bedaquiline profile

bedaquiline: a diarylquinoline Antitubercular Agent [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

bedaquiline : A quinoline-based antimycobacterial drug used (as its fumarate salt) for the treatment of pulmonary multi-drug resistant tuberculosis by inhibition of ATP synthase, an enzyme essential for the replication of the mycobacteria. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

ID Source	ID
PubMed CID	5388906
CHEMBL ID	376488
CHEBI ID	72292
SCHEMBL ID	295482
MeSH ID	M0492968

Synonym
bromo-2-methoxy-quinolin-3-yl)-4-dimethylamino-2-naphthalen-1-yl-1-phenyl-butan-2-ol
3-quinolineethanol, 6-bromo-alpha-(2-(dimethylamino)ethyl)-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-, (alphar,betas)-rel-
r-207910
1-(1r)-(6-bromo-2-methoxy-quinolin-3-yl)-4-dimethylamino-2-(2s)-(naphthalen-1-yl)-1-phenyl-butan-2-ol
bedaquiline
(1r,2s)-1-(6-bromo-2-methoxy-3-quinolyl)-4-(dimethylamino)-2-(1-naphthyl)-1-phenyl-butan-2-ol
843663-66-1
r 207910
r207910 ,
tmc207
(1r,2s)-1-(6-bromo-2-methoxy-quinolin-3-yl)-4-methyl-amino-2-naphthalen-1-yl-1-phenyl-butan-2-ol
bdq ,
tmc-207
chebi:72292 ,
CHEMBL376488
(1r,2s)-1-(6-bromo-2-methoxyquinolin-3-yl)-4-(dimethylamino)-2-naphthalen-1-yl-1-phenylbutan-2-ol
D09872
bedaquiline (usan/inn)
hsdb 8217
3-quinolineethanol, 6-bromo-alpha-(2-(dimethylamino)ethyl)-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-, (alphas,betar)-
aids 222089
aids-222089
78846i289y ,
tmc 207
1-(6-bromo-2-methoxy-quinolin-3-yl)-4-dimethylamino-2-naphthalen-1-yl-1-phenyl-butan-2-ol
bedaquiline [usan:inn]
unii-78846i289y
bedaquilinum
bedaquilina
(1r,2s)-1-(6-bromo-2-methoxyquinolin-3-yl)-4-(dimethylamino)-2-(1-naphthyl)-1-phenylbutan-2-ol
NCGC00348215-01
S5623
(1r)-(6-bromo-2-methoxyquinolin-3-yl)-4-(dimethylamino)-2(s)-(1-naphthyl)-1-phenylbutan-2-ol
bedaquiline [inn]
bedaquiline [mi]
DB08903
bedaquiline [who-dd]
3-quinolineethanol, 6-bromo-.alpha.-(2-(dimethylamino)ethyl)-2-methoxy-.alpha.-1-naphthalenyl-.beta.-phenyl-, (.alpha.s,.beta.r)-
bedaquiline [usan]
(1r,2s) 6-bromo-alpha-(2-(dimethylamino)ethyl)-2-methoxy-alpha-(1-naphthyl)-beta-phenyl-3-quinolineethanol
(1r,2s)-1-(6-bromo-2-methoxyquinolin-3-yl)-4-(dimethylamino)-2-(naphthalen-1-yl)-1- phenylbutan-2-ol
bedaquiline [vandf]
HY-14881
SCHEMBL295482
AKOS022186476
(1r,2s)-1-(6-bromo-2-methoxyquinolin-3-yl)-4-(dimethylamino)-2-(naphthalen-1-yl)-1-phenylbutan-2-ol
J-500265
bq1 ,
AC-28385
(\|as,\|ar)-bedaquiline
bdbm50063995
gtpl11171
compound 1a [pmid: 17496888]
(alphas,betar)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol
NCGC00348215-04
mmv689758
r403323; tmc207; r207910
c32h31brn2o2
DTXSID80903989 ,
(1r,2s)-1-(6-bromo-2-methoxy-quinolin-3-yl)-4-dimethylamino-2-(3-fluorophenyl)-1-phenyl-butan-2-ol
Q1257318
CCG-270030
NCGC00348215-03
EX-A4133
(1r,2s)-1-(6-bromo-2-methoxy-3-quinolyl)-4-dimethylamino-2-(1-naphthyl)-1-phenyl-butan-2-ol
843663-66-1 (free base)
SR-05000022473-1
sr-05000022473
rel-(1r,2s)-1-(6-bromo-2-methoxyquinolin-3-yl)-4-(dimethylamino)-2-(naphthalen-1-yl)-1-phenylbutan-2-ol
DTXSID101027810
compound 1a (pmid: 17496888)
1-(6-bromo-2-methoxy-quinolin-3-yl)-4-dimethylamino-2-(3-fluorophenyl)-1-phenyl-butan-2-ol
3-quinolineethanol, 6-bromo-alpha-(2-(dimethylamino)ethyl)-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-, (alpha-s,beta-r)-
dtxcid501331924
j04ak05

Excerpt	Reference	Relevance
"Bedaquiline is a new drug of the diarylquinoline class that has proven to be clinically effective against drug-resistant tuberculosis, but has a cardiac liability (prolongation of the QT interval) due to its potent inhibition of the cardiac potassium channel protein hERG. "	( 3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel. Blaser, A; Choi, PJ; Conole, D; Cooper, CB; Denny, WA; Franzblau, SG; Lotlikar, MU; Palmer, BD; Sutherland, HS; Tong, AST; Upton, AM, 2019)	2.24
"Bedaquiline (BDQ) is an anti-microbial agent, approved for clinical use, that inhibits ATP synthase of Mycobacteria; however recently it has been shown to act on mitochondrial ATP synthase, inhibiting both ATP synthesis and hydrolysis in low micromolar concentrations."	( Neuroprotective Effect of a Novel ATP-Synthase Inhibitor Bedaquiline in Cerebral Ischemia-Reperfusion Injury. Arandarcikaite, O; Borutaite, V; Grigaleviciute, R; Stakauskas, R; Umbrasas, D, 2021)	1.59
"Bedaquiline (BDQ) is a new drug approved by United States Food and Drug Administration (USFDA) in 2012 for the treatment of drug-resistant tuberculosis, which has become a major threat globally. "	( Separation and Characterization of Novel Degradation and Process Related Impurities of Bedaquiline Bulk Drug. Rajput, SJ; Vanavi, PJ, 2022)	2.39
"Bedaquiline is a crucial drug for control of rifampicin-resistant tuberculosis. "	( Genetic variants and their association with phenotypic resistance to bedaquiline in Huo, S; Ismail, N; Limberis, J; Metcalfe, JZ; Rivière, E; Van Rie, A; Warren, RM, 2021)	2.3
"Bedaquiline is an orally administered drug active against Mycobacterium tuberculosis and is indicated for patients with confirmed multi-drug-resistant tuberculosis."	( A Scoping Review of the Clinical Pharmacokinetics of Bedaquiline. Wilby, KJ, 2022)	1.69
"Bedaquiline is a novel adenosine triphosphate synthase inhibitor anti-tuberculosis drug. "	( The Chemical Property Position of Bedaquiline Construed by a Chemical Global Positioning System-Natural Product. Alajlani, MM, 2022)	2.44
"Bedaquiline is a new ATP synthesis inhibitor developed as an anti-tuberculosis agent. "	( A case of primary multidrug-resistant pulmonary tuberculosis with high minimum inhibitory concentration value for bedaquiline. Aono, A; Hirano, H; Kobayashi, M; Mitarai, S; Motoki, Y; Nonaka, M; Saito, T; Yamagishi, T, 2022)	2.37
"Bedaquiline is a crucial medicine in the global fight against tuberculosis, yet its high price places it out of reach for many patients. "	( Diastereoselectivity is in the Details: Minor Changes Yield Major Improvements to the Synthesis of Bedaquiline. Ahlqvist, GP; Dietz, JP; Jamison, TF; Khairnar, PV; Lucas, T; Maity, S; Mear, SJ; Nelson, RC; Opatz, T; Robey, JMS; Snead, DR; Williams, CL, 2022)	2.38
"Bedaquiline (BDQ) is a core drug for rifampicin-resistant tuberculosis (RR-TB) treatment. "	( Bedaquiline resistance probability to guide treatment decision making for rifampicin-resistant tuberculosis: insights from a qualitative study. Anlay, DZ; Conceição, EC; Dippenaar, A; Loos, J; Tu, PHT; Van Rie, A, 2022)	3.61
"Bedaquiline (BDQ) is a new class of anti-tubercular (anti-TB) drugs and is currently reserved for multiple drug resistance (MDR-TB). "	( Molecular mechanism for the involvement of CYP2E1/NF-κB axis in bedaquiline-induced hepatotoxicity. Dhiman, S; Dhiman, SK; Khajuria, P; Kotwal, P; Kour, D; Kumar, A; Nandi, U, 2023)	2.59
"Bedaquiline is a core drug for the treatment of multidrug-resistant tuberculosis; however, the understanding of resistance mechanisms is poor, which is hampering rapid molecular diagnostics. "	( Bedaquiline and clofazimine resistance in Mycobacterium tuberculosis: an in-vitro and in-silico data analysis. Carter, JJ; Cirillo, DM; Fowler, PW; Hunt, M; Iqbal, Z; Malone, KM; Merker, M; Niemann, S; Nilgiriwala, KS; Rodrigues, C; Sonnenkalb, L; Spitaleri, A; Utpatel, C, 2023)	3.8
"Bedaquiline (BDQ) is a potent drug for treating drug-resistant tuberculosis (TB). "	( Bedaquiline resistance pattern in clofazimine-resistant clinical isolates of tuberculosis patients. Chen, S; Chu, N; Dong, L; Huang, H; Huo, F; Jiang, G; Jing, W; Nie, W; Shang, Y; Shi, W; Xue, Y, 2023)	3.8
"Bedaquiline is a core drug for treatment of rifampicin-resistant tuberculosis. "	( A Bayesian approach to estimate the probability of resistance to bedaquiline in the presence of a genomic variant. Abrams, S; Anlay, DZ; Rivière, E; Tu, PHT; Van Rie, A, 2023)	2.59
"Bedaquiline (BDQ) is a relatively new core drug, targeting the respiratory chain in Mycobacterium tuberculosis (Mtb)."	( Bedaquiline- and clofazimine- selected Mycobacterium tuberculosis mutants: further insights on resistance driven largely by Rv0678. Andries, K; Coeck, N; de Jong, BC; Mulders, W; Rigouts, L; Snobre, J; Tzfadia, O; Villellas, MC, 2023)	3.07
"Bedaquiline is a life-saving tuberculosis drug undergoing global scale-up. "	( Bedaquiline resistance in patients with drug-resistant tuberculosis in Cape Town, South Africa: a retrospective longitudinal cohort study. Alberts, R; Allender, C; Cox, H; de Vos, M; Derendinger, B; Dheda, K; Dippenaar, A; Dolby, T; Engelthaler, DM; Folkerts, M; Gagneux, S; Huo, S; Lemmer, D; Limberis, J; Metcalfe, J; Reuter, A; Rigouts, L; Sirgel, F; Spies, C; Tadokera, R; Te Riele, J; Theron, G; Van Rie, A; Warren, R, 2023)	3.8
"Bedaquiline (BDQ) is a new antituberculosis (TB) drug effectively used for the treatment of multidrug-resistant and extensively drug-resistant TB. "	( Validation of bedaquiline drug-susceptibility testing by BACTEC MGIT 960 system for Golla, R; Kumar, MP; Mondal, R; Sivaramakrishnan, G; Subramanyam, B; Tripathy, SP, )	1.93
"Bedaquiline (TMC-207) is a recently approved drug for the treatment of multidrug-resistant tuberculosis (MDR-TB). "	( Effect of Natural Phenolics on Pharmacokinetic Modulation of Bedaquiline in Rat to Assess the Likelihood of Potential Food-Drug Interaction. Bhatt, S; Dogra, A; Gour, A; Kotwal, P; Kumar, A; Nandi, U; Sharma, A; Sharma, S; Singh, PP; Wazir, P, 2020)	2.24
"Bedaquiline is an effective drug used to treat MDR and XDR tuberculosis, providing high cure rates in complex therapy. "	( Reduced susceptibility and resistance to bedaquiline in clinical M. tuberculosis isolates. Antonova, OV; Borisov, SE; Kholina, MS; Krylova, LY; Kulagina, EV; Nosova, EY; Peretokina, IV; Safonova, SG; Zimenkov, DV, 2020)	2.27
"Bedaquiline is a novel drug approved in 2012 by the FDA for treatment of drug-resistant tuberculosis (TB). "	( Synthetic Studies to Help Elucidate the Metabolism of the Preclinical Candidate TBAJ-876-A Less Toxic and More Potent Analogue of Bedaquiline. Blaser, A; Choi, PJ; Conole, D; Cooper, CB; Denny, WA; Palmer, BD; Sutherland, HS; Tong, AST; Upton, AM, 2020)	2.21
"Bedaquiline is a diarylquinoline drug that demonstrates potent and selective inhibition of mycobacterial ATP synthase, and is clinically administered for the treatment of multi-drug resistant tuberculosis. "	( Synthetic approaches towards bedaquiline and its derivatives. Brimble, MA; Calvert, MB; Cooper, CB; Furkert, DP, 2020)	2.29
"Bedaquiline is a diarylquinoline that inhibits mycobacterial ATP-synthase."	( Successful bedaquiline-containing antimycobacterial treatment in post-traumatic skin and soft-tissue infection by Mycobacterium fortuitum complex: a case report. Erber, J; Rothe, K; Schmid, RM; Schneider, J; Spinner, CD; Tschaikowsky, T; Weidlich, S, 2020)	1.67
"Bedaquiline is a promising novel agent for NTM treatment, although clinical data are limited and trials evaluating efficacy, safety, and resistance of bedaquiline are required. "	( Successful bedaquiline-containing antimycobacterial treatment in post-traumatic skin and soft-tissue infection by Mycobacterium fortuitum complex: a case report. Erber, J; Rothe, K; Schmid, RM; Schneider, J; Spinner, CD; Tschaikowsky, T; Weidlich, S, 2020)	2.39
"Bedaquiline (BDQ) is an antibiotic to treat pulmonary multidrug-resistant tuberculosis (MDR-TB). "	( Dose- and Time-dependency of the Toxicity and Pharmacokinetic Profiles of Bedaquiline and Its N-desmethyl Metabolite in Dogs. De Jonghe, S; Lampo, A; Looszova, A; Mannens, G; Rouan, MC; Smyej, I; Starckx, S; Thijssen, S; Verhaeghe, T, 2017)	2.13
"Bedaquiline (BDQ) is a newly approved anti-tuberculosis drug in treating multidrug-resistant tuberculosis. "	( Supramolecular strategy for reducing the cardiotoxicity of bedaquiline without compromising its antimycobacterial efficacy. Chan, DPC; In Ng, PC; Ji, X; Kuok, KI; Lee, SMY; Wang, C; Wang, R; Yew, WW; Zheng, J, 2018)	2.17
"Bedaquiline (BDQ) is a novel agent approved for use in combination treatment of multi-drug resistant tuberculosis (MDR-TB). "	( Defining Bedaquiline Susceptibility, Resistance, Cross-Resistance and Associated Genetic Determinants: A Retrospective Cohort Study. Blows, L; Dreyer, AW; Govender, N; Ismail, F; Ismail, NA; Joseph, L; Kaniga, K; Koornhof, H; Ndjeka, N; Omar, SV, 2018)	2.34
"Bedaquiline (BDQ) is a new drug from the family of diarylquinolines, which has a potent bactericidal activity against Mycobacterium tuberculosis. "	( Interaction of the anti-tuberculous drug bedaquiline with artificial membranes and rat erythrocytes. Agafonov, AV; Belosludtsev, KN; Belosludtseva, NV; Dubinin, MV; Gudkov, SV; Penkov, NV; Starinets, VS; Stepanova, AE; Talanov, EY; Tenkov, KS; Vashchenko, OV, 2019)	2.22
"Bedaquiline is a novel bactericidal and sterilizing anti-TB drug with the potential to eradicate RPF-dependent persistent M."	( Bedaquiline kills persistent Mycobacterium tuberculosis with no disease relapse: an in vivo model of a potential cure. Coates, A; Davies, G; Hu, Y; Liu, Y; Pertinez, H, 2019)	2.68
"Bedaquiline is a novel anti-tuberculosis drug that inhibits Mycobacterial ATP synthase. "	( Design, Synthesis and Biological Evaluation of Anti-tuberculosis Agents based on Bedaquiline Structure. Cai, Z; Chen, Y; Luo, J; Meng, F; Sun, T; Wu, C; Wu, M, 2020)	2.23
"Bedaquiline (BDQ) is a recently approved antibiotic for the treatment of multidrug-resistant tuberculosis, but its potential against slow-growing mycobacteria (SGM) is still unknown. "	( In vitro activity of bedaquiline against slow-growing nontuberculous mycobacteria. Aguilar-Ayala, DA; Godino, IT; Lounis, N; Martin, A; Mathys, V; Villalobos, HR, 2019)	2.28
"Bedaquiline is a new antituberculosis agent targeting ATP synthase. "	( Randomized dose-ranging study of the 14-day early bactericidal activity of bedaquiline (TMC207) in patients with sputum microscopy smear-positive pulmonary tuberculosis. Becker, P; Conradie, A; Dawson, R; Diacon, AH; Donald, PR; Egizi, E; Erondu, N; Ginsberg, AM; Mendel, CM; Symons, G; Venter, A; Von Groote-Bidlingmaier, F; Winter, H, 2013)	2.06
"Bedaquiline (BDQ) is a promising new anti-TB drug, and efavirenz (EFV) is a commonly used antiretroviral."	( Model-based estimates of the effects of efavirenz on bedaquiline pharmacokinetics and suggested dose adjustments for patients coinfected with HIV and tuberculosis. Aweeka, F; Dooley, KE; Karlsson, MO; Marzan, F; Park, JG; Svensson, EM, 2013)	1.36
"Bedaquiline is a recently approved drug for the treatment of multidrug-resistant tuberculosis. "	( Bedaquiline metabolism: enzymes and novel metabolites. Dorko, K; Li, F; Liu, K; Liu, S; Lu, J; Ma, X; Xie, W, 2014)	3.29
"Bedaquiline is a novel oral diarylquinoline approved by Food and Drug administration (FDA) for the treatment of adults with pulmonary MDR-TB on the basis of Phase IIb trial data under the provisions of the accelerated approval regulations for serious or life-threatening conditions."	( Bedaquiline for the treatment of resistant tuberculosis: promises and pitfalls. Dahiya, N; Kakkar, AK, 2014)	2.57
"Bedaquiline is a novel agent for the treatment of pulmonary multidrug-resistant Mycobacterium tuberculosis infections, in combination with other agents. "	( Population pharmacokinetics of bedaquiline (TMC207), a novel antituberculosis drug. Green, B; McLeay, SC; van Heeswijk, RP; Vis, P, 2014)	2.13
"Bedaquiline is a novel drug for the treatment of multidrug-resistant (MDR) TB; combined use with antiretroviral drugs, nevirapine, or ritonavir-boosted lopinavir (LPV/r) is anticipated, but no clinical data from coinfected patients are available."	( Impact of lopinavir-ritonavir or nevirapine on bedaquiline exposures and potential implications for patients with tuberculosis-HIV coinfection. Dooley, KE; Karlsson, MO; Svensson, EM, 2014)	1.38
"Bedaquiline is a new antituberculous drug belonging to the diarylquinoline class that efficiently inhibits the adenosine triphosphate synthase enzyme of Mycobacterium tuberculosis."	( Bedaquiline: a novel antitubercular drug for multidrug-resistant tuberculosis. Nagabushan, H; Roopadevi, HS, )	2.3
"Bedaquiline is a diarylquinoline antitubercular drug with a novel mechanism of action against Mycobacterium tuberculosis. "	( Bedaquiline: a novel antitubercular agent for the treatment of multidrug-resistant tuberculosis. Estrada, SJ; Worley, MV, 2014)	3.29
"Bedaquiline is a new antibiotic that was approved for the treatment of multidrug-resistant (MDR) tuberculosis. "	( Compassionate use of bedaquiline for the treatment of multidrug-resistant and extensively drug-resistant tuberculosis: interim analysis of a French cohort. Caumes, E; Guglielmetti, L; Henry, B; Jachym, M; Le Dû, D; Martin, D; Métivier, N; Robert, J; Veziris, N, 2015)	2.18
"Bedaquiline is a newly approved drug for the treatment of multidrug-resistant tuberculosis, but there are concerns about its safety in humans. "	( Verapamil increases the bactericidal activity of bedaquiline against Mycobacterium tuberculosis in a mouse model. Bishai, WR; Gupta, S; Tyagi, S, 2015)	2.11
"Bedaquiline is an oral antimycobacterial agent belonging to a new class of drugs called diarylquinolines. "	( Preliminary Results of Bedaquiline as Salvage Therapy for Patients With Nontuberculous Mycobacterial Lung Disease. Aksamit, TR; Benwill, JL; Brown-Elliott, BA; Griffith, DE; Philley, JV; Taskar, V; Thakkar, F; Wallace, RJ, 2015)	2.17
"Bedaquiline is a much-needed novel drug which is highly effective against drug-resistant tuberculosis. "	( Bedaquiline for the treatment of drug-resistant tuberculosis. Bélard, S; Grobusch, MP; Heuvelings, CC; Janssen, S, 2015)	3.3
"Bedaquiline is a new anti-TB drug, which is metabolized by cytochrome P450 (CYP) 3A4. "	( Drug-drug interactions between bedaquiline and the antiretrovirals lopinavir/ritonavir and nevirapine in HIV-infected patients with drug-resistant TB. Conradie, F; Hughes, J; Maartens, G; McIlleron, H; Pandie, M; Siwendu, S; Variava, E; Wiesner, L, 2016)	2.16
"Bedaquiline is a new drug used for the treatment of multidrug-resistant tuberculosis (MDR-TB). "	( Cost-effectiveness of Bedaquiline for the Treatment of Multidrug-resistant Tuberculosis in the Republic of Korea. Hwa Lim, K; Ku, HM; Kwon, JW; Park, HY; Seo, HS; Sohn, HS; Yung Lee, H, 2016)	2.19
"Bedaquiline is an effective treatment modality for MDR-TB but needs to be balanced against significant mortality. "	( Bedaquiline versus placebo for management of multiple drug-resistant tuberculosis: A systematic review. Charan, J; Kumar, A; Reljic, T, )	3.02
"Bedaquiline is an ATP synthase inhibitor specific for M."	( Bedaquiline as part of combination therapy in adults with pulmonary multi-drug resistant tuberculosis. Akkerman, OW; Alffenaar, JW; Cao, TB; Nguyen, TV; Tiberi, S; Vu, DH, 2016)	2.6
"Bedaquiline is a first-in-class diaryl-quinoline compound, that mechanistically inhibits the bacterial ATP-synthase, and shows potent activity against both drug-sensitive and drug-resistant TB."	( Bedaquiline, an FDA-approved antibiotic, inhibits mitochondrial function and potently blocks the proliferative expansion of stem-like cancer cells (CSCs). Cappello, AR; Fiorillo, M; Lamb, R; Lisanti, MP; Martinez-Outschoorn, UE; Sotgia, F; Tanowitz, HB, 2016)	2.6
"Bedaquiline (BDQ) is a novel and highly potent last-line antituberculosis drug that was approved by the US FDA in 2013. "	( Structural Simplification of Bedaquiline: the Discovery of 3-(4-(N,N-Dimethylaminomethyl)phenyl)quinoline-Derived Antitubercular Lead Compounds. Cui, H; Fu, L; He, C; Meier, T; Preiss, L; Wang, B; Wen, H; Yin, D; Zhang, X, 2017)	2.19

