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PMC6989238 | core_pubmed_pmc | Simultaneous quantification of ticagrelor and its active metabolite, AR-C124910XX, in human plasma by liquid chromatography-tandem mass spectrometry: Applications in steady-state pharmacokinetics in patients | Simultaneous quantification of ticagrelor and its active metabolite, AR-C124910XX, in human plasma by liquid chromatography-tandem mass spectrometry: Applications in steady-state pharmacokinetics in patients Abstract A sensitive and simple liquid chromatography-tandem mass spectrometry method was developed and validate... |
PMC4913717 | core_pubmed_pmc | "Influence of methadone on clopidogrel in addicts on methadone maintenance therapy" Drug interaction between methadone and clopidogrel | "Influence of methadone on clopidogrel in addicts on methadone maintenance therapy" Drug interaction between methadone and clopidogrel Abstract Abstract Background: Clopidogrel is a prodrug that converts in the liver to an active thiol metabolite, which irreversibly inhibits the platelet P2Y 12 adenosine diphosphate re... |
PMC6206206 | core_pubmed_pmc | Behavioral and Pharmacokinetic Profile of Indole-Derived Synthetic Cannabinoids JWH-073 and JWH-210 as Compared to the Phytocannabinoid Δ 9 -THC in Rats | Behavioral and Pharmacokinetic Profile of Indole-Derived Synthetic Cannabinoids JWH-073 and JWH-210 as Compared to the Phytocannabinoid Δ 9 -THC in Rats Abstract Synthetic cannabinoid compounds are marketed as “legal” marijuana substitutes, even though little is known about their behavioral effects in relation to their... |
PMC9584256 | core_pubmed_pmc | Influence of UGT1A1 and SLC22A6 polymorphisms on the population pharmacokinetics and pharmacodynamics of raltegravir in HIV-infected adults: a NEAT001/ANRS143 sub-study | Influence of UGT1A1 and SLC22A6 polymorphisms on the population pharmacokinetics and pharmacodynamics of raltegravir in HIV-infected adults: a NEAT001/ANRS143 sub-study Abstract Abstract Using concentration-time data from the NEAT001/ARNS143 study (single sample at week 4 and 24), we determined raltegravir pharmacokine... |
PMC7576615 | core_pubmed_pmc | Exposure–response relationships of dapagliflozin on cardiorenal risk markers and adverse events: A pooled analysis of 13 phase II/III trials | Exposure–response relationships of dapagliflozin on cardiorenal risk markers and adverse events: A pooled analysis of 13 phase II/III trials Abstract Abstract Aims Dapagliflozin is a sodium–glucose co‐transporter 2 inhibitor that has been developed as oral glucose lowering drug. The original dosefinding studies focused... |
PMC5748442 | core_pubmed_pmc | Population pharmacokinetics of treosulfan and development of a limited sampling strategy in children prior to hematopoietic stem cell transplantation | Population pharmacokinetics of treosulfan and development of a limited sampling strategy in children prior to hematopoietic stem cell transplantation Abstract Abstract Purpose There is an increasing interest in use of treosulfan (TREO), a structural analogue of busulfan, as an agent in conditioning regimens prior to he... |
PMC12402799 | core_pubmed_pmc | Efficacy of ATR Kinase Inhibitor Elimusertib Monotherapy or Combination in Tumors with DNA Damage Response Pathway and Other Genomic Alterations | Efficacy of ATR Kinase Inhibitor Elimusertib Monotherapy or Combination in Tumors with DNA Damage Response Pathway and Other Genomic Alterations Abstract Abstract The ataxia telangiectasia and RAD3-related (ATR) kinase functions with ataxia telangiectasia–mutated (ATM) kinase as a modulator of DNA damage response (DDR)... |
PMC7591087 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Interaction Between Evogliptin and Pioglitazone in Healthy Male Subjects | Pharmacokinetic/Pharmacodynamic Interaction Between Evogliptin and Pioglitazone in Healthy Male Subjects Abstract Aim Evogliptin is a newly developed oral glucose-lowering medication of the dipeptidyl peptidase 4 (DPP-4) inhibitor class for type 2 diabetes mellitus. The combination of a DPP-4 inhibitor with pioglitazon... |
PMC6972493 | core_pubmed_pmc | Population Pharmacokinetics of Galcanezumab, an Anti‐CGRP Antibody, Following Subcutaneous Dosing to Healthy Individuals and Patients With Migraine | Population Pharmacokinetics of Galcanezumab, an Anti‐CGRP Antibody, Following Subcutaneous Dosing to Healthy Individuals and Patients With Migraine Abstract Abstract Galcanezumab is a humanized immunoglobulin G (IgG) monoclonal antibody (mAb) indicated for the prevention of migraine that binds to calcitonin gene‐relate... |
PMC10667676 | core_pubmed_pmc | Pharmacokinetics and bioequivalence of sunitinib and Sutent ® in Chinese healthy subjects: an open-label, randomized, crossover study | Pharmacokinetics and bioequivalence of sunitinib and Sutent ® in Chinese healthy subjects: an open-label, randomized, crossover study Abstract Abstract Purpose: The purpose of this study was to examine the pharmacokinetics (PK), bioequivalence and safety of generic sunitinib and its original product Sutent ® in healthy... |
PMC10293548 | core_pubmed_pmc | Bioavailability of Cariban ® Capsules: A Modified-Release Fixed-Dose Combination of Doxylamine and Pyridoxine to Relieve Nausea and Vomiting During Pregnancy | Bioavailability of Cariban ® Capsules: A Modified-Release Fixed-Dose Combination of Doxylamine and Pyridoxine to Relieve Nausea and Vomiting During Pregnancy Abstract Background Nausea and vomiting is a very prevalent condition during pregnancy. Combination of doxylamine and pyridoxine is placed as first-line pharmacol... |
PMC12025224 | core_pubmed_pmc | Drugs Repurposing of Molecules Modulating Human Delta Globin Gene Expression via a Model of Transgenic Foetal Liver Cells: Implications for Beta-Hemoglobinopathy Therapeutics | Drugs Repurposing of Molecules Modulating Human Delta Globin Gene Expression via a Model of Transgenic Foetal Liver Cells: Implications for Beta-Hemoglobinopathy Therapeutics Abstract Beta-hemoglobinopathies such as beta-thalassemia and sickle cell disease are severe genetic blood disorders affecting the beta globin ch... |
