Chemical Biology and Drug Design

SEPTEMBER 20, 2023

The pharmacokinetic study was performed on male Sprague–Dawley rats randomly grouped as the single administration of luteolin and the co-administration of luteolin and magnoflorine with six rats of each. Luteolin was co-administrated with magnoflorine to evaluate their potential interaction.

Pharmacokinetics 100

Pharmacokinetics Metabolic Stability Regulations Research 100

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 100

Pharmacokinetics Pharmacogenetics Production Drugs 100

Chemical Biology and Drug Design

JANUARY 25, 2025

Compounds 4 , 5 , 9 11 displayed a remarkable EGFR-TK invitro inhibitory activity, induced apoptosis in NCI-H522 cell line, and showed predicted ADME pharmacokinetic profile. They showed a remarkable invitro EGFR inhibitory activity that was comparable to erlotinib, and a predicted ADME pharmacokinetic profile.

Pharmacokinetics 100

Pharmacokinetics Trials Research 100

Chemical Biology and Drug Design

JUNE 11, 2025

The host-guest interactions of quinolinequinones were also studied in detail using thorough in silico docking simulations with pharmacokinetic studies. QQ1 inhibited ACHN cell proliferation via cell cycle arrest.

Pharmacokinetics 100

Pharmacokinetics Research 100

ASPET

MAY 22, 2024

Yet, the absence of established systemic and brain pharmacokinetic (PK) parameters at relevant pre-clinical doses presents a significant knowledge gap. Our findings emphasize the importance of metformin dose selection based on pharmacokinetic parameters for pre-clinical pharmacological studies.

Pharmacokinetics 100

Pharmacokinetics Metabolic Stability Clinical Pharmacology Disease 100

Chemical Biology and Drug Design

FEBRUARY 6, 2025

In general, existence of sp 3 -O slightly outperforms sp 2 -O, which is associated with balancing various factors such as flexibility, solubility, stability, and pharmacokinetics, in addition to activity and selectivity. The analysis focuses on various types of oxygen atoms, including sp 3 , sp 2 -hybridized, ring, and nonring.

FDA Approval 100

FDA Approval FDA Small Molecule Pharmacokinetics 100

Chemical Biology and Drug Design

JUNE 8, 2023

The co-administration of cryptotanshinone with ophiopogonin D induced pharmacokinetic interaction prolonging the systemic exposure and improving metabolic stability of cryptotanshinone. Abstract Cryptotanshinone and ophiopogonin D are sourced from herbs with similar indications.

Pharmacokinetics 100

Pharmacokinetics Metabolic Stability Research 100

Drug Target Review

DECEMBER 4, 2024

What are the primary considerations in optimising the pharmacokinetics (PK) and biodistribution of MC4R-specific nanobodies in preclinical obesity models, and how does Confo Therapeutics plan to address challenges related to blood-brain barrier penetration?

Small Molecule 122

Small Molecule Pharmacokinetics Therapies Immune Response 122

Chemical Biology and Drug Design

MARCH 14, 2025

Drug-membrane interactions can affect the apparent binding stoichiometry and affinity, as well as the kinetics of ligands for a particular target, which is important for the extrapolation to pharmacokinetic studies.

Fragment Screening 100

Fragment Screening Pharmacokinetics Drugs Marketing 100

Chemical Biology and Drug Design

DECEMBER 5, 2024

The synthesized molecules were assessed for their pharmacological potential via cell viability, drug metabolism and pharmacokinetics (DMPK), and MERTK inhibition studies corroborated by in silico studies. The molecules were synthesized via a multi-step synthetic approach.

Immune Response 100

Immune Response Pharmacokinetics Regulations Treatment 100

Molecular Design

MARCH 31, 2019

Controllability of exposure is the focus of pharmacokinetic optimization and I recently became aware of an exciting new development that will surely reshape the pharmacokinetic field and transform drug discovery beyond all recognition.

Pharmacokinetics 52

Pharmacokinetics Treatment Drugs 52

ASPET

JULY 15, 2024

Mathematical modeling combining pharmacokinetics (PK) and toxicodynamics (TD) is a promising approach for optimizing dosing strategies and reducing toxicity. XELOX therapy, which comprises capecitabine and oxaliplatin, is the standard first-line chemotherapeutic regimen for colorectal cancer.

Pharmacokinetics 100

Pharmacokinetics Drugs Therapies Treatment 100

Alta Sciences

JANUARY 31, 2024

Pharmacokinetics, Pharmacodynamics and Toxicokinetics Demystified pmjackson Wed, 01/31/2024 - 14:55 Understanding the effects of a drug, and how it interacts with the body, and vice versa, is critical to ensure it is safe for human use. This is where pharmacokinetic (PK), pharmacodynamic (PD) , and toxicokinetic (TK) analyses step in.