Excerpt	Reference	Relevance
"Bedaquiline has a long terminal half-life; therefore, restarting after an interruption without a loading dose could increase the risk of suboptimal treatment outcome and resistance development."	( Optimized Loading Dose Strategies for Bedaquiline When Restarting Interrupted Drug-Resistant Tuberculosis Treatment. Brust, JCM; Koele, SE; Maartens, G; Svensson, EM; van Beek, SW, 2022)	1.71
"Bedaquiline has an excellent in vitro activity against Mycobacterium tuberculosis, including multidrug resistant M tuberculosis; however, its side effect profile limits its use against MDR-TB when no other effective regimen can be provided."	( Bedaquiline: a novel diarylquinoline for multidrug-resistant tuberculosis. Chahine, EB; Karaoui, LR; Mansour, H, 2014)	2.57
"Bedaquiline has been classified as a group A drug for the treatment of multidrug-resistant tuberculosis (MDR-TB) by the World Health Organization; however, globally emerging resistance threatens the effectivity of novel MDR-TB treatment regimens."	( Emergence of bedaquiline resistance in a high tuberculosis burden country. Andres, S; Barilar, I; Chesov, D; Chesov, E; Crudu, V; Donica, A; Heyckendorf, J; Lange, C; Maurer, FP; Merker, M; Niemann, S; Reimann, M; Utpatel, C, 2022)	2.53
"Bedaquiline (BDQ) has become a drug of choice in treating MDR-TB and helps in reducing the treatment span."	( Current Perspective of ATP Synthase Inhibitors in the Management of the Tuberculosis. Divita, KM; Khatik, GL, 2021)	1.34
"Bedaquiline (BDQ) has shown great value in the treatment of multidrug-resistant tuberculosis (MDR-TB) in recent years. "	( Exposure-safety analysis of QTc interval and transaminase levels following bedaquiline administration in patients with drug-resistant tuberculosis. Karlsson, MO; Rossenu, S; Svensson, EM; Tanneau, L, 2021)	2.29
"Bedaquiline has a long terminal half-life; therefore, restarting after an interruption without a loading dose could increase the risk of suboptimal treatment outcome and resistance development."	( Optimized Loading Dose Strategies for Bedaquiline When Restarting Interrupted Drug-Resistant Tuberculosis Treatment. Brust, JCM; Koele, SE; Maartens, G; Svensson, EM; van Beek, SW, 2022)	1.71
"Bedaquiline (BDQ) has been recently approved for drug resistant tuberculosis with active drug safety monitoring under programmatic condition. "	( Early treatment outcome of bedaquiline plus optimised background regimen in drug resistant tuberculosis patients. Barvaliya, SV; Desai, MK; Panchal, JR; Solanki, RN, 2020)	2.3
"Bedaquiline (BDQ) has been proven to be effective in the treatment of multidrug-resistant tuberculosis. "	( In vitro activity of bedaquiline against rapidly growing nontuberculous mycobacteria. Aguilar-Ayala, DA; André, E; Andries, K; Cnockaert, M; Gonzalez-Y-Merchand, JA; Martin, A; Palomino, JC; Vandamme, P, 2017)	2.22
"Bedaquiline (BDQ) has been approved in India for the treatment of multidrug-resistant tuberculosis (MDR-TB), but is currently recommended for MDR-TB patients who have failed initial treatment with standard regimens. "	( Modeling the impact of bedaquiline treatment strategies on the multidrug-resistant tuberculosis burden in India. Kambili, C; Mehra, M; Potluri, R; Rhines, A; Singh, V; Thomas, A, 2017)	2.21
"Bedaquiline has been shown to reduce time to sputum culture conversion (SCC) and increase cure rates in patients with drug-resistant TB, but the influence of drug exposure remains uncharacterized."	( Modelling of mycobacterial load reveals bedaquiline's exposure-response relationship in patients with drug-resistant TB. Karlsson, MO; Svensson, EM, 2017)	2.17
"Bedaquiline and delamanid have been approved for treatment of multidrug-resistant (MDR) tuberculosis in the past 5 years. "	( Early safety and efficacy of the combination of bedaquiline and delamanid for the treatment of patients with drug-resistant tuberculosis in Armenia, India, and South Africa: a retrospective cohort study. Cox, H; De Avezedo, V; Egazaryan, L; Ferlazzo, G; Furin, J; Hewison, C; Hughes, J; Isaakidis, P; Jonckheere, S; Kalon, S; Khachatryan, N; Laxmeshwar, C; Mohr, E; Shroufi, A, 2018)	2.18
"Bedaquiline (BDQ) has been approved for the treatment of multidrug- and extensively drug-resistant tuberculosis (MDR/XDR-TB). "	( Long-term plasma pharmacokinetics of bedaquiline for multidrug- and extensively drug-resistant tuberculosis. Bouvet, E; Fréchet-Jachym, M; Gonzales, MC; Grall, N; Lachâtre, M; Lê, MP; Loubet, P; Perrineau, S; Peytavin, G; Rioux, C; Veziris, N; Yazdanpanah, Y, 2019)	2.23
"Bedaquiline has an excellent in vitro activity against Mycobacterium tuberculosis, including multidrug resistant M tuberculosis; however, its side effect profile limits its use against MDR-TB when no other effective regimen can be provided."	( Bedaquiline: a novel diarylquinoline for multidrug-resistant tuberculosis. Chahine, EB; Karaoui, LR; Mansour, H, 2014)	2.57
"Bedaquiline has recently been approved for the treatment of pulmonary multidrug-resistant tuberculosis (TB) as part of combination therapy in adults. "	( Bedaquiline: a review of human pharmacokinetics and drug-drug interactions. Dannemann, B; Hoetelmans, RM; van Heeswijk, RP, 2014)	3.29
"Bedaquiline has also recently been included in clinical trials for new regimens with the aim of improving and shortening treatment periods."	( Efflux pump inhibitors: targeting mycobacterial efflux systems to enhance TB therapy. Black, PA; Louw, GE; Pule, CM; Sampson, SL; van Helden, PD; Victor, TC; Warren, RM, 2016)	1.16
"Bedaquiline has recently emerged as a new drug developed to specifically treat MDR-TB."	( New synthetic approaches towards analogues of bedaquiline. Baell, JB; Barbaro, L; Priebbenow, DL, 2016)	1.41
"Bedaquiline has excellent potential for use in patients with MAC infections, although for reasons of its metabolism by the cytochrome P450 system, it should not be given with rifampin."	( In Vitro Susceptibility Testing of Bedaquiline against Mycobacterium avium Complex. Brown-Elliott, BA; Griffith, DE; Philley, JV; Thakkar, F; Wallace, RJ, 2017)	1.45

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"Bedaquiline treatment leads to an elevated bedaquiline MIC and the acquisition of mmpR and atpE gene mutations in tuberculosis strains. "	( Reduced susceptibility and resistance to bedaquiline in clinical M. tuberculosis isolates. Antonova, OV; Borisov, SE; Kholina, MS; Krylova, LY; Kulagina, EV; Nosova, EY; Peretokina, IV; Safonova, SG; Zimenkov, DV, 2020)	2.27
"Bedaquiline treatment significantly improves multidrug-resistant tuberculosis (MDR-TB) patient treatment outcomes. "	( Early outcome and safety of bedaquiline-containing regimens for treatment of MDR- and XDR-TB in China: a multicentre study. Cai, Q; Chen, W; Chen, X; Chen, Y; Du, J; Fan, L; Gao, J; Gao, M; Jin, L; Li, G; Li, L; Li, M; Liu, Y; Mei, Z; Pang, Y; Pei, Y; Shu, W; Tang, P; Wu, G; Wu, Q; Xie, L; Xiong, Y, 2021)	2.36
"Bedaquiline-based MDR-TB treatment regimens result in better disease resolution when compared with bedaquiline-sparing MDR-TB treatment regimens under programmatic conditions in a country with a high burden of MDR-TB."	( Impact of bedaquiline on treatment outcomes of multidrug-resistant tuberculosis in a high-burden country. Alexandru, S; Botnaru, V; Chesov, D; Chesov, E; Crudu, V; Donica, A; Heyckendorf, J; Lange, C; Reimann, M, 2021)	2.47
"Bedaquiline improves treatment outcomes in patients with rifampin-resistant (RR) tuberculosis but prolongs the QT interval and carries a black-box warning from the US Food and Drug Administration. "	( Effectiveness and Cardiac Safety of Bedaquiline-Based Therapy for Drug-Resistant Tuberculosis: A Prospective Cohort Study. Allana, S; Brust, JCM; Campbell, A; Ebrahim, I; Franczek, M; Gandhi, NR; Hahn, A; Hernandez-Romieu, AC; Ismail, NA; Joseph, L; Maartens, G; Master, I; Meintjes, G; Mlisana, K; Omar, SV; Ramangoaela, L; Te Riele, J; Viljoen, CA; Wasserman, S; Zalta, B; Zhang, C, 2021)	2.34

Excerpt	Reference	Relevance
" There were no grade 3 or 4 clinical adverse events."	( Safety, tolerability, and pharmacokinetic interactions of the antituberculous agent TMC207 (bedaquiline) with efavirenz in healthy volunteers: AIDS Clinical Trials Group Study A5267. Allen, R; Aweeka, F; Cramer, Y; Dooley, KE; Flexner, C; Gupta, A; Haas, DW; Lizak, P; Park, JG; Qasba, S; Swindells, S; van Heeswijk, R; Wiggins, I, 2012)	0.6
" MDR TB is difficult to cure, requiring 18-24 months of treatment after sputum culture conversion with a regimen that consists of four to six medications with toxic side effects, and carries a mortality risk greater than that of drug-susceptible TB."	( Provisional CDC guidelines for the use and safety monitoring of bedaquiline fumarate (Sirturo) for the treatment of multidrug-resistant tuberculosis. , 2013)	0.63
"Increasing numbers of children with drug-resistant tuberculosis are accessing second-line antituberculosis drugs; these are more toxic than first-line drugs."	( Adverse effects of oral second-line antituberculosis drugs in children. Garcia-Prats, AJ; Hesseling, AC; Schaaf, HS; Thee, S; van der Laan, L, 2016)	0.43
"A Pubmed search was performed to identify articles addressing adverse effects of second-line antituberculosis drugs; a general search was done for the new drugs delamanid and bedaquiline."	( Adverse effects of oral second-line antituberculosis drugs in children. Garcia-Prats, AJ; Hesseling, AC; Schaaf, HS; Thee, S; van der Laan, L, 2016)	0.63
"Although children may experience fewer adverse effects from oral second-line antituberculosis drugs than adults, evidence from prospective studies of the incidence of adverse events in children is limited."	( Adverse effects of oral second-line antituberculosis drugs in children. Garcia-Prats, AJ; Hesseling, AC; Schaaf, HS; Thee, S; van der Laan, L, 2016)	0.43
" Severe and serious adverse events were recorded in 60% and 18% of patients, respectively."	( Long-term outcome and safety of prolonged bedaquiline treatment for multidrug-resistant tuberculosis. Bernard, C; Caumes, E; Fréchet-Jachym, M; Guglielmetti, L; Jaspard, M; Lachâtre, M; Le Dû, D; Marigot-Outtandy, D; Robert, J; Veziris, N; Yazdanpanah, Y, 2017)	0.72
" Treatment at a low dose, reaching exposures approximating therapeutic exposures, was without adverse effects and not associated with PLD."	( Dose- and Time-dependency of the Toxicity and Pharmacokinetic Profiles of Bedaquiline and Its N-desmethyl Metabolite in Dogs. De Jonghe, S; Lampo, A; Looszova, A; Mannens, G; Rouan, MC; Smyej, I; Starckx, S; Thijssen, S; Verhaeghe, T, 2017)	0.69
" We report serious adverse events, QTc corrected using the Fridericia formula (QTcF) interval data, and culture conversion data during the first 6 months of treatment."	( Early safety and efficacy of the combination of bedaquiline and delamanid for the treatment of patients with drug-resistant tuberculosis in Armenia, India, and South Africa: a retrospective cohort study. Cox, H; De Avezedo, V; Egazaryan, L; Ferlazzo, G; Furin, J; Hewison, C; Hughes, J; Isaakidis, P; Jonckheere, S; Kalon, S; Khachatryan, N; Laxmeshwar, C; Mohr, E; Shroufi, A, 2018)	0.74
" 16 serious adverse events were reported in seven patients."	( Early safety and efficacy of the combination of bedaquiline and delamanid for the treatment of patients with drug-resistant tuberculosis in Armenia, India, and South Africa: a retrospective cohort study. Cox, H; De Avezedo, V; Egazaryan, L; Ferlazzo, G; Furin, J; Hewison, C; Hughes, J; Isaakidis, P; Jonckheere, S; Kalon, S; Khachatryan, N; Laxmeshwar, C; Mohr, E; Shroufi, A, 2018)	0.74
" Patients were followed up for sputum smear and culture conversion and adverse events during the treatment."	( Early efficacy and safety of Bedaquiline and Delamanid given together in a "Salvage Regimen" for treatment of drug-resistant tuberculosis. Khalid, UK; Mathuria, KK; Munjal, SK; Myneedu, VP; Puri, MM; Sarin, R; Singla, N; Singla, R; Verma, A; Vohra, V, 2019)	0.81
" 29 adverse events (AE) were reported among 17 patients and there were 11 deaths."	( Early efficacy and safety of Bedaquiline and Delamanid given together in a "Salvage Regimen" for treatment of drug-resistant tuberculosis. Khalid, UK; Mathuria, KK; Munjal, SK; Myneedu, VP; Puri, MM; Sarin, R; Singla, N; Singla, R; Verma, A; Vohra, V, 2019)	0.81
"BDQ and DLM given together in a salvage regimen is efficacious with low rate of adverse events."	( Early efficacy and safety of Bedaquiline and Delamanid given together in a "Salvage Regimen" for treatment of drug-resistant tuberculosis. Khalid, UK; Mathuria, KK; Munjal, SK; Myneedu, VP; Puri, MM; Sarin, R; Singla, N; Singla, R; Verma, A; Vohra, V, 2019)	0.81
" The aim of the aDSM project is to demonstrate the feasibility of implementing national aDSM registers and to describe the type and the frequency of adverse events (AEs) associated with exposure to the new anti-TB drugs."	( Surveillance of adverse events in the treatment of drug-resistant tuberculosis: A global feasibility study. Akkerman, O; Al-Marzouqi, NH; Aleksa, A; Alffenaar, JW; Arias-Guillén, M; Belilovski, E; Bernal, E; Boeree, MJ; Borisov, SE; Bruchfeld, J; Cadiñanos Loidi, J; Cai, Q; Caminero, JA; Cebrian Gallardo, JJ; Centis, R; Codecasa, LR; D'Ambrosio, L; Dalcolmo, M; Danila, E; Dara, M; Davidavičienė, E; Davies Forsman, L; De Los Rios Jefe, J; Denholm, J; Duarte, R; Elamin, SE; Ferrarese, M; Filippov, A; Ganatra, S; Garcia, A; García-García, JM; Gayoso, R; Giraldo Montoya, AM; Gomez Rosso, RG; Gualano, G; Hoefsloot, W; Ilievska-Poposka, B; Jonsson, J; Khimova, E; Kuksa, L; Kunst, H; Laniado-Laborín, R; Li, Y; Magis-Escurra, C; Manfrin, V; Manga, S; Marchese, V; Martínez Robles, E; Maryandyshev, A; Matteelli, A; Migliori, GB; Mullerpattan, JB; Munoz-Torrico, M; Mustafa Hamdan, H; Nieto Marcos, M; Noordin, NM; Palmero, DJ; Palmieri, F; Payen, MC; Piubello, A; Pontali, E; Pontarelli, A; Quirós, S; Rendon, A; Skrahina, A; Šmite, A; Solovic, I; Sotgiu, G; Souleymane, MB; Spanevello, A; Stošić, M; Tadolini, M; Tiberi, S; Udwadia, ZF; van den Boom, M; Vescovo, M; Viggiani, P; Visca, D; Zhurkin, D; Zignol, M, 2019)	0.51
" Additionally, the frequency and type of adverse events during treatment were similar in both groups, and 1 patient (5."	( Bedaquiline in multidrug-resistant tuberculosis treatment: Safety and efficacy in a Korean subpopulation. Hwang, S; Kim, JH; Kim, YS; Kwon, OJ; Park, MS; Shim, TS, 2020)	2
" These drugs are associated with numerous adverse events that can cause severe morbidity, such as deafness, and in some instances can lead to death."	( Drug-associated adverse events in the treatment of multidrug-resistant tuberculosis: an individual patient data meta-analysis. Ahmad, N; Baghaei, P; Barkane, L; Benedetti, A; Brode, SK; Brust, JCM; Campbell, JR; Chang, VWL; Falzon, D; Guglielmetti, L; Isaakidis, P; Kempker, RR; Kipiani, M; Kuksa, L; Lan, Z; Lange, C; Laniado-Laborín, R; Menzies, D; Nahid, P; Rodrigues, D; Singla, R; Udwadia, ZF, 2020)	0.56
"We did a meta-analysis using individual-level patient data that were obtained from studies that reported adverse events that resulted in permanent discontinuation of anti-tuberculosis medications."	( Drug-associated adverse events in the treatment of multidrug-resistant tuberculosis: an individual patient data meta-analysis. Ahmad, N; Baghaei, P; Barkane, L; Benedetti, A; Brode, SK; Brust, JCM; Campbell, JR; Chang, VWL; Falzon, D; Guglielmetti, L; Isaakidis, P; Kempker, RR; Kipiani, M; Kuksa, L; Lan, Z; Lange, C; Laniado-Laborín, R; Menzies, D; Nahid, P; Rodrigues, D; Singla, R; Udwadia, ZF, 2020)	0.56
" Using meta-analysis of proportions, drugs with low risks of adverse event occurrence leading to permanent discontinuation included levofloxacin (1·3% [95% CI 0·3-5·0]), moxifloxacin (2·9% [1·6-5·0]), bedaquiline (1·7% [0·7-4·2]), and clofazimine (1·6% [0·5-5·3])."	( Drug-associated adverse events in the treatment of multidrug-resistant tuberculosis: an individual patient data meta-analysis. Ahmad, N; Baghaei, P; Barkane, L; Benedetti, A; Brode, SK; Brust, JCM; Campbell, JR; Chang, VWL; Falzon, D; Guglielmetti, L; Isaakidis, P; Kempker, RR; Kipiani, M; Kuksa, L; Lan, Z; Lange, C; Laniado-Laborín, R; Menzies, D; Nahid, P; Rodrigues, D; Singla, R; Udwadia, ZF, 2020)	0.75
"Fluoroquinolones, clofazimine, and bedaquiline had the lowest incidence of adverse events leading to permanent drug discontinuation, whereas second-line injectable drugs, aminosalicylic acid, and linezolid had the highest incidence."	( Drug-associated adverse events in the treatment of multidrug-resistant tuberculosis: an individual patient data meta-analysis. Ahmad, N; Baghaei, P; Barkane, L; Benedetti, A; Brode, SK; Brust, JCM; Campbell, JR; Chang, VWL; Falzon, D; Guglielmetti, L; Isaakidis, P; Kempker, RR; Kipiani, M; Kuksa, L; Lan, Z; Lange, C; Laniado-Laborín, R; Menzies, D; Nahid, P; Rodrigues, D; Singla, R; Udwadia, ZF, 2020)	0.84
" Use of BDQ with additional monitoring may be safe and effective even in the field settings."	( Effectiveness and safety of bedaquiline under conditional access program for treatment of drug-resistant tuberculosis in India: An interim analysis. Gupta, M; Jaju, J; Kalaiselvan, V; Khaparde, S; Kshirsagar, N; Mehandru, L; Padmapriyadarsini, C; Parmar, M; Patel, Y; Ponnuraja, C; Ramachandran, R; Sachdeva, KS; Salhotra, VS; Shamim, A; Swaminathan, S, 2020)	0.85
"401) were at significantly high risk of unfavourable outcomes, with serious adverse events noted in 15 (8."	( Early outcome and safety of bedaquiline-containing regimens for treatment of MDR- and XDR-TB in China: a multicentre study. Cai, Q; Chen, W; Chen, X; Chen, Y; Du, J; Fan, L; Gao, J; Gao, M; Jin, L; Li, G; Li, L; Li, M; Liu, Y; Mei, Z; Pang, Y; Pei, Y; Shu, W; Tang, P; Wu, G; Wu, Q; Xie, L; Xiong, Y, 2021)	0.92
"Bedaquiline, when included in background regimens for treatment of MDR-TB and XDR-TB patients in China, was safe and associated with a high rate of culture conversion."	( Early outcome and safety of bedaquiline-containing regimens for treatment of MDR- and XDR-TB in China: a multicentre study. Cai, Q; Chen, W; Chen, X; Chen, Y; Du, J; Fan, L; Gao, J; Gao, M; Jin, L; Li, G; Li, L; Li, M; Liu, Y; Mei, Z; Pang, Y; Pei, Y; Shu, W; Tang, P; Wu, G; Wu, Q; Xie, L; Xiong, Y, 2021)	2.36
" The adverse effects were systematically monitored."	( Outcomes and adverse events of pre- and extensively drug-resistant tuberculosis patients in Kinshasa, Democratique Republic of the Congo: A retrospective cohort study. Aloni, M; Anshambi, N; Kashongwe, IM; Kashongwe, ZM; Kaswa, M; Kayembe, JMN; Lepira, FB; Losenga, L; Mawete, F; Mbulula, L; Nsuela, DJ; Umba, P, 2020)	0.56
" The most common adverse events were vomiting, Skin rash, anemia and peripheral neuropathy."	( Outcomes and adverse events of pre- and extensively drug-resistant tuberculosis patients in Kinshasa, Democratique Republic of the Congo: A retrospective cohort study. Aloni, M; Anshambi, N; Kashongwe, IM; Kashongwe, ZM; Kaswa, M; Kayembe, JMN; Lepira, FB; Losenga, L; Mawete, F; Mbulula, L; Nsuela, DJ; Umba, P, 2020)	0.56
"The study aimed to analyze frequency and severity of adverse events (AEs) and other reasons for interruption of treatment and loss to follow up (LTFU) during first six months of treatment among tuberculosis patients on bedaquiline containing regimens."	( Treatment interruption patterns and adverse events among patients on bedaquiline containing regimen under programmatic conditions in India. Caminero, JA; Chakraborty, A; Gupta, A; Kumar, V; Natarajan, S; Singla, N; Singla, R, )	0.55
" Among a total 192 adverse event episodes, (49."	( Treatment interruption patterns and adverse events among patients on bedaquiline containing regimen under programmatic conditions in India. Caminero, JA; Chakraborty, A; Gupta, A; Kumar, V; Natarajan, S; Singla, N; Singla, R, )	0.37
" Anemia was the most frequent severe adverse event (AE)."	( Safety and Effectiveness of an All-Oral, Bedaquiline-Based, Shorter Treatment Regimen for Rifampicin-Resistant Tuberculosis in High Human Immunodeficiency Virus (HIV) Burden Rural South Africa: A Retrospective Cohort Analysis. Bulti, AB; Dumicho, A; Furin, J; Isaakidis, P; Mbatha, M; Ohler, L; Shigayeva, A; Tack, I; White, K, 2021)	0.89
" In this nationwide descriptive cohort study from Belarus, we examined adverse drug events, time to culture conversion, treatment outcomes including post-treatment recurrence among children and adolescents (<18 years of age) treated with bedaquiline and/or delamanid containing regimens from 2015 to 2019."	( Effectiveness and safety of delamanid- or bedaquiline-containing regimens among children and adolescents with multidrug resistant or extensively drug resistant tuberculosis: A nationwide study from Belarus, 2015-19. Auchynka, V; Charnysh, I; Hurevich, H; Katovich, D; Klimuk, D; Kumar, AMV; Sereda, Y; Setkina, S; Skrahin, A; Skrahina, A; Solodovnikova, V; Yedilbayev, A, 2021)	1.07
"World Health Organization recommends countries introducing new drug and short treatment regimen for drug resistant tuberculosis (DR-TB) should develop and implement a system for active pharmacovigilance that allows for detection, reporting and management of adverse events."	( Bedaquiline-containing regimens in patients with pulmonary multidrug-resistant tuberculosis in China: focus on the safety. Bai, DP; Cai, C; Cai, QS; Chen, W; Chen, XH; Chen, Y; Cheng, LL; Du, J; Fan, L; Gao, JT; Gao, MQ; Geng, SJ; Guan, WL; Jin, L; Li, GB; Li, MW; Li, TX; Li, XJ; Liu, YH; Martinez, L; Miao, YF; Ning, YJ; Pei, Y; Shi, JC; Shu, W; Sun, YX; Tang, PJ; Teng, F; Wang, H; Wang, JY; Wu, GH; Wu, QH; Xie, L; Xie, SH; Xiong, Y; Xu, L; Yan, XF; Yang, GL; Zeng, Y; Zhang, LJ; Zhou, Y; Zhuo, M; Zong, PL, 2021)	2.06
"Multicentre (16 countries), prospective, observational study reporting incidence and frequency of clinically relevant adverse events of special interest (AESIs) among patients who received MDR/RR-TB treatment containing bedaquiline and/or delamanid."	( Safety of Treatment Regimens Containing Bedaquiline and Delamanid in the endTB Cohort. Adenov, M; Adnan, S; Ahmed, S; Bastard, M; Coutisson, S; Danielyan, N; Franke, MF; Hewison, C; Huerga, H; Islam, S; Janmohamed, A; Kamene Kimenye, M; Karakozian, H; Khan, P; Khan, U; Kholikulov, B; Kirakosyan, O; Krisnanda, A; Kumsa, A; Lachenal, N; Leblanc, G; Lecca, L; Mamsa, S; Melikyan, N; Mitnick, CD; Nkuebe, M; Osso, E; Padayachee, S; Rich, ML; Seung, KJ; Thit, P; Varaine, F, 2022)	1.17
" In conclusion, we here propose a strategy for BDQ re-introduction providing guidance to clinicians for safe and efficacious BDQ dosing."	( A modeling-based proposal for safe and efficacious reintroduction of bedaquiline after dose interruption: A population pharmacokinetics study. Akhondipour Salehabad, Y; Davies Forsman, L; Keutzer, L; Simonsson, USH, 2022)	0.96
" All serious adverse events and adverse events of special interest (AESI), leading to a treatment change, or judged significant by a clinician, were systematically monitored and documented."	( Safety and Effectiveness Outcomes From a 14-Country Cohort of Patients With Multi-Drug Resistant Tuberculosis Treated Concomitantly With Bedaquiline, Delamanid, and Other Second-Line Drugs. Ahmed, S; Bastard, M; Franke, MF; Grium Tefera, D; Hewison, C; Holtzman, D; Huerga, H; Islam, S; Jacques Leblanc, G; Khan, PY; Khan, U; Kumsa, A; Lachenal, N; Leonovich, O; Mamsa, S; Manzur-Ul-Alam, M; Melikyan, N; Mitnick, CD; Myint, Z; Osso, E; Padayachee, S; Rafi Siddiqui, M; Rashitov, M; Rich, ML; Salahuddin, N; Salia, G; Sánchez, E; Serobyan, A; Seung, KJ; Varaine, F; Vetushko, D; Yeghiazaryan, L, 2022)	0.92
"Concomitant use of Bdq and Dlm, along with linezolid and clofazimine, is safe and effective for MDR/RR-TB patients with extensive disease."	( Safety and Effectiveness Outcomes From a 14-Country Cohort of Patients With Multi-Drug Resistant Tuberculosis Treated Concomitantly With Bedaquiline, Delamanid, and Other Second-Line Drugs. Ahmed, S; Bastard, M; Franke, MF; Grium Tefera, D; Hewison, C; Holtzman, D; Huerga, H; Islam, S; Jacques Leblanc, G; Khan, PY; Khan, U; Kumsa, A; Lachenal, N; Leonovich, O; Mamsa, S; Manzur-Ul-Alam, M; Melikyan, N; Mitnick, CD; Myint, Z; Osso, E; Padayachee, S; Rafi Siddiqui, M; Rashitov, M; Rich, ML; Salahuddin, N; Salia, G; Sánchez, E; Serobyan, A; Seung, KJ; Varaine, F; Vetushko, D; Yeghiazaryan, L, 2022)	0.92
" Ten children experienced 27 adverse events at least possibly related to bedaquiline; no adverse events led to bedaquiline withdrawal."	( Pharmacokinetics and Safety of Bedaquiline in Human Immunodeficiency Virus (HIV)-Positive and Negative Older Children and Adolescents With Rifampicin-Resistant Tuberculosis. Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Hughes, JA; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; van der Laan, L; Wiesner, L; Winckler, JL, 2022)	1.24
"The evaluated doses of bedaquiline in children ≥ 6 years of age were safe but achieved slightly lower plasma concentrations compared to adults receiving the recommended dose, possibly due to delayed food intake relative to bedaquiline administration."	( Pharmacokinetics and Safety of Bedaquiline in Human Immunodeficiency Virus (HIV)-Positive and Negative Older Children and Adolescents With Rifampicin-Resistant Tuberculosis. Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Hughes, JA; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; van der Laan, L; Wiesner, L; Winckler, JL, 2022)	1.32
" A shorter, less toxic and more efficacious regimen would improve outcomes for people with rifampicin-resistant tuberculosis."	( TB-PRACTECAL: study protocol for a randomised, controlled, open-label, phase II-III trial to evaluate the safety and efficacy of regimens containing bedaquiline and pretomanid for the treatment of adult patients with pulmonary multidrug-resistant tubercul Berry, C; du Cros, P; Fielding, K; Gajewski, S; Kazounis, E; McHugh, TD; Merle, C; Moore, DAJ; Motta, I; Nyang'wa, BT, 2022)	0.92
"TB-PRACTECAL is an ambitious trial using adaptive design to accelerate regimen assessment and bring novel treatments that are effective and safe to patients quicker."	( TB-PRACTECAL: study protocol for a randomised, controlled, open-label, phase II-III trial to evaluate the safety and efficacy of regimens containing bedaquiline and pretomanid for the treatment of adult patients with pulmonary multidrug-resistant tubercul Berry, C; du Cros, P; Fielding, K; Gajewski, S; Kazounis, E; McHugh, TD; Merle, C; Moore, DAJ; Motta, I; Nyang'wa, BT, 2022)	0.92
" The trial results will help establish evidence towards a safe and effective dose of LZD that can be used in a fully, all-oral short course regimen for highly DR-TB patients."	( Randomised trial to evaluate the effectiveness and safety of varying doses of linezolid with bedaquiline and pretomanid in adults with pre-extensively drug-resistant or treatment intolerant/non-responsive multidrug-resistant pulmonary tuberculosis: study Devaleenal, B; Mandal, S; Mattoo, S; Padmapriyadarsini, C; Parmar, M; Ponnuraja, C; Ramraj, B; Singla, R, 2022)	0.94
"Refractory rifampicin-resistant/multidrug resistant/extensively-drug resistant tuberculosis (RR/MDR/XDR-TB) were defined as patients infected with Mycobacterium tuberculosis (MTB) resistant to rifampicin(RR-TB), or at least resistant to rifampicin and isoniazid (MDR-TB) or added resistant to fluoroquinolones (FQs) and one of second line injectable agents (XDR-TB), a patient for whom an effective regimen (fewer than 4 effective agents due to adverse events (AEs) or multiple drug resistances) cannot be developed."	( Effectiveness and safety of bedaquiline-containing regimens for treatment on patients with refractory RR/MDR/XDR-tuberculosis: a retrospective cohort study in East China. Fan, L; Li, YP; Sun, WW; Xiao, HP; Yang, Y; Zhang, SJ; Zhang, ZM; Zhang, ZS, 2022)	1.02
" Of 106 evaluated, 95 (90%) were successfully treated, six (6%) were lost-to-follow-up, one (1%) died, and four (4%) had treatment failure, including three with permanent regimen change owing to adverse events (AE) and one with culture reversion."	( Effectiveness and safety of bedaquiline-based, modified all-oral 9-11-month treatment regimen for rifampicin-resistant tuberculosis in Vietnam. Decroo, T; Hoang, TTT; Le, THM; Merle, CSC; Nguyen, BH; Nguyen, NL; Nguyen, TMP; Nguyen, VN; Pedrazzoli, D, 2023)	1.2
"The study aimed to summarise the existing evidence of bedaquiline's safety on drugresistant tuberculosis treatment outcome and look for bedaquiline-related adverse drug reactions in the Pharmacovigilance Programme of India and World Health Organisation - Uppsala Monitoring Centre database."	( Bedaquiline's Safety Profile Monitoring in India: Considerations for Future - A Systematic Review. Thangaraju, P; Velmurugan, H; Yella, SST, 2024)	3.13
"We searched the PubMed database for relevant studies on the safety profile of bedaquiline used in the treatment of drug-resistant tuberculosis and bedaquiline-related adverse drug reactions in the Pharmacovigilance Programme of India and World Health Organisation - Uppsala Monitoring Centre database published up to April 25, 2022."	( Bedaquiline's Safety Profile Monitoring in India: Considerations for Future - A Systematic Review. Thangaraju, P; Velmurugan, H; Yella, SST, 2024)	3.11
"Linezolid is an effective, but toxic anti-tuberculosis drug that is currently recommended for the treatment of drug-resistant tuberculosis."	( A phase IIb, open-label, randomized controlled dose ranging multi-centre trial to evaluate the safety, tolerability, pharmacokinetics and exposure-response relationship of different doses of delpazolid in combination with bedaquiline delamanid moxifloxaci Aarnoutse, R; Boeree, M; Cho, YL; Dierig, A; Geiter, L; Gong, X; Heinrich, N; Hoelscher, M; Hoffmann, L; Jarchow-MacDonald, A; Liyoyo, A; Mbeya, B; McHugh, TD; Mhimbira, FA; Minja, LT; Mpagama, S; Ntinginya, N; Phillips, P; Rassool, M; Schultz, S; Sebe, M; Svensson, EM; Te Brake, L; Wallis, RS; Wildner, LM, 2023)	1.1
"DECODE is an innovative dose-finding trial, designed to support exposure-response modelling for safe and effective dose selection."	( A phase IIb, open-label, randomized controlled dose ranging multi-centre trial to evaluate the safety, tolerability, pharmacokinetics and exposure-response relationship of different doses of delpazolid in combination with bedaquiline delamanid moxifloxaci Aarnoutse, R; Boeree, M; Cho, YL; Dierig, A; Geiter, L; Gong, X; Heinrich, N; Hoelscher, M; Hoffmann, L; Jarchow-MacDonald, A; Liyoyo, A; Mbeya, B; McHugh, TD; Mhimbira, FA; Minja, LT; Mpagama, S; Ntinginya, N; Phillips, P; Rassool, M; Schultz, S; Sebe, M; Svensson, EM; Te Brake, L; Wallis, RS; Wildner, LM, 2023)	1.1