PMC12242394 | core_pubmed_pmc | Pharmacokinetic comparison between the fixed-dose combination of rosuvastatin/ezetimibe 2.5/10 mg and the co-administration of individual formulations in healthy subjects | Pharmacokinetic comparison between the fixed-dose combination of rosuvastatin/ezetimibe 2.5/10 mg and the co-administration of individual formulations in healthy subjects Abstract Abstract The combination therapy of low-dose rosuvastatin and ezetimibe has shown similar efficacy in decreasing low-density lipoprotein cho... |
PMC6565689 | core_pubmed_pmc | Supplying a pharmacy for NASA exploration spaceflight: challenges and current understanding | Supplying a pharmacy for NASA exploration spaceflight: challenges and current understanding Abstract Abstract In order to maintain crew health and performance during long-duration spaceflight outside of low-Earth orbit, NASA and its international partners must be capable of providing a safe and effective pharmacy. Give... |
PMC4791863 | core_pubmed_pmc | Phase 1b/2a study of trastuzumab emtansine (T-DM1), paclitaxel, and pertuzumab in HER2-positive metastatic breast cancer | Phase 1b/2a study of trastuzumab emtansine (T-DM1), paclitaxel, and pertuzumab in HER2-positive metastatic breast cancer Abstract Abstract Background In pre-clinical studies, the anti-tumor activity of T-DM1 was enhanced when combined with taxanes or pertuzumab. This phase 1b/2a study evaluated the safety/tolerability ... |
PMC10118160 | core_pubmed_pmc | Translation and cultural adaptation of MedStopper®—A web-based decision aid for deprescribing in older adults: A protocol | Translation and cultural adaptation of MedStopper®—A web-based decision aid for deprescribing in older adults: A protocol Abstract Background Older patients are more likely to have medication-related problems, which are associated with changes in pharmacokinetics and pharmacodynamics, multimorbidity, and polypharmacy. ... |
PMC12362515 | core_pubmed_pmc | ADORE: an open platform study of ruxolitinib in combination with other novel therapies in patients with myelofibrosis ∗ | ADORE: an open platform study of ruxolitinib in combination with other novel therapies in patients with myelofibrosis ∗ Abstract Key Points • ADORE was an open platform study of 5 ruxolitinib combinations in patients with MF and suboptimal response to ruxolitinib alone. • Most patients received the siremadlin combinati... |
PMC10569162 | core_pubmed_pmc | Dose-sparing effect of lapatinib co-administered with a high-fat enteral nutrition emulsion: preclinical pharmacokinetic study | Dose-sparing effect of lapatinib co-administered with a high-fat enteral nutrition emulsion: preclinical pharmacokinetic study Abstract Abstract Background Lapatinib is an oral small-molecule tyrosine kinase inhibitor indicated for advanced or metastatic HER2-positive breast cancer. In order to reduce the treatment cos... |
PMC11106164 | core_pubmed_pmc | Pharmacokinetics of Monoclonal Antibodies Throughout Pregnancy: A Systematic Literature Review | Pharmacokinetics of Monoclonal Antibodies Throughout Pregnancy: A Systematic Literature Review Abstract Background and Objective Although little information is available on the pharmacokinetics (PK) of monoclonal antibodies (mAbs) during pregnancy, multiple mAbs are being used during pregnancy for various indications. ... |
PMC8655510 | core_pubmed_pmc | Pharmacokinetics of the disialoganglioside, G D2 , a circulating tumor biomarker for neuroblastoma, in nonhuman primates | Pharmacokinetics of the disialoganglioside, G D2 , a circulating tumor biomarker for neuroblastoma, in nonhuman primates Abstract ABSTRACT Background: The ganglioside G D2 is a potential circulating tumor biomarker for the childhood cancer neuroblastoma. Interpreting the levels of a circulating tumor biomarker depends ... |
PMC10527299 | core_pubmed_pmc | Mind the Gap: Model-Based Switching from Selatogrel to Maintenance Therapy with Oral P2Y12 Receptor Antagonists | Mind the Gap: Model-Based Switching from Selatogrel to Maintenance Therapy with Oral P2Y12 Receptor Antagonists Abstract Abstract Background: The P2Y 12 receptor antagonist selatogrel is being developed for subcutaneous self-administration with a ready-to-use autoinjector at the onset of acute myocardial infarction (AM... |
PMC12551014 | core_pubmed_pmc | Dimethoxybenzohomoadamantane-based soluble epoxide hydrolase inhibitors: in vivo efficacy in a murine model of chemotherapy-induced neuropathic pain | Dimethoxybenzohomoadamantane-based soluble epoxide hydrolase inhibitors: in vivo efficacy in a murine model of chemotherapy-induced neuropathic pain Abstract Abstract The soluble epoxide hydrolase (sEH) has recently emerged as a promising target for the treatment of several pain-related conditions. Herein, we report th... |
PMC10663225 | core_pubmed_pmc | Development and characterization of narsoplimab, a selective MASP-2 inhibitor, for the treatment of lectin-pathway–mediated disorders | Development and characterization of narsoplimab, a selective MASP-2 inhibitor, for the treatment of lectin-pathway–mediated disorders Abstract Abstract Introduction Overactivation of the lectin pathway of complement plays a pathogenic role in a broad range of immune-mediated and inflammatory disorders; mannan-binding l... |
PMC12862949 | core_pubmed_pmc | Efficacy, pharmacokinetics and safety of liposomal synthetic cannabidiol injected subcutaneously in dogs: a randomized, blinded, placebo-controlled, crossover clinical trial | Efficacy, pharmacokinetics and safety of liposomal synthetic cannabidiol injected subcutaneously in dogs: a randomized, blinded, placebo-controlled, crossover clinical trial Abstract Abstract Background Cannabidiol (CBD) has anti-nociceptive and anti-inflammatory characteristics, and was reported to provide analgesia i... |