Pharmacokinetics 52

Pharmacokinetics Clinical Trials Drug Development Trials 52

ASPET

MAY 22, 2024

In this review, we will examine what is currently known about CBC with regards to pharmacodynamics, pharmacokinetics, and receptor profile. While the cannabinoids share a common precursor molecule, cannabigerol, they are structurally and pharmacologically unique. These differences may engender differing therapeutic potentials.

Pharmacokinetics 185

Pharmacokinetics Disease Production Research 185

Covalent Modifiers

JANUARY 29, 2024

However, a majority of reported GPX4 inhibitors utilize chloroacetamide as a reactive electrophilic warhead, and the selectivity and pharmacokinetic properties still need to be improved. Thus, there is a broad interest in the development of GPX4 inhibitors.

Therapies 173

Therapies Pharmacokinetics Treatment 173

Covalent Modifiers

JUNE 5, 2023

Finally, in vivo pharmacokinetic studies indicated that the agent was long-lived and orally bioavailable. We also compared the cellular efficacy of the agent in two-dimensional (2D) and three-dimensional (3D) cell cultures, side by side with the clinical candidate reversible IAP inhibitor LCL161.

Pharmacokinetics 130

Pharmacokinetics 130

Broad Institute

JULY 17, 2024

Together, the tools estimate how a drug may impact diverse outcomes of interest to drug developers: general cellular health, pharmacokinetics, and heart and liver function. Drug developers also assess pharmacokinetic effects, or how an organism absorbs, distributes, metabolizes, and clears a drug.

Pharmacokinetics 124

Pharmacokinetics Molecular Biology Drugs FDA 124

Covalent Modifiers

MARCH 13, 2024

Performing structure-guided modifications of BPV, we developed a picomolar-affinity inhibitor, ML2006a4, with antiviral activity, oral pharmacokinetics, and therapeutic efficacy similar or superior to those of NTV.

Pharmacokinetics 162

Pharmacokinetics Virus Treatment Drugs 162

Alta Sciences

AUGUST 16, 2023

Microsampling for Pediatric Baricitinib Pharmacokinetics shajjar Wed, 08/16/2023 - 19:06 Publication bio-2023-0044_3.pdf pdf Tags Bioanalysis Category Journal Article Weight 1

Pharmacokinetics 40

Pharmacokinetics 40

Alta Sciences

AUGUST 22, 2023

34 — Toxicokinetics, Pharmacokinetics, and Pharmacodynamics mecabana Tue, 08/22/2023 - 17:31 Publication the-altascientist-issue-34-toxicokinetics-pharmacokinetics-and-pharmacodynamics.pdf URL [link] Weight 1 Tags Research Support

Pharmacokinetics 40

Pharmacokinetics Research 40

Alta Sciences

AUGUST 22, 2023

34 — TOXICOKINETICS, PHARMACOKINETICS, AND PHARMACODYNAMICS mecabana Tue, 08/22/2023 - 17:31 Publication the-altascientist-issue-34-toxicokinetics-pharmacokinetics-and-pharmacodynamics.pdf URL [link] Weight 1 Tags Manufacturing and Analytical Services

Pharmacokinetics 40

Pharmacokinetics 40

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 100

Pharmacogenetics Pharmacokinetics FDA Approval Virus 100

ASPET

SEPTEMBER 28, 2023

These protocols were then used to determine the plasma pharmacokinetics of agmatine and the extent of distribution to the CNS. Upon application of this protocol to pharmacokinetic study, IV agmatine showed a half-life in plasma ranging between 18.9 The protocol also adequately withstood stability and dilution conditions.

Pharmacokinetics 100

Pharmacokinetics FDA Therapies Drugs 100

Drug Target Review

MARCH 24, 2025

Promising areas for AI implementation When discussing the most transformative AI applications in drug discovery, Sujeegar identifies a particularly ambitious goal: developing AI models that can simulate human pharmacokinetics and pharmacodynamics (PK/PD) using only preliminary laboratory data.

Clinical Trials 59

Clinical Trials Animal Testing Drugs Pharmacokinetics 59

ASPET

JUNE 27, 2024

Furthermore, we evaluated the in vivo pharmacokinetics of the analogs following single dose IV and oral administration. Surprisingly, and at odds with their pharmacokinetic and in vitro human activity data, most analogs potently induced uterotrophic effects in estrogen-naïve female mice.