Excerpt	Reference	Relevance
" Pharmacokinetic sampling was performed on day 7 of TMC207 administration up to 24 h postdose."	( Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis. Allen, J; De Beule, K; De Marez, T; Diacon, AH; Donald, PR; Kerstens, R; Koul, A; McNeeley, DF; Mthiyane, TC; Patientia, RF; Reddy, C; Rustomjee, R; van Heeswijk, R; Venter, A, 2008)	0.35
"This was a phase 1 pharmacokinetic drug interaction trial."	( Safety, tolerability, and pharmacokinetic interactions of the antituberculous agent TMC207 (bedaquiline) with efavirenz in healthy volunteers: AIDS Clinical Trials Group Study A5267. Allen, R; Aweeka, F; Cramer, Y; Dooley, KE; Flexner, C; Gupta, A; Haas, DW; Lizak, P; Park, JG; Qasba, S; Swindells, S; van Heeswijk, R; Wiggins, I, 2012)	0.6
" Based on data from a phase I, single-dose pharmacokinetic study, a nonlinear mixed-effects model characterizing BDQ pharmacokinetics and interaction with multiple-dose EFV was developed."	( Model-based estimates of the effects of efavirenz on bedaquiline pharmacokinetics and suggested dose adjustments for patients coinfected with HIV and tuberculosis. Aweeka, F; Dooley, KE; Karlsson, MO; Marzan, F; Park, JG; Svensson, EM, 2013)	0.64
" This review summarizes the pharmacokinetic profile of bedaquiline as well as the results of the drug-drug interaction studies."	( Bedaquiline: a review of human pharmacokinetics and drug-drug interactions. Dannemann, B; Hoetelmans, RM; van Heeswijk, RP, 2014)	2.09
" The objective of this study was to develop a population pharmacokinetic (PK) model for bedaquiline to describe the concentration-time data from phase I and II studies in healthy subjects and patients with drug-susceptible or multidrug-resistant tuberculosis (TB)."	( Population pharmacokinetics of bedaquiline (TMC207), a novel antituberculosis drug. Green, B; McLeay, SC; van Heeswijk, RP; Vis, P, 2014)	0.91
" The pharmacokinetic profiles of bedaquiline and M2 were compared over 336 h after the administration of bedaquiline alone and in combination with steady-state rifapentine or rifampin."	( Evaluation of the pharmacokinetic interaction between repeated doses of rifapentine or rifampin and a single dose of bedaquiline in healthy adult subjects. Egizi, E; Erondu, N; Ginsberg, A; Murray, S; Pauli, E; Rouse, DJ; Severynse-Stevens, D; Winter, H, 2015)	0.91
" We have compared non-compartmental analysis (NCA) and model-based predictions of DDIs for long half-life drugs by conducting simulation studies and reviewing published trials, using antituberculosis drug bedaquiline (BDQ) as a model compound."	( Pharmacokinetic Interactions for Drugs with a Long Half-Life—Evidence for the Need of Model-Based Analysis. Acharya, C; Clauson, B; Dooley, KE; Karlsson, MO; Svensson, EM, 2016)	0.62
" Here we aimed to quantify nevirapine and LPV/r drug-drug interaction effects on bedaquiline and M2 in patients co-infected with HIV and multidrug-resistant tuberculosis (MDR-TB) using population pharmacokinetic (PK) analysis and compare these with model-based predictions from single-dose studies in subjects without TB."	( Confirming model-predicted pharmacokinetic interactions between bedaquiline and lopinavir/ritonavir or nevirapine in patients with HIV and drug-resistant tuberculosis. Brill, MJ; Karlsson, MO; Maartens, G; Pandie, M; Svensson, EM, 2017)	0.92
" As CFZ is an inhibitor of the cytochrome P450 isoenzyme 3A4 (CYP3A4) in vitro, and BDQ a substrate of CYP3A4, there is a potential for pharmacokinetic (PK) drug-drug interaction that may result in increased BDQ exposure when co-administered with CFZ, which could increase the toxicity of BDQ."	( Pharmacokinetic interaction between bedaquiline and clofazimine in patients with drug-resistant tuberculosis. Brill, MJE; Maartens, G; Pandie, M; Svensson, EM, 2018)	0.76
"To help fill existing knowledge gaps, we evaluated the pharmacokinetic parameters of novel and repurposed anti-tuberculosis drugs among patients with drug-resistant pulmonary tuberculosis."	( Pharmacokinetics of bedaquiline, delamanid and clofazimine in patients with multidrug-resistant tuberculosis. Al-Shaer, MH; Alghamdi, WA; Barbakadze, K; Kempker, RR; Kipiani, M; Mikiashvili, L; Peloquin, CA, 2021)	0.94
" Being a cytochrome P450 3A substrate, pharmacokinetic interactions of bedaquiline are anticipated with clarithromycin (a cytochrome P450 3A inhibitor), which is routinely used in pulmonary nontuberculous mycobacteria treatment."	( Population Pharmacokinetic Analysis of Bedaquiline-Clarithromycin for Dose Selection Against Pulmonary Nontuberculous Mycobacteria Based on a Phase 1, Randomized, Pharmacokinetic Study. Biewenga, J; Ernault, E; Kambili, C; Kurosawa, K; Ouwerkerk-Mahadevan, S; Rossenu, S; Willems, W, 2021)	1.12
" Given its long terminal half-life and safety concerns, such as QTc-prolongation, re-introducing BDQ after multiple dose interruption is not intuitive and there are currently no existing guidelines."	( A modeling-based proposal for safe and efficacious reintroduction of bedaquiline after dose interruption: A population pharmacokinetics study. Akhondipour Salehabad, Y; Davies Forsman, L; Keutzer, L; Simonsson, USH, 2022)	0.96
"Individuals with rifampicin-resistant pulmonary TB established on a 24 week course of treatment with bedaquiline underwent a lumbar puncture along with multiple blood sample collections over 24 h for CSF and plasma pharmacokinetic assessment, respectively."	( Pharmacokinetics of bedaquiline in cerebrospinal fluid (CSF) in patients with pulmonary tuberculosis (TB). Diacon, AH; Dooley, KE; Maartens, G; Steele, CI; Upton, CM; Wiesner, L, 2022)	1.26
"In this observational cohort study, children aged 6-17 years receiving bedaquiline at recommended doses as part of MDR/RR-TB treatment underwent semi-intensive pharmacokinetic sampling."	( Pharmacokinetics and Safety of Bedaquiline in Human Immunodeficiency Virus (HIV)-Positive and Negative Older Children and Adolescents With Rifampicin-Resistant Tuberculosis. Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Hughes, JA; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; van der Laan, L; Wiesner, L; Winckler, JL, 2022)	1.24
" A bedaquiline pharmacokinetic model was adapted to be allometrically scaled in clearance and volume, centered in the median child population weight."	( Pharmacokinetics and Safety of Bedaquiline in Human Immunodeficiency Virus (HIV)-Positive and Negative Older Children and Adolescents With Rifampicin-Resistant Tuberculosis. Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Hughes, JA; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; van der Laan, L; Wiesner, L; Winckler, JL, 2022)	1.63
" The aims of this analysis were to develop a population pharmacokinetic (PK) model to characterize the concentration-time course of delamanid and DM-6705 in adults with drug-resistant tuberculosis and to explore a potential drug-drug interaction with bedaquiline when coadministered."	( Population Pharmacokinetics of Delamanid and its Main Metabolite DM-6705 in Drug-Resistant Tuberculosis Patients Receiving Delamanid Alone or Coadministered with Bedaquiline. De Los Rios, J; Diacon, AH; Dooley, KE; Karlsson, MO; Maartens, G; Shenje, J; Svensson, EM; Tanneau, L; Upton, CM; Wiesner, L, 2022)	1.1
" Predicted terminal half-life values for delamanid and DM-6705 were 15."	( Population Pharmacokinetics of Delamanid and its Main Metabolite DM-6705 in Drug-Resistant Tuberculosis Patients Receiving Delamanid Alone or Coadministered with Bedaquiline. De Los Rios, J; Diacon, AH; Dooley, KE; Karlsson, MO; Maartens, G; Shenje, J; Svensson, EM; Tanneau, L; Upton, CM; Wiesner, L, 2022)	0.92
" The objective of this work was to predict bedaquiline and pretomanid site-of-action exposures using a translational minimal physiologically based pharmacokinetic (mPBPK) approach to understand the probability of target attainment (PTA)."	( Predictions of Bedaquiline and Pretomanid Target Attainment in Lung Lesions of Tuberculosis Patients using Translational Minimal Physiologically Based Pharmacokinetic Modeling. Guo, T; Mehta, K; van der Graaf, PH; van Hasselt, JGC, 2023)	1.53