PMC6791168 | core_pubmed_pmc | Enhanced sustained release of furosemide in long circulating chitosan-conjugated PLGA nanoparticles | Enhanced sustained release of furosemide in long circulating chitosan-conjugated PLGA nanoparticles Abstract Furosemide (FSM) is commonly used in the treatment of edema associated with congestive cardiac failure, cirrhosis of the liver, renal disease, including the nephrotic syndrome and hypertension. However, in ascit... |
PMC10001409 | core_pubmed_pmc | Insomnia among Cancer Patients in the Real World: Optimising Treatments and Tailored Therapies | Insomnia among Cancer Patients in the Real World: Optimising Treatments and Tailored Therapies Abstract Abstract Background: Insomnia is commonly reported by cancer patients. Its multifaceted pathophysiology makes this symptom a complex challenge for the clinician, who should bear in mind the manifold world of causes a... |
PMC9020733 | core_pubmed_pmc | Novel aerosol treatment of airway hyper-reactivity and inflammation in a murine model of asthma with a soluble epoxide hydrolase inhibitor | Novel aerosol treatment of airway hyper-reactivity and inflammation in a murine model of asthma with a soluble epoxide hydrolase inhibitor Abstract Asthma currently affects more than 339 million people worldwide. In the present preliminary study, we examined the efficacy of a new, inhalable soluble epoxide hydrolase in... |
PMC9277925 | core_pubmed_pmc | Discovery of a novel ALK/ROS1/FAK inhibitor, APG-2449, in preclinical non-small cell lung cancer and ovarian cancer models | Discovery of a novel ALK/ROS1/FAK inhibitor, APG-2449, in preclinical non-small cell lung cancer and ovarian cancer models Abstract Background Tyrosine kinase inhibitors (TKIs) are mainstays of cancer treatment. However, their clinical benefits are often constrained by acquired resistance. To overcome such outcomes, we... |
PMC9559901 | core_pubmed_pmc | A Phase I, Single Ascending Dose Study of GEM103 (Recombinant Human Complement Factor H) in Patients with Geographic Atrophy | A Phase I, Single Ascending Dose Study of GEM103 (Recombinant Human Complement Factor H) in Patients with Geographic Atrophy Abstract Purpose To establish the safety, tolerability, pharmacokinetics, and pharmacodynamics of an intravitreal injection of recombinant human complement factor H (CFH), GEM103, in individuals ... |
PMC7894403 | core_pubmed_pmc | Concentration‐QTc Modeling of Ozanimod’s Major Active Metabolites in Adult Healthy Subjects | Concentration‐QTc Modeling of Ozanimod’s Major Active Metabolites in Adult Healthy Subjects Abstract Ozanimod, approved by regulatory agencies in multiple countries for the treatment of adults with relapsing multiple sclerosis, is a sphingosine 1‐phosphate (S1P) receptor modulator, which binds with high affinity select... |
PMC12944294 | core_pubmed_pmc | Span Value as a Critical Quality Attribute for PLGA Microspheres: Controlling Burst Release and Enhancing Therapeutic Efficacy via Wet Sieving | Span Value as a Critical Quality Attribute for PLGA Microspheres: Controlling Burst Release and Enhancing Therapeutic Efficacy via Wet Sieving Abstract Abstract Background/Objectives: Poly(lactic-co-glycolic acid) (PLGA) microspheres offer sustained drug delivery but often suffer from broad particle size distribution (... |
PMC12406654 | core_pubmed_pmc | Pharmacokinetics and safety of single and repeat doses of ceftibuten in healthy participants: a phase 1 dose escalation study | Pharmacokinetics and safety of single and repeat doses of ceftibuten in healthy participants: a phase 1 dose escalation study Abstract ABSTRACT Ledaborbactam etzadroxil, the prodrug of the active β-lactamase inhibitor ledaborbactam, is being developed in combination with ceftibuten to treat serious infections caused by... |
PMC4590757 | core_pubmed_pmc | Insights into PBDE Uptake, Body Burden, and Elimination Gained from Australian Age–Concentration Trends Observed Shortly after Peak Exposure | Insights into PBDE Uptake, Body Burden, and Elimination Gained from Australian Age–Concentration Trends Observed Shortly after Peak Exposure Abstract Background Population pharmacokinetic models combined with multiple sets of age–concentration biomonitoring data facilitate back-calculation of chemical uptake rates from... |
PMC10034069 | core_pubmed_pmc | The therapeutic mechanism of Curcumae Radix against primary dysmenorrea based on 5-HTR/Ca 2+ /MAPK and fatty acids metabolomics | The therapeutic mechanism of Curcumae Radix against primary dysmenorrea based on 5-HTR/Ca 2+ /MAPK and fatty acids metabolomics Abstract Abstract Background: Curcumae Radix (CW) is traditionally used to treat primary dysmenorrea (PD). However, the mechanisms of action of CW in the treatment of PD have not yet been comp... |
PMC8533485 | core_pubmed_pmc | Long-Term Pharmacokinetics of Dalbavancin in ABSSSI and Osteoarticular Settings: A Real-Life Outpatient Context | Long-Term Pharmacokinetics of Dalbavancin in ABSSSI and Osteoarticular Settings: A Real-Life Outpatient Context Abstract Abstract Dalbavancin is a lipoglycopeptide approved for treatment of Gram-positive infections of skin and skin-associated structures (ABSSSI). Currently, off-label use at high dosages for osteoarticu... |
PMC9851407 | core_pubmed_pmc | Antiviral effects and tissue exposure of tetrandrine against SARS‐CoV‐2 infection and COVID‐19 | Antiviral effects and tissue exposure of tetrandrine against SARS‐CoV‐2 infection and COVID‐19 Abstract Abstract Tetrandrine (TET) has been used to treat silicosis in China for decades. The aim of this study was to facilitate rational repurposing of TET against SARS‐CoV‐2 infection. In this study, we confirmed that TET... |
PMC12959151 | core_pubmed_pmc | Population pharmacokinetic model and dosing nomogram for daptomycin in adult patients with serious Gram-positive infections: emphasizing the role of loading doses and renal function-based adjustment | Population pharmacokinetic model and dosing nomogram for daptomycin in adult patients with serious Gram-positive infections: emphasizing the role of loading doses and renal function-based adjustment Abstract ABSTRACT Current recommendations for daptomycin dosing are based on body weight. However, it can be hypothesized... |
