Preparation and Evaluation of Progesterone Nanocrystals to Decrease Muscle Irritation and Improve Bioavailability.

Preparation and Evaluation of Progesterone Nanocrystals to Decrease Muscle Irritation and Improve Bioavailability.

Authors: Li L, Li W, Sun J, Zhang H, Gao J, Guo F, Yang X, Zhang X, Li Y, Zheng A
Publication: AAPS PharmSciTech
Keywords: absorption, formulations, nanoparticles, pkplus
Software: GastroPlus®

Progesterone (PG) is a crucial immunomodulatory agent during early pregnancy, and nowadays PG oil-based injection (PG/OI) has a huge market all over the world.

Model-informed drug development for malaria therapeutics

Model-informed drug development for malaria therapeutics

Authors: Andrews KA, Wesche D, McCarthy J, Möhrle JJ, Tarning J, Phillips L, Kern S, Grasela TH
Publication: Annu Rev Pharmacol Toxicol
Keywords: controlled human malaria infection, disease-drug model, malaria, model-informed drug development, pharmacodynamics, pharmacokinetics
Division: Clinical Pharmacology and Pharmacometrics (CPP)

Malaria is a critical public health problem resulting in substantial morbidity and mortality, particularly in developing countries. Owing to the development of resistance toward current therapies, novel approaches to accelerate...

Developing a mechanistic absorption model to predict the pharmacokinetics of immediate-release weak base drugs with a long Tmax by incorporating lysosomal trapping.

Developing a mechanistic absorption model to predict the pharmacokinetics of immediate-release weak base drugs with a long Tmax by incorporating lysosomal trapping.

Authors: Li J, Dong Z, Wu F, Zhao P, Lee SC, Seo P, Zhang L
Publication: Drug Metab Pharmacokinet
Keywords: delayed absorption, enterocytes, lysosomal trapping, PBPK
Software: GastroPlus®

The objectives of this study were 1) to develop and verify mechanistic absorption models to predict the pharmacokinetics (PK) of two immediate-release weak base drug (WBD) products (Drug X and Drug Y) with a...

In Vitro Dissolution Methodology And Estimated Consequences Of Biowaiver Extension For Immediate Release Solid Oral Dosage Forms With Metformin Hydrochloride

In Vitro Dissolution Methodology And Estimated Consequences Of Biowaiver Extension For Immediate Release Solid Oral Dosage Forms With Metformin Hydrochloride

Authors: Ardelean M, Stoicescu SM, Stanescu AA, Lupuliasa D, StăNicioiu DM, Radulescu FS, Miron DS
Publication: Farmacia
Keywords: absorption modeling, dissolution method, dissolution specifications, PBPK modeling
Software: GastroPlus®

The in vitro dissolution methodologies are frequently used as quality control tools for the assessment of solid oral dosage forms.

Physiologically Based Oral Absorption Modelling to Study Gut-Level Drug Interactions

Physiologically Based Oral Absorption Modelling to Study Gut-Level Drug Interactions

Authors: Chung J, Kesisoglou F
Publication: J Pharm Sci
Keywords: ACAT, cytochrome P450, drug interactions, food interactions, gastrointestinal transit, gi tract, in silico modeling, intestinal metabolism, mechanistic oral absorption, oral drug delivery, PBPK, transporters
Software: GastroPlus®

Physiologically based oral absorption models are in silico tools primarily used to guide formulation development and project the clinical performance of formulation variants.

The Combination of GIS and Biphasic to Better Predict In Vivo Dissolution of BCS Class IIb Drugs, Ketoconazole and Raloxifene

The Combination of GIS and Biphasic to Better Predict In Vivo Dissolution of BCS Class IIb Drugs, Ketoconazole and Raloxifene

Authors: Tsume Y, Igawa N, Drelich AJ, Amidon GE, Amidon GL
Publication: J Pharm Sci
Keywords: absorption modeling, ASD, BCS class II drug, biorelevant dissolution, gastrointestinal simulator, GIS, in vivo performance, ketoconazole, PBPK, raloxifene, simulation
Software: GastroPlus®

The formulation developments and the in vivo assessment of Biopharmaceutical Classification System (BCS) class II drugs are challenging due to their low solubility and high permeability in the...

