The influence of lead discovery strategies on the properties of drug candidates

GM Keserü, GM Makara - nature reviews Drug Discovery, 2009 - nature.com
drug-like compounds have all contributed to the introduction of several novel alternative lead
… In this article, we consider HTS-based lead discovery to be HTS of large lead-like or drug-…

Requirements for a lead compound to become a clinical candidate

FF Hefti - BMC neuroscience, 2008 - Springer
… it relatively easy to identify initial lead candidates for new drug targets [1]. High … drug
candidate. Chemists at Pfizer developed the so-called rule of five for leads and drug candidates [2]. …

Strategy of utilizing in vitro and in vivo ADME tools for lead optimization and drug candidate selection

SK Balani, GT Miwa, LS Gan, JT Wu… - Current topics in …, 2005 - ingentaconnect.com
drug design. However, in vitro methods are certainly important to the understanding of the
specific factors contributing to drug … during drug discovery for lead optimization and candidate

Drug efficiency: a new concept to guide lead optimization programs towards the selection of better clinical candidates

S Braggio, D Montanari, T Rossi… - Expert Opinion on Drug …, 2010 - Taylor & Francis
… the best potential clinical candidate. We introduce the concept of drug efficiency as a new
tool both to guide the drug discovery program teams during the lead optimization phase and to …

Lead identification to clinical candidate selection: drugs for Chagas disease

RJ Neitz, S Chen, F Supek, V Yeh… - Journal of …, 2015 - journals.sagepub.com
… cruzi strains may respond differently to a chemotherapy, 19,20 we believe a druglead
series are also being evaluated, and we aim to define two or three preclinical candidates

Application of formulation technologies in lead candidate selection and optimization

MV Chaubal - Drug discovery today, 2004 - Elsevier
… A tosylate salt was identified as a promising candidate for further evaluation. This case study
provides an example of identification of a less common salt of an insoluble drug, leading to …

Strategies to optimize drug half-life in lead candidate identification

F Broccatelli, C ECA Hop, M Wright - Expert Opinion on Drug …, 2019 - Taylor & Francis
… engaged in drug design. Strategies to prolong the oral t 1/2 of a promising candidate drug
via … administration, which is often a key objective during hit-to-lead phases of drug discovery. …

Safety lead optimization and candidate identification: integrating new technologies into decision-making

DM Dambach, D Misner, M Brock… - Chemical research in …, 2016 - ACS Publications
… and progress the drug candidate with the best overall drug safety profile … drug candidate
with the best overall drug safety profile for a therapeutic area, [b] remove the severely toxic drugs

Privileged structures: a useful concept for the rational design of new lead drug candidates

CD Duarte, EJ Barreiro… - Mini reviews in medicinal …, 2007 - ingentaconnect.com
… in the research of new drugs and medicines redirected the … of obtaining new hits
candidate to drug prototypes, which … the physicochemical properties of drugs and lead-compounds …

Promising lead compounds in the development of potential clinical drug candidate for drug-resistant tuberculosis

S Alghamdi, SU Rehman, NT Shesha, H Faidah… - Molecules, 2020 - mdpi.com
drug substitute among available favorite drug candidates that … to find the potential drug
candidates and their precise … of antimicrobial peptides and the lead derivatives of coumarin, …