PMC11597389 | core_pubmed_pmc | Intratracheal Administration of Itraconazole-Loaded Hyaluronated Glycerosomes as a Promising Nanoplatform for the Treatment of Lung Cancer: Formulation, Physiochemical, and In Vivo Distribution | Intratracheal Administration of Itraconazole-Loaded Hyaluronated Glycerosomes as a Promising Nanoplatform for the Treatment of Lung Cancer: Formulation, Physiochemical, and In Vivo Distribution Abstract Abstract Background: Itraconazole (ITZ) is an antiangiogenic agent recognized as a potent suppressor of endothelial c... |
PMC10826136 | core_pubmed_pmc | Exploring a novel long-acting glucagon-like peptide-1 receptor agonist built on the albumin-binding domain and XTEN scaffolds | Exploring a novel long-acting glucagon-like peptide-1 receptor agonist built on the albumin-binding domain and XTEN scaffolds Abstract In recent years, glucagon-like peptide-1 (GLP-1) has demonstrated considerable potential in the treatment of type 2 diabetes (T2D) and obesity. However, the half-life of naturally occur... |
PMC4946019 | core_pubmed_pmc | Antiretroviral Choice for HIV Impacts Antimalarial Exposure and Treatment Outcomes in Ugandan Children | Antiretroviral Choice for HIV Impacts Antimalarial Exposure and Treatment Outcomes in Ugandan Children Abstract Pharmacokinetic/pharmacodynamic studies of artemether-lumefantrine and 3 antiretroviral regimens were conducted in malaria-infected Ugandan children. Efavirenz-based treatment was associated with significant ... |
PMC6066326 | core_pubmed_pmc | Clinical outcomes of prolonged infusion (extended infusion or continuous infusion) versus intermittent bolus of meropenem in severe infection: A meta-analysis | Clinical outcomes of prolonged infusion (extended infusion or continuous infusion) versus intermittent bolus of meropenem in severe infection: A meta-analysis Abstract Abstract Background Meropenem exhibits time-dependent antimicrobial activity and prolonged infusion (PI) (extended infusion or continuous infusion, EI o... |
PMC8359386 | core_pubmed_pmc | Model‐based meta‐analysis of the time to first acute urinary retention or benign prostatic hyperplasia‐related surgery in patients with moderate or severe symptoms | Model‐based meta‐analysis of the time to first acute urinary retention or benign prostatic hyperplasia‐related surgery in patients with moderate or severe symptoms Abstract Aims Combination therapy of 5α‐reductase inhibitor and α‐blocker is a guideline‐endorsed therapeutic approach for patients with moderate‐to‐severe ... |
PMC11218722 | core_pubmed_pmc | A Phase 0 Study to Assess the Biodistribution and Pharmacokinetics of a Radiolabeled Antibody Targeting Human Kallikrein 2 in Participants with Metastatic Castration-Resistant Prostate Cancer | A Phase 0 Study to Assess the Biodistribution and Pharmacokinetics of a Radiolabeled Antibody Targeting Human Kallikrein 2 in Participants with Metastatic Castration-Resistant Prostate Cancer Abstract Abstract Despite the inclusion of multiple agents within the prostate cancer treatment landscape, new treatment options... |
PMC8212713 | core_pubmed_pmc | A Randomized Phase I Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Recombinant Erwinia Asparaginase (JZP‐458) in Healthy Adult Volunteers | A Randomized Phase I Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Recombinant Erwinia Asparaginase (JZP‐458) in Healthy Adult Volunteers Abstract Abstract L‐asparaginase has been an important component of acute lymphoblastic leukemia (ALL) therapy for over 40 years, and is standard therapy during... |
PMC12454681 | core_pubmed_pmc | Navigating Drug–Drug Interactions in Clinical Drug Development: A Tutorial | Navigating Drug–Drug Interactions in Clinical Drug Development: A Tutorial Abstract ABSTRACT This tutorial provides essential guidelines and insights, in addition to regulatory guidance, for the evaluation of drug–drug interactions (DDIs), with a focus on the tools and timing of assessment critical for effective manage... |
PMC5146859 | core_pubmed_pmc | Phase 1/2 study of pacritinib, a next generation JAK2/FLT3 inhibitor, in myelofibrosis or other myeloid malignancies | Phase 1/2 study of pacritinib, a next generation JAK2/FLT3 inhibitor, in myelofibrosis or other myeloid malignancies Abstract Background Pacritinib (SB1518) is a highly selective kinase inhibitor with specificity for JAK2, FLT3, IRAK1, and CFS1R. This multicenter phase 1/2 study evaluated the maximum tolerated dose (MT... |
PMC12706393 | core_pubmed_pmc | AI for NONMEM Coding in Pharmacometrics Research and Education: Shortcut or Pitfall? | AI for NONMEM Coding in Pharmacometrics Research and Education: Shortcut or Pitfall? Abstract ABSTRACT Artificial intelligence (AI) is increasingly being explored as a tool to support pharmacometric modeling, particularly in addressing the coding challenges associated with NONMEM. In this study, we evaluated the abilit... |
PMC5909626 | core_pubmed_pmc | Pharmacodynamics of the Novel Antifungal Agent F901318 for Acute Sinopulmonary Aspergillosis Caused by Aspergillus flavus | Pharmacodynamics of the Novel Antifungal Agent F901318 for Acute Sinopulmonary Aspergillosis Caused by Aspergillus flavus Abstract Abstract Background Aspergillus flavus is one of the most common agents of invasive aspergillosis and is associated with high mortality. The orotomides are a new class of antifungal agents ... |
PMC12529147 | core_pubmed_pmc | Dynamic PET Imaging of EpCAM-Positive Colorectal Cancer Using Radiolabeled DTN-SYL3C Aptamer Conjugates | Dynamic PET Imaging of EpCAM-Positive Colorectal Cancer Using Radiolabeled DTN-SYL3C Aptamer Conjugates Abstract DNA tetrahedra (DTN) could enhance the circulation and targeting capabilities of aptamers. This study constructs a gallium-68 ( 68 Ga) radiolabeled DTN-SYL3C aptamer conjugate to evaluate their imaging poten... |