Pharmacokinetics 100

Pharmacokinetics Drug Development Disease Drugs 100

Drug Patent Watch

DECEMBER 10, 2024

The Importance of Scientific Expertise Generic drug development involves a deep understanding of the scientific principles underlying drug development, including pharmacology, pharmacokinetics, and bioequivalence. Scientific experts in these fields are critical in ensuring that generic drugs are developed to meet the required standards.

Drug Development 93

Drug Development Pharmacokinetics Compliance Drugs 93

Drug Target Review

APRIL 7, 2025

As pharmacological indicators, biomarkers overcome the static nature of traditional in vitro cellular studies by providing more dynamic models of pharmacokinetic processes that reflect active biological mechanisms. Trial design and statistical methods are also key to determining the utility and validity of biomarkers.

Clinical Development 69

Clinical Development Clinical Trials Clinical Pharmacology Trials 69

Drug Patent Watch

OCTOBER 30, 2023

Over the past two decades, Bayer Pharma has developed an in silico absorption, distribution, metabolism, and excretion (ADMET) platform with the aim of generating models for various pharmacokinetic and physicochemical… The post Advancements in In Silico ADMET Modeling: A 20-Year Journey of Machine Learning in Drug Discovery at Bayer Pharma appeared (..)

Pharmacokinetics 107

Pharmacokinetics Drugs 107

ASPET

SEPTEMBER 12, 2023

This first-in-human, randomized, double-blind, placebo-controlled study (NCT04497662) evaluated safety, pharmacokinetics, receptor occupancy, and pharmacodynamics of the humanized anti-CD40 monoclonal antibody KPL-404. Nonlinear dose-dependent changes in various pharmacokinetic parameters were identified following the range of IV doses.

Pharmacokinetics 100

Pharmacokinetics Immune Response Trials Clinical Trials 100

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 100

Pharmacogenetics Treatment DNA Pharmacokinetics 100

Common Sense for Drug Policy Blog

OCTOBER 29, 2024

The only studies reported in the FDA package inserts for both products are pharmacokinetic studies in healthy volunteers, which demonstrated substantially higher naloxone plasma levels than standard doses of naloxone (0.4 mg IM vs. 8 mg IN and 2 mg IM vs. 5 mg IM, respectively). In 2023, the FDA approved a 2.7

FDA Approval 52

FDA Approval Pharmacokinetics Packaging FDA 52

Drug Target Review

JUNE 6, 2025

And in the small molecule space, it’s about overcoming pharmacokinetic factors and formulation issues.” Greally explains that this iterative approach allows for more rigorous evaluation of ADC candidates, particularly in relation to pharmacokinetics and in vivo performance.

Small Molecule 52

Small Molecule Pharmacokinetics Packaging Drugs 52

ASPET

SEPTEMBER 7, 2023

The DDI covered in this review include pharmacokinetic DDI arising from enzyme inhibition or induction, primarily due to inhibition of cytochrome p450 enzymes (CYPs). This review focuses on the current knowledge of common opioid drug-drug interactions (DDI), focusing specifically on hydrocodone, oxycodone, and morphine DDI.

Pharmacokinetics 100

Pharmacokinetics Drugs Treatment Disease 100

ASPET

SEPTEMBER 16, 2024

PF-06952229 (MDV6058) selected using rational drug design is a potent and selective TGFβRI inhibitor (TGFβRIi) with a relatively clean off-target selectivity profile and good pharmacokinetic properties across species.

Pharmacokinetics 100

Pharmacokinetics Packaging Drugs 100

New Drug Approvals

JUNE 5, 2025

Gamcemetinib CAS 1887069-10-4 CC-99677 , OS2IR8TV1O Molecular Weight 469.94 nM) and cell based assays ( EC 50 =89 nM).

Cell Based Assays 52

Cell Based Assays Clinical Pharmacology Pharmacokinetics Trials 52

Drug Patent Watch

DECEMBER 30, 2024

Key Requirements for Generic Drug Approval Bioequivalence Studies : The PMDA requires bioequivalence studies to ensure that the generic drug is equivalent to the RLD in terms of its pharmacokinetic and pharmacodynamic properties.

Drug Development 52

Drug Development Clinical Pharmacology Clinical Trials Pharmaceutical Companies 52

SCIENMAG: Medicine & Health

NOVEMBER 1, 2023

A small clinical trial with a pharmacokinetic sub-study, led by a world-renowned pharmacologist at the University of Houston, has demonstrated the promising effectiveness of the drug Riluzole for improving functionality in people with acute spinal cord injuries (SCI) if the drug is taken within 12 hours post-injury.

Clinical Trials 86

Clinical Trials Trials Pharmacokinetics Drugs 86