A decade of FDA-approved drugs (2010–2019): trends and future directions

DG Brown, HJ Wobst - Journal of medicinal chemistry, 2021 - ACS Publications
A total of 378 novel drugs and 27 biosimilars approved by the US Food and Drug
Administration (FDA) between 2010 and 2019 were evaluated according to approval …

The time and place for nature in drug discovery

RJ Young, SL Flitsch, M Grigalunas, PD Leeson… - Jacs Au, 2022 - ACS Publications
The case for a renewed focus on Nature in drug discovery is reviewed; not in terms of
natural product screening, but how and why biomimetic molecules, especially those …

[HTML][HTML] Trends in amorphous solid dispersion drug products approved by the US Food and Drug Administration between 2012 and 2023

DE Moseson, TB Tran, B Karunakaran… - International journal of …, 2024 - Elsevier
Abstract Forty-eight (48) drug products (DPs) containing amorphous solid dispersions
(ASDs) have been approved by the US Food and Drug Administration in the 12-year period …

Trends in molecular properties, bioavailability, and permeability across the bayer compound collection: miniperspective

DH O'Donovan, C De Fusco, L Kuhnke… - Journal of medicinal …, 2023 - ACS Publications
For oral drugs, medicinal chemists aim to design compounds with high oral bioavailability, of
which permeability is a key determinant. Taking advantage of> 2000 compounds tested in …

Property-based drug design merits a Nobel prize

LD Pennington, MJ Hesse, DC Koester… - Journal of Medicinal …, 2024 - ACS Publications
Drug design is central to the discovery of a new medicine, as the drug molecule embodies
the therapeutic hypothesis of a drug discovery program and encodes the properties …

Peptidomimetic α-acyloxymethylketone warheads with six-membered lactam P1 glutamine mimic: SARS-CoV-2 3CL protease inhibition, coronavirus antiviral activity …

B Bai, A Belovodskiy, M Hena… - Journal of Medicinal …, 2021 - ACS Publications
Recurring coronavirus outbreaks, such as the current COVID-19 pandemic, establish a
necessity to develop direct-acting antivirals that can be readily administered and are active …

Trends in small molecule drug properties: A developability molecule assessment perspective

P Agarwal, J Huckle, J Newman, DL Reid - Drug discovery today, 2022 - Elsevier
Developability molecule assessment is a key interfacial capability across the
biopharmaceutical industry, screening and staging molecules discovered by medicinal …

[HTML][HTML] Trends in oral small-molecule drug discovery and product development based on product launches before and after the Rule of Five

S Stegemann, C Moreton, S Svanbäck, K Box… - Drug Discovery …, 2023 - Elsevier
Highlights•Orally delivered drug products gradually continue to exceed the Rule-of-five on
Molecular Weight and clogP.•New predictive descriptors and tools, advanced chemistry and …

Challenges of peptide and protein drug delivery by oral route: Current strategies to improve the bioavailability

S Verma, UK Goand, A Husain… - Drug development …, 2021 - Wiley Online Library
Advancement in biotechnology provided a notable expansion of peptide and protein
therapeutics, used as antigens, vaccines, hormones. It has a prodigious potential to treat a …

Target-based evaluation of “drug-like” properties and ligand efficiencies

PD Leeson, AP Bento, A Gaulton… - Journal of Medicinal …, 2021 - ACS Publications
Physicochemical descriptors commonly used to define “drug-likeness” and ligand efficiency
measures are assessed for their ability to differentiate marketed drugs from compounds …