Synaptophysin expression on circulating tumor cells in patients with castration resistant prostate cancer undergoing treatment with abiraterone acetate or enzalutamide

Synaptophysin expression on circulating tumor cells in patients with castration resistant prostate cancer undergoing treatment with abiraterone acetate or enzalutamide

Authors: Pal SK, He M, Chen L, Yang L, Pillai R, Twardowski P, Hsu J, Kortylewski M, Jones JO
Publication: Urol Oncol
Keywords: abiraterone, androgen receptor, Circulating tumor cell, enzalutamide, prostate cancer, Synaptophysin

Background: With the advent of secondary androgen receptor (AR)-targeted therapies in metastatic castration resistant prostate cancer (PC), nonadenocarcinoma PCs are...

Identification of mechanisms of resistance to treatment with abiraterone acetate or enzalutamide in patients with castration-resistant prostate cancer (CRPC)

Identification of mechanisms of resistance to treatment with abiraterone acetate or enzalutamide in patients with castration-resistant prostate cancer (CRPC)

Authors: Pal SK, Patel J, He M, Foulk B, Kraft K, Smirnov DA, Twardowski P, Kortylewski M, Bhargava V, Jones JO
Publication: Cancer
Keywords: androgen receptor, circulating tumor cells, RNA sequencing, targeted therapies

Background: Two androgen receptor (AR)-targeted therapies, enzalutamide and abiraterone acetate plus prednisone (abiraterone), have been approved for the treatment...

IVIVC using in silico and PBPK methods for inhaled drug product development

IVIVC using in silico and PBPK methods for inhaled drug product development

Authors: Lukacova V, Woltosz WS, Patterson B
Conference: DDL
Keywords: drug development, in silico, in vitro-in vivo correlation (IVIVC), inhaled, lung deposition, PBPK, pulmonary playlist
Software: GastroPlus®
Division: PBPK

The physiologically based model of the lung included in GastroPlus™ was used to simulate the absorption, distribution, and pharmacokinetics of two APIs from an inhaled combination product.

2017 White Paper: rise of hybrid LBA/LCMS immunogenicity assays (Part 2: hybrid LBA/LCMS biotherapeutics, biomarkers & immunogenicity assays and regulatory agencies’ inputs)

2017 White Paper: rise of hybrid LBA/LCMS immunogenicity assays (Part 2: hybrid LBA/LCMS biotherapeutics, biomarkers & immunogenicity assays and regulatory agencies’ inputs)

Authors: Neubert H, Song A, Lee A, Wei C, Duggan J, Xu K, Woolf E, Evans C, Palandra J, Laterza O, Amur S, Berger I, Bustard M, Cancilla M, Chen SC, Cho SJ, Ciccimaro E, Cludts I, Cocea L, D’Arienzo C, Danan-Leon L, Donato LD, Garofolo F, Haidar S, Ishii-Watabe A, Jiang H, Kadavil J, Kassim S, Kurki P, Blaye OL, Liu K, Mathews R, Santos GML, Niwa M, Pedras-Vasconcelos J, Qian M, Rago B, Saad O, Saito Y, Savoie N, Su D, Szapacs M, Tampal N, Vinter S, Wang J, Welink J, Whale E, Wilson A, Xue YJ
Publication: Bioanalysis
Keywords: bioanalysis, biotherapeutics, immunogenicity assays, LCMS, Workshop on Recent Issues in Bioanalysis (WRIB)
Division: Cheminformatics

The 2017 11th Workshop on Recent Issues in Bioanalysis (11th WRIB) took place in Los Angeles/Universal City, California on 3-7 April 2017 with participation of close to 750 professionals from pharmaceutical/biopharmaceutical companies, biotechnology companies, contract research organizations and regulatory agencies worldwide.

Refining Liver Safety Risk Assessment: Application of Mechanistic Modeling and Serum Biomarkers to Cimaglermin Alfa (GGF2) Clinical Trials

Refining Liver Safety Risk Assessment: Application of Mechanistic Modeling and Serum Biomarkers to Cimaglermin Alfa (GGF2) Clinical Trials

Authors: Longo DM, Generaux GT, Howell BA, Siler SQ, Antoine DJ, Button D, Caggiano A, Eisen A, Iaci J, Stanulis R, Parry T, Mosedale M, Watkins PB
Publication: Clin Pharmacol Ther
Keywords: clinical trials, heart failure, hepatocytes, humans, protein growth, safety risk assessment, United States Food and Drug Administration
Software: DILIsym®
Division: Quantitative Systems Pharmacology (QSP)

Cimaglermin alfa (GGF2) is a recombinant human protein growth factor in development for heart failure.