Excerpt	Reference	Relevance
"In previous studies, the diarylquinoline R207910 (also known as TMC207) was demonstrated to have high bactericidal activity when combined with first- or second-line antituberculous drugs."	( Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis. Andries, K; Chauffour, A; Ibrahim, M; Jarlier, V; Lounis, N; Truffot-Pernot, C; Veziris, N, 2007)	0.34
" Quantification of the bromine species was accomplished using high performance liquid chromatography coupled to inductively coupled plasma-mass spectrometry (HPLC/ICP-MS) in combination with on-line isotope dilution (on-line ID), while structural elucidation of the species was performed using HPLC coupled to electrospray ionization-mass spectrometry."	( Speciation analysis of bromine-containing drug metabolites in feces samples from a human in vivo study by means of HPLC/ICP-MS combined with on-line isotope dilution. Bockx, M; Cuyckens, F; Laenen, A; Meermann, B; Van Looveren, C; Vanhaecke, F, 2012)	0.38
" Phase I and Phase II studies in healthy subjects and patients with drug-susceptible or multidrug-resistant TB have assessed the pharmacokinetics and drug-drug interaction profile of bedaquiline."	( Bedaquiline: a review of human pharmacokinetics and drug-drug interactions. Dannemann, B; Hoetelmans, RM; van Heeswijk, RP, 2014)	2.04
" Single-dose drug-drug interaction studies found no significant interactions with nevirapine or lopinavir/ritonavir, but these findings could be misleading, especially because of bedaquiline's long terminal t1/2."	( Drug-drug interactions between bedaquiline and the antiretrovirals lopinavir/ritonavir and nevirapine in HIV-infected patients with drug-resistant TB. Conradie, F; Hughes, J; Maartens, G; McIlleron, H; Pandie, M; Siwendu, S; Variava, E; Wiesner, L, 2016)	0.91
" Some severe side effects and drug-drug interactions are associated with the treatment of bedaquiline."	( Assessment of preclinical drug interactions of bedaquiline by a highly sensitive LC-ESI-MS/MS based bioanalytical method. Bhatt, S; Dogra, A; Gour, A; Kotwal, P; Magotra, A; Nandi, U; Sharma, S; Singh, G; Singh, PP; Wazir, P, 2019)	0.99
"We explored the potential synergistic effect of bedaquiline (BDQ) combined with moxifloxacin (MFX), gatifloxacin (GAT), clofazimine (CLO), and linezolid (LZD) for treatment of extensively drug-resistant tuberculosis (XDR-TB)."	( No in vitro synergistic effect of bedaquiline combined with fluoroquinolones, linezolid, and clofazimine against extensively drug-resistant tuberculosis. Chu, N; Dai, G; Dong, L; Huang, H; Huo, F; Jing, W; Li, Y; Lu, J; Pang, Y; Zong, Z, 2019)	1.05
"Our in vitro data demonstrate no observed synergistic effects against XDR-TB for drug combinations that included BDQ in combination with MFX, GAT, LZD, or CLO."	( No in vitro synergistic effect of bedaquiline combined with fluoroquinolones, linezolid, and clofazimine against extensively drug-resistant tuberculosis. Chu, N; Dai, G; Dong, L; Huang, H; Huo, F; Jing, W; Li, Y; Lu, J; Pang, Y; Zong, Z, 2019)	0.79
" The results of our Greco universal response surface analysis showed that CFZ was at least additive with a clear trend towards synergy when combined with PMD, BDQ and LZD against Mtb in all explored metabolic states under in vitro checkerboard assay conditions."	( Evaluating the effect of clofazimine against Mycobacterium tuberculosis given alone or in combination with pretomanid, bedaquiline or linezolid. Almoslem, M; Drusano, GL; Duncanson, B; Kim, S; Louie, A; Myrick, J; Neely, M; Nole, J; Peloquin, CA; Scanga, CA; Schmidt, S; Yamada, W, 2022)	0.93
" Given the prohibitive drug-drug interactions between bedaquiline and rifampin or rifapentine, the BZMRb regimen represents the best opportunity to combine, in one regimen, the treatment-shortening potential of the rifamycin class with that of BZM and deserves high priority for evaluation in clinical trials."	( Novel Regimens of Bedaquiline-Pyrazinamide Combined with Moxifloxacin, Rifabutin, Delamanid and/or OPC-167832 in Murine Tuberculosis Models. Carr, W; Converse, PJ; Dartois, V; Dooley, KE; Garcia, A; Kurbatova, E; Nuermberger, EL; Stout, JE; Tasneen, R; Vernon, AA; Zimmerman, MD, 2022)	1.3
" The aims of this analysis were to develop a population pharmacokinetic (PK) model to characterize the concentration-time course of delamanid and DM-6705 in adults with drug-resistant tuberculosis and to explore a potential drug-drug interaction with bedaquiline when coadministered."	( Population Pharmacokinetics of Delamanid and its Main Metabolite DM-6705 in Drug-Resistant Tuberculosis Patients Receiving Delamanid Alone or Coadministered with Bedaquiline. De Los Rios, J; Diacon, AH; Dooley, KE; Karlsson, MO; Maartens, G; Shenje, J; Svensson, EM; Tanneau, L; Upton, CM; Wiesner, L, 2022)	1.1
" Delpazolid is administered in combination with bedaquiline, delamanid and moxifloxacin."	( A phase IIb, open-label, randomized controlled dose ranging multi-centre trial to evaluate the safety, tolerability, pharmacokinetics and exposure-response relationship of different doses of delpazolid in combination with bedaquiline delamanid moxifloxaci Aarnoutse, R; Boeree, M; Cho, YL; Dierig, A; Geiter, L; Gong, X; Heinrich, N; Hoelscher, M; Hoffmann, L; Jarchow-MacDonald, A; Liyoyo, A; Mbeya, B; McHugh, TD; Mhimbira, FA; Minja, LT; Mpagama, S; Ntinginya, N; Phillips, P; Rassool, M; Schultz, S; Sebe, M; Svensson, EM; Te Brake, L; Wallis, RS; Wildner, LM, 2023)	1.35

Excerpt	Reference	Relevance
" We thought of improving their bioavailability by prodrugs approach."	( Synthesis and antimycobacterial activity of prodrugs of indeno[2,1-c]quinoline derivatives. Bawane, AN; Chattopadhyaya, J; Dixit, SS; Földesi, A; Gitay, PN; Kadam, SA; Kardile, RA; Lahore, SV; Sayyed, AY; Shinde, PD; Upadhayaya, RS, 2011)	0.37
" The model included between-subject variability on apparent clearance (CL/F), apparent central volume of distribution (Vc/F), the fraction of dose via the first input, and bioavailability (F)."	( Population pharmacokinetics of bedaquiline (TMC207), a novel antituberculosis drug. Green, B; McLeay, SC; van Heeswijk, RP; Vis, P, 2014)	0.69
" Bedaquiline should be administered with food, which increases the bioavailability 2-fold."	( Bedaquiline: a novel antitubercular agent for the treatment of multidrug-resistant tuberculosis. Estrada, SJ; Worley, MV, 2014)	2.76
"2h) and low absolute bioavailability (1."	( Novel, potent, orally bioavailable and selective mycobacterial ATP synthase inhibitors that demonstrated activity against both replicating and non-replicating M. tuberculosis. Chaturvedi, V; Dasgupta, A; Gupta, AD; Jaiswal, S; Kashyap, VK; Khan, SR; Krishnan, MY; Lal, J; Roy, KK; Saxena, AK; Sharma, A; Sharma, SK; Singh, S; Sinha, S; Srivastava, R, 2015)	0.42
" CFZ did not have a statistically significant effect on BDQ bioavailability (-9."	( Pharmacokinetic interaction between bedaquiline and clofazimine in patients with drug-resistant tuberculosis. Brill, MJE; Maartens, G; Pandie, M; Svensson, EM, 2018)	0.76
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51
" However, this route of administration passes through the body's first-pass metabolism which reduces the drugs' bioavailability and toxicates the liver and kidneys."	( Active pulmonary targeting against tuberculosis (TB) via triple-encapsulation of Q203, bedaquiline and superparamagnetic iron oxides (SPIOs) in nanoparticle aggregates. Ab Rahman, N; Loo, SCJ; Ostrovski, Y; Pethe, K; Poh, W; Sznitman, J, 2019)	0.74
" Bedaquiline bioavailability was 57% of that in adults."	( Pharmacokinetics and Safety of Bedaquiline in Human Immunodeficiency Virus (HIV)-Positive and Negative Older Children and Adolescents With Rifampicin-Resistant Tuberculosis. Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Hughes, JA; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; van der Laan, L; Wiesner, L; Winckler, JL, 2022)	1.92

Excerpt	Relevance	Reference
" After optimization of the method, HPLC-ICP-MS was applied for metabolite profiling of faeces samples after dosing of (14)C-radiolabelled R207910 to dogs and rats."	( Hyphenation of reverse-phase HPLC and ICP-MS for metabolite profiling--application to a novel antituberculosis compound as a case study. Balcaen, LI; Cuyckens, F; De Samber, B; De Wolf, K; Vanhaecke, F, 2007)	0.34
" All treatments were found to be bactericidal, suggesting that both low and intermittent dosing with R207910 holds promise for leprosy patients."	( The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently. Andaya, CE; Andries, K; Burgos, J; Gelber, R; Paredes, RM, 2009)	0.35
" tuberculosis and following administration of different doses of TMC207 at various dosing frequencies for 6 weeks starting 2 weeks after infection."	( Pharmacokinetics and pharmacodynamics of TMC207 and its N-desmethyl metabolite in a murine model of tuberculosis. Andries, K; Dillen, L; Gevers, T; Gilissen, R; Lounis, N; Raoof, A; Rouan, MC, 2012)	0.38
" Evaluation in clinical trials of adjusted regimens is necessary to ensure appropriate dosing for HIV-infected TB patients on an EFV-based regimen."	( Model-based estimates of the effects of efavirenz on bedaquiline pharmacokinetics and suggested dose adjustments for patients coinfected with HIV and tuberculosis. Aweeka, F; Dooley, KE; Karlsson, MO; Marzan, F; Park, JG; Svensson, EM, 2013)	0.64
" Regimens should contain at least one new class of drug; be broadly applicable for use against MDR and extensively drug-resistant Mycobacterium tuberculosis complex strains; contain three to five effective drugs, each from a different drug class; be delivered orally; have a simple dosing schedule; have a good side-effect profile that allows limited monitoring; last a maximum of 6 months; and have minimal interaction with antiretrovirals."	( Principles for designing future regimens for multidrug-resistant tuberculosis. Balasegaram, M; Brigden, G; du Cros, P; Horsburgh, CR; Hughes, J; McIlleron, H; Mitnick, CD; Nuermberger, E; Nyang'wa, BT; Phillips, PP; Rich, M; Varaine, F, 2014)	0.4
" Efficacious, safe bedaquiline dosing for MDR-TB patients receiving antiretrovirals is important."	( Impact of lopinavir-ritonavir or nevirapine on bedaquiline exposures and potential implications for patients with tuberculosis-HIV coinfection. Dooley, KE; Karlsson, MO; Svensson, EM, 2014)	0.99
" The recommended bedaquiline dosage is 400 mg orally once/day for 2 weeks followed by 200 mg orally 3 times/week for 22 weeks."	( Bedaquiline: a novel antitubercular agent for the treatment of multidrug-resistant tuberculosis. Estrada, SJ; Worley, MV, 2014)	2.18
" Simulations indicated that increasing the bedaquiline dosage to mitigate the interaction would yield elevated M2 concentrations during the first treatment weeks."	( Rifampicin and rifapentine significantly reduce concentrations of bedaquiline, a new anti-TB drug. Dooley, KE; Karlsson, MO; Murray, S; Svensson, EM, 2015)	0.92
" To normalise bedaquiline exposure in patients with concomitant LPV/r therapy, an adjusted bedaquiline dosing regimen is proposed for further study."	( Confirming model-predicted pharmacokinetic interactions between bedaquiline and lopinavir/ritonavir or nevirapine in patients with HIV and drug-resistant tuberculosis. Brill, MJ; Karlsson, MO; Maartens, G; Pandie, M; Svensson, EM, 2017)	1.05
" Intermittent dosing was better tolerated at high doses."	( Dose- and Time-dependency of the Toxicity and Pharmacokinetic Profiles of Bedaquiline and Its N-desmethyl Metabolite in Dogs. De Jonghe, S; Lampo, A; Looszova, A; Mannens, G; Rouan, MC; Smyej, I; Starckx, S; Thijssen, S; Verhaeghe, T, 2017)	0.69
"Subjects were randomly assigned to receive two single 400 mg doses of bedaquiline, alone, and, after a 4 week washout period, in combination with steady-state daily dosing of either rifabutin 300 mg or rifampin 600 mg."	( Mycobactericidal activity of bedaquiline plus rifabutin or rifampin in ex vivo whole blood cultures of healthy volunteers: A randomized controlled trial. Blumer, JL; Good, CE; Griffiss, JM; Healan, A; Jacobs, MR; O'Riordan, MA; Salata, RA; Wallis, RS, 2018)	1.01
" Combined dosing with rifampin or rifabutin produced maximal effects of -0."	( Mycobactericidal activity of bedaquiline plus rifabutin or rifampin in ex vivo whole blood cultures of healthy volunteers: A randomized controlled trial. Blumer, JL; Good, CE; Griffiss, JM; Healan, A; Jacobs, MR; O'Riordan, MA; Salata, RA; Wallis, RS, 2018)	0.77
" Combinations of optimal dose and release rates were simulated such that plasma concentrations were maintained over the epidemiological cut-off or minimum inhibitory concentration for the dosing interval."	( Modelling the long-acting administration of anti-tuberculosis agents using PBPK: a proof of concept study. Flexner, C; Moss, DM; Owen, A; Podany, AT; Rajoli, RKR; Siccardi, M; Swindells, S, 2018)	0.48
" Due to error, dosage received comprised 4 pills of 100 mg every second day in the 60 days following the first two weeks of 4 pills of 100 mg every day."	( Bedaquiline overdose: A case report. Alvarez, V; du Cros, P; Graglia, E; Molfino, L; Rich, M; Telnov, O, 2019)	1.96
" Studies of explanted lungs from patients with drug-resistant tuberculosis have shown substantial drug-specific gradients across pulmonary cavities, suggesting that alternative dosing and drug delivery strategies are needed to reduce functional monotherapy at the site of disease."	( The Lancet Respiratory Medicine Commission: 2019 update: epidemiology, pathogenesis, transmission, diagnosis, and management of multidrug-resistant and incurable tuberculosis. Dheda, K; Dooley, KE; Furin, J; Gumbo, T; Maartens, G; Murray, M; Nardell, EA; Warren, RM, 2019)	0.51
"To externally validate an earlier characterized relationship between bedaquiline exposure and decline in bacterial load in a more difficult-to-treat patient population, and to explore the performances of alternative dosing regimens through simulations."	( Understanding the drug exposure-response relationship of bedaquiline to predict efficacy for novel dosing regimens in the treatment of multidrug-resistant tuberculosis. Karlsson, MO; Svensson, EM; Tanneau, L, 2020)	1.04
" Alternative dosing regimens were simulated for tuberculosis patients with different types of drug resistance."	( Understanding the drug exposure-response relationship of bedaquiline to predict efficacy for novel dosing regimens in the treatment of multidrug-resistant tuberculosis. Karlsson, MO; Svensson, EM; Tanneau, L, 2020)	0.8
" Achievement of the same treatment response for (pre-)XDR TB patients as for MDR TB patients would be possible by adjusting the dose and dosing frequency."	( Understanding the drug exposure-response relationship of bedaquiline to predict efficacy for novel dosing regimens in the treatment of multidrug-resistant tuberculosis. Karlsson, MO; Svensson, EM; Tanneau, L, 2020)	0.8
"The confirmed bedaquiline exposure-response relationship offers the possibility to predict efficacy under alternative dosing regimens, and provides a useful tool for potential treatment optimization."	( Understanding the drug exposure-response relationship of bedaquiline to predict efficacy for novel dosing regimens in the treatment of multidrug-resistant tuberculosis. Karlsson, MO; Svensson, EM; Tanneau, L, 2020)	1.16
" Using C3HeB/FeJ and BALB/c mouse models of tuberculosis disease, thrice-weekly linezolid dosing was compared with daily dosing, with intermittent dosing introduced (i) from treatment initiation or (ii) after an initial period of daily dosing."	( Preserved Efficacy and Reduced Toxicity with Intermittent Linezolid Dosing in Combination with Bedaquiline and Pretomanid in a Murine Tuberculosis Model. Bigelow, KM; Chang, YS; Dooley, KE; Nuermberger, EL; Tasneen, R, 2020)	0.78
"We found a strong association of weight with bedaquiline and clofazimine exposure parameters, suggesting the need for weight-based dosing for those agents."	( Pharmacokinetics of bedaquiline, delamanid and clofazimine in patients with multidrug-resistant tuberculosis. Al-Shaer, MH; Alghamdi, WA; Barbakadze, K; Kempker, RR; Kipiani, M; Mikiashvili, L; Peloquin, CA, 2021)	1.2
" Second, dosing may be optimized through greater understanding of specific factors that may influence observed concentrations, including patient demographics and comorbidities."	( A Scoping Review of the Clinical Pharmacokinetics of Bedaquiline. Wilby, KJ, 2022)	0.97
" Predictions with the final model suggested a similar QT prolonging potential with simplified, once-daily dosing regimens compared with the approved regimens, with a maximum median change from baseline QTcF increase of 20 milliseconds in both regimens."	( Assessing Prolongation of the Corrected QT Interval with Bedaquiline and Delamanid Coadministration to Predict the Cardiac Safety of Simplified Dosing Regimens. Cramer, YS; Diacon, AH; Dooley, KE; Karlsson, MO; Maartens, G; Morganroth, J; Rosenkranz, SL; Shenje, J; Svensson, EM; Tanneau, L; Upton, CM, 2022)	0.97
"The translational mPBPK model predicted that the standard bedaquiline continuation phase and standard pretomanid dosing may not achieve optimal exposures to eradicate non-replicating bacteria in most patients."	( Predictions of Bedaquiline and Pretomanid Target Attainment in Lung Lesions of Tuberculosis Patients using Translational Minimal Physiologically Based Pharmacokinetic Modeling. Guo, T; Mehta, K; van der Graaf, PH; van Hasselt, JGC, 2023)	1.51
" Linezolid dosing and clinical management was provider driven, and most patients had linezolid adjusted by therapeutic drug monitoring."	( Implementation of Bedaquiline, Pretomanid, and Linezolid in the United States: Experience Using a Novel All-Oral Treatment Regimen for Treatment of Rifampin-Resistant or Rifampin-Intolerant Tuberculosis Disease. Andrino, BB; Ashkin, D; Burgos, M; Caloia, LA; Chen, L; Colon-Semidey, A; DeSilva, MB; Dhanireddy, S; Dorman, SE; Dworkin, FF; Easton, AV; Gaensbauer, JT; Ghassemieh, B; Gomez, ME; Goswami, ND; Haley, CA; Hammond-Epstein, H; Horne, D; Jasuja, S; Jones, BA; Kaplan, LJ; Khan, AE; Kracen, E; Labuda, S; Landers, KM; Lardizabal, AA; Lasley, MT; Letzer, DM; Lopes, VK; Lubelchek, RJ; Mihalyov, A; Misch, EA; Murray, JA; Narita, M; Nilsen, DM; Ninneman, MJ; Ogawa, L; Oladele, A; Overman, M; Patricia Macias, C; Peloquin, CA; Peter Cegielski, J; Ray, SM; Ritger, KA; Rowlinson, MC; Sabuwala, N; Schechter, MC; Schiller, TM; Schwartz, LE; Spitters, C; Thomson, DB; Tresgallo, RR; Valois, P, 2023)	1.24
" Use of individualized linezolid dosing and monitoring likely enhanced safety and treatment completion."	( Implementation of Bedaquiline, Pretomanid, and Linezolid in the United States: Experience Using a Novel All-Oral Treatment Regimen for Treatment of Rifampin-Resistant or Rifampin-Intolerant Tuberculosis Disease. Andrino, BB; Ashkin, D; Burgos, M; Caloia, LA; Chen, L; Colon-Semidey, A; DeSilva, MB; Dhanireddy, S; Dorman, SE; Dworkin, FF; Easton, AV; Gaensbauer, JT; Ghassemieh, B; Gomez, ME; Goswami, ND; Haley, CA; Hammond-Epstein, H; Horne, D; Jasuja, S; Jones, BA; Kaplan, LJ; Khan, AE; Kracen, E; Labuda, S; Landers, KM; Lardizabal, AA; Lasley, MT; Letzer, DM; Lopes, VK; Lubelchek, RJ; Mihalyov, A; Misch, EA; Murray, JA; Narita, M; Nilsen, DM; Ninneman, MJ; Ogawa, L; Oladele, A; Overman, M; Patricia Macias, C; Peloquin, CA; Peter Cegielski, J; Ray, SM; Ritger, KA; Rowlinson, MC; Sabuwala, N; Schechter, MC; Schiller, TM; Schwartz, LE; Spitters, C; Thomson, DB; Tresgallo, RR; Valois, P, 2023)	1.24

