Pharmacokinetic/pharmacodynamic modeling of drug interactions at the P2Y12 receptor between selatogrel and oral P2Y12 antagonists

Pharmacokinetic/pharmacodynamic modeling of drug interactions at the P2Y12 receptor between selatogrel and oral P2Y12 antagonists

Authors: Henrich A, Claussen CH, Dingemanse J, Krause A
Publication: CPT Pharmacometrics Syst Pharmacol
Keywords: P2Y12 receptor antagonists, pharmacodynamics, pharmacokinetics (PK)

Selatogrel is a potent and reversible P2Y12 receptor antagonist developed for subcutaneous self‐administration by patients with suspected acute myocardial infarction.

Human-on-a-Chip combined with PBPK modeling for in vitro/in vivo PK/PD extrapolation

Human-on-a-Chip combined with PBPK modeling for in vitro/in vivo PK/PD extrapolation

Authors: Hickman J, Lukacova V
Keywords: drug-drug interactions (DDIs), gastroplus, Human-on-a-Chip (HoaC) systems, in vitro, PK prediction
Software: GastroPlus®
Division: PBPK

Human-on-a-Chip (HoaC) systems are becoming valuable tools to study, understand disease physiology, and expand the prediction of pharmacodynamic effects before first-in-human studies. They can also be used to evaluate the toxic effects of compounds in non-pharma industries where these effects cannot be examined in vivo.

Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis

Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis

Authors: Thomas M, Brand S, De Rycker M, Zuccotto F, Lukac I, Dodd PG, Ko EJ, Manthri S, McGonagle K, Osuna-Cabello M, Riley J, Pont C, Simeons F, Stojanovski L, Thomas J, Thompson S, Viayna E, Fiandor JM, Martin J, Wyatt PG, Miles TJ, Read KD, Marco M, Gilbert IH
Publication: J Med Chem
Keywords: admet predictor, aqueous solubility, drug design, drug discovery, gastroplus, machine learning
Software: GastroPlus®

There is an urgent need for new treatments for visceral leishmaniasis (VL), a parasitic infection which impacts heavily large areas of East Africa, Asia, and South America

Quantitative Systems Toxicology Modeling Using DILIsym Suggests That Drug-Induced Liver Injury (DILI) Can Be Enhanced by Co-administered Drugs and Mitigated by Mitochondrial Biogenesis

Quantitative Systems Toxicology Modeling Using DILIsym Suggests That Drug-Induced Liver Injury (DILI) Can Be Enhanced by Co-administered Drugs and Mitigated by Mitochondrial Biogenesis

Authors: Yang K
Conference: AASLD
Keywords: DILI, DILIsym, quantitative systems toxicology (QST) model, Toxicity
Software: DILIsym®
Division: Quantitative Systems Pharmacology (QSP)

Drug-induced liver injury (DILI) can be enhanced by polypharmacy if co-administered drugs induce toxicity via mechanisms that have overlapping pathways.

Assessing the Potential for Hepatotoxicity for Combination Therapy of Valproate (VPA) and CBDusing Quantitative Systems Toxicology (QST) DILIsym Correctly Predicts CBD ALT Elevations and Evaluates Interaction Mechanism(s)

Assessing the Potential for Hepatotoxicity for Combination Therapy of Valproate (VPA) and CBDusing Quantitative Systems Toxicology (QST) DILIsym Correctly Predicts CBD ALT Elevations and Evaluates Interaction Mechanism(s)

Authors: Lakhani VV
Conference: AASLD
Keywords: ALT, DILIsym, gastroplus, hepatotoxicity, metabolites, QST
Software: DILIsym®, GastroPlus®
Division: Quantitative Systems Pharmacology (QSP)

Epidiolex (highly purified CBD) is efficacious in treating seizures associated with Dravetsyndrome (DS), Lennox-Gastautsyndrome (LGS), and Tuberous Sclerosis Complex (TSC)