PMC11109879 | core_pubmed_pmc | Expression of gemcitabine metabolizing enzymes and stromal components reveal complexities of preclinical pancreatic cancer models for therapeutic testing | Expression of gemcitabine metabolizing enzymes and stromal components reveal complexities of preclinical pancreatic cancer models for therapeutic testing Abstract Abstract Background Pancreatic ductal adenocarcinoma (PDAC) poorly responds to antineoplastic agents. Discrepancies between preclinical success and clinical ... |
PMC3671720 | core_pubmed_pmc | In Vitro-In Vivo Correlation Evaluation of Generic Alfuzosin Modified Release Tablets | In Vitro-In Vivo Correlation Evaluation of Generic Alfuzosin Modified Release Tablets Abstract Alfuzosin, a selective alpha-1a antagonistis is the most recently approved AARAS, with limited cardiac toxicity and exclusively used for lower urinary tract syndromes (LUTS). In order to reduce pill burden and better patient ... |
PMC10275028 | core_pubmed_pmc | Multi-dose enteral L-citrulline administration in premature infants at risk of developing pulmonary hypertension associated with bronchopulmonary dysplasia | Multi-dose enteral L-citrulline administration in premature infants at risk of developing pulmonary hypertension associated with bronchopulmonary dysplasia Abstract Abstract Objective. Information is needed to guide the design of randomized controlled trials (RCTs) evaluating L-citrulline as a therapy for premature inf... |
PMC9543968 | core_pubmed_pmc | Interactions of the protease inhibitor, ritonavir, with common anesthesia drugs | Interactions of the protease inhibitor, ritonavir, with common anesthesia drugs Abstract Abstract The protease inhibitor, ritonavir, is a strong inhibitor of CYP 3A. The drug is used for management of the human immunovirus and is currently part of an oral antiviral drug combination (nirmatrelvir–ritonavir) for the earl... |
PMC7770995 | core_pubmed_pmc | The impact of omeprazole on mycophenolate pharmacokinetics in kidney transplant recipients | The impact of omeprazole on mycophenolate pharmacokinetics in kidney transplant recipients Abstract Background The absorption rates of mycophenolate mofetil (MMF) and enteric-coated mycophenolate sodium (EC-MPS) may be influenced by the concomitant use of omeprazole. Methods One hundred kidney transplant patients were ... |
PMC12510855 | core_pubmed_pmc | Pharmacokinetic-pharmacodynamic target attainment analyses as support for meropenem dosing regimens in critically ill adult and elderly patients with Pseudomonas aeruginosa infections | Pharmacokinetic-pharmacodynamic target attainment analyses as support for meropenem dosing regimens in critically ill adult and elderly patients with Pseudomonas aeruginosa infections Abstract Abstract Background Critically ill patients often undergo profound pathophysiological changes that alter the pharmacokinetics (... |
PMC3409074 | core_pubmed_pmc | Pharmacokinetics of dasatinib for Philadelphia-positive acute lymphocytic leukemia with acquired T315I mutation | Pharmacokinetics of dasatinib for Philadelphia-positive acute lymphocytic leukemia with acquired T315I mutation Abstract Background The BCR-ABL T315I kinase domain mutation is insensitive to dasatinib therapy for Philadelphia-positive acute lymphoid leukemia (Ph + ALL) patients. Resistant T315I clone may be present pri... |
PMC12799929 | core_pubmed_pmc | A humanized transferrin receptor 1-transferrin model supports functional iron homeostasis and therapeutic delivery across the blood–brain barrier | A humanized transferrin receptor 1-transferrin model supports functional iron homeostasis and therapeutic delivery across the blood–brain barrier Abstract The transferrin receptor 1 (TfR1)–transferrin (TF) axis is central to iron homeostasis and represents a validated route for delivering biologics across the blood–bra... |
PMC8038096 | core_pubmed_pmc | Magnetic Core–Shell Molecularly Imprinted Nano-Conjugates for Extraction of Antazoline and Hydroxyantazoline from Human Plasma—Material Characterization, Theoretical Analysis and Pharmacokinetics | Magnetic Core–Shell Molecularly Imprinted Nano-Conjugates for Extraction of Antazoline and Hydroxyantazoline from Human Plasma—Material Characterization, Theoretical Analysis and Pharmacokinetics Abstract Abstract The aim of this study was to develop magnetic molecularly imprinted nano-conjugate sorbent for effective d... |
PMC6390132 | core_pubmed_pmc | Phase IIa, placebo-controlled, randomised study of lutikizumab, an anti-interleukin-1α and anti-interleukin-1β dual variable domain immunoglobulin, in patients with erosive hand osteoarthritis | Phase IIa, placebo-controlled, randomised study of lutikizumab, an anti-interleukin-1α and anti-interleukin-1β dual variable domain immunoglobulin, in patients with erosive hand osteoarthritis Abstract Abstract Objective To assess the efficacy, safety, pharmacokinetics and pharmacodynamics of the anti-interleukin (IL)-... |
PMC10319390 | core_pubmed_pmc | Pharmacokinetics of rifampicin, isoniazid & pyrazinamide during daily & intermittent dosing: A preliminary study | Pharmacokinetics of rifampicin, isoniazid & pyrazinamide during daily & intermittent dosing: A preliminary study Abstract Abstract Background & objectives: The National Tuberculosis (TB) Control Programme has transitioned from thrice-weekly to daily drug treatment regimens in India. This preliminary study was conceived... |
PMC5719405 | core_pubmed_pmc | Sex-related pharmacokinetic differences and mechanisms of metapristone (RU486 metabolite) | Sex-related pharmacokinetic differences and mechanisms of metapristone (RU486 metabolite) Abstract Metapristone is the primary metabolite of the abortifacient mifepristone (RU486), and is being developed as a safe and effective cancer metastatic chemopreventive agent for both sexes. Here, we systematically investigated... |
PMC5829905 | core_pubmed_pmc | Evaluating the impact of type 2 diabetes mellitus on CYP450 metabolic activities: protocol for a case–control pharmacokinetic study | Evaluating the impact of type 2 diabetes mellitus on CYP450 metabolic activities: protocol for a case–control pharmacokinetic study Abstract Introduction Diabetes affects more than 9% of the adult population worldwide. Patients with type 2 diabetes mellitus (T2DM) show variable responses to some drugs which may be due,... |