Role	Description
antitubercular agent	A substance that kills or slows the growth of Mycobacterium tuberculosis and is used in the treatment of tuberculosis.
ATP synthase inhibitor	A mitochondrial respiratory-chain inhibitor that interferes with the action of ATP synthase.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
quinolines	A class of aromatic heterocyclic compounds each of which contains a benzene ring ortho fused to carbons 2 and 3 of a pyridine ring.
naphthalenes	Any benzenoid aromatic compound having a skeleton composed of two ortho-fused benzene rings.
organobromine compound	A compound containing at least one carbon-bromine bond.
aromatic ether	Any ether in which the oxygen is attached to at least one aryl substituent.
tertiary alcohol	A tertiary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has three other carbon atoms attached to it.
tertiary amino compound	A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	18.9991	0.0123	7.9835	43.2770	AID1645841
G	Vesicular stomatitis virus	Potency	3.7908	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2D6	Homo sapiens (human)	Potency	7.5637	0.0010	8.3798	61.1304	AID1645840
Interferon beta	Homo sapiens (human)	Potency	3.7908	0.0033	9.1582	39.8107	AID1645842
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	3.7908	0.0123	8.9648	39.8107	AID1645842
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	Potency	39.8107	0.0096	10.5250	35.4813	AID1479145
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	3.7908	0.0123	8.9648	39.8107	AID1645842
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	3.7908	0.0123	8.9648	39.8107	AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Cytochrome P450 1A2	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0001	1.7740	10.0000	AID1861201
Cytochrome P450 3A4	Homo sapiens (human)	IC50 (µMol)	35.0000	0.0001	1.7536	10.0000	AID1367752; AID1638959; AID1639007; AID1861205
Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2	IC50 (µMol)	4.3600	0.0002	2.4585	9.9600	AID1640021
Cytochrome P450 2D6	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0000	2.0151	10.0000	AID1861204
Cytochrome P450 2C9	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0000	2.8005	10.0000	AID1861202
Cytochrome P450 2C19	Homo sapiens (human)	IC50 (µMol)	5.8000	0.0000	2.3983	10.0000	AID1389805; AID1861203
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	IC50 (µMol)	4.8425	0.0009	1.9014	10.0000	AID1367747; AID1389805; AID1389808; AID1503834; AID1638948; AID1639008; AID1650508; AID1861206
ATP synthase subunit c	Mycolicibacterium smegmatis	IC50 (µMol)	0.0119	0.0025	0.0119	0.0250	AID502989; AID544553; AID544555
Sigma intracellular receptor 2	Rattus norvegicus (Norway rat)	IC50 (µMol)	1.6000	0.0143	1.3756	7.5000	AID1389805
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
ATP synthase subunit c	Bacillus sp. PS3	Kd	0.5000	0.5000	0.5000	0.5000	AID503001
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	EC50 (µMol)	15.0000	0.0019	2.6756	8.0000	AID1726775
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell activation involved in immune response	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway	Interferon beta	Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STAT	Interferon beta	Homo sapiens (human)
response to virus	Interferon beta	Homo sapiens (human)
positive regulation of autophagy	Interferon beta	Homo sapiens (human)
cytokine-mediated signaling pathway	Interferon beta	Homo sapiens (human)
natural killer cell activation	Interferon beta	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT protein	Interferon beta	Homo sapiens (human)
cellular response to interferon-beta	Interferon beta	Homo sapiens (human)
B cell proliferation	Interferon beta	Homo sapiens (human)
negative regulation of viral genome replication	Interferon beta	Homo sapiens (human)
innate immune response	Interferon beta	Homo sapiens (human)
positive regulation of innate immune response	Interferon beta	Homo sapiens (human)
regulation of MHC class I biosynthetic process	Interferon beta	Homo sapiens (human)
negative regulation of T cell differentiation	Interferon beta	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Interferon beta	Homo sapiens (human)
defense response to virus	Interferon beta	Homo sapiens (human)
type I interferon-mediated signaling pathway	Interferon beta	Homo sapiens (human)
neuron cellular homeostasis	Interferon beta	Homo sapiens (human)
cellular response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
cellular response to virus	Interferon beta	Homo sapiens (human)
negative regulation of Lewy body formation	Interferon beta	Homo sapiens (human)
negative regulation of T-helper 2 cell cytokine production	Interferon beta	Homo sapiens (human)
positive regulation of apoptotic signaling pathway	Interferon beta	Homo sapiens (human)
response to exogenous dsRNA	Interferon beta	Homo sapiens (human)
B cell differentiation	Interferon beta	Homo sapiens (human)
natural killer cell activation involved in immune response	Interferon beta	Homo sapiens (human)
adaptive immune response	Interferon beta	Homo sapiens (human)
T cell activation involved in immune response	Interferon beta	Homo sapiens (human)
humoral immune response	Interferon beta	Homo sapiens (human)
positive regulation of T cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
adaptive immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independent	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of T cell anergy	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
defense response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
detection of bacterium	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-12 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of interleukin-6 production	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protection from natural killer cell mediated cytotoxicity	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
innate immune response	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
regulation of dendritic cell differentiation	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class Ib	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 1A2	Homo sapiens (human)
porphyrin-containing compound metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
toxin biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
post-embryonic development	Cytochrome P450 1A2	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
regulation of gene expression	Cytochrome P450 1A2	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
dibenzo-p-dioxin metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 1A2	Homo sapiens (human)
lung development	Cytochrome P450 1A2	Homo sapiens (human)
methylation	Cytochrome P450 1A2	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 1A2	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
cellular respiration	Cytochrome P450 1A2	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
hydrogen peroxide biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 1A2	Homo sapiens (human)
cellular response to cadmium ion	Cytochrome P450 1A2	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 1A2	Homo sapiens (human)
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
coumarin metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
isoquinoline alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of cellular organofluorine metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
arachidonic acid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
urea metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
amide metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
icosanoid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2C9	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C19	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C19	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C19	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C19	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by hormone	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of DNA-templated transcription	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion homeostasis	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cardiac muscle contraction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cellular response to xenobiotic stimulus	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane depolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion import across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inositol phosphate metabolic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
negative regulation of cold-induced thermogenesis	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol phosphate biosynthetic process	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cytokine activity	Interferon beta	Homo sapiens (human)
cytokine receptor binding	Interferon beta	Homo sapiens (human)
type I interferon receptor binding	Interferon beta	Homo sapiens (human)
protein binding	Interferon beta	Homo sapiens (human)
chloramphenicol O-acetyltransferase activity	Interferon beta	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
signaling receptor binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
peptide antigen binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
TAP binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
protein-folding chaperone binding	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 1A2	Homo sapiens (human)
iron ion binding	Cytochrome P450 1A2	Homo sapiens (human)
protein binding	Cytochrome P450 1A2	Homo sapiens (human)
electron transfer activity	Cytochrome P450 1A2	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 1A2	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 1A2	Homo sapiens (human)
enzyme binding	Cytochrome P450 1A2	Homo sapiens (human)
heme binding	Cytochrome P450 1A2	Homo sapiens (human)
demethylase activity	Cytochrome P450 1A2	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 1A2	Homo sapiens (human)
aromatase activity	Cytochrome P450 1A2	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 1A2	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 1A2	Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activity	Cytochrome P450 1A2	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
3'-5'-RNA exonuclease activity	Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2
RNA-dependent RNA polymerase activity	Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2
cysteine-type endopeptidase activity	Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2
mRNA 5'-cap (guanine-N7-)-methyltransferase activity	Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2
mRNA (nucleoside-2'-O-)-methyltransferase activity	Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2
mRNA guanylyltransferase activity	Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2
RNA endonuclease activity, producing 3'-phosphomonoesters	Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2
ISG15-specific peptidase activity	Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2
5'-3' RNA helicase activity	Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2
protein guanylyltransferase activity	Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2
monooxygenase activity	Cytochrome P450 2D6	Homo sapiens (human)
iron ion binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2D6	Homo sapiens (human)
heme binding	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 2C9	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C9	Homo sapiens (human)
heme binding	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C9	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C19	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C19	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C19	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
oxygen binding	Cytochrome P450 2C19	Homo sapiens (human)
enzyme binding	Cytochrome P450 2C19	Homo sapiens (human)
heme binding	Cytochrome P450 2C19	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C19	Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activity	Cytochrome P450 2C19	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C19	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C19	Homo sapiens (human)
transcription cis-regulatory region binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ubiquitin protein ligase binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
identical protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein homodimerization activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
C3HC4-type RING finger domain binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
scaffold protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol heptakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
protein binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
ATP binding	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 1-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol hexakisphosphate 3-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activity	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
extracellular space	Interferon beta	Homo sapiens (human)
extracellular region	Interferon beta	Homo sapiens (human)
Golgi membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endoplasmic reticulum	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
Golgi apparatus	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
cell surface	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
ER to Golgi transport vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
secretory granule membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
phagocytic vesicle membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
early endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
recycling endosome membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular exosome	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
lumenal side of endoplasmic reticulum membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
MHC class I protein complex	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
extracellular space	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
external side of plasma membrane	HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 1A2	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 1A2	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 1A2	Homo sapiens (human)
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
double membrane vesicle viral factory outer membrane	Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2
mitochondrion	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2D6	Homo sapiens (human)
cytoplasm	Cytochrome P450 2D6	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C19	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C19	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C19	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C19	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C19	Homo sapiens (human)
virion membrane	Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cell surface	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
perinuclear region of cytoplasm	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
fibrillar center	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytosol	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
nucleus	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
cytoplasm	Inositol hexakisphosphate kinase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (446)

