Covalent Modifiers

NOVEMBER 22, 2024

4c01541 Covalent drugs provide pharmacodynamic and pharmacokinetic advantages over reversible agents. Among other nucleophilic residues that could be in principle used for the design of covalent drugs, histidine (His) has not been given proper attention despite being in principle an attractive residue to pursue but underexplored.

Pharmacokinetics 162

Pharmacokinetics Drugs 162

Drug Target Review

DECEMBER 4, 2024

G protein-coupled receptors (GPCRs) represent a cornerstone of modern drug discovery due to their crucial role in regulating human physiology and their involvement in numerous diseases. In the early days, each GPCR target required its own structure-modulating ConfoBody to be identified before starting any drug discovery.

Small Molecule 122

Small Molecule Pharmacokinetics Therapies Immune Response 122

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

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 100

Metabolic Stability Pharmacokinetics Pharmacogenetics Treatment 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

DECEMBER 5, 2024

A hybrid drug design approach was employed to develop novel leads ( 1K11K5 ). A hybrid drug design approach was employed by hybridization of pyrrolo[2,1- f ][1,2,4]triazine and 1-(methylpiperidin-4-yl)aniline pharmacophoric systems to develop novel leads ( 1K11K5 ). Studies were corroborated by in silico studies.

Immune Response 100

Immune Response Pharmacokinetics Regulations Treatment 100

Drug Target Review

MARCH 24, 2025

Sujeegar Jeevanandam, an expert with 13 years of experience in life sciences R&D, offers valuable insights into the current state and future trajectory of artificial intelligence in drug discovery. This breakthrough could fundamentally change how drugs are developed and tested.

Clinical Trials 59

Clinical Trials Animal Testing Drugs Pharmacokinetics 59

ASPET

JULY 15, 2024

Mathematical modeling combining pharmacokinetics (PK) and toxicodynamics (TD) is a promising approach for optimizing dosing strategies and reducing toxicity. In addition to dose determination, these data will lay the groundwork for advancing drug development processes in oncology.

Pharmacokinetics 100

Pharmacokinetics Therapies Drugs Treatment 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 124

Pharmacokinetics Molecular Biology Drugs FDA 124

Molecular Design

MARCH 31, 2019

Drug design is a multi-objective endeavor. Other objectives such as controllability of exposure are much less easily defined and this means that drug design is indirect. Some objectives such as maximization of affinity against target(s) and minimization of affinity against anti-targets are easily defined.

Pharmacokinetics 52

Pharmacokinetics Treatment Drugs 52

Drug Patent Watch

DECEMBER 30, 2024

The regulatory environment in Japan for generic drug development is complex and has undergone significant changes in recent years. Regulatory Authority: Pharmaceuticals and Medical Devices Agency (PMDA) The PMDA is the primary regulatory authority responsible for overseeing the drug approval process in Japan.

Drug Development 52

Drug Development Clinical Pharmacology Clinical Trials Pharmaceutical Companies 52

Drug Patent Watch

DECEMBER 10, 2024

Generic drug development is a complex process that involves not only scientific and medical expertise but also adherence to strict legal and ethical standards. Scientific expertise plays a crucial role in ensuring that generic drugs are held to the same standards of quality, safety, and efficacy as their brand-name counterparts.

Drug Development 96

Drug Development Pharmacokinetics Compliance Drugs 96

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

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

Drug Target Review

APRIL 7, 2025

In a recent survey conducted by ICON, Plc, biomarker selection was identified by 35 percent of respondents as a top challenge among drug developers for phase I trials, second only to navigating regulatory compliance (- 38 percent). To qualify as endpoints, biomarkers used in early phases must be relevant to later stages of drug development.

