Population Pharmacokinetic Analysis of Dorzagliatin in Healthy Subjects and Patients with Type 2 Diabetes Mellitus
ConclusionThe two-compartment linear pharmacokinetic model with zero- and first-order sequential absorption adequately described the pharmacokinetic characteristics of dorzagliatin. Body weight, aspartate aminotransferase, and age had a statistically significant effect on the CL/F of dorzagliatin. Body weight and sex had a statistically significant effect onVc/F. However, considering the clinically insignificant changes in the magnitude of steady-state exposure caused by these covariates, as well as the minimal changes in the steady-state exposure for individuals with mild and moderate impaired hepatic function and all sta...
Source: Clinical Pharmacokinetics - August 3, 2023 Category: Drugs & Pharmacology Source Type: research
Correction: A Review of Population Pharmacokinetic Analyses of Linezolid
(Source: Clinical Pharmacokinetics)
Source: Clinical Pharmacokinetics - August 3, 2023 Category: Drugs & Pharmacology Source Type: research
Population Pharmacokinetic Analysis of Dorzagliatin in Healthy Subjects and Patients with Type 2 Diabetes Mellitus
ConclusionThe two-compartment linear pharmacokinetic model with zero- and first-order sequential absorption adequately described the pharmacokinetic characteristics of dorzagliatin. Body weight, aspartate aminotransferase, and age had a statistically significant effect on the CL/F of dorzagliatin. Body weight and sex had a statistically significant effect onVc/F. However, considering the clinically insignificant changes in the magnitude of steady-state exposure caused by these covariates, as well as the minimal changes in the steady-state exposure for individuals with mild and moderate impaired hepatic function and all sta...
Source: Clinical Pharmacokinetics - August 3, 2023 Category: Drugs & Pharmacology Source Type: research
Correction: A Review of Population Pharmacokinetic Analyses of Linezolid
(Source: Clinical Pharmacokinetics)
Source: Clinical Pharmacokinetics - August 3, 2023 Category: Drugs & Pharmacology Source Type: research
CYP3A and CYP2C19 Activity Determined by Microdosed Probe Drugs Accurately Predict Voriconazole Clearance in Healthy Adults
ConclusionMicrodosed midazolam and omeprazole accurately described and predicted total CLVRZTrial RegistrationEudraCT No: 2020-001017-20, registered on March 5th, 2020. DRKS: DRKS00022547, registered on August 6th, 2020. (Source: Clinical Pharmacokinetics)
Source: Clinical Pharmacokinetics - July 28, 2023 Category: Drugs & Pharmacology Source Type: research
Significant Effects of Renal Function on Mycophenolic Acid Total Clearance in Pediatric Kidney Transplant Recipients with Population Pharmacokinetic Modeling
ConclusionWe have successfully constructed and validated a novel population pharmacokinetic model of MPA in pediatric kidney transplant patients. A positive, nonlinear relationship between eGFR and total MPA clearance identified in our model is likely attributed to multiple concurrent mechanisms, which warrant further systematic investigations. (Source: Clinical Pharmacokinetics)
Source: Clinical Pharmacokinetics - July 26, 2023 Category: Drugs & Pharmacology Source Type: research
Clinical Pharmacology of Brigatinib: A Next-Generation Anaplastic Lymphoma Kinase Inhibitor
AbstractBrigatinib, a next-generation anaplastic lymphoma kinase (ALK) inhibitor designed to overcome mechanisms of resistance associated with crizotinib, is approved for the treatment ofALK-positive advanced or metastatic non-small cell lung cancer. After oral administration of single doses of brigatinib 30 –240 mg, the median time to reach maximum plasma concentration ranged from 1 to 4 h. In patients with advanced malignancies, brigatinib showed dose linearity over the dose range of 60–240 mg once daily. A high-fat meal had no clinically meaningful effect on systemic exposures of brigatinib (area under the plasma co...
Source: Clinical Pharmacokinetics - July 26, 2023 Category: Drugs & Pharmacology Source Type: research
Significant Effects of Renal Function on Mycophenolic Acid Total Clearance in Pediatric Kidney Transplant Recipients with Population Pharmacokinetic Modeling
ConclusionWe have successfully constructed and validated a novel population pharmacokinetic model of MPA in pediatric kidney transplant patients. A positive, nonlinear relationship between eGFR and total MPA clearance identified in our model is likely attributed to multiple concurrent mechanisms, which warrant further systematic investigations. (Source: Clinical Pharmacokinetics)
Source: Clinical Pharmacokinetics - July 26, 2023 Category: Drugs & Pharmacology Source Type: research
Clinical Pharmacology of Brigatinib: A Next-Generation Anaplastic Lymphoma Kinase Inhibitor
AbstractBrigatinib, a next-generation anaplastic lymphoma kinase (ALK) inhibitor designed to overcome mechanisms of resistance associated with crizotinib, is approved for the treatment ofALK-positive advanced or metastatic non-small cell lung cancer. After oral administration of single doses of brigatinib 30 –240 mg, the median time to reach maximum plasma concentration ranged from 1 to 4 h. In patients with advanced malignancies, brigatinib showed dose linearity over the dose range of 60–240 mg once daily. A high-fat meal had no clinically meaningful effect on systemic exposures of brigatinib (area under the plasma co...
Source: Clinical Pharmacokinetics - July 26, 2023 Category: Drugs & Pharmacology Source Type: research
Status and Quality of Guidelines for Therapeutic Drug Monitoring Based on AGREE II Instrument
ConclusionThe number of TDM guidelines, especially technical and comprehensive ones, has significantly increased in recent years. Most guidelines are confronted with the problems of unclear methodology and low quality of evidence according to AGREE II. More evidence-based research on TDM and high-quality guideline development is recommended to promote individualized therapy. (Source: Clinical Pharmacokinetics)
Source: Clinical Pharmacokinetics - July 25, 2023 Category: Drugs & Pharmacology Source Type: research
Clinical Pharmacokinetics and Pharmacodynamics of the Next Generation Androgen Receptor Inhibitor —Darolutamide
AbstractDarolutamide is a next-generation androgen receptor signaling inhibitor (ARSI) currently approved for the treatment of nonmetastatic castration-resistant prostate cancer (nmCRPC) and metastatic hormone sensitive prostate cancer (mHSPC). Studies suggest that darolutamide also has the potential to be used to treat other stages of prostate cancer (PC), suggesting that its indications will broaden in the near future. Since ARSIs show similar efficacy for the treatment of PC, pharmacokinetic properties of these drugs and patient characteristics could help physicians decide which drug to select. This review provides an o...
Source: Clinical Pharmacokinetics - July 17, 2023 Category: Drugs & Pharmacology Source Type: research