Assay ID	Title	Year	Journal	Article
AID502972	Antimicrobial activity against Mycobacterium tuberculosis by alamar blue assay	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1650518	Protein binding in human plasma	2020	Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1	Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.
AID503006	Binding affinity to Bacillus PS3 ATP synthase subunit beta by mass spectroscopy	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1900066	AUC in mouse at 100 mg/kg, po administered as single dose	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Synthesis and structure-activity relationships for a new class of tetrahydronaphthalene amide inhibitors of Mycobacterium tuberculosis.
AID1900064	Intrinsic clearance in mouse liver microsomes	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Synthesis and structure-activity relationships for a new class of tetrahydronaphthalene amide inhibitors of Mycobacterium tuberculosis.
AID529105	Cardiotoxicity in pulmonary tuberculosis patient assessed as increase in QT interval at 400 mg/kg, po once daily for 7 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1639015	AUC (0 to infinity) in po dosed mouse	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
AID502980	Ratio of MIC for Mycobacterium tuberculosis H37Rv isolate LV13 expressing ATP synthase atpE I66M mutant protein to MIC for Mycobacterium tuberculosis H37Rv	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1503834	Inhibition of human ERG
AID1861199	Microsomal stability in rat liver microsomes assessed as clearance	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1483726	Inhibition of oxygen consumption in Mycobacterium smegmatis inverted membrane vesicles lacking cytochrome bc1 complex treated between 250 to 450 secs post NADH addition	2017	Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4	Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis.
AID283244	Reduction of lung lesions in Mycobacterium tuberculosis H37Rv infected Swiss mouse at 25 mg/kg, po for 5 days/week after 2 months	2007	Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3	Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis.
AID1154327	Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 5 days by standard microdilution method	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID544557	Inhibition of human ATP synthase mediated ATP production at 100 nM	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue.
AID565299	Antitubercular activity against Mycobacterium avium infected in C57BL/6J mouse assessed as reduction of CFU counts in spleen at 200 mg/kg, po administered one month post-infection five times weekly for 2 months (Rvb = 9.4 +/- 0.2 log10CFU)	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	ATP synthase inhibition of Mycobacterium avium is not bactericidal.
AID1389804	Inhibition of CYP3A4 in human liver microsomes after 20 mins	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.
AID1194570	Antimycobacterial activity against Mycobacterium tuberculosis H37Rv expressing Lux assessed as reduction in growth measured after 3 weeks by bioluminescence assay	2015	Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9	Design and synthesis of novel anti-tuberculosis agents from the celecoxib pharmacophore.
AID698993	Cmax in human at 10 mg, po	2012	European journal of medicinal chemistry, May, Volume: 51	Tuberculosis: the drug development pipeline at a glance.
AID529093	Steady-state plasma concentration in pulmonary tuberculosis patient at 25 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID528932	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 100 mg/kg, po once daily measured after 2 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID525522	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 5 expressing wild type atpE Ile66Met mutant selected after 30 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID1861226	Drug concentration in CD-1 mouse plasma at 6.25 mg/kg,po measured after 96 hrs	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID528931	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 100 mg/kg, po once daily measured after 1 day	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID544545	Inhibition of ATP synthase mediated ATP production in human OVCAR3 cells	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue.
AID528965	Drug uptake in pulmonary tuberculosis patient at 100 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID562292	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 25 mg/kg, po administered once monthly during logarithmic multiplication from day 60 to day 150 post infection measured on day 152 p	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1367750	Growth inhibition of Mycobacterium tuberculosis H37Rv under aerobic condition after 4 days by MABA method	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23	Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units.
AID528928	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 25 mg/kg, po once daily measured after 5 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1181170	Antimicrobial activity against second mutant generation Mycobacterium tuberculosis 1024_8.12 assessed as fold shift in MIC relative to parent strain	2014	Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15	Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID528926	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 25 mg/kg, po once daily measured after 3 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID372788	Antimicrobial activity against Mycobacterium intracellular 14 after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1861227	Ratio of drug concentration in CD-1 mouse lung to plasma at 6.25 mg/kg,po measured after 96 hrs	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1888139	Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate HD5 assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay	2022	European journal of medicinal chemistry, Jan-05, Volume: 227	Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID780666	Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as parasite growth inhibition	2013	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22	Rational drug design based synthesis of novel arylquinolines as anti-tuberculosis agents.
AID1698409	Inhibition of human ATPsynthase	2020	Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22	Synthesis and structure-activity relationships for tetrahydroisoquinoline-based inhibitors of Mycobacterium tuberculosis.
AID372662	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1367748	Intrinsic clearance in human liver microsomes at 1 mg/ml after 60 mins	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23	Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units.
AID1726777	Antitubercular activity against Mycobacterium tuberculosis H37Rv by broth microdilution method	2021	RSC medicinal chemistry, Jun-23, Volume: 12, Issue:6	Synthesis and evaluation of pyridine-derived bedaquiline analogues containing modifications at the A-ring subunit.
AID562285	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 6 mg/kg, po administered 5 times weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 152	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID698990	AUC at steady state (0 to 24 hrs) in human at 400 mg, po qd for 14 days	2012	European journal of medicinal chemistry, May, Volume: 51	Tuberculosis: the drug development pipeline at a glance.
AID1389810	Antitubercular activity against Mycobacterium tuberculosis Erdman infected in BALB/c mouse assessed as reduction in bacterial burden in lungs at 20 mg/kg, po qd for 12 continuous days from day 11 post infection measured on day 25 relative to 10 mg/kg beda	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.
AID1639013	Clearance in iv dosed mouse	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
AID529099	Toxicity in pulmonary tuberculosis patient assessed as rash at 100 mg/kg, po once daily	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1265239	Antituberculosis activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days	2015	European journal of medicinal chemistry, Dec-01, Volume: 106	Structure activity relationships of 4-hydroxy-2-pyridones: A novel class of antituberculosis agents.
AID1580694	Inhibition of ATP-synthase (unknown origin)	2019	Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23	Changing the Rules of TB-Drug Discovery.
AID1861212	Oral bioavailability in mouse at 6.25 mg/kg	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1861215	Half life in Sprague-Dawley rat at 1 mg/kg,iv	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID562298	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 6 mg/kg, po administered 5 times weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 228	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1639007	Inhibition of CYP3A4 (unknown origin)	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
AID1650520	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by MTS-PBS assay	2020	Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1	Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.
AID372803	Antimicrobial activity against Mycobacterium conspicuum after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID739412	Antitubercular activity against Mycobacterium tuberculosis H37Rv	2013	Journal of medicinal chemistry, May-23, Volume: 56, Issue:10	Preliminary structure-activity relationships and biological evaluation of novel antitubercular indolecarboxamide derivatives against drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID503001	Binding affinity to Bacillus PS3 ATP synthase subunit c	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1900065	Intrinsic clearance in human liver microsomes	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Synthesis and structure-activity relationships for a new class of tetrahydronaphthalene amide inhibitors of Mycobacterium tuberculosis.
AID562468	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 100 mg/kg, po administered once weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 302 t	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1861204	Inhibition of CYP2D6 (unknown origin)	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID372805	Antimicrobial activity against Mycobacterium xenopi after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID562470	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 120 mg/kg, po administered once monthly during logarithmic multiplication from day 60 to day 150 post infection measured on day 302	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID562290	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 50 mg/kg, po administered once weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 152 po	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1883682	Potency index, ratio of Suda-pyridine MIC90 to test compound MIC90 for antibacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth	2022	Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11	Tuberculosis Drug Discovery: Challenges and New Horizons.
AID1650506	Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition under replicating, aerobic condition by microplate Alamar blue assay	2020	Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1	Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.
AID502986	Antimicrobial activity against Mycobacterium smegmatis expressing ATP synthase AtpE D32V mutant protein by 7H9 agar dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1603257	Antibacterial activity against INH-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay
AID502975	Antimicrobial activity against Mycobacterium tuberculosis H37Rv isolate LV13 expressing ATP synthase atpE I66M mutant protein by 7H9 broth dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID565301	Antimicrobial activity against Mycobacterium avium	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	ATP synthase inhibition of Mycobacterium avium is not bactericidal.
AID544541	Antimicrobial activity against Mycobacterium tuberculosis	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue.
AID565298	Antitubercular activity against Mycobacterium avium infected in C57BL/6J mouse assessed as reduction of CFU counts in spleen at 25 mg/kg, po administered one month post-infection five times weekly for 1 month (Rvb = 7.4 +/- 1.7 log10CFU)	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	ATP synthase inhibition of Mycobacterium avium is not bactericidal.
AID562307	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 100 mg/kg, po administered once monthly during logarithmic multiplication from day 60 to day 150 post infection measured on day 228	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1367749	Half life in human liver microsomes	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23	Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units.
AID1659808	Antimycobacterial activity against Mycobacterium smegmatis	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17	Molecule Property Analyses of Active Compounds for
AID372661	Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis isolate after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID528933	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 100 mg/kg, po once daily measured after 3 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID528942	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 400 mg/kg, po once daily measured after 5 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID529097	Toxicity in pulmonary tuberculosis patient assessed as hemoptysis at 400 mg/kg, po once daily	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1389806	Intrinsic clearance in human liver microsomes at 1 uM after 60 mins	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.
AID1650516	Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse model of acute infection assessed as log reduction in bacterial burden in lung at 20 mg/kg, po via gavage administered as single dose for 12 days starting from 10	2020	Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1	Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.
AID1861187	Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as mycobacterial growth inhibition by microplate alamar blue assay	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID502989	Inhibition of Mycobacterium smegmatis ATCC 607 ATP synthase subunit c-mediated ATP synthesis after 60 mins by luminometry	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID529080	Drug uptake in pulmonary tuberculosis patient at 400 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID544563	Inhibition of ATP synthase in bovine heart mitochondria assessed as effect on oxygen consumption at 175 uM	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue.
AID669834	Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate alamar blue assay	2012	Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8	Discovery of selective menaquinone biosynthesis inhibitors against Mycobacterium tuberculosis.
AID562287	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 25 mg/kg, po administered 5 times weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 152	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1181171	Antimicrobial activity against second mutant generation Mycobacterium tuberculosis 1024_16.5 assessed as fold shift in MIC relative to parent strain	2014	Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15	Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID1821091	Antibacterial activity against Mycobacterium tuberculosis mc2 6230 assessed as bacterial growth inhibition incubated for 5 days by resazurin microtiter assay
AID502984	Ratio of MIC for Mycobacterium smegmatis isolate R09 expressing ATP synthase AtpE D32V mutant protein to MIC for wild type Mycobacterium smegmatis	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID581002	Antimicrobial activity against compound-susceptible Mycobacterium tuberculosis	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID1861193	Apparent permeability across apical side to basolateral side in dog MDCK cells	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1639009	Aqueous solubility of the compound at pH 7.4	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
AID502973	Antimicrobial activity against Mycobacterium bovis BCG by alamar blue assay	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1888135	Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate HD1 assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay	2022	European journal of medicinal chemistry, Jan-05, Volume: 227	Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID529083	Cmin in pulmonary tuberculosis patient at 400 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID525531	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 2 expressing atpE Glu61Asp mutant selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID502971	Antimicrobial activity against Mycobacterium smegmatis ATCC 607 by alamar blue assay	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID525520	Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis H37Rv expressing wild type atpE Ala63Pro mutant selected after 30 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID529091	AUC (0 to 24 hrs) in pulmonary tuberculosis patient at 100 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID562306	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 50 mg/kg, po administered once monthly during logarithmic multiplication from day 60 to day 150 post infection measured on day 228 p	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID581000	Tmax in human	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID528959	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 25 mg/kg, po once daily measured on day 8 after starting standard TB therapy	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID372779	Antimicrobial activity against Mycobacterium avium 6 after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1639014	Apparent volume of distribution during terminal phase in iv dosed mouse	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
AID604585	Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 16 to 24 hrs by microplate alamar blue assay	2011	European journal of medicinal chemistry, Apr, Volume: 46, Issue:4	Synthesis and antimycobacterial activity of prodrugs of indeno[2,1-c]quinoline derivatives.
AID502988	Ratio of MIC for Mycobacterium smegmatis expressing ATP synthase AtpE D32V mutant protein to MIC for wild type Mycobacterium smegmatis ATCC 607 expressing vector pSD5	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1888136	Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate HD2 assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay	2022	European journal of medicinal chemistry, Jan-05, Volume: 227	Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID1181169	Antimicrobial activity against second mutant generation Mycobacterium tuberculosis 1024_18 assessed as fold shift in MIC relative to parent strain	2014	Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15	Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID1639008	Inhibition of human ERG	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
AID1861239	AUC in Sprague-Dawley rat at 200 mg/kg,po measured after 12 days	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1367751	Antitubercular activity against Mycobacterium tuberculosis H37Rv incubated for 10 days in non-replicating anaerobic condition followed by incubation for 28 hrs in ambient gaseous condition measured after day 11 by LORA assay	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23	Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units.
AID528941	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 400 mg/kg, po once daily measured after 4 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1861225	Drug concentration in CD-1 mouse lung at 6.25 mg/kg,po measured after 96 hrs	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1389808	Inhibition of human ERG assessed as prolongation of QT interval	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.
AID521903	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 5 expressing wild type atpE and F0 operon selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID372806	Antimicrobial activity against Mycobacterium shimoidei after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID502998	Antimicrobial activity against wild-type Mycobacterium tuberculosis expressing ATP synthase AtpE assessed as growth inhibition in early log-phase by 7H10 agar dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1861198	Microsomal stability in human liver microsomes assessed as clearance	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID372784	Antimicrobial activity against Mycobacterium avium 21 after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1639005	Antitubercular activity against Mycobacterium tuberculosis H37Rv incubated for 10 days in non-replicating anaerobic condition followed by incubation for 28 hrs in ambient gaseous condition and measured after day 11 by LORA assay	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
AID1726774	Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition incubated for 5 days by resazurin microtiter assay	2021	RSC medicinal chemistry, Jun-23, Volume: 12, Issue:6	Synthesis and evaluation of pyridine-derived bedaquiline analogues containing modifications at the A-ring subunit.
AID544551	Inhibition of ATP synthase mediated ATP production in human OVCAR3 cells at 1 uM	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue.
AID502982	Antimicrobial activity against wild type Mycobacterium smegmatis ATCC 607 by 7H9 agar dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1483722	Selectivity ratio of IC50 for NDH2 in Mycobacterium smegmatis inverted membrane vesicles using NADH as substrate to IC50 for SDH in Mycobacterium smegmatis inverted membrane vesicles using succinate as substrate	2017	Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4	Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis.
AID372791	Antimicrobial activity against Mycobacterium mageritense after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1639017	Protein binding in human plasma	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
AID1861242	Toxicity in Beagle dog assessed as effect on electrocardiogram at 200 mg/kg,po	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1638951	Intrinsic clearance in human liver microsomes	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.
AID1162176	Antitubercular activity against Mycobacterium tuberculosis assessed as growth inhibition by alamar blue assay	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	SAR analysis of new anti-TB drugs currently in pre-clinical and clinical development.
AID544549	Inhibition of ATP synthase mediated ATP production in human OVCAR3 cells at 5 uM	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue.
AID1743152	Inhibition of ATP synthase in bedaquiline-resistant Mycobacterium tuberculosis assessed as reduction in bacterial growth incubated for 7 days by microplate alamar blue assay	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Design, synthesis and biological evaluation of diamino substituted cyclobut-3-ene-1,2-dione derivatives for the treatment of drug-resistant tuberculosis.
AID525533	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 1 expressing atpE Glu63Asp mutant selected after 30 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID562300	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 25 mg/kg, po administered 5 times weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 228	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1861205	Inhibition of CYP3A4 (unknown origin)	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1639010	Intrinsic clearance in human liver microsomes assessed per mg protein	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
AID502999	Antimicrobial activity against wild-type Mycobacterium tuberculosis isolate BK12 expressing ATP synthase AtpE A63P mutant protein assessed as growth inhibition in early log-phase by 7H10 agar dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID544559	Selectivity index, ratio of IC50 for human ATP synthase to IC50 for Mycobacterium smegmatis ATP synthase subunit c	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue.
AID765269	fT>MIC in Mycobacterium tuberculosis infected mouse	2013	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17	A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID525513	Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis isolate 4 expressing wild type atpE Glu61Asp mutant selected after 30 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID1685617	Inhibition of cytochrome-bd oxidase in Mycobacterium bovis BCG assessed as replicating ATP by measuring ATP depletion incubated for 15 hrs in absence of Q203 by BacTiter-Glo luminescence assay	2021	RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1	Structure guided generation of thieno[3,2-
AID525521	Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis H37Rv expressing wild type atpE selected after 30 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID698992	AUC at steady state (0 to 24 hrs) in human at 150 mg, po qd for 14 days	2012	European journal of medicinal chemistry, May, Volume: 51	Tuberculosis: the drug development pipeline at a glance.
AID1638958	Ratio of AUC in mouse to MIC90 of replicating Mycobacterium tuberculosis H37Rv after 4 days by Alamar blue assay	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.
AID1192645	Inhibition of human ERG channel	2015	Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4	Novel, potent, orally bioavailable and selective mycobacterial ATP synthase inhibitors that demonstrated activity against both replicating and non-replicating M. tuberculosis.
AID562469	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 50 mg/kg, po administered once monthly during logarithmic multiplication from day 60 to day 150 post infection measured on day 302 t	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1861233	Antimycobacterial activity against Mycobacterium tuberculosis infected by aerosol in mouse chronic infection model assessed as reduction in colony forming unit in lungs at 5 mg/kg, po treated 5 days per week from day 28 to day 58 post infection	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID765271	fAUC/MIC in Mycobacterium tuberculosis infected mouse	2013	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17	A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID283235	Reduction of bacterial counts in Mycobacterium tuberculosis H37Rv infected Swiss mouse lung at 25 mg/kg, po for 5 days/week after 1 month	2007	Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3	Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis.
AID502981	Ratio of MIC for Mycobacterium tuberculosis H37Rv isolate BK12 expressing ATP synthase atpE A63P mutant protein to MIC for Mycobacterium tuberculosis H37Rv	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1389796	Antitubercular activity against Mycobacterium tuberculosis H37Rv after 24 hrs under aerobic condition by MABA	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.
AID525535	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 1 expressing atpE Glu61Asp mutant selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID1900061	Inhibition of Mycobacterium smegmatis ATP synthase	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Synthesis and structure-activity relationships for a new class of tetrahydronaphthalene amide inhibitors of Mycobacterium tuberculosis.
AID502994	Antimicrobial activity against wild-type Mycobacterium smegmatis ATCC 607 expressing ATP synthase AtpE subunit by 7H10 agar dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID525517	Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis isolate 6 expressing wild type atpE selected after 30 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID1375999	Inhibition of Mycobacterium tuberculosis H37Rv cytochrome bc1 oxidase assessed as reduction in ATP level measured up to 24 hrs under anaerobic condition	2016	MedChemComm, Nov-01, Volume: 7, Issue:11	SAR and identification of 2-(quinolin-4-yloxy)acetamides as
AID503005	Binding affinity to Bacillus PS3 ATP synthase subunit alpha by mass spectroscopy	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1772301	Non-covalent inhibition of DprE1 in Mycobacterium tuberculosis H37Rv measured after 7 days by microplate Alamar blue assay
AID1154349	Antimycobacterial activity against Mycobacterium tuberculosis over expressing TopA after 5 days by standard microdilution method	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1638955	AUC in mouse	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.
AID1639006	Cytotoxicity against African green monkey Vero cells measured after 72 hrs by MTT assay	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
AID1861234	Antimycobacterial activity against Mycobacterium tuberculosis infected by aerosol in mouse chronic infection model assessed as reduction in colony forming unit in lungs at 20 mg/kg, po treated 5 days per week from day 28 to day 58 post infection	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1154352	Antimycobacterial activity against TMC207R-resistant Mycobacterium tuberculosis clone 8.1 over expressing DprE1 mutant after 5 days by standard microdilution method	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID372785	Antimicrobial activity against Mycobacterium avium 23 after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1897864	Bactericidal activity against Non-replicating Mycobacterium tuberculosis ss18b-lux model assessed as decrease in luminescence at 10 to 10000 nM
AID1367746	Terminal half life in healthy human subjects dosed as single 400 mg dose on Day 1 followed by PK sampling (Days 1 to 14)	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23	Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units.
AID502990	Antimicrobial activity against wild type Mycobacterium smegmatis ATCC 607 by 7H10 agar dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID525532	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 2 expressing atpE Ala28Val mutant selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID1861200	Microsomal stability in mouse liver microsomes assessed as clearance	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID525525	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 3 expressing wild type atpE and F0 operon selected after 30 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID529087	Tmax in pulmonary tuberculosis patient at 25 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1154353	Antimycobacterial activity against moxifloxacin-resistant Mycobacterium tuberculosis clone 4.1 over expressing DprE1 mutant after 5 days by standard microdilution method	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID525526	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 3 expressing wild type atpE selected after 30 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID502974	Antimicrobial activity against Mycobacterium tuberculosis H37Rv by 7H9 broth dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID562288	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 25 mg/kg, po administered once weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 152 po	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1181172	Antimicrobial activity against second mutant generation Mycobacterium tuberculosis 1024_16.6 assessed as fold shift in MIC relative to parent strain	2014	Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15	Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID1639011	Intrinsic clearance in mouse liver microsomes assessed per mg protein	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
AID1154350	Antimycobacterial activity against Mycobacterium tuberculosis over expressing PimA after 5 days by standard microdilution method	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID529096	Toxicity in pulmonary tuberculosis patient assessed as hemoptysis at 100 mg/kg, po once daily	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1638960	Protein binding in human plasma	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.
AID370056	Antimycobacterial activity against Mycobacterium tuberculosis	2005	Antimicrobial agents and chemotherapy, Jun, Volume: 49, Issue:6	New small-molecule synthetic antimycobacterials.
AID1650508	Inhibition of human ERG	2020	Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1	Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.
AID1861202	Inhibition of CYP2C9 (unknown origin)	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID544555	Inhibition of Mycobacterium smegmatis MC2 155 ATP synthase subunit c-mediated ATP production at 100 nM	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue.
AID1483723	Selectivity ratio of IC50 for NADH dependent ATP synthesis in Mycobacterium smegmatis inverted membrane vesicles lacking cytochrome-bc1 complex to IC50 for cytochrome c oxidase in Mycobacterium smegmatis inverted membrane vesicles assessed as decrease in	2017	Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4	Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis.
AID565294	Antitubercular activity against Mycobacterium avium infected in C57BL/6J mouse assessed as reduction of CFU counts in spleen at 150 mg/kg, sc administered one month post-infection five times weekly for 3 months (Rvb = 7.9 +/- 0.7 log10CFU)	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	ATP synthase inhibition of Mycobacterium avium is not bactericidal.
AID1603259	Selectivity index, ratio of IC50 for African green monkey Vero cells to MIC>=90 for Mycobacterium tuberculosis H37Rv
AID1638948	Inhibition of human ERG by manual patch clamp electrophysiology assay	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.
AID372798	Antimicrobial activity against Mycobacterium scrofulaceum after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1861211	AUC (0 to last) in mouse at 6.25 mg/kg,po	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID529088	Tmax in pulmonary tuberculosis patient at 100 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID310930	Antituberculosis activity against Mycobacterium tuberculosis	2007	Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7	Antituberculosis drugs: ten years of research.
AID525510	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis H37Rv	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID1861191	Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis assessed as mycobacterial growth inhibition	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID529095	Steady-state plasma concentration in pulmonary tuberculosis patient at 400 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID372889	Antimicrobial activity against Mycobacterium avium 2 after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID525536	Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis H37Rv	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID372663	Antimicrobial activity against Mycobacterium avium complex isolate after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID372801	Antimicrobial activity against Mycobacterium szulgai after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1616089	Selectivity index, ratio of CC50 for human HepG2 cells to MIC of Mycobacterium tuberculosis H37Rv	2019	European journal of medicinal chemistry, Nov-15, Volume: 182	Recent advancements in mechanistic studies and structure activity relationship of F
AID372792	Antimicrobial activity against Mycobacterium phlei after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1577421	Antitubercular activity against Mycobacterium tuberculosis H37Rv	2019	Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17	Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID1678479	Inhibition of recombinant His6-tagged SARS-CoV-2 main protease using Dabcyl-KTSAVLQ-SGFRKM-E(Edans-NH2) as substrate preincubated for 15 mins followed by substrate addition by FRET based assay	2020	ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12	Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2.
AID1861196	Plasma protein binding in human assessed as bound fraction	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID372795	Antimicrobial activity against Mycobacterium malmoense after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1897848	Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in human A-THP1 macrophages assessed as viability of infected macrophages incubated for 96 hrs by fluorescence microplate assay
AID372780	Antimicrobial activity against Mycobacterium avium 8 after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID503003	Binding affinity to Mycobacterium smegmatis ATCC 607 ATP synthase subunit alpha by mass spectroscopy	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1638947	Cytotoxicity against African green monkey Vero cells after 72 hrs by MTS-PMS assay	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.
AID1883681	Antibacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth	2022	Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11	Tuberculosis Drug Discovery: Challenges and New Horizons.
AID525523	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 5 expressing wild type atpE Ala63Pro mutant selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID529084	Cmax in pulmonary tuberculosis patient at 25 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID372799	Antimicrobial activity against Mycobacterium hiberniae after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID502978	Antimicrobial activity against Mycobacterium tuberculosis H37Rv isolate LV13 expressing ATP synthase atpE I66M mutant protein by 7H10 broth dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1603258	Cytotoxicity against African green monkey Vero cells measured after 72 hrs by CellTiter 96 aqueous non-radioactive cell proliferation assay
AID1476362	Antitubercular activity against bedaquiline resistant Mycobacterium tuberculosis H37Rv after 24 hrs by MABA method	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID765268	T>MIC in Mycobacterium tuberculosis infected mouse	2013	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17	A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID544567	Inhibition of ATP synthase in bovine heart mitochondria assessed as inhibition of oxygen consumption	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue.
AID1698407	Metabolic stability in mouse liver microsomes assessed as intrinsic clearance	2020	Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22	Synthesis and structure-activity relationships for tetrahydroisoquinoline-based inhibitors of Mycobacterium tuberculosis.
AID1678478	Inhibition of recombinant His6-tagged SARS-CoV-2 main protease assessed as residual enzyme activity at 100 uM using Dabcyl-KTSAVLQ-SGFRKM-E(Edans-NH2) as substrate preincubated for 15 mins followed by substrate addition by FRET based assay relative to con	2020	ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12	Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2.
AID1616093	Inhibition of ATP synthase in Mycobacterium smegmatis	2019	European journal of medicinal chemistry, Nov-15, Volume: 182	Recent advancements in mechanistic studies and structure activity relationship of F
AID1861214	Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg,iv	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID529110	Bactericidal activity against Mycobacterium tuberculosis selected on 100 times compound MIC measured after 6 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1861229	Drug concentration in Sprague-Dawley rat plasma at 5 mg/kg,po measured after 96 hrs	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID529100	Toxicity in pulmonary tuberculosis patient assessed as diarrhea at 400 mg/kg, po once daily	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID503000	Antimicrobial activity against wild-type Mycobacterium tuberculosis isolate LV13 expressing ATP synthase AtpE I66M mutant protein assessed as growth inhibition in early log-phase by 7H10 agar dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1685619	Inhibition of cytochrome-bd oxidase in Mycobacterium tuberculosis H37Rv assessed as replicating ATP by measuring ATP depletion incubated for 15 hrs in absence of Q203 by BacTiter-Glo luminescence assay	2021	RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1	Structure guided generation of thieno[3,2-
AID1483725	Inhibition of cytochrome c oxidase in Mycobacterium smegmatis inverted membrane vesicles lacking cytochrome-bd complex assessed as reduction of oxygen consumption treated between 250 to 450 secs post NADH addition	2017	Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4	Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis.
AID1162175	Antitubercular activity against drug-susceptible Mycobacterium tuberculosis clinical isolates assessed as growth inhibition	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	SAR analysis of new anti-TB drugs currently in pre-clinical and clinical development.
AID544565	Inhibition of ATP synthase in M18 mouse liver mitochondria assessed as inhibition of oxygen consumption	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue.
AID562305	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 25 mg/kg, po administered once monthly during logarithmic multiplication from day 60 to day 150 post infection measured on day 228 p	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID528927	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 25 mg/kg, po once daily measured after 4 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1580695	Inhibition of Mycobacterium phlei DSM-43239 C-terminal ATP-synthase assessed as reduction in luciferase activity incubated for 10 mins in presence of ATP by luminometric method	2019	Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23	Changing the Rules of TB-Drug Discovery.
AID1638953	Clearance in iv dosed mouse	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.
AID1389803	Half life in human liver microsomes at 1 uM in presence of CYP3A4 inhibitor ketoconazole	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.
AID529092	AUC (0 to 24 hrs) in pulmonary tuberculosis patient at 400 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1861192	Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis assessed as mycobacterial growth inhibition	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID372790	Antimicrobial activity against Mycobacterium fortuitum after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1162172	Antitubercular activity against drug-resistant Mycobacterium tuberculosis clinical isolates assessed as growth inhibition	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	SAR analysis of new anti-TB drugs currently in pre-clinical and clinical development.
AID1888138	Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate HD4 assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay	2022	European journal of medicinal chemistry, Jan-05, Volume: 227	Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID1900067	Half-life in mouse at 100 mg/kg, po administered as single dose	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Synthesis and structure-activity relationships for a new class of tetrahydronaphthalene amide inhibitors of Mycobacterium tuberculosis.
AID1698406	Metabolic stability in human liver microsomes assessed as intrinsic clearance	2020	Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22	Synthesis and structure-activity relationships for tetrahydroisoquinoline-based inhibitors of Mycobacterium tuberculosis.
AID1389799	Kinetic solubility of the compound in pH 7.4 KH2PO4/KOAc/KCl buffer	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.
AID1638959	Inhibition of CYP3A4 (unknown origin)	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.
AID372800	Antimicrobial activity against Mycobacterium interjectum after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID529106	Cardiotoxicity in pulmonary tuberculosis patient assessed as increase in QT interval at 25 mg/kg, po once daily for 7 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1389800	Protein binding in human plasma	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.
AID525519	Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis Mycobacterium tuberculosis H37Rv expressing wild type atpE and F0 operon selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID562467	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 50 mg/kg, po administered once weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 302 to	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID529086	Cmax in pulmonary tuberculosis patient at 400 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1650512	Clearance in CD-1 mouse at 2 to 3 mg/kg, iv administered as single bolus dose	2020	Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1	Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.
AID1601486	Antimycobacterial activity against Mycobacterium bovis assessed as 90 percent growth inhibition measured after 120 hrs by turbidometric analysis	2019	Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20	Synthesis and evaluation of a novel quinoline-triazole analogs for antitubercular properties via molecular hybridization approach.
AID529109	Bactericidal activity against Mycobacterium tuberculosis selected on 10 times compound MIC measured after 6 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1861216	Cmax in Sprague-Dawley rat at 5 mg/kg,po	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1154348	Antimycobacterial activity against Mycobacterium tuberculosis over expressing InhA after 5 days by standard microdilution method	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID529108	Antimicrobial activity against drug-resistant Mycobacterium tuberculosis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID528924	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 25 mg/kg, po once daily measured after 1 day	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1638954	Apparent volume of distribution during terminal phase in iv dosed mouse	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.
AID1685620	Inhibition of cytochrome-bcc aa3 in Mycobacterium tuberculosis H37Rv assessed as replicating ATP by measuring ATP depletion incubated for 15 hrs in presence of Q203 by BacTiter-Glo luminescence assay	2021	RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1	Structure guided generation of thieno[3,2-
AID562295	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 120 mg/kg, po administered once monthly during logarithmic multiplication from day 60 to day 150 post infection measured on day 152	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID528939	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 400 mg/kg, po once daily measured after 2 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1698408	Inhibition of Mycobacterium smegmatis ATPsynthase	2020	Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22	Synthesis and structure-activity relationships for tetrahydroisoquinoline-based inhibitors of Mycobacterium tuberculosis.
AID562297	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 3 mg/kg, po administered 5 times weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 228	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1639004	Antitubercular activity against Mycobacterium tuberculosis H37Rv after 4 days by microplate alamar blue assay	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
AID1389802	Half life in human liver microsomes at 1 uM	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.
AID1154347	Antimycobacterial activity against Mycobacterium tuberculosis over expressing DprE1 after 5 days by standard microdilution method	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1181167	Antimicrobial activity against first mutant generation Mycobacterium tuberculosis 1024_1 assessed as fold shift in MIC relative to parent strain	2014	Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15	Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID502979	Antimicrobial activity against Mycobacterium tuberculosis H37Rv isolate BK12 expressing ATP synthase atpE A63P mutant protein by 7H10 broth dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1861194	Apparent permeability across basolateral side to apical side in dog MDCK cells	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID544553	Inhibition of Mycobacterium smegmatis MC2 155 ATP synthase subunit c-mediated ATP production	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue.
AID529090	AUC (0 to 24 hrs) in pulmonary tuberculosis patient at 25 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID562289	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 30 mg/kg, po administered once weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 152 po	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID528930	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 25 mg/kg, po once daily measured after 7 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1861228	Drug concentration in Sprague-Dawley rat lung at 5 mg/kg,po measured after 96 hrs	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1638945	Antitubercular activity against replicating Mycobacterium tuberculosis H37Rv after 4 days by Alamar blue assay	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.
AID669835	Antibacterial activity against non-replicating Mycobacterium tuberculosis H37Rv ATCC 27294 by low oxygen recovery assay	2012	Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8	Discovery of selective menaquinone biosynthesis inhibitors against Mycobacterium tuberculosis.
AID502997	Inhibition of Mycobacterium tuberculosis ATP synthase subunit c-mediated ATP synthesis after 24 hrs mins by luminometry	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1638952	Intrinsic clearance in mouse liver microsomes	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.
AID562293	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 50 mg/kg, po administered once monthly during logarithmic multiplication from day 60 to day 150 post infection measured on day 152 p	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1861206	Inhibition of human ERG	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID528943	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 400 mg/kg, po once daily measured after 6 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID765273	fCmax/MIC in Mycobacterium tuberculosis infected mouse	2013	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17	A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID525512	Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis isolate 4 expressing wild type atpE and F0 operon selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID525518	Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis H37Rv expressing wild type atpE selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID528944	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 400 mg/kg, po once daily measured after 7 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID529104	Cardiotoxicity in pulmonary tuberculosis patient assessed as increase in QT interval at 100 mg/kg, po once daily for 7 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1679141	Inhibition of Mycobacterium bovis BCG QcrB assessed as decrease in ATP level at 0.01 to 10 uM incubated for 20 hrs by Bactiter-Glo microbial cell viability assay	2021	RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1	Hydride-induced Meisenheimer complex formation reflects activity of nitro aromatic anti-tuberculosis compounds.
AID1504967	Cytotoxicity against African green monkey Vero cells after 72 hrs by MTS/PMS assay	2017	ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12	Antitubercular Nitroimidazoles Revisited: Synthesis and Activity of the Authentic 3-Nitro Isomer of Pretomanid.
AID1530552	Antimycobacterial activity against Mycobacterium tuberculosis	2019	European journal of medicinal chemistry, Jan-01, Volume: 161	Naphthalene, a versatile platform in medicinal chemistry: Sky-high perspective.
AID1861209	Half life in mouse at 1 mg/kg,iv	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID562304	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 100 mg/kg, po administered once weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 228 p	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1476360	Antitubercular activity against rifampicin resistant Mycobacterium tuberculosis H37Rv ATCC 35838 after 24 hrs by MABA method	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID529081	Cmin in pulmonary tuberculosis patient at 25 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID529101	Toxicity in pulmonary tuberculosis patient assessed as somnolence at 400 mg/kg, po once daily for 7 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID503002	Binding affinity to Bacillus PS3 ATP synthase subunit c A63P mutant	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1772305	Non-covalent inhibition of DprE1 in bedaquiline-resistant Mycobacterium tuberculosis measured after 7 days by microplate Alamar blue assay