Clinical Development 69

Clinical Development Clinical Trials Clinical Pharmacology Trials 69

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 162

Pharmacokinetics Virus Treatment Drugs 162

Drug Patent Watch

DECEMBER 11, 2024

Generic drugs play a crucial role in providing affordable healthcare options to millions of patients worldwide. One of the key tools that generic drug manufacturers rely on to navigate the complex regulatory environment is the FDA’s Product Specific Guidances (PSGs). ” – Dr.

Drug Development 86

Drug Development Production FDA Drugs 86

Drug Target Review

JUNE 16, 2025

Unlike traditional pharmacokinetic (PK) studies that rely on plasma measurements alone, MSI, when combined with traditional histology, enables spatial mapping of drug distribution, metabolism and target engagement. Toxicological investigations play a key role in assessing drug safety and, importantly, inform development decisions.

Drugs 52

Drugs Organic Chemistry Laboratories Pharmaceuticals 52

Drug Target Review

JULY 7, 2025

Non-human primates (NHPs), such as macaques and cynomolgus monkeys, have long served as a cornerstone in preclinical drug development due to their close genetic, anatomical and physiological resemblance to humans. Conventional models often fail to predict cardiac side effects, especially with biologics.

Drug Research 52

Drug Research Research Animal Testing Drugs 52

New Drug Approvals

JULY 5, 2025

Oral Administration: Palazestrant is an orally available drug. Combination Therapy: Palazestrant is being evaluated in combination with other drugs like CDK4/6 inhibitors (e.g., Promising Results: Preliminary results from clinical trials have shown promising antitumor efficacy and favorable pharmacokinetic properties for palazestrant.

Small Molecule 62

Small Molecule Clinical Trials Pharmacokinetics FDA 62

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 110

Pharmacokinetics Drugs 110

Alta Sciences

FEBRUARY 19, 2025

Regulatory Guidance for Oligonucleotide Bioanalysis in Drug Development pmjackson Wed, 02/19/2025 - 21:30 The unique physicochemical properties of oligonucleotides require the use of specialized bioanalytical approaches, with key considerations including selectivity and specificity, sensitivity, stability, and matrix effects.

Drug Development 52

Drug Development Clinical Pharmacology Immune Response Drugs 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

DrugBank

SEPTEMBER 19, 2024

Oral drug delivery remains the gold standard in pharmaceutical administration. Compared to other routes, like injectables, oral drugs are cost-effective to manufacture and administer. However, translating a promising therapeutic candidate into a successful oral medication presents pharmacokinetic and pharmacodynamic challenges.

Drugs 98

Drugs Pharmacokinetics Treatment Disease 98

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

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

Drug Patent Watch

JANUARY 14, 2025

The Generic Drug Revolution: Setting the Stage Before we dive into the nitty-gritty, let’s take a moment to appreciate the impact of generic drugs. Did you know that generic drugs now make up about 90% of all prescription drug purchases in the United States, while accounting for only 20% of prescription drug spending[1]?

Drug Development 71

Drug Development Drugs FDA Production 71

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 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

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

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

Drug Target Review

JUNE 6, 2025

As antibody-drug conjugates (ADCs) gain traction across oncology and begin to expand into other therapeutic areas, a persistent challenge remains: the design and optimisation of payloads. And in the small molecule space, it’s about overcoming pharmacokinetic factors and formulation issues.”

Small Molecule 52

Small Molecule Pharmacokinetics Packaging Drugs 52

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 Treatment Pharmacokinetics 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 98

Drug Development Metabolic Stability Clinical Trials Drugs 98

Conversations in Drug Development Trends

JANUARY 21, 2025

Jayaprakash Kotha, MBBS, PhD, ASCP (SH), Vice President, Bioanalytical Laboratory Satish Kumar, MBB, Head of Process Improvement Continuous Innovation is a Cornerstone of Bioanalysis Approximately 80% of drugs that begin the research process fail to reach approval. Rigorous procedures to ensure that drugs are effective and safe.

Clinical Trials 78

Clinical Trials Laboratories Trials Drug Development 78

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

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