Results 51 to 60 of about 29,860 (191)

Semi‐Mechanistic Joint Population Pharmacokinetic Modeling of the Novel Antituberculosis Drug Sorfequiline and Its Metabolite M3 in Healthy Volunteers

CPT: Pharmacometrics &Systems Pharmacology, Volume 15, Issue 9, September 2026.
ABSTRACTSorfequiline is a novel diarylquinoline in development for treatment of tuberculosis. In vitro data suggest metabolism via CYP3A4, carrying the potential for presystemic metabolism and drug–drug interactions. Its major metabolite, M3, is pharmacologically active.
Jose M. Calderin, Jerry Nedelman, David H. Salinger, Thanakorn Vongjarudech, Paolo Denti, Elin M. Svensson   +5 more
wiley   +1 more source

Outcomes of Multidrug-Resistant Tuberculosis Treated With Bedaquiline or Delamanid

, 2021
Background. Since 1 September 2016, bedaquiline and delamanid have been administered for the treatment of patients with multidrug-resistant/rifampicin-resistant tuberculosis after the official approval in South Korea.
Hyungseok Kang, Jeon, Doosoo, Yong-Soo Kwon, Hwang, Hyeontaek, Shim, Tae Sun, Yim, Jae-Joon, 심태선, Doosoo Jeon, Jae-Joon Yim, Hyeontaek Hwang, Kang, Hyungseok, Kwon, Yong-Soo   +11 more
core   +1 more source

Emerging bedaquiline resistance: A threat to the global fight against drug-resistant tuberculosis

Journal of Biosafety and Biosecurity
Bedaquiline resistance is increasingly observed in the treatment of rifampicin-resistant tuberculosis (TB), yet standardized regimens for managing bedaquiline-resistant TB are lacking.
Prakasini Satapathy, Ramaiah Itumalla, Ahmad Neyazi, Abdul Mobin Nabizai Taraki, Mahalaqua Nazli Khatib, Shilpa Gaidhane, Quazi Syed Zahiruddin, Sarvesh Rustagi, Mehrab Neyazi   +8 more
doaj   +1 more source

Cardiac toxicity of fluoroquinolones and bedaquiline [PDF]

, 2019
The review analyzes data on the impact of fluoroquinolones and bedaquiline on the cardiac conduction system. The dependence of the cardiotoxic effect of fluoroquinolones on their influence on the potassium channels of cardiomyocytes is presented.
A. G. Sаmoylovа, G. N. Mozhokinа
core   +1 more source

A Review on Green Synthetic Approaches in the Development of Quinoline Analogues

ChemistrySelect, Volume 11, Issue 33, 1 September 2026.
This review highlights recent advances in environmentally friendly approaches, including metal‐free systems, solvent‐free approaches, microwave, and ultrasonic‐assisted techniques, organo‐ and biocatalysis, ionic liquids, nanoparticle catalysis, electrochemical, and photocatalytic strategies for the synthesis of quinoline scaffolds.
Demis Zelelew, Ajay Bissessur, Parvesh Singh, Hogantharanni Govender   +3 more
wiley   +1 more source

Bedaquiline and clofazimine : successes and challenges [PDF]

, 2020
Bedaquiline, a novel therapeutic drug, and clofazimine, a re-purposed drug, are front-line therapies recommended by WHO to treat rifampicin-resistant or multidrugresistant tuberculosis.
Ndjeka, Norbert, Ismail, Nazir Ahmed
core   +1 more source

Bedaquiline: what might the future hold? [PDF]

Tuberculosis drug development has stagnated for decades, so the recent availability of bedaquiline is welcome. Bedaquiline-containing regimens, now the first-line therapy recommended by WHO, have transformed the treatment of drug-resistant tuberculosis ...
Shaw, Emily S, Conradie, Francesca, Pinto, Lancelot, Sloan, Derek J, Leslie, Alasdair, Chiang, Chen-Yuan, Lipman, Marc, Esmail, Hanif, Potter, Jessica L, Warren, Robin M, Tweed, Conor D, Stoker, Neil G, Voo, Teck Chuan, Lange, Christoph, Claassen, Helgard, Lebina, Limakatso, Theron, Grant, Rucsineanu, Oxana, Tisile, Phumeza   +18 more
core   +4 more sources

High Prevalence of atpE Mutations in Bedaquiline-Resistant Mycobacterium tuberculosis Isolates, Russia

Emerging Infectious Diseases
Bedaquiline is a cornerstone drug for treating drug-resistant tuberculosis. We analyzed 11 isolates from 9 patients who were treated with a bedaquiline-based regimen and remained culture-positive long after treatment start. In 4 of 8 resistant isolates,
Danila Zimenkov, Anastasia Ushtanit, Elizaveta Gordeeva, Elena Guselnikova, Yakov Schwartz, Natalia Stavitskaya   +5 more
doaj   +1 more source

Design, Synthesis, Antimycobacterial Evaluation, and In Silico Investigation of Benzisothiazole‐Based Hydrazide Derivatives as Potential Anti‐Tuberculosis Agents

Chemical Biology &Drug Design, Volume 108, Issue 3, September 2026.
A novel series of benzisothiazole‐based hydrazide derivatives was designed, synthesized, and evaluated for antitubercular activity. Compound 8k emerged as the most potent candidate (MIC = 0.25 μg/mL) with a high selectivity index (SI = 42) and bactericidal activity. Molecular docking and 100 ns simulations identified InhA as the probable target.
Vivek Sharma, Arun Sharma, Ruchi Poria, Pardeep Kumar   +3 more
wiley   +1 more source

Bactericidal mode of action of bedaquiline.

, 2015
Objectives: It is not fully understood why inhibiting ATP synthesis in Mycobacterium species leads to death in non-replicating cells. We investigated the bactericidal mode of action of the anti-tubercular F1Fo-ATP synthase inhibitor bedaquiline (Sirturo™)
Shaw, L., Berney, M., Andries, K., Koul, A., Robson, J.R., Hards, K., Bald, D., Cook, G.M.   +7 more
core   +1 more source