Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis

…, Y Ko, I Choi, R Kim, SY Kim, SB Lim, SA Yim, J Nam… - Nature medicine, 2013 - nature.com
New therapeutic strategies are needed to combat the tuberculosis pandemic and the spread
of multidrug-resistant (MDR) and extensively drug-resistant (XDR) forms of the disease, …

Lead Optimization of a Novel Series of Imidazo[1,2-a]pyridine Amides Leading to a Clinical Candidate (Q203) as a Multi- and Extensively-Drug-Resistant Anti …

…, JJ Seo, Y Ko, I Choi, J Jang, J Nam… - Journal of medicinal …, 2014 - ACS Publications
A critical unmet clinical need to combat the global tuberculosis epidemic is the development
of potent agents capable of reducing the time of multi-drug-resistant (MDR) and extensively-…

[HTML][HTML] Telacebec (Q203), a new antituberculosis agent

…, L van der Merwe, J Choi, K Nam… - … England Journal of …, 2020 - Mass Medical Soc
Telacebec (Q203), a New Antituberculosis Agent Telacebec (Q203) is a novel drug that
targets Mycobacterium tuberculosis cellular energy production through inhibition of the …

Glucocorticoid receptor antagonism by cyproterone acetate and RU486

C Honer, K Nam, C Fink, P Marshall, G Ksander… - Molecular …, 2003 - ASPET
The steroid compound cyproterone acetate was identified in a high-throughput screen for
glucocorticoid receptor (GR) binding compounds. Cyproterone (Schering AG) is clinically used …

Safety, tolerability, and pharmacokinetics of telacebec (Q203), a new antituberculosis agent, in healthy subjects

…, D Park, J Kim, Y Jeon, K Nam… - Antimicrobial Agents …, 2022 - Am Soc Microbiol
Telacebec (Q203) is a potent drug candidate under clinical development for the treatment of
drug-naïve and drug-resistant tuberculosis. The first-in-human randomized, placebo-…

Synthesis and structure-activity studies of side chain analogues of the anti-tubercular agent, Q203

S Kang, YM Kim, RY Kim, MJ Seo, Z No, K Nam… - European journal of …, 2017 - Elsevier
The anti-tubercular activity of 6-chloro-2-ethyl-N-(4-(4-(4-(trifluoromethoxy)phenyl)piperidin-1-yl)benzyl)imidazo
[1,2-a]pyridine-3-carboxamide (Q203) is modified by varying its side …

Safety, tolerability, pharmacokinetics, and metabolism of telacebec (Q203) for the treatment of tuberculosis: a randomized, placebo-controlled, multiple ascending …

…, C Niekerk, J Kim, Y Jeon, K Nam… - Antimicrobial Agents …, 2023 - Am Soc Microbiol
A phase 1b, randomized, placebo-controlled, double-blind, multiple ascending dose study (NCT02858973)
was conducted to assess the safety, tolerability, and pharmacokinetics of the …

Synthesis and structure-activity relationships of novel fused ring analogues of Q203 as antitubercular agents

…, MJ Seo, S Lee, D Park, J Nam, S Lee, K Nam… - European journal of …, 2017 - Elsevier
A set of fused ring analogues of a new antitubercular agent, Q203, was designed and
synthesized. To reduce the lipophilicity of Q203 caused by linearly extended side chains, shorter …

QSAR models for predicting the similarity in binding profiles for pairs of protein kinases and the variation of models between experimental data sets

RP Sheridan, K Nam, VN Maiorov… - Journal of chemical …, 2009 - ACS Publications
We propose a direct QSAR methodology to predict how similar the inhibitor-binding profiles
of two protein kinases are likely to be, based on the properties of the residues surrounding …

[HTML][HTML] A novel selective Axl/Mer/CSF1R kinase inhibitor as a cancer immunotherapeutic agent targeting both immune and tumor cells in the tumor microenvironment

…, H Kang, Y Yang, D Park, B Choi, J Kim, J Kim, K Nam - Cancers, 2022 - mdpi.com
Simple Summary Immune checkpoint blockade has had great success over the past decade,
but many patients with cancer do not benefit because most immune checkpoint inhibitors …