir 400/100mg twice daily is der ...
Synthesis and in vitro activities of a new antiviral duplex drug linking
... The first synthesized antiviral molecules linking AZT and PFA were conjugates, in which the carboxyl or phosphonyl group of PFA ester derivatives was directly covalently linked to the 50 -hydroxyl group of AZT or other inhibitory dideoxynucleoside analogues.16–19 The evaluated antiviral activity of t ...
... The first synthesized antiviral molecules linking AZT and PFA were conjugates, in which the carboxyl or phosphonyl group of PFA ester derivatives was directly covalently linked to the 50 -hydroxyl group of AZT or other inhibitory dideoxynucleoside analogues.16–19 The evaluated antiviral activity of t ...
Download CV
... Popik P, Kozela E, Wrobel M, Wozniak KM, Slusher BS. "Morphine tolerance and reward but not expression of morphine dependence are inhibited by the selective glutamate carboxypeptidase II (GCP II, NAALADase) inhibitor, 2-PMPA." Neuropsychopharmacology, 2003, 28(3):457-67 Stoermer D, Liu Q, Hall MR, F ...
... Popik P, Kozela E, Wrobel M, Wozniak KM, Slusher BS. "Morphine tolerance and reward but not expression of morphine dependence are inhibited by the selective glutamate carboxypeptidase II (GCP II, NAALADase) inhibitor, 2-PMPA." Neuropsychopharmacology, 2003, 28(3):457-67 Stoermer D, Liu Q, Hall MR, F ...
ACNE
... SMT D002 is a new promising and potentially safe medication (Oxybutynin chloride), it has successfully completed two Phase I trials in healthy volunteers and believed to treat seborrhoea, a symptom of Parkinson's disease and the primary cause of acne. Topical formulation of the drug is currently bei ...
... SMT D002 is a new promising and potentially safe medication (Oxybutynin chloride), it has successfully completed two Phase I trials in healthy volunteers and believed to treat seborrhoea, a symptom of Parkinson's disease and the primary cause of acne. Topical formulation of the drug is currently bei ...
A Multifaceted GABAA Receptor Modulator
... general anesthetic etomidate. The negligible activities displayed by methaqualone at numerous neurotransmitter receptors and transporters in an elaborate screening for additional putative central nervous system (CNS) targets suggest that it is a selective GABAAR modulator. The mode of action of meth ...
... general anesthetic etomidate. The negligible activities displayed by methaqualone at numerous neurotransmitter receptors and transporters in an elaborate screening for additional putative central nervous system (CNS) targets suggest that it is a selective GABAAR modulator. The mode of action of meth ...
Guidelines for the Use of Antiretroviral Agents in
... formulations for treatment-naive individuals. On the basis of data from long-term follow-up studies and experience in clinical practice, the Panel recognizes that options for initial therapy have expanded. Consequently, the Panel now refers to options for initial treatment as “Recommended” rather t ...
... formulations for treatment-naive individuals. On the basis of data from long-term follow-up studies and experience in clinical practice, the Panel recognizes that options for initial therapy have expanded. Consequently, the Panel now refers to options for initial treatment as “Recommended” rather t ...
IDENTIFICATION OF NATURAL PRODUCTS AS ANTIDIABETIC AGENTS Laura Guasch Pàmies
... Diabetes mellitus (DM) is a metabolic syndrome that constitutes a major health problem [1,2]. It is estimated that 246 million people worldwide have diabetes and that 380 million people will be afflicted with diabetes by 2025. In addition, 3.8 million people die each year from diabetes [3]. DM is ch ...
... Diabetes mellitus (DM) is a metabolic syndrome that constitutes a major health problem [1,2]. It is estimated that 246 million people worldwide have diabetes and that 380 million people will be afflicted with diabetes by 2025. In addition, 3.8 million people die each year from diabetes [3]. DM is ch ...