Identification of GDC-1971 (RLY-1971), a SHP2 inhibitor designed for the treatment of solid tumors

AM Taylor, BR Williams, F Giordanetto… - Journal of Medicinal …, 2023 - ACS Publications
Protein tyrosine phosphatase SHP2 mediates RAS-driven MAPK signaling and has
emerged in recent years as a target of interest in oncology, both for treating with a single …

Current approaches for predicting human PK for small molecule development candidates: findings from the IQ human PK prediction working group survey

C Petersson, X Zhou, J Berghausen, D Cebrian… - The AAPS journal, 2022 - Springer
Accurate prediction of human clearance (CL) and volume of distribution at steady state (Vd,
ss) for small molecule drug candidates is an essential component of assessing likely …

[HTML][HTML] Humans are animals, but are animals human enough? A systematic review and meta-analysis on interspecies differences in renal drug clearance

K Jansen, CP Casellas, L Groenink, KE Wever… - Drug Discovery …, 2020 - Elsevier
Highlights•Allometric scaling is suitable for prediction of human renal drug clearance
(CLr).•The average CLr of a diverse set of 20 drugs scales to the ¾ power of body mass.•Rat …

New approach methodologies (NAMs) for human-relevant biokinetics predictions: Meeting the paradigm shift in toxicology towards an animal-free chemical risk …

A Punt, H Bouwmeester, BJ Blaauboer, S Coecke… - Altex, 2020 - research.utwente.nl
For almost fifteen years, the availability and regulatory acceptance of new approach
methodologies (NAMs) to assess the absorption, distribution, metabolism and excretion …

Towards best use and regulatory acceptance of generic physiologically based kinetic (PBK) models for in vitro-to-in vivo extrapolation (IVIVE) in chemical risk …

A Najjar, A Punt, J Wambaugh, A Paini, C Ellison… - Archives of …, 2022 - Springer
With an increasing need to incorporate new approach methodologies (NAMs) in chemical
risk assessment and the concomitant need to phase out animal testing, the interpretation of …

Discovery of BIIB068: a selective, potent, reversible Bruton's tyrosine kinase inhibitor as an orally efficacious agent for autoimmune diseases

B Ma, T Bohnert, KL Otipoby, E Tien… - Journal of Medicinal …, 2020 - ACS Publications
Autoreactive B cell-derived antibodies form immune complexes that likely play a pathogenic
role in autoimmune diseases. In systemic lupus erythematosus (SLE), these antibodies bind …

Recent developments in in vitro and in vivo models for improved translation of preclinical pharmacokinetics and pharmacodynamics data

J Yadav, M El Hassani, J Sodhi… - Drug metabolism …, 2021 - Taylor & Francis
Improved pharmacokinetics/pharmacodynamics (PK/PD) prediction in the early stages of
drug development is essential to inform lead optimization strategies and reduce attrition …

Toxicokinetics and toxicodynamics of the fentanyl homologs cyclopropanoyl-1-benzyl-4-fluoro-4-anilinopiperidine and furanoyl-1-benzyl-4-anilinopiperidine

TM Gampfer, L Wagmann, YM Park, A Cannaert… - Archives of …, 2020 - Springer
The two fentanyl homologs cyclopropanoyl-1-benzyl-4´-fluoro-4-anilinopiperidine (4F-Cy-
BAP) and furanoyl-1-benzyl-4-anilinopiperidine (Fu-BAP) have recently been seized as new …

Antiparasitic effects of sulfated polysaccharides from marine hydrobionts

NN Besednova, TS Zaporozhets, BG Andryukov… - Marine Drugs, 2021 - mdpi.com
This review presents materials characterizing sulfated polysaccharides (SPS) of marine
hydrobionts (algae and invertebrates) as potential means for the prevention and treatment of …

Human risk assessment of 4-n-nonylphenol (4-n-NP) using physiologically based pharmacokinetic (PBPK) modeling: analysis of gender exposure differences and …

SH Jeong, JH Jang, HY Cho, YB Lee - Archives of Toxicology, 2022 - Springer
As a toxic substance, 4-n-nonylphenol (4-n-NP) or 4-nonylphenol (4-NP) is widely present in
the environment. 4-n-NP is a single substance with a linear-alkyl side chain, but 4-NP …