ASPET

SEPTEMBER 7, 2023

Awareness of drug interactions involving opioids is critical for patient treatment as they are common therapeutics used in numerous care settings including both chronic and disease related pain. Not only do opioids have narrow therapeutic indexes and are extensively used, but they have the potential to cause severe toxicity.

Pharmacokinetics 100

Pharmacokinetics Drugs Treatment Disease 100

Broad Institute

JULY 17, 2024

Still, more than 90 percent of drug candidates fail in clinical trials, with even more that never make it to the clinical stage. Many drugs fail because they simply aren’t safe. Seal began this work after wondering if more toxicology insights could be gleaned from a drug candidate’s chemical structure.

Pharmacokinetics 84

Pharmacokinetics Molecular Biology Drugs FDA 84

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

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. The volume of distribution was moderate in nonclinical species and consistent with the tissue distribution observed by whole body autoradiography in rats.

Pharmacogenetics 100

Pharmacogenetics Pharmacokinetics FDA Approval Virus 100

ASPET

SEPTEMBER 16, 2024

GBM has a poor prognosis despite aggressive treatment, in part due to lack of adequate drug permeability at the BBB. CNS distribution of elimusertib is partially limited by P-gp efflux at the BBB, and high binding to CNS tissues leads to low levels of pharmacologically active (unbound) drug in the brain.

Pharmacogenetics 100

Pharmacogenetics DNA Pharmacokinetics Treatment 100

ASPET

AUGUST 5, 2024

Proinflammatory cytokines, elevated during inflammation caused by infection and/or autoimmune disorders, result in reduced clearance of drugs eliminated primarily by cytochrome P450 enzymes (CYPs). However, the effect of cytokines on hepatic drug transporter expression or activity has not been well-studied. or 1 ng/mL).

Pharmacogenetics 100

Pharmacogenetics Pharmacokinetics Drugs 100

Alta Sciences

JUNE 24, 2023

Design and Validation of a Bioanalytical Method to Support a Clinical Pharmacokinetic Study Involving the Use of Multiple Lots of the Biological Therapeutic Drug lperez Sat, 06/24/2023 - 08:07 Publication Altasciences_WRIB_2023_Design_and_Validation_of_a_Bioanalytical_Method_to_Support_a_Clinical_Pharmacokinetic_Study.pdf Tags Bioanalysis Date of publication (..)

Pharmacokinetics 40

Pharmacokinetics Drugs 40

ASPET

AUGUST 21, 2024

ICH established S7B and E14 guidelines in 2005 to prevent drug-induced torsade de pointes (TdP), effectively preventing the development of high-risk drugs. However, those guidelines unfortunately hampered the development of some potentially valuable drug candidates despite not being proven to be proarrhythmic.

Compliance 100

Compliance Pharmacokinetics Drugs Engineering 100

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

ASPET

SEPTEMBER 28, 2023

These protocols were then used to determine the plasma pharmacokinetics of agmatine and the extent of distribution to the CNS. Precision and accuracy of the protocol met Food and Drug Administration (FDA) standards in surrogate matrix, as well as in corrected concentrations in appropriate matrices.

Pharmacokinetics 100

Pharmacokinetics FDA Therapies Drugs 100

ASPET

OCTOBER 24, 2023

The pharmacokinetic and pharmacodynamic properties of orally administered BBP-671 evaluated in cannulated rats showed that CoA concentrations were elevated in blood, liver and brain. Significance Statement The blood brain barrier represents a major hurdle for drugs targeting brain metabolism.

Metabolic Stability 100

Metabolic Stability Pharmacokinetics Regulations Treatment 100

DrugBank

OCTOBER 17, 2024

Data science has emerged as an innovative tool in the biopharmaceutical industry, leveraging the power of machine learning and artificial intelligence to drive innovation and efficiency across the entire drug development lifecycle.

Drug Development 63

Drug Development Metabolic Stability Clinical Trials Drugs 63

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 93

Pharmacokinetics Drugs 93

Alta Sciences

SEPTEMBER 27, 2024

Featuring two scenarios that explore the complexities of bioanalysis for immunomodulators, The Altascientist offers practical considerations for ensuring accurate bioanalysis, as well as pharmacokinetic, pharmacodynamic , and safety data in clinical trials. Each class of immunomodulator has a defined complexity and mechanism of action.

