Journal ArticleDOI
Bridging solubility between drug discovery and development.
Li Di,Paul V. Fish,Takashi Mano +2 more
TLDR
A large number of compounds with low solubility have been developed in the past few years for use in drug discovery and drug development, and these include polymethine-like compounds, which have shown promise in the treatment of cancer.About:
This article is published in Drug Discovery Today.The article was published on 2012-05-01. It has received 362 citations till now. The article focuses on the topics: Drug development & Drug discovery.read more
Citations
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Journal ArticleDOI
Strategies to Address Low Drug Solubility in Discovery and Development
Hywel David Williams,Natalie L. Trevaskis,Susan A. Charman,Ravi Mysore Shanker,William N. Charman,Colin W. Pouton,Christopher J.H. Porter +6 more
TL;DR: The article provides an integrated and contemporary discussion of current approaches to solubility and dissolution enhancement but has been deliberately structured as a series of stand-alone sections to allow also directed access to a specific technology where required.
Journal ArticleDOI
The expanding role of prodrugs in contemporary drug design and development
TL;DR: This Review highlights prodrug design strategies for improved formulation and pharmacokinetic and targeting properties, with a focus on the most recently marketed prodrugs.
Journal ArticleDOI
Multifunctional polymeric micelles for delivery of drugs and siRNA
TL;DR: The purpose of this review is to highlight recent advances in the development of multifunctional polymeric micelles specifically for delivery of drugs and siRNA, as well as discuss the potential and suitability of multi-functional polymeric mouselles, including lipid-based micella, as promising vehicles for both siRNA and drugs.
Journal ArticleDOI
Structure–activity relationships for ruthenium and osmium anticancer agents – towards clinical development
Samuel M. Meier-Menches,Samuel M. Meier-Menches,Christopher Gerner,Walter Berger,Walter Berger,Christian G. Hartinger,Bernhard K. Keppler +6 more
TL;DR: Global structure-activity relationships are discussed for ruthenium and osmium metallodrugs with respect to in vitro antiproliferative/cytotoxic activity and in vivo tumor-inhibiting properties, as well as pharmacokinetics.
Journal ArticleDOI
Early pharmaceutical profiling to predict oral drug absorption: current status and unmet needs
Christel A. S. Bergström,René Holm,Søren Astrup Jørgensen,Sara B. E. Andersson,Per Artursson,Stefania Beato,Anders Borde,Karl J. Box,Marcus E. Brewster,Jennifer B. Dressman,Kung I. Feng,Gavin Halbert,Edmund Kostewicz,Mark McAllister,Uwe Muenster,Julian Thinnes,Robert Taylor,Anette Müllertz +17 more
TL;DR: In silico and in vitro models typically used to forecast active pharmaceutical ingredient's in vivo performance after oral administration and state-of-the art methodologies to study API properties impacting on oral absorption are reviewed.
References
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Journal ArticleDOI
Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
TL;DR: Experimental and computational approaches to estimate solubility and permeability in discovery and development settings are described in this article, where the rule of 5 is used to predict poor absorption or permeability when there are more than 5 H-bond donors, 10 Hbond acceptors, and the calculated Log P (CLogP) is greater than 5 (or MlogP > 415).
Journal ArticleDOI
A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability
TL;DR: A biopharmaceutics drug classification scheme for correlating in vitro drug product dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling rate and extent of drug absorption.
Journal ArticleDOI
Drug-like properties and the causes of poor solubility and poor permeability
TL;DR: There are currently about 10000 drug-like compounds, and true diversity does not exist in experimental combinatorial chemistry screening libraries because current ADME experimental screens are multi-mechanisms, and predictions get worse as more data accumulates.
Book
Encyclopedia of Pharmaceutical Technology
TL;DR: Compounding, Contemporary, andProcess Chemistry in the Pharmaceutical Industry: Characterization and Function, Volume 19.
Journal ArticleDOI
Physiological Parameters in Laboratory Animals and Humans
Brian E. Davies,Tim Morris +1 more