PMC8239543 | core_pubmed_pmc | A phase I study of high dose camostat mesylate in healthy adults provides a rationale to repurpose the TMPRSS2 inhibitor for the treatment of COVID‐19 | A phase I study of high dose camostat mesylate in healthy adults provides a rationale to repurpose the TMPRSS2 inhibitor for the treatment of COVID‐19 Abstract Abstract Camostat mesylate, an oral serine protease inhibitor, is used to treat chronic pancreatitis and reflux esophagitis. Recently, camostat mesylate and its... |
PMC9181373 | core_pubmed_pmc | Active Compounds in Zingiber officinale as Possible Redox Inhibitors of 5-Lipoxygenase Using an In Silico Approach | Active Compounds in Zingiber officinale as Possible Redox Inhibitors of 5-Lipoxygenase Using an In Silico Approach Abstract 5-Lipoxygenase (5-LOX) converts arachidonic acid to lipidic inflammatory mediators such as leukotrienes (LTs). In diseases such as asthma, LTs contribute to a physiopathology that could be reverte... |
PMC9639395 | core_pubmed_pmc | Phase I dose escalation and expansion trial of single agent ONC201 in pediatric diffuse midline gliomas following radiotherapy | Phase I dose escalation and expansion trial of single agent ONC201 in pediatric diffuse midline gliomas following radiotherapy Abstract Abstract Background ONC201, a dopamine receptor D2 (DRD2) antagonist and caseinolytic protease P (ClpP) agonist, has induced durable tumor regressions in adults with recurrent H3 K27M-... |
PMC11546283 | core_pubmed_pmc | Complex Pharmacodynamics of Aripiprazole and Haloperidol in Schizophrenia Management: A Case Report | Complex Pharmacodynamics of Aripiprazole and Haloperidol in Schizophrenia Management: A Case Report Abstract Abstract Schizophrenia is a complex psychotic disorder characterized by positive symptoms, such as hallucinations and delusions, and negative symptoms, including emotional withdrawal and apathy. Its profound imp... |
PMC4716722 | core_pubmed_pmc | Preparation, characterization, and in vivo evaluation of intranasally administered liposomal formulation of donepezil | Preparation, characterization, and in vivo evaluation of intranasally administered liposomal formulation of donepezil Methods Materials Donepezil used in the study was procured from Fluka, St Louis, MO, USA. Carboxymethyl cellulose, 1,2-distearyl-sn-glycero-3-phosphocholine (DSPC), cholesterol (CHE), polyethylene glyco... |
PMC8843782 | core_pubmed_pmc | Pharmacodynamics and Cellular Uptake of Peimine and Peiminine in Inflammatory Model Non-Small-Cell Lung Cancer Epithelial Cells (A549) | Pharmacodynamics and Cellular Uptake of Peimine and Peiminine in Inflammatory Model Non-Small-Cell Lung Cancer Epithelial Cells (A549) Abstract Abstract Peimine and peiminine are isosteroidal alkaloids with multiple biological activities, such as anticancer and anti-inflammatory activities, but their cellular uptake an... |
PMC12829308 | core_pubmed_pmc | Klebsiella pneumoniae and pyogenic liver abscess: Emerging clinical threats, virulence mechanisms and therapeutic strategies (Review) | Klebsiella pneumoniae and pyogenic liver abscess: Emerging clinical threats, virulence mechanisms and therapeutic strategies (Review) Abstract Klebsiella pneumoniae has emerged as a leading cause of pyogenic liver abscess (PLA), driven by hypervirulent and multidrug-resistant (MDR) strains that pose major diagnostic an... |
PMC6602958 | core_pubmed_pmc | Pharmacokinetics of anti-infectious reagents in silkworms | Pharmacokinetics of anti-infectious reagents in silkworms Abstract Abstract Silkworm microorganism infection models are useful for screening novel therapeutically effective antimicrobial agents. In this study, we used silkworms to investigate the pharmacokinetics and metabolism of antimicrobial agents, in which cytochr... |
PMC10583245 | core_pubmed_pmc | Pharmacometrics enhanced Bayesian borrowing approach to improve clinical trial efficiency: Case of empagliflozin in type 2 diabetes | Pharmacometrics enhanced Bayesian borrowing approach to improve clinical trial efficiency: Case of empagliflozin in type 2 diabetes Abstract Abstract We report use of a pharmacometrics enhanced Bayesian borrowing (PEBB) approach to leverage historical clinical trial data on a drug product to build models, project the o... |
PMC3114728 | core_pubmed_pmc | Statistical Inference Methods for Sparse Biological Time Series Data | Statistical Inference Methods for Sparse Biological Time Series Data Abstract Abstract Background Comparing metabolic profiles under different biological perturbations has become a powerful approach to investigating the functioning of cells. The profiles can be taken as single snapshots of a system, but more informatio... |
PMC5485720 | core_pubmed_pmc | Model‐Informed Development and Registration of a Once‐Daily Regimen of Extended‐Release Tofacitinib | Model‐Informed Development and Registration of a Once‐Daily Regimen of Extended‐Release Tofacitinib Abstract Abstract Extended‐release (XR) formulations enable less frequent dosing vs. conventional (e.g., immediate release (IR)) formulations. Regulatory registration of such formulations typically requires pharmacokinet... |
PMC7768647 | core_pubmed_pmc | In silico ranking of phenolics for therapeutic effectiveness on cancer stem cells | In silico ranking of phenolics for therapeutic effectiveness on cancer stem cells Abstract Background Cancer stem cells (CSCs) have features such as the ability to self-renew, differentiate into defined progenies and initiate the tumor growth. Treatments of cancer include drugs, chemotherapy and radiotherapy or a combi... |
PMC7331374 | core_pubmed_pmc | PK‐tailored tertiary prophylaxis in patients with severe hemophilia A at Beijing Children's Hospital | PK‐tailored tertiary prophylaxis in patients with severe hemophilia A at Beijing Children's Hospital Abstract Abstract Importance Tertiary prophylaxis using a low‐dose regimen is usually insufficient to prevent recurrent joint bleeding and deterioration in joint diseases in children with severe hemophilia A. Pharmacoki... |
