Pharmacogenetics and Pharmacokinetics

Pharmacogenetics

Pharmacokinetics

Pharmacokinetics of panobinostat: Inter-species difference in metabolic stability [Metabolism, Transport, and Pharmacogenetics]

ASPET

FEBRUARY 26, 2024

The objective of this study was to examine the in vitro metabolic stability of panobinostat in different matrices and assess the influence of that metabolic stability on the in vivo pharmacokinetics and CNS delivery of panobinostat.

Metabolic Stability

Metabolic Stability Pharmacokinetics Pharmacogenetics Treatment

An Integrative Approach to Elucidate Mechanisms Underlying the Pharmacokinetic Goldenseal-Midazolam Interaction: Application of In Vitro Assays and Physiologically Based Pharmacokinetic Models to Understand Clinical Observations [Metabolism, Transport, and Pharmacogenetics]

ASPET

AUGUST 4, 2023

The objective of this study was to mechanistically assess the pharmacokinetic goldenseal-midazolam interaction using an integrated in vitro - in vivo - in silico approach. min -1 , respectively). The objective of the current work was to evaluate fundamental mechanisms underlying the clinically observed goldenseal-midazolam interaction.

Pharmacokinetics

Pharmacokinetics Pharmacogenetics Production Drugs

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Chemical Biology and Drug Design

Preclinical systemic pharmacokinetics, dose-proportionality, and CNS distribution of the ATM inhibitor WSD0628, a novel radiosensitizer for the treatment of brain tumors [Metabolism, Transport, and Pharmacogenetics]

ASPET

JUNE 10, 2024

The objective of this study was to evaluate the systemic pharmacokinetics and mechanisms that influence the CNS distribution of WSD0628, a novel and potent ATM inhibitor, in the mouse. Thus, WSD0628 has favorable pharmacokinetic properties and potential for further exploration to determine the PK-PD-efficacy relationship in CNS tumors.

Pharmacokinetics

Pharmacokinetics Pharmacogenetics Treatment DNA

Lenacapavir Exhibits Atropisomerism - Mechanistic Pharmacokinetics and Disposition Studies of Lenacapavir Reveal Intestinal Excretion as a Major Clearance Pathway [Metabolism, Transport, and Pharmacogenetics]

ASPET

AUGUST 8, 2024

Lenacapavir (LEN), a long-acting injectable, is the first approved human immunodeficiency virus type 1 capsid inhibitor and one of a few FDA-approved drugs that exhibit atropisomerism.

Pharmacogenetics

Pharmacogenetics Pharmacokinetics FDA Approval Virus

Dysregulation of Human Hepatic Drug Transporters by Proinflammatory Cytokines [Metabolism, Transport, and Pharmacogenetics]

ASPET

AUGUST 5, 2024

The data obtained can be used in the future to predict transporter-mediated drug clearance changes during inflammation through physiologically-based pharmacokinetic modeling and simulation.

Pharmacogenetics

Pharmacogenetics Pharmacokinetics Drugs

Central Nervous System Distributional Kinetics of Selected Histone Deacetylase Inhibitors [Metabolism, Transport, and Pharmacogenetics]

ASPET

APRIL 26, 2024

In this study, we investigated the systemic pharmacokinetics and subsequent CNS distribution of two potent HDACIs, vorinostat and quisinostat, in the murine model. Although many HDACIs have shown potential in in vitro studies, they have had modest efficacy in vivo.

Pharmacogenetics

Pharmacogenetics Pharmacokinetics Clinical Trials Trials

Factors influencing the Central Nervous System (CNS) distribution of the ATR inhibitor elimusertib (BAY1895344): Implications for the treatment of CNS tumors [Metabolism, Transport, and Pharmacogenetics]

ASPET

SEPTEMBER 16, 2024

Acknowledging the potential for inter-species differences in pharmacokinetics, these data suggest that clinical translation of elimusertib in combination with temozolomide for treatment of GBM may be limited.

Pharmacogenetics

Pharmacogenetics DNA Treatment Pharmacokinetics

A Pilot Study to Assess the Suitability of Riboflavin as A Surrogate Marker of Breast Cancer Resistance Protein (BCRP) in Healthy Participants [Metabolism, Transport, and Pharmacogenetics]

ASPET

JANUARY 31, 2024

The effects of BMS-986371, a potent in vitro inhibitor of BCRP ( IC 50 0.40 µM), on the pharmacokinetics of riboflavin, isobutyryl carnitine, and arginine were then examined in healthy male adults (N = 14 or 16) following oral administration of methotrexate (MTX) (7.5

Pharmacogenetics

Pharmacogenetics Pharmacokinetics Drug Development Drugs

Significance of organic anion transporter 2 and organic cation transporter 2 in creatinine clearance: Mechanistic evaluation using freshly-prepared human primary renal proximal tubule cells [Metabolism, Transport, and Pharmacogenetics]

ASPET

NOVEMBER 17, 2023

Quantitative pharmacokinetic models should therefore focus on OCT2/MATE when describing serum creatinine and creatinine clearance modulation by inhibitor drugs and genotype- or disease-related activity changes.

Pharmacogenetics

Pharmacogenetics Pharmacokinetics Disease Drugs

Drug Discovery Digest

Pharmacokinetics of panobinostat: Inter-species difference in metabolic stability [Metabolism, Transport, and Pharmacogenetics]

An Integrative Approach to Elucidate Mechanisms Underlying the Pharmacokinetic Goldenseal-Midazolam Interaction: Application of In Vitro Assays and Physiologically Based Pharmacokinetic Models to Understand Clinical Observations [Metabolism, Transport, and Pharmacogenetics]

Trending Sources

Preclinical systemic pharmacokinetics, dose-proportionality, and CNS distribution of the ATM inhibitor WSD0628, a novel radiosensitizer for the treatment of brain tumors [Metabolism, Transport, and Pharmacogenetics]

Lenacapavir Exhibits Atropisomerism - Mechanistic Pharmacokinetics and Disposition Studies of Lenacapavir Reveal Intestinal Excretion as a Major Clearance Pathway [Metabolism, Transport, and Pharmacogenetics]

Dysregulation of Human Hepatic Drug Transporters by Proinflammatory Cytokines [Metabolism, Transport, and Pharmacogenetics]

Central Nervous System Distributional Kinetics of Selected Histone Deacetylase Inhibitors [Metabolism, Transport, and Pharmacogenetics]

Factors influencing the Central Nervous System (CNS) distribution of the ATR inhibitor elimusertib (BAY1895344): Implications for the treatment of CNS tumors [Metabolism, Transport, and Pharmacogenetics]

A Pilot Study to Assess the Suitability of Riboflavin as A Surrogate Marker of Breast Cancer Resistance Protein (BCRP) in Healthy Participants [Metabolism, Transport, and Pharmacogenetics]

Significance of organic anion transporter 2 and organic cation transporter 2 in creatinine clearance: Mechanistic evaluation using freshly-prepared human primary renal proximal tubule cells [Metabolism, Transport, and Pharmacogenetics]

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