Clinical Trials 52

Clinical Trials Trials Pharmacokinetics Small Molecule 52

FDA Law Blog: Biosimilars

JULY 23, 2024

Lenz, Principal Medical Device Regulation Expert — For several years, FDA has requested that sponsors of drug or biologic led combination products identify essential performance requirements (EPRs) related to the device constituent in their applications. By Adrienne R. does not use this term.

FDA 105

FDA Drugs Pharmacokinetics Production 105

Drug Target Review

APRIL 22, 2024

What are the primary methods used for bioconjugation in antibody drug-conjugate (ADC) development, and how do they influence the stability and efficacy of the resulting ADCs? Despite excellent pharmacokinetic and stable antibody-linker connections, such ADCs have yet to receive market approval.

Pharmacokinetics 76

Pharmacokinetics Organic Chemistry Drugs Engineering 76

ASPET

JUNE 27, 2024

The primary endpoint was the peak effect (Emax) on a bipolar Drug Liking visual analog scale (VAS). Secondary VAS and pharmacokinetic (PK) endpoints and adverse events were assessed. Compared to placebo, a 20mg dose of lenabasum did not increase ratings of Drug Liking and had no distinguishable effect on other VAS endpoints.

Pharmacokinetics 100

Pharmacokinetics FDA Approval FDA Disease 100

Chemical Biology and Drug Design

MARCH 7, 2024

The physicochemical, pharmacokinetic, drug-like, and drug-score features of all synthesized compounds were assessed using the online Swiss ADME and Protein Plus software. All of them met Lipinski's rule of five and had drug-likeness and drug score values of 0.55 AutoDock 4.2 kJ/mol, respectively.

Pharmacokinetics 100

Pharmacokinetics Drugs Research 100

ASPET

JANUARY 22, 2024

Currently, drugs targeting NF-B inhibition have not yet been applied in clinical practice. The pharmacokinetics was measured by LC-MS/MS analysis. Nuclear factor-B (NF-B) plays a central role in inflammatory responses, while its physiological functions are essential for cell survival and proliferation.

Immune Response 100

Immune Response Pharmacokinetics Production Drugs 100

ASPET

MAY 4, 2023

Drug biliary clearance (CL bile ) in vivo is among the most difficult pharmacokinetic parameters to predict accurately and quantitatively because biliary excretion is influenced by metabolic enzymes, transporters, and passive diffusion across hepatocyte membranes.

Pharmacokinetics 100

Pharmacokinetics Drugs 100

Chemical Biology and Drug Design

JANUARY 29, 2024

In silico ADME prediction of these compounds revealed the good drug-likeness nature and followed Lipinski's rule of five. In-silico ADME studies significant values of pharmacokinetic parameters and demonstrated good drug like characteristics based on Lipinski's rule of five.

Pharmacokinetics 100

Pharmacokinetics Production Drugs Research 100

New Drug Approvals

OCTOBER 12, 2024

Clinical Pharmacokinetics and Safety of ALZ-801, a Novel Prodrug of Tramiprosate in Development for the Treatment of Alzheimer’s Disease. Clin Pharmacokinet. Discovery and Identification of an Endogenous Metabolite of Tramiprosate and Its Prodrug ALZ-801 that Inhibits Beta Amyloid Oligomer Formation in the Human Brain.

Pharmacokinetics 62

Pharmacokinetics Small Molecule Disease Licensing 62

biobide

SEPTEMBER 29, 2023

Within the field of Drug Discovery and Development the term “ New Alternative Methodologies ” (NAMs) refers to the use of new and innovative testing methods that come to replace traditional animal models. The use of in silico models allows the fastening of the first steps of Drug Discovery, representing an immense advance in the field.

Animal Testing 106

Animal Testing Drugs Pharmacokinetics Regulations 106

The Premier Consulting Blog

AUGUST 8, 2024

On July 31, 2024, the US Food and Drug Administration (FDA) announced Fiscal Year 2025 (FY2025) Prescription Drug User Fee Amendments of 2022 (PDUFA VII) fee rates for the review of human drug and biological product applications along with prescription drug program fees.

Pharmacokinetics 52

Pharmacokinetics Drugs FDA Production 52

Chemical Biology and Drug Design

MARCH 5, 2024

The outcomes of the tested compounds 5d , 5e , and 5f have shown more potent activity when compared to the standard drug erlotinib. The potent compounds 5d , 5e , and 5f were subjected to in silico pharmacokinetic assessment by SWISS, ADME, and pkCSM.