PMC7661413 | core_pubmed_pmc | Evaluation of drug-drug interaction of lusutrombopag, a thrombopoietin receptor agonist, via metabolic enzymes and transporters | Evaluation of drug-drug interaction of lusutrombopag, a thrombopoietin receptor agonist, via metabolic enzymes and transporters Abstract Purpose Drug-drug interaction (DDI) potentials of lusutrombopag, a thrombopoietin receptor agonist, on the activity of cytochrome P450 (CYP) 3A and of cyclosporine, which inhibits P-g... |
PMC6611478 | core_pubmed_pmc | Fixed doses of N8‐GP prophylaxis maintain moderate‐to‐mild factor VIII levels in the majority of patients with severe hemophilia A | Fixed doses of N8‐GP prophylaxis maintain moderate‐to‐mild factor VIII levels in the majority of patients with severe hemophilia A Abstract Abstract Background N8‐GP is an extended half‐life recombinant factor VIII developed for prophylaxis and treatment of bleeds in patients with hemophilia A. Objective To assess phar... |
PMC8453771 | core_pubmed_pmc | Meta‐Analysis of Noncompartmental Pharmacokinetic Parameters of Ertugliflozin to Evaluate Dose Proportionality and UGT1A9 Polymorphism Effect on Exposure | Meta‐Analysis of Noncompartmental Pharmacokinetic Parameters of Ertugliflozin to Evaluate Dose Proportionality and UGT1A9 Polymorphism Effect on Exposure Abstract Abstract Ertugliflozin, a sodium‐glucose cotransporter 2 inhibitor, is primarily metabolized via glucuronidation by the uridine 5′‐diphospho‐glucuronosyltran... |
PMC9372426 | core_pubmed_pmc | Evolution of preclinical characterization and insights into clinical pharmacology of checkpoint inhibitors approved for cancer immunotherapy | Evolution of preclinical characterization and insights into clinical pharmacology of checkpoint inhibitors approved for cancer immunotherapy Abstract Abstract Cancer immunotherapy has significantly advanced the treatment paradigm in oncology, with approvals of immuno‐oncology agents for over 16 indications, many of the... |
PMC12540056 | core_pubmed_pmc | Phage therapy as a revitalized weapon for treating clinical diseases | Phage therapy as a revitalized weapon for treating clinical diseases Abstract Abstract The rising prevalence of multidrug-resistant (MDR) bacterial infections, coupled with the diminishing efficacy of antibiotics, has reinvigorated interest in bacteriophage (phage) therapy as a promising alternative, leveraging its uni... |
PMC5103374 | core_pubmed_pmc | In vivo human adipose-derived mesenchymal stem cell tracking after intra-articular delivery in a rat osteoarthritis model | In vivo human adipose-derived mesenchymal stem cell tracking after intra-articular delivery in a rat osteoarthritis model Abstract Abstract Background Human adipose-derived mesenchymal stem cells (haMSCs) have shown efficacy in treating osteoarthritis (OA) both preclinically and clinically via intra-articular (IA) inje... |
PMC8019567 | core_pubmed_pmc | Pharmacokinetics of a novel endectoparasiticide topical formulation for cats, combining esafoxolaner, eprinomectin and praziquantel | Pharmacokinetics of a novel endectoparasiticide topical formulation for cats, combining esafoxolaner, eprinomectin and praziquantel Abstract Abstract Esafoxolaner, a purified enantiomer of afoxolaner with insecticidal and acaricidal properties, is combined with eprinomectin and praziquantel in NexGard ® Combo, a novel ... |
PMC5818563 | core_pubmed_pmc | A Phase 1 Pharmacokinetic Study of Cysteamine Bitartrate Delayed-Release Capsules Following Oral Administration with Orange Juice, Water, or Omeprazole in Cystinosis | A Phase 1 Pharmacokinetic Study of Cysteamine Bitartrate Delayed-Release Capsules Following Oral Administration with Orange Juice, Water, or Omeprazole in Cystinosis Abstract Abstract Introduction Cystinosis is a rare, metabolic, autosomal recessive, genetic lysosomal storage disorder characterized by an accumulation o... |
PMC12314114 | core_pubmed_pmc | A Randomized Thorough QT Trial Using Concentration‐QT Analysis to Evaluate the Effects of Centanafadine on Cardiac Repolarization | A Randomized Thorough QT Trial Using Concentration‐QT Analysis to Evaluate the Effects of Centanafadine on Cardiac Repolarization Abstract Abstract Centanafadine is a norepinephrine/dopamine/serotonin reuptake inhibitor in development for treatment of attention‐deficit/hyperactivity disorder. This double‐blind, placebo... |
PMC10031009 | core_pubmed_pmc | Understanding the dosing-time-dependent antihypertensive effect of valsartan and aspirin through mathematical modeling | Understanding the dosing-time-dependent antihypertensive effect of valsartan and aspirin through mathematical modeling Abstract Chronopharmacology of arterial hypertension impacts the long-term cardiovascular risk of hypertensive subjects. Therefore, clinical and computational studies have proposed optimizing antihyper... |
PMC9092151 | core_pubmed_pmc | Targeting HCV polymerase: a structural and dynamic perspective into the mechanism of selective covalent inhibition | Targeting HCV polymerase: a structural and dynamic perspective into the mechanism of selective covalent inhibition Abstract Abstract Background : Concerns have been raised over the emerging pandemic status of hepatitis C virus (HCV). Current available drugs lack specificity, stability and potency. The HCV NS5B RNA-depe... |
PMC8537445 | core_pubmed_pmc | D-Peptide-Based Probe for CXCR4-Targeted Molecular Imaging and Radionuclide Therapy | D-Peptide-Based Probe for CXCR4-Targeted Molecular Imaging and Radionuclide Therapy Abstract Abstract Positron emission tomography (PET) imaging of the C-X-C chemokine receptor 4 (CXCR4) with [ 68 Ga]PentixaFor has intrinsic diagnostic value and is used to select patients for personalized CXCR4-targeted radionuclide th... |
PMC10681481 | core_pubmed_pmc | Building an adaptive dose simulation framework to aid dose and schedule selection | Building an adaptive dose simulation framework to aid dose and schedule selection Abstract Abstract Establishing a dosing regimen that maximizes clinical benefit and minimizes adverse effects for novel therapeutics is a key objective for drug developers. Finding an optimal dose and schedule can be particularly challeng... |
PMC12030412 | core_pubmed_pmc | Advancements in Cyclodextrin Complexes with Bioactive Secondary Metabolites and Their Pharmaceutical Applications | Advancements in Cyclodextrin Complexes with Bioactive Secondary Metabolites and Their Pharmaceutical Applications Abstract Abstract Cyclodextrins (CDs) have largely been investigated during the last decades for their outstanding properties, such as biocompatibility and biodegradability, with wide applications in the ph... |
PMC4894406 | core_pubmed_pmc | Results of an abbreviated phase-II study with the Akt Inhibitor MK-2206 in Patients with Advanced Biliary Cancer | Results of an abbreviated phase-II study with the Akt Inhibitor MK-2206 in Patients with Advanced Biliary Cancer Abstract Abstract Biliary cancers (BC) are rare, chemoresistant and are associated with a poor prognosis. Targeting the Akt pathway is of significance in BC. We hypothesized that the allosteric inhibitor MK-... |
PMC6687118 | core_pubmed_pmc | Safety, pharmacokinetics, and immunogenicity of the combination of the broadly neutralizing anti-HIV-1 antibodies 3BNC117 and 10-1074 in healthy adults: A randomized, phase 1 study | Safety, pharmacokinetics, and immunogenicity of the combination of the broadly neutralizing anti-HIV-1 antibodies 3BNC117 and 10-1074 in healthy adults: A randomized, phase 1 study Abstract Abstract Background Additional forms of pre-exposure prophylaxis are needed to prevent HIV-1 infection. 3BNC117 and 10–1074 are br... |
PMC10278029 | core_pubmed_pmc | Steady-State Pharmacokinetics of Intravenous Hydromorphone in Japanese Patients With Renal Impairment and Cancer Pain | Steady-State Pharmacokinetics of Intravenous Hydromorphone in Japanese Patients With Renal Impairment and Cancer Pain Abstract Abstract Background: The opioid analgesic hydromorphone has a low renal excretion ratio; however, exposure after oral administration is several times higher in those with moderate or severe ren... |
PMC11564280 | core_pubmed_pmc | Pharmacokinetics and Tolerability of the Novel Myeloperoxidase Inhibitor Mitiperstat in Healthy Japanese and Chinese Volunteers | Pharmacokinetics and Tolerability of the Novel Myeloperoxidase Inhibitor Mitiperstat in Healthy Japanese and Chinese Volunteers Abstract Abstract Background and Objective Mitiperstat (AZD4831) is a novel irreversible oral myeloperoxidase inhibitor in clinical development for heart failure with preserved ejection fracti... |
PMC5119845 | core_pubmed_pmc | Population Pharmacokinetics of Inhaled Fluticasone Furoate and Vilanterol in Subjects with Chronic Obstructive Pulmonary Disease | Population Pharmacokinetics of Inhaled Fluticasone Furoate and Vilanterol in Subjects with Chronic Obstructive Pulmonary Disease Abstract Abstract Background and Objectives Previous pharmacokinetic studies of the inhaled corticosteroid, fluticasone furoate (FF), and the long-acting, beta2-receptor agonist, vilanterol (... |
PMC12712829 | core_pubmed_pmc | Vixarelimab in Patients With Prurigo Nodularis | Vixarelimab in Patients With Prurigo Nodularis Abstract Key Points Question What were the long-term efficacy, safety, and pharmacokinetic profiles of monthly dosed vixarelimab in participants with prurigo nodularis? Findings In this randomized clinical trial including 181 participants, vixarelimab demonstrated a signif... |
PMC9469697 | core_pubmed_pmc | Efficient and relevant stepwise covariate model building for pharmacometrics | Efficient and relevant stepwise covariate model building for pharmacometrics Abstract Abstract Covariate modeling is an important opportunity for pharmacometrics to influence decision making in drug development. The stepwise covariate model (SCM) building procedure is the most common method for covariate model developm... |
PMC12934412 | core_pubmed_pmc | High-dose versus standard-dose intermittent meropenem in critically ill patients: An observational cohort study | High-dose versus standard-dose intermittent meropenem in critically ill patients: An observational cohort study Abstract Abstract Background The impact of high-dose versus standard-dose meropenem on outcomes in critically ill patients remains uncertain. Methods We conducted an observational cohort study in Vienna, Aust... |
PMC10685666 | core_pubmed_pmc | In silico prediction of bioequivalence of atorvastatin tablets based on GastroPlus™ software | In silico prediction of bioequivalence of atorvastatin tablets based on GastroPlus™ software Abstract The prediction of intestinal absorption of various drugs based on computer simulations has been a reality. However, in vivo pharmacokinetic simulations and virtual bioequivalence evaluation based on GastroPlus™ have no... |
PMC5694423 | core_pubmed_pmc | Pharmacokinetics of a New Oral Vitamin D Receptor Activator (2-Methylene-19-Nor-(20S)-1α,25-Dihydroxyvitamin D 3 ) in Patients with Chronic Kidney Disease and Secondary Hyperparathyroidism on Hemodialysis | Pharmacokinetics of a New Oral Vitamin D Receptor Activator (2-Methylene-19-Nor-(20S)-1α,25-Dihydroxyvitamin D 3 ) in Patients with Chronic Kidney Disease and Secondary Hyperparathyroidism on Hemodialysis Abstract Abstract Background 2-Methylene-19-nor-(20S)-1α,25-dihydroxyvitamin D 3 (DP001 or 2MD) is a novel, potent ... |
PMC12515199 | core_pubmed_pmc | Safety and efficacy of semi-dose venetoclax plus azacitidine in unfit acute myeloid leukemia patients in China: a real-world single-center study | Safety and efficacy of semi-dose venetoclax plus azacitidine in unfit acute myeloid leukemia patients in China: a real-world single-center study Abstract Abstract Acute myeloid leukemia (AML) carries a poor prognosis in elderly or medically unfit patients, with median overall survival (OS) of only 7–8 months for those ... |
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