Pharmacokinetics 100

Pharmacokinetics Drugs Research 100

ASPET

APRIL 26, 2024

This lack of activity could be due to insufficient CNS exposure to the unbound drug. In this study, we investigated the systemic pharmacokinetics and subsequent CNS distribution of two potent HDACIs, vorinostat and quisinostat, in the murine model.

Pharmacogenetics 100

Pharmacogenetics Pharmacokinetics Clinical Trials Trials 100

ASPET

JANUARY 31, 2024

First, we assessed the substrate potential of riboflavin towards other major drug transporters using established transfected cell systems. Overall, these data indicate that plasma riboflavin is a promising biomarker of BCRP that may offer a possibility to assess drug candidate as a BCRP modulator in early drug development.

Pharmacogenetics 100

Pharmacogenetics Pharmacokinetics Drug Development Drugs 100

ASPET

JANUARY 22, 2024

Profiling NT-0796 in mice humanized with respect to CES-1 biology enables critical modeling of the pharmacokinetics and pharmacodynamics of this novel therapeutic candidate. Significance Statement Inhibition of NLRP3 represents a desirable therapeutic strategy for the treatment of multiple human disorders.

Pharmacokinetics 100

Pharmacokinetics DNA Engineering International 100

Covalent Modifiers

MARCH 13, 2024

Second-generation oral drugs that retain function against these mutants are thus urgently needed. We hypothesized that the covalent hepatitis C virus protease inhibitor boceprevir (BPV) could serve as the basis for orally bioavailable drugs that inhibit SARS-CoV-2 Mpro more efficiently than existing drugs.

Pharmacokinetics 64

Pharmacokinetics Virus Treatment Drugs 64

Alta Sciences

OCTOBER 15, 2024

Jason started his career as a research assistant carrying out operational phases of drug metabolism and pharmacokinetic studies. As my experience in preclinical research grew, so did my curiosity in the overall drug development process; I wanted to expand into clinical research. What Was your dream job as a child? jpg Weight 1

Pharmacokinetics 52

Pharmacokinetics Drug Development Clinical Trials Science 52

Chemical Biology and Drug Design

MARCH 6, 2024

Thus, polonilignan has been identified as a new pan-cytokine and NO inhibitor, it is recommended to optimise a method for the synthesis of this small molecular weight lignan and explore its pharmacokinetic characteristics, toxicity and therapeutic effect under various chronic inflammatory disease models.

Pharmacokinetics 100

Pharmacokinetics Regulations Production Disease 100

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 100

Pharmacogenetics Pharmacokinetics Disease Drugs 100

New Drug Approvals

SEPTEMBER 14, 2024

Zamaporvint displays a favorable pharmacokinetic profile and shows potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines. Zamaporvint targete membrane-bound o-acyltransferase Porcupine and inhibited Wnt ligand palmitoylation, secretion, and pathway activation.

Pharmacokinetics 57

Pharmacokinetics Research Drugs 57

Fierce BioTech

MAY 1, 2024

Join us on Monday, June 19, 2024 for one hour all about oral cyclic peptide drug development. With “specialized for peptide” drug metabolism and pharmacokinetics (DMPK) and biological evaluation, we’re able to solve certain synthesis issues found across different cyclic peptides, complexes peptides and mimetic peptides.

Pharmacokinetics 52

Pharmacokinetics Drug Development Drugs 52

Sygnature Discovery

JANUARY 26, 2024

Here at Sygnature Discovery, we offer specialised expertise in early-stage drug formulation. Working closely with our colleagues in Process Chemistry and Scale-Up, Drug Metabolism and Pharmacokinetics (DMPK), Pharmacology, and Separation Science, we can apply the right tools to solve the most complex challenges in your project.

Process Chemistry 52

Process Chemistry Pharmacokinetics Clinical Development Laboratories 52

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

Drug Target Review

DECEMBER 12, 2023

We use hydrophilic linkers, which prevent ADC aggregation and generate highly stable ADCs, in combination with a unique attachment site on the antibody to create ADCs that retain pharmacokinetic properties similar to the original unconjugated antibody. This helps to maximize the targeted payload delivery to tumor cells.

Treatment 115

Treatment Engineering Pharmacokinetics Doctors 115