AID529082	Cmin in pulmonary tuberculosis patient at 100 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1861190	Cytotoxicity against African green monkey Vero cells	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID525527	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 3 expressing wild type atpE and ATP synthase selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID565295	Antitubercular activity against Mycobacterium avium infected in C57BL/6J mouse assessed as reduction of CFU counts in spleen at 25 mg/kg, po administered one month post-infection five times weekly for 4 months (Rvb = 8.9 +/- 0.3 log10CFU)	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	ATP synthase inhibition of Mycobacterium avium is not bactericidal.
AID372664	Antimicrobial activity against Mycobacterium avium 1 after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID529094	Steady-state plasma concentration in pulmonary tuberculosis patient at 100 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID502985	Antimicrobial activity against wild type Mycobacterium smegmatis ATCC 607 expressing vector pSD5 by 7H9 agar dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1650511	Intrinsic clearance in mouse liver microsomes assessed per mg protein	2020	Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1	Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.
AID1861218	Oral bioavailability in Sprague-Dawley rat at 5 mg/kg	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID372787	Antimicrobial activity against Mycobacterium intracellular 20 after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1726776	Terminal half life in human	2021	RSC medicinal chemistry, Jun-23, Volume: 12, Issue:6	Synthesis and evaluation of pyridine-derived bedaquiline analogues containing modifications at the A-ring subunit.
AID562466	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 30 mg/kg, po administered once weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 302 to	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID544543	Antimicrobial activity against Mycobacterium smegmatis	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue.
AID1650507	Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition incubated for 10 days under anerobic condition followed by incubation under ambient gaseous condition for 28 days by low oxygen recovery assay	2020	Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1	Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.
AID1832953	Antitubercular activity against Mycobacterium tuberculosis mc2 6230 assessed as inhibition of bacterial growth incubated for 7 days	2021	Bioorganic & medicinal chemistry, 11-01, Volume: 49	Discovery of 5-methylpyrimidopyridone analogues as selective antimycobacterial agents.
AID528929	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 25 mg/kg, po once daily measured after 6 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1871986	Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Tuberculosis drug discovery: Progression and future interventions in the wake of emerging resistance.
AID372783	Antimicrobial activity against Mycobacterium avium 16 after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1638956	Oral bioavailability in mouse	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.
AID562303	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 50 mg/kg, po administered once weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 228 po	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1861241	Toxicity in Sprague-Dawley rat assessed as death at 200 mg/kg,po measured after 12 days	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID529085	Cmax in pulmonary tuberculosis patient at 100 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID372796	Antimicrobial activity against Mycobacterium gordonae after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1367747	Inhibition of human ERG	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23	Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units.
AID525514	Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis isolate 6 expressing wild type atpE selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID1367753	Oral bioavailability in rat	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23	Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units.
AID1861189	Cytotoxicity against human HeLa cells	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID372782	Antimicrobial activity against Mycobacterium avium 11 after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1861207	Clearance in mouse at 1 mg/kg,iv	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID525534	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 1 expressing wild type atpE selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID525524	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 5 expressing wild type atpE selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID502991	Antimicrobial activity against Mycobacterium smegmatis isolate R09 expressing ATP synthase AtpE D32V mutant protein by 7H10 agar dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1679140	Inhibition of Mycobacterium bovis BCG QcrB harboring CydAB deletion mutant assessed as decrease in ATP level at 0.01 to 10 uM incubated for 20 hrs by Bactiter-Glo microbial cell viability assay	2021	RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1	Hydride-induced Meisenheimer complex formation reflects activity of nitro aromatic anti-tuberculosis compounds.
AID1650517	Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse model of acute infection assessed as log reduction in bacterial burden in lung at 16.7 mg/kg, po via gavage administered as single dose for 12 days starting from	2020	Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1	Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.
AID502976	Antimicrobial activity against Mycobacterium tuberculosis H37Rv isolate BK12 expressing ATP synthase atpE A63P mutant protein by 7H9 broth dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1639012	Half life in human liver microsomes	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
AID528961	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 400 mg/kg, po once daily measured on day 8 after starting standard TB therapy	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1650514	AUC (0 to infinity) in CD-1 mouse at 10 mg/kg, po via gavage administered as single dose	2020	Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1	Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.
AID1616096	Antimicrobial activity against Mycobacterium tuberculosis H37Rv	2019	European journal of medicinal chemistry, Nov-15, Volume: 182	Recent advancements in mechanistic studies and structure activity relationship of F
AID1685622	Inhibition of cytochrome-bcc aa3 Mycobacterium tuberculosis clinical isolate N0145 assessed as replicating ATP by measuring ATP depletion incubated for 15 hrs in presence of Q203 by BacTiter-Glo luminescence assay	2021	RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1	Structure guided generation of thieno[3,2-
AID521902	Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis isolate 4 expressing wild type atpE Asp28Pro mutant selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID372797	Antimicrobial activity against Mycobacterium simiae after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1638946	Antitubercular activity against non-replicating Mycobacterium tuberculosis H37Rv after 10 days by LORA	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.
AID698991	AUC at steady state (0 to 24 hrs) in human at 50 mg, po qd for 14 days	2012	European journal of medicinal chemistry, May, Volume: 51	Tuberculosis: the drug development pipeline at a glance.
AID1181168	Antimicrobial activity against first mutant generation Mycobacterium tuberculosis 1024_18 assessed as fold shift in MIC relative to parent strain	2014	Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15	Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID699004	Antimycobacterial activity against Mycobacterium tuberculosis H37Rv	2012	European journal of medicinal chemistry, May, Volume: 51	Tuberculosis: the drug development pipeline at a glance.
AID1367752	Inhibition of CYP3A4 (unknown origin) after 20 mins	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23	Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units.
AID1503833	Lipophilicity, log P of the compound
AID565302	Antimicrobial activity against Mycobacterium tuberculosis	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	ATP synthase inhibition of Mycobacterium avium is not bactericidal.
AID525516	Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis isolate 6 expressing wild type atpE Ala63Pro mutant selected after 30 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID528934	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 100 mg/kg, po once daily measured after 4 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID698819	Antimycobacterial activity against Mycobacterium tuberculosis infected in human assessed as log reduction of bacterial count at 400 mg, qd measured up to 7 days	2012	European journal of medicinal chemistry, May, Volume: 51	Tuberculosis: the drug development pipeline at a glance.
AID562283	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 1 mg/kg, po administered 5 times weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 152	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID372781	Antimicrobial activity against Mycobacterium avium 9 after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID562302	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 30 mg/kg, po administered once weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 228 po	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1367754	Cytotoxicity against African green monkey Vero cells after 72 hrs by MTS-PMS assay	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23	Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units.
AID544561	Inhibition of ATP synthase in M18 mouse liver mitochondria assessed as effect on oxygen consumption at 175 uM	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue.
AID1726775	Inhibition of fluorescently labelled tracer binding to human ERG by competitive binding assay	2021	RSC medicinal chemistry, Jun-23, Volume: 12, Issue:6	Synthesis and evaluation of pyridine-derived bedaquiline analogues containing modifications at the A-ring subunit.
AID765270	AUC/MIC in Mycobacterium tuberculosis infected mouse	2013	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17	A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID528940	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 400 mg/kg, po once daily measured after 3 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID562286	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 12.5 mg/kg, po administered 5 times weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 1	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1861208	Volume of distribution at steady state in mouse at 1 mg/kg,iv	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1504965	Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 7 days under aerobic condition by alamar blue assay	2017	ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12	Antitubercular Nitroimidazoles Revisited: Synthesis and Activity of the Authentic 3-Nitro Isomer of Pretomanid.
AID525511	Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis isolate 4 expressing wild type atpE selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID1888137	Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate HD3 assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay	2022	European journal of medicinal chemistry, Jan-05, Volume: 227	Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID1476364	Antitubercular activity against streptomycin resistant Mycobacterium tuberculosis H37Rv ATCC 35820 after 24 hrs by MABA method	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID562296	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 1 mg/kg, po administered 5 times weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 228	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1743153	Ratio of MIC for inhibition of ATP synthase in bedaquiline-resistant Mycobacterium tuberculosis to MIC for inhibition of ATP synthase in Mycobacterium tuberculosis H37Rv	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Design, synthesis and biological evaluation of diamino substituted cyclobut-3-ene-1,2-dione derivatives for the treatment of drug-resistant tuberculosis.
AID1650515	Oral bioavailability in CD-1 mouse at 10 mg/kg administered via gavage as single dose	2020	Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1	Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.
AID372804	Antimicrobial activity against R207910 resistant Mycobacterium novocastrense after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID528938	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 400 mg/kg, po once daily measured after 1 day	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1861201	Inhibition of CYP1A2 (unknown origin)	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID502987	Antimicrobial activity against Mycobacterium smegmatis ATCC 607 expressing ATP synthase AtpE subunit by 7H9 agar dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1861217	AUC (0 to last) in Sprague-Dawley rat at 5 mg/kg,po	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1900063	Selectivity ratio of IC50 for Mycobacterium smegmatis ATP synthase over IC50 for human ATP synthase	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Synthesis and structure-activity relationships for a new class of tetrahydronaphthalene amide inhibitors of Mycobacterium tuberculosis.
AID502992	Antimicrobial activity against wild type Mycobacterium smegmatis ATCC 607 expressing vector pSD5 by 7H10 agar dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID699003	Antimycobacterial activity against Mycobacterium tuberculosis clinical isolate	2012	European journal of medicinal chemistry, May, Volume: 51	Tuberculosis: the drug development pipeline at a glance.
AID1743131	Inhibition of ATP synthase in Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth incubated for 7 days by microplate alamar blue assay	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Design, synthesis and biological evaluation of diamino substituted cyclobut-3-ene-1,2-dione derivatives for the treatment of drug-resistant tuberculosis.
AID1389811	Antitubercular activity against Mycobacterium tuberculosis Erdman infected in BALB/c mouse assessed as reduction in bacterial burden in lungs at 20 mg/kg, po qd for 12 continuous days from day 11 post infection measured on day 25 relative to 20 mg/kg beda	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.
AID1861213	Clearance in Sprague-Dawley rat at 1 mg/kg,iv	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID502993	Antimicrobial activity against Mycobacterium smegmatis expressing ATP synthase AtpE D32V mutant protein by 7H10 agar dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID502983	Antimicrobial activity against Mycobacterium smegmatis isolate R09 expressing ATP synthase AtpE D32V mutant protein by 7H9 agar dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID525537	Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis isolate 4 expressing wild type atpE Glu61Asp mutant selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID1154351	Antimycobacterial activity against BTZ043-resistant Mycobacterium tuberculosis over expressing DprE1 C387S mutant after 5 days by standard microdilution method	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID502996	Inhibition of Mycobacterium tuberculosis isolate LV13 ATP synthase subunit c I66M mutant-mediated ATP synthesis after 24 hrs by luminometry	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1650513	Apparent volume of distribution during terminal phase in CD-1 mouse at 2 to 3 mg/kg, iv administered as single bolus dose	2020	Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1	Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.
AID528964	Drug uptake in pulmonary tuberculosis patient at 25 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1685621	Inhibition of cytochrome-bd oxidase in Mycobacterium tuberculosis clinical isolate N0145 assessed as replicating ATP by measuring ATP depletion incubated for 15 hrs in absence of Q203 by BacTiter-Glo luminescence assay	2021	RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1	Structure guided generation of thieno[3,2-
AID503004	Binding affinity to Mycobacterium smegmatis ATCC 607 ATP synthase subunit beta by mass spectroscopy	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1389801	Oral bioavailability in CD-1 mouse at 10 mg/kg	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.
AID581001	Antimicrobial activity against multiple drug-resistant Mycobacterium tuberculosis	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID699002	Cmax in human at 400 mg, po	2012	European journal of medicinal chemistry, May, Volume: 51	Tuberculosis: the drug development pipeline at a glance.
AID1639018	Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse assessed as log reduction in lung colony forming units at 20 mg/kg, po administered daily via gavage for 12 days starting from 10 days post-infection	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
AID283243	Reduction of lung lesions in Mycobacterium tuberculosis H37Rv infected Swiss mouse at 25 mg/kg, po for 5 days/week after 1 month	2007	Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3	Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis.
AID528925	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 25 mg/kg, po once daily measured after 2 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1476361	Antitubercular activity against moxifloxacin resistant Mycobacterium tuberculosis H37Rv after 24 hrs by MABA method	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID528935	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 100 mg/kg, po once daily measured after 5 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1861203	Inhibition of CYP2C19 (unknown origin)	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID502995	Inhibition of Mycobacterium tuberculosis isolate BK12 ATP synthase subunit c A63P mutant-mediated ATP synthesis after 24 hrs by luminometry	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID372778	Antimicrobial activity against Mycobacterium avium 4 after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID1861210	Cmax in mouse at 6.25 mg/kg,po	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1504966	Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 10 days under low oxygen condition followed by second incubation under aerobic condition for 28 hrs by LORA	2017	ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12	Antitubercular Nitroimidazoles Revisited: Synthesis and Activity of the Authentic 3-Nitro Isomer of Pretomanid.
AID529107	Antimicrobial activity against drug-sensitive Mycobacterium tuberculosis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1164300	Inhibition of oxidative phosphorylation in Mycobacterium smegmatis membrane vesicles assessed as inhibition of NADH driven ATP synthesis by luciferin/luciferase assay	2014	ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9	2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
AID1603254	Antibacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay
AID562299	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 12.5 mg/kg, po administered 5 times weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 2	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID372794	Antimicrobial activity against Mycobacterium kansasii after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID562465	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 120 mg/kg, po administered once monthly during logarithmic multiplication from day 60 to day 150 post infection measured on day 228	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1639016	Oral bioavailability in mouse	2019	Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7	3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.
AID372789	Antimicrobial activity against Mycobacterium chelonae after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID562294	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 100 mg/kg, po administered once monthly during logarithmic multiplication from day 60 to day 150 post infection measured on day 152	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1503832	Antitubercular activity against Mycobacterium tuberculosis H37Rv after 4 days by MABA method
AID1861197	Plasma protein binding in rat assessed as bound fraction	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1861188	Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as mycobacterial growth inhibition by low oxygen recovery assay	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID525515	Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis isolate 6 expressing wild type atpE Glu61Asp mutant selected after 30 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID580999	Half life in human	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID1389797	Antitubercular activity against Mycobacterium tuberculosis H37Rv incubated for 10 days in non-replicating anaerobic condition followed by incubation for 28 hrs in ambient gaseous condition measured on day 11 by LORA assay	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.
AID1685618	Inhibition of cytochrome-bd oxidase in Mycobacterium bovis BCG assessed as replicating ATP by measuring ATP depletion incubated for 15 hrs in presence of Q203 by BacTiter-Glo luminescence assay	2021	RSC medicinal chemistry, Jan-01, Volume: 12, Issue:1	Structure guided generation of thieno[3,2-
AID1900062	Inhibition of human ATP synthase	2022	European journal of medicinal chemistry, Feb-05, Volume: 229	Synthesis and structure-activity relationships for a new class of tetrahydronaphthalene amide inhibitors of Mycobacterium tuberculosis.
AID528936	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 100 mg/kg, po once daily measured after 6 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1476363	Antitubercular activity against capreomycin resistant Mycobacterium tuberculosis H37Rv after 24 hrs by MABA method	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID1603256	Antibacterial activity against RMP-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay
AID1268503	Antibacterial activity against Mycobacterium tuberculosis	2016	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2	Identification of a novel class of quinoline-oxadiazole hybrids as anti-tuberculosis agents.
AID372802	Antimicrobial activity against Mycobacterium terrae after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID765272	Cmax/MIC in Mycobacterium tuberculosis infected mouse	2013	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17	A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID525530	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 2 expressing wild type atpE selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID529089	Tmax in pulmonary tuberculosis patient at 400 mg/kg, po once daily for 7 days by liquid chromatography-MS/MS analysis	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID283236	Reduction of bacterial counts in Mycobacterium tuberculosis H37Rv infected Swiss mouse lung at 25 mg/kg, po for 5 days/week after 2 months	2007	Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3	Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis.
AID698995	Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis	2012	European journal of medicinal chemistry, May, Volume: 51	Tuberculosis: the drug development pipeline at a glance.
AID562291	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 100 mg/kg, po administered once weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 152 p	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1389805	Inhibition of human ERG by patch clamp assay	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.
AID1650510	Intrinsic clearance in human liver microsomes assessed per mg protein	2020	Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1	Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.
AID372793	Antimicrobial activity against Mycobacterium vaccae after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID528937	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 100 mg/kg, po once daily measured after 7 days	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1861230	Ratio of drug concentration in Sprague-Dawley rat lung to plasma at 5 mg/kg,po measured after 96 hrs	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID562284	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 3 mg/kg, po administered 5 times weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 152	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID525528	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 3 expressing wild type atpE and F0 operon selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID562301	Antimycobacterial activity against Mycobacterium leprae infected in CBA/J mouse assessed as microbial growth inhibition at 25 mg/kg, po administered once weekly during logarithmic multiplication from day 60 to day 150 post infection measured on day 228 po	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
AID1861195	Efflux ratio of apparent permeability across basolateral to apical over apical to basolateral membrane in dog MDCK cells	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID565307	Antitubercular activity against Mycobacterium avium infected in C57BL/6J mouse assessed as reduction of CFU counts in spleen at 25 mg/kg, po administered one day post-infection five times weekly for 1 month (Rvb = 8.0 +/- 0.9 log10CFU)	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	ATP synthase inhibition of Mycobacterium avium is not bactericidal.
AID544547	Inhibition of ATP synthase mediated ATP production in human OVCAR3 cells at 200 uM	2009	Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3	Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue.
AID528960	Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 100 mg/kg, po once daily measured on day 8 after starting standard TB therapy	2008	Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8	Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1476350	Antitubercular activity against isoniazid resistant Mycobacterium tuberculosis H37Rv ATCC 35822 after 24 hrs by MABA method	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20	Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID525529	Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 3 expressing wild type atpE selected after 10 times MIC drug exposure	2010	Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3	Rates and mechanisms of resistance development in Mycobacterium tuberculosis to a novel diarylquinoline ATP synthase inhibitor.
AID372786	Antimicrobial activity against Mycobacterium intracellular 7 after 2 to 4 weeks by two fold dilution method	2007	Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11	In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
AID502977	Antimicrobial activity against Mycobacterium tuberculosis H37Rv by 7H10 broth dilution method	2007	Nature chemical biology, Jun, Volume: 3, Issue:6	Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1861231	Antimycobacterial activity against Mycobacterium tuberculosis infected by aerosol in mouse acute infection model assessed as reduction in colony forming unit in lungs at 5 to 20 mg/kg, po treated 5 days per week from day 28 to day 38 post infection	2022	Bioorganic & medicinal chemistry letters, 09-01, Volume: 71	Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID698994	Antimycobacterial activity against drug-resistant Mycobacterium tuberculosis	2012	European journal of medicinal chemistry, May, Volume: 51	Tuberculosis: the drug development pipeline at a glance.
AID1897867	Bactericidal activity against Non-replicating Mycobacterium tuberculosis ss18b-lux assessed as decrease in colony forming unit measured at 1 uM after 1 weeks
AID1367755	Lipophilicity log P of the compound	2017	Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23	Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	41 (5.96)	29.6817
2010's	398 (57.85)	24.3611
2020's	249 (36.19)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	41 (5.82%)	5.53%
Reviews	101 (14.35%)	6.00%
Case Studies	38 (5.40%)	4.05%
Observational	19 (2.70%)	0.25%
Other	505 (71.73%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (61)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
A Phase 2/3, Multicenter, Randomized, Open-label, Active-controlled Study to Evaluate the Efficacy and Safety of Bedaquiline Administered as Part of a Treatment Regimen With Clarithromycin and Ethambutol in Adult Patients With Treatment-refractory Mycobac [NCT04630145]	Phase 2/Phase 3	124 participants (Anticipated)	Interventional	2021-01-08	Recruiting
An Open-Label Study to Evaluate the Efficacy and Safety of TMC207 in Subjects With Multibacillary Leprosy [NCT03384641]	Phase 2	11 participants (Actual)	Interventional	2018-09-26	Active, not recruiting
A Phase 2, Open-label, Multicenter, Single-arm Study to Evaluate the Pharmacokinetics, Safety, Tolerability and Anti-mycobacterial Activity of TMC207 in Combination With a Background Regimen (BR) of Multidrug Resistant Tuberculosis (MDR-TB) Medications fo [NCT02354014]	Phase 2	60 participants (Anticipated)	Interventional	2016-05-31	Recruiting
Patient-reported Experiences and Quality of Life Outcomes in the TB-PRACTECAL Clinical Trial [NCT03942354]	Phase 2/Phase 3	54 participants (Anticipated)	Interventional	2019-09-01	Recruiting
Evaluating Newly Approved Drugs for Multidrug-resistant TB (endTB): A Clinical Trial [NCT02754765]	Phase 3	754 participants (Actual)	Interventional	2016-12-31	Completed
A Double-blind, Randomized, Placebo- and Active-controlled, Parallel-group Trial to Evaluate the Effect of Single-dose TMC207 on the QT/QTc Interval in Healthy Subjects [NCT01291563]	Phase 1	88 participants (Actual)	Interventional	2011-02-28	Completed
A Phase 2 Trial to Evaluate the Early Bactericidal Activity and Safety of Meropenem With Amoxicillin/Clavulanate Plus Either Pyrazinamde or Bedaquiline in Adults With Newly Diagnosed Rifampicin-susceptible Pulmonary Tuberculosis [NCT04629378]	Phase 2	22 participants (Actual)	Interventional	2020-08-17	Completed
A Trial of the Safety, Tolerability, and Pharmacokinetics of Bedaquiline and Delamanid, Alone and in Combination, Among Participants Taking Multidrug Treatment for Drug-Resistant Pulmonary Tuberculosis [NCT02583048]	Phase 2	84 participants (Actual)	Interventional	2016-08-15	Completed
STREAM: The Evaluation of a Standard Treatment Regimen of Anti-tuberculosis Drugs for Patients With MDR-TB [NCT02409290]	Phase 3	588 participants (Actual)	Interventional	2016-03-31	Completed
An Open-Label Phase 2 Trial to Evaluate the Male Reproductive Safety of a 6-Month Combination Treatment for Pulmonary Tuberculosis (TB) of Bedaquiline Plus Pretomanid Plus Moxifloxacin Plus Pyrazinamide (BPaMZ) in Adult Male Participants With Drug Resista [NCT04179500]	Phase 2	26 participants (Actual)	Interventional	2021-09-16	Active, not recruiting
Population Pharmacokinetics of Anti-tuberculosis Drugs in Children With Tuberculosis [NCT03625739]		800 participants (Anticipated)	Observational [Patient Registry]	2018-07-01	Recruiting
A Phase IIb, Open Label, Randomized Controlled Dose Ranging Multi-Center Trial to Evaluate the Safety, Tolerability, Pharmacokinetics and Exposure-Response Relationship of Different Doses of Delpazolid in Combination With Bedaquiline Delamanid Moxifloxaci [NCT04550832]	Phase 2	76 participants (Actual)	Interventional	2021-10-22	Active, not recruiting
A Parallel Group, Phase 2A, Randomised, Open Label Treatment Study to Assess the Early Bactericidal Activity, Safety and Tolerability of GSK3036656 Administered as a Two Drug Combination With Novel and Established Antitubercular Agents, or Standard of Car [NCT05382312]	Phase 2	70 participants (Anticipated)	Interventional	2022-07-26	Recruiting
Evaluating Newly Approved Drugs in Combination Regimens for Multidrug-Resistant TB With Fluoroquinolone Resistance (endTB-Q) [NCT03896685]	Phase 3	323 participants (Actual)	Interventional	2020-04-06	Active, not recruiting
A Phase 2, Partially-blinded, Randomised Trial Assessing the Safety and Efficacy of TBAJ876 or Bedaquiline, in Combination With Pretomanid and Linezolid in Adult Participants With Newly Diagnosed, Drug-sensitive, Smear-positive Pulmonary Tuberculosis [NCT06058299]	Phase 2	300 participants (Anticipated)	Interventional	2023-10-31	Not yet recruiting
A Seamless Phase 2B/C Platform Trial to Evaluate Multiple Regimens and Durations of Treatment in Pulmonary Tuberculosis [NCT06114628]	Phase 2	2,500 participants (Anticipated)	Interventional	2023-12-08	Not yet recruiting
Pharmacokinetic Properties of Antiretroviral and Related Drugs During Pregnancy and Postpartum [NCT00042289]		1,578 participants (Actual)	Observational	2003-06-09	Completed
Finding the Optimal Regimen for Mycobacterium Abscessus Treatment (FORMaT) [NCT04310930]	Phase 2/Phase 3	300 participants (Anticipated)	Interventional	2020-03-02	Recruiting
A Phase I, Open-label, Randomized Crossover Trial to Investigate the Pharmacokinetic Interaction Between Steady-state Lopinavir/Ritonavir and Single-dose TMC207 in Healthy Subjects. [NCT00828529]	Phase 1	16 participants (Actual)	Interventional	2009-02-28	Completed
A Phase II, Placebo-controlled, Double-blind, Randomized Trial to Evaluate the Anti-bacterial Activity, Safety, and Tolerability of TMC207 in Subjects With Newly Diagnosed Sputum Smear-positive Pulmonary Infection With Multi-drug Resistant Mycobacterium T [NCT00449644]	Phase 2	208 participants (Actual)	Interventional	2007-06-30	Completed
A Phase IIb, Open-Label, Randomized Controlled Dose Ranging Multi-Center Trial to Evaluate the Safety, Tolerability, Pharmacokinetics and Exposure-Response Relationship of Different Doses of BTZ-043 in Combination With Bedaquiline and Delamanid in Adult S [NCT05926466]	Phase 2	90 participants (Anticipated)	Interventional	2023-09-21	Recruiting
A Multi-center, Randomized, Positive-controlled Phase 2 Clinical Trial to Evaluate the Early Bactericidal Activity, Safety and Tolerability of WX-081 in Participants With Drug-naive&Susceptible or Drug-Resistant Pulmonary Tuberculosis [NCT04608955]	Phase 2	99 participants (Actual)	Interventional	2020-10-16	Completed
An Open-Label Study to Explore the Safety, Efficacy and Pharmacokinetics of TMC207 in Japanese Patients With Pulmonary Multi-Drug Resistant Tuberculosis (MDR-TB) [NCT02365623]	Phase 2	6 participants (Actual)	Interventional	2015-02-18	Completed
A Phase II, Open-label Trial With TMC207 as Part of a Multi-drug Resistant Tuberculosis (MDR-TB) Treatment Regimen in Subjects With Sputum Smear-positive Pulmonary Infection With MDR-TB. [NCT00910871]	Phase 2	241 participants (Actual)	Interventional	2009-09-30	Completed
Pharmacokinetics, Safety, and Tolerability of TMC207 in Subjects With Moderately Impaired Hepatic Function [NCT01012284]	Phase 1	16 participants (Actual)	Interventional	2010-01-31	Completed
Pharmacokinetics and Pharmacodynamics Sub-study for TB-PRACTECAL Clinical Trial ( PRACTECAL-PKPD) [NCT04081077]	Phase 2/Phase 3	240 participants (Anticipated)	Interventional	2019-08-06	Active, not recruiting
A Randomised, Controlled, Open-Label, Phase II-III Trial to Evaluate the Safety and Efficacy of Regimens Containing Bedaquiline and Pretomanid for the Treatment of Adult Patients With Pulmonary Multidrug Resistant Tuberculosis [NCT02589782]	Phase 2/Phase 3	552 participants (Actual)	Interventional	2017-01-31	Active, not recruiting
A Phase I Open-label Trial to Investigate the Pharmacokinetic Interaction Between Rifapentine or Rifampicin and a Single Dose of TMC207 in Healthy Subjects [NCT02216331]	Phase 1	32 participants (Actual)	Interventional	2010-03-31	Completed
A Randomized, Controlled, Multi-center Clinical Trial of Short Course Treatment for Newly Diagnosed Rifampicin Resistant Tuberculosis [NCT04545788]		200 participants (Anticipated)	Interventional	2020-08-01	Recruiting
Economic Evaluation of New MDR TB Regimens (PRACTECAL EE) [NCT04207112]	Phase 2/Phase 3	200 participants (Anticipated)	Interventional	2020-10-20	Recruiting
Phase 1, Open-label, Randomized Crossover Study in Healthy Adult Subjects to Assess the Relative Oral Bioavailability and Food Effect of Bedaquiline 100-mg Tablets Administered as Different Test Formulations Compared to the Commercial Tablet Formulation ( [NCT04087759]	Phase 1	36 participants (Actual)	Interventional	2019-09-16	Completed
An Open-label Study to Evaluate the Extended Early Bactericidal Activity, Safety, Tolerability and Pharmacokinetics of Multiple Oral Doses of TMC207 in Treatment-na�ve Subjects With Sputum Smear Positive Pulmonary Tuberculosis. [NCT00523926]	Phase 2	75 participants (Actual)	Interventional	2005-05-31	Completed
TASK-002: Bioequivalence of Bedaquiline 400mg Administered in Crushed Form Compared to Tablet Form in Healthy Male and Female Adults Under Fed Conditions (BDQ Crush Study) [NCT03032367]	Early Phase 1	24 participants (Actual)	Interventional	2016-11-10	Completed
A Phase 1, Open-label, Randomized, Crossover Study to Assess the Drug-Drug Interaction Between Bedaquiline and Clarithromycin in Healthy Adult Volunteers [NCT03800550]	Phase 1	16 participants (Actual)	Interventional	2019-02-13	Completed
Phase 2C Clinical Trial of Novel, Short-course Regimens for the Treatment of Pulmonary Tuberculosis: CRUSH-TB (Combination Regimens for Shortening TB Treatment) [NCT05766267]	Phase 2/Phase 3	288 participants (Anticipated)	Interventional	2023-03-01	Not yet recruiting
Early Access of TMC207 in Combination With Other Anti-Tuberculosis (TB) Drugs in Subjects With Extensively Drug Resistant (XDR) or Pre-XDR Pulmonary Tuberculosis [NCT01464762]		0 participants	Expanded Access		Approved for marketing
A Phase 3 Partially-blinded, Randomized Trial Assessing the Safety and Efficacy of Various Doses and Treatment Durations of Linezolid Plus Bedaquiline and Pretomanid in Participants With Pulmonary Infection of Either Extensively Drug-resistant Tuberculosi [NCT03086486]	Phase 3	181 participants (Actual)	Interventional	2017-11-21	Completed
A Phase III Placebo-controlled, Double-blind, Randomized Trial to Evaluate the Efficacy and Safety of TMC207 in Subjects With Sputum Smear-positive Pulmonary Infection With Multi-drug Resistant Mycobacterium Tuberculosis (MDR-TB) [NCT01600963]	Phase 3	0 participants (Actual)	Interventional	2014-03-31	Withdrawn(stopped due to PhIII program revised; TMC207-C210 cancelled)
A Phase IIB, Open-Label, Randomized Controlled Dose Ranging Multi-Center Trial to Evaluate the Safety, Tolerability, Pharmacokinetics and Exposure-Response Relationship of Different Doses of Sutezolid in Combination With Bedaquiline, Delamanid and Moxiflo [NCT03959566]	Phase 2	75 participants (Actual)	Interventional	2021-05-06	Completed
Refining MDR-TB Treatment (T) Regimens (R) for Ultra(U) Short(S) Therapy(T) (TB-TRUST)-PLUS [NCT04717908]		89 participants (Actual)	Interventional	2021-01-20	Active, not recruiting
A Phase II Dose Ranging Trial to Evaluate the Extended Early Bactericidal Activity, Safety, Tolerability, and Pharmacokinetics of TMC207 in Adult Patients With Newly Diagnosed, Uncomplicated, Smear-Positive, Pulmonary Tuberculosis. [NCT01215110]	Phase 2	68 participants (Actual)	Interventional	2010-04-30	Completed
A Multiple Arm, Multiple Stage (MAMS), Phase 2B/C, Open Label, Randomized, Controlled Platform Trial to Evaluate Experimental Arms Including an Increased Dose of Rifampicin, an Optimized Dose of Pyrazinamide, Moxifloxacin and Sutezolid, in Adult Subjects [NCT05807399]	Phase 2	360 participants (Anticipated)	Interventional	2023-04-14	Recruiting
Two-month Regimens Using Novel Combinations to Augment Treatment Effectiveness for Drug-sensitive Tuberculosis [NCT03474198]	Phase 2/Phase 3	675 participants (Actual)	Interventional	2018-03-21	Completed
A Multicenter, Phase 2b/c, Open-label, Randomized, Dose-finding Trial to Evaluate the Safety and Efficacy of a 4 Month Regimen of OPC-167832 in Combination With Delamanid and Bedaquiline in Subjects With Drug-susceptible Pulmonary Tuberculosis in Comparis [NCT05221502]	Phase 2	120 participants (Anticipated)	Interventional	2022-04-12	Recruiting
An Open Label, Randomized Controlled Trial to Establish the Efficacy and Safety of a Study Strategy Consisting of 6 Months of Bedaquiline (BDQ), Delamanid (DLM), and Linezolid (LNZ), With Levofloxacin (LVX) and Clofazimine (CFZ) Compared to the Current So [NCT04062201]	Phase 3	402 participants (Actual)	Interventional	2019-08-22	Active, not recruiting
A Multicenter, Randomized, Open-Label Study To Evaluate The Efficacy And Safety Of A Contezolid, Delamanid and Bedaquiline-Containing Short Regimen For The Treatment Of Rifampicin-Resistant Pulmonary Tuberculosis [NCT06081361]	Phase 3	186 participants (Anticipated)	Interventional	2023-11-01	Not yet recruiting
Bedaquiline Enhanced Post ExpOsure Prophylaxis for Leprosy: Phase 2 Study [NCT05406479]	Phase 2	321 participants (Actual)	Interventional	2022-07-14	Completed
Prospective, Randomized, Partially Blinded, Phase 2 Study of the Efficacy and Tolerability of Bedaquiline, Delamanid, Levofloxacin, Linezolid, and Clofazimine for Treatment of Patients With MDR-TB [NCT03828201]	Phase 2	220 participants (Anticipated)	Interventional	2022-06-07	Recruiting
A Phase II, Prospective, Randomized, Multicenter Trial to Evaluate the Efficacy and Safety/Tolerability of Two Linezolid Dosing Strategies in Combination With a Short Course Regimen for the Treatment of Drug-Resistant Pulmonary Tuberculosis [NCT05007821]	Phase 2	132 participants (Anticipated)	Interventional	2022-08-11	Recruiting
A Phase I/II, Open-Label, Single Arm Study to Evaluate the Pharmacokinetics, Safety and Tolerability of Bedaquiline (BDQ) Given in Combination With an Individualized Rifampin-Resistant Tuberculosis (RR-TB) Therapy in Infants, Children, and Adolescents Wit [NCT02906007]	Phase 1/Phase 2	84 participants (Anticipated)	Interventional	2017-09-21	Recruiting
A Pragmatic Randomized Controlled Trial to Evaluate the Efficacy and Safety of an Oral Short-course Regimen Including Bedaquiline for the Treatment of Patients With Multidrug-resistant Tuberculosis in China [NCT05306223]	Phase 4	212 participants (Anticipated)	Interventional	2022-05-10	Recruiting
A Phase 2b/c, Multi-Arm, 2-Stage, Duration Randomized Trial of the Efficacy and Safety of Two to Four Months Treatment With Regimens Containing Bedaquiline, OPC-167832, and Sutezolid, Plus Either Pretomanid or Delamanid, in Adults With Pulmonary Tuberculo [NCT05971602]	Phase 2	514 participants (Anticipated)	Interventional	2023-07-26	Recruiting
Bedaquiline Enhanced Post ExpOsure Prophylaxis for Leprosy: Phase 3 Study [NCT05597280]	Phase 3	124,000 participants (Anticipated)	Interventional	2023-03-22	Recruiting
A Multicenter, Randomized, Double-blind, Positive Control Study to Evaluate the Efficacy and Safety of Sudapyridine (WX-081) Tables in Patients With Rifampicin-resistant Pulmonary Tuberculosis [NCT05824871]	Phase 3	450 participants (Anticipated)	Interventional	2022-09-02	Enrolling by invitation
A Phase 3 Open-label Trial Assessing the Safety and Efficacy of Bedaquiline Plus PA-824 Plus Linezolid in Subjects With Pulmonary Infection of Either Extensively Drug-resistant Tuberculosis (XDR-TB) or Treatment Intolerant / Non-responsive Multi-drug Resi [NCT02333799]	Phase 3	109 participants (Actual)	Interventional	2015-03-31	Completed
An Open-Label, Partially Randomized Trial to Evaluate the Efficacy, Safety and Tolerability of a 4-month Treatment of Bedaquiline Plus Pretomanid Plus Moxifloxacin Plus Pyrazinamide (BPaMZ) Compared to a 6-month Treatment of HRZE/HR (Control) in Adult Par [NCT03338621]	Phase 2/Phase 3	455 participants (Actual)	Interventional	2018-07-30	Completed
Evaluate the Effectiveness, Safety and Tolerability of Various Doses of Linezolid in Combination With Bedaquiline and Pretomanid in Adults With Pre-Extensively Drug-Resistant (Pre-XDR), Or Treatment Intolerant/Non-responsive Multidrug-Resistant (MDRTI/NR) [NCT05040126]	Phase 3	400 participants (Anticipated)	Interventional	2021-10-07	Recruiting
A Novel 4-month Pan-TB Regimen Targeting Both Host and Microbe (panTB-HM) [NCT05686356]	Phase 2/Phase 3	352 participants (Anticipated)	Interventional	2023-07-28	Recruiting
Evaluating a New Treatment Regimen for Patients With Multidrug-resistant TB (MDR-TB) - a Prospective Open-label Randomised Controlled Trial [NCT02454205]	Phase 2/Phase 3	154 participants (Actual)	Interventional	2015-11-12	Completed
A Phase IIc, Open-Label, Randomized Controlled Trial of Ultra-Short Course Bedaquiline, Clofazimine, Pyrazinamide and Delamanid Versus Standard Therapy for Drug-Susceptible Tuberculosis (PRESCIENT) [NCT05556746]	Phase 2	156 participants (Anticipated)	Interventional	2023-10-31	Not yet recruiting
A Phase 2 Open-Label Partially Randomized Trial to Evaluate the Efficacy, Safety and Tolerability of Combinations of Bedaquiline, Moxifloxacin, PA-824 and Pyrazinamide During 8 Weeks of Treatment in Adult Subjects With Newly Diagnosed Drug-Sensitive or Mu [NCT02193776]	Phase 2	240 participants (Actual)	Interventional	2014-10-23	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00042289 (26) [back to overview]	Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00042289 (26) [back to overview]	Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	Plasma Concentration for Contraceptives
NCT00042289 (26) [back to overview]	PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]	Area Under the Curve From 0 to 24 Hours (AUC24) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]	Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00449644 (6) [back to overview]	The Percentage of Participants With Sputum Culture Conversion (Stage 2)
NCT00449644 (6) [back to overview]	The Percentage of Participants With Sputum Culture Conversion (Stage 1)
NCT00449644 (6) [back to overview]	The Time to Sputum Culture Conversion at Week 8 (Stage 1)
NCT00449644 (6) [back to overview]	The Time to Sputum Culture Conversion at Week 72 (Stage 2)
NCT00449644 (6) [back to overview]	The Time to Sputum Culture Conversion at Week 24 (Stage 2)
NCT00449644 (6) [back to overview]	The Time to Sputum Culture Conversion at Week 24 (Stage 1)
NCT00910871 (2) [back to overview]	The Percentage of Participants With Sputum Culture Conversion
NCT00910871 (2) [back to overview]	The Median Time to Sputum Culture Conversion
NCT01215110 (11) [back to overview]	Rate of Change in Time to Sputum Culture Positivity (TTP)(Hours) in Liquid Culture Media (Days 7-14)
NCT01215110 (11) [back to overview]	Summary of Statistical Analysis of TMC207 Area Under the Concentration-time Curve Over the Dose Interval of 0 to 24 h (AUC(0-24)) on Day 1 and Day 14
NCT01215110 (11) [back to overview]	Summary of Statistical Analysis of TMC207 Maximum Plasma Concentration Following Dosing (C(Max)) on Days 1 and 14
NCT01215110 (11) [back to overview]	Summary of Statistical Analysis of TMC207 Time of Maximum Plasma Concentration (T(Max)) on Days 1 and 14
NCT01215110 (11) [back to overview]	Rate of Change in Time to Sputum Culture Positivity (TTP)(Hours) in Liquid Culture Media (Days 0-2)
NCT01215110 (11) [back to overview]	Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 0-14).
NCT01215110 (11) [back to overview]	Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 0-2).
NCT01215110 (11) [back to overview]	Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 2-14).
NCT01215110 (11) [back to overview]	Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 7-14).
NCT01215110 (11) [back to overview]	Rate of Change in Time to Sputum Culture Positivity (TTP)(Hours) in Liquid Culture Media (Days 0-14)
NCT01215110 (11) [back to overview]	Rate of Change in Time to Sputum Culture Positivity (TTP)(Hours) in Liquid Culture Media (Days 2-14)
NCT02193776 (2) [back to overview]	Rate of Change in Time to Sputum Culture Positivity (TTP) Over 8 Weeks in the Mycobacterial Growth Indicator Tube (MGIT) System
NCT02193776 (2) [back to overview]	Number of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT02409290 (5) [back to overview]	STREAM Stage 2 Primary Outcome Measure (the Proportion of Patients With a Favourable Outcome at Week 76)
NCT02409290 (5) [back to overview]	Proportion of Patients With Acquired Drug Resistance
NCT02409290 (5) [back to overview]	Favourable Outcome After Long-term Follow-up (132 Weeks)
NCT02409290 (5) [back to overview]	Failure or Recurrence (FoR)
NCT02409290 (5) [back to overview]	Failure or Recurrence (FoR)
NCT02583048 (22) [back to overview]	Mean Change From Baseline in QTcF
NCT02583048 (22) [back to overview]	Percentage of Participants Who Died
NCT02583048 (22) [back to overview]	Percentage of Participants Who Discontinued Study TB Drug(s) For Any Reason
NCT02583048 (22) [back to overview]	Percentage of Participants With an Increase in QTcF From Baseline of Greater Than 60 Milliseconds (ms)
NCT02583048 (22) [back to overview]	DLM PK Parameter Cmin Determined Based on DLM Levels From Individual Participants Enrolled in Arms 2 and 3
NCT02583048 (22) [back to overview]	DLM PK Parameter Cmax Determined Based on DLM Levels From Individual Participants Enrolled in Arms 2 and 3
NCT02583048 (22) [back to overview]	DLM PK Area Under the Concentration Time Curve (AUC 0-11h) Determined Based on Intensive PK Samples Obtained From Individual Participants Enrolled in Arms 2 and 3
NCT02583048 (22) [back to overview]	DLM Metabolite DM6705 PK Parameter Cmin Determined Based on DLM Metabolite Levels From Individual Participants Enrolled in Arms 2 and 3
NCT02583048 (22) [back to overview]	DLM Metabolite DM6705 PK Parameter Cmax Determined Based on DLM Metabolite Levels From Individual Participants Enrolled in Arms 2 and 3
NCT02583048 (22) [back to overview]	DLM Metabolite DM6705 PK AUC 0-11h Determined Based on Intensive PK Samples Obtained From Individual Participants Enrolled in Arms 2 and 3
NCT02583048 (22) [back to overview]	Changes in QTcF From Baseline
NCT02583048 (22) [back to overview]	BDQ PK Parameter Maxmum Plasma Concentration (Cmax) Determined Based on BDQ Levels From Individual Participants Enrolled in Arms 1 and 3
NCT02583048 (22) [back to overview]	BDQ PK Parameter Area Under the Concentration Time Curve (AUC 0-22h) Calculated Based on Intensive PK Samples Obtained From Individual Participants Enrolled in Arms 1 and 3
NCT02583048 (22) [back to overview]	Percentage of Participants With an Occurrence of QTcF Increase From Baseline of >30 and ≤60 Milliseconds (ms)
NCT02583048 (22) [back to overview]	Percentage of Participants With an Occurrence of QTcF Greater Than 500 Milliseconds (ms)
NCT02583048 (22) [back to overview]	Percentage of Participants With an Occurrence of QTcF >480 and ≤500 Milliseconds (ms)
NCT02583048 (22) [back to overview]	BDQ PK Parameter Minimum Plasma Concentration (Cmin) Determined Based on BDQ Levels From Individual Participants Enrolled in Arms 1 and 3
NCT02583048 (22) [back to overview]	Post-Baseline QTcF
NCT02583048 (22) [back to overview]	Percentage of Participants With an Occurrence of Grade 3 or Higher Adverse Event
NCT02583048 (22) [back to overview]	N-monodesmethyl Metabolite of BDQ PK Parameter Cmin Determined Based on BDQ Metabolite Levels From Individual Participants Enrolled in Arms 1 and 3
NCT02583048 (22) [back to overview]	N-monodesmethyl Metabolite of BDQ PK Parameter Cmax Determined Based on BDQ Metabolite Levels From Individual Participants Enrolled in Arms 1 and 3
NCT02583048 (22) [back to overview]	N-monodesmethyl Metabolite of BDQ PK Parameter AUC 0-22h Calculated Based on Intensive PK Samples Obtained From Individual Participants Enrolled in Arms 1 and 3
NCT03086486 (1) [back to overview]	Time to Sputum Culture Conversion to Negative Status Through the Treatment Period
NCT03338621 (2) [back to overview]	Number of Participants With Culture Negative Status by 8 Weeks
NCT03338621 (2) [back to overview]	Time to Culture Negative Status

Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC (area under the curve) were determined using the linear trapezoidal rule. See PK target in the Protocol Appendix V. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 (and 24) hours post dosing.

,,,,,,,,,,,,,,,,,,,,,,

Intervention	Participants (Count of Participants)
	2nd Trimester	3rd Trimester	Postpartum
ATV/RTV Arm 1: 300/100mg q.d.	1	12	12
DRV/COBI 800/150 mg q.d.	3	4	14
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.	7	16	22
DRV/RTV 600/100mg b.i.d.	7	19	22
DRV/RTV 800/100mg q.d.	9	19	22
DTG 50mg q.d.	9	20	23
EFV 600 mg q.d. (Outside THA)	12	33	34
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.	8	29	27
ETR 200mg b.i.d.	5	13	7
EVG/COBI 150/150mg q.d.	8	10	18
FPV/RTV 700/100mg b.i.d.	8	26	22
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)	10	19	26
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.	9	30	27
ATV/COBI 300/150 mg q.d.	1	2	5
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.	NA	15	14
RAL 400mg b.i.d.	11	33	30
RPV 25mg q.d.	14	26	25
TAF 10mg q.d. w/COBI	15	23	22
TAF 25mg q.d.	13	23	24
TAF 25mg q.d. w/COBI or RTV Boosting	10	24	18
TFV 300mg q.d.	2	27	27
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.	1	11	12
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.	7	23	32

Intervention	mcg/mL (Median)
	2-10 hours after birth	18-28 hours after birth	36-72 hours after birth	5-9 days after birth
DRV/COBI 800/150 mg q.d.	0.35	1.43	1.87	1.72
DTG 50mg q.d.	1.73	1.53	1.00	0.06
EFV 600 mg q.d. (Outside THA)	1.1	1.0	0.9	0.4
EVG/COBI 150/150mg q.d.	0.132	0.032	0.005	0.005

Intervention	hour (Median)
DTG 50mg q.d.	32.8
EVG/COBI 150/150mg q.d.	7.6
DRV/COBI 800/150 mg q.d.	NA
EFV 600 mg q.d. (Outside THA)	65.6

Intervention	unitless (Median)
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.	0.15
DTG 50mg q.d.	1.25
EVG/COBI 150/150mg q.d.	0.91
DRV/COBI 800/150 mg q.d.	0.07
ATV/COBI 300/150 mg q.d.	0.07
TFV 300mg q.d.	0.88

Intervention	pg/mL (Median)
ATV/RTV/TFV 300/100/300mg q.d. With ENG	604
LPV/RTV 400/100 b.i.d. With ENG	428
EFV 600mg q.d. With ENG	125

Intervention	mcg*hr/mL (Median)
	Before contraceptive initiation	After contraceptive initiation
LPV/RTV 400/100 b.i.d. With ENG	115.97	100.20

Intervention	Participants (Count of Participants)
	3rd Trimester	Postpartum
EFV 600mg q.d.	20	21
MVC 150 or 300mg b.i.d.	8	7

Intervention	Percentage of Participants (Number)
	Week 24	Week 72	Week 120
Placebo / BR (Stage 2)	57.6	56.1	43.9
TMC207 / BR (Stage 2)	78.8	71.2	62.1

Intervention	Percentage of Participants (Number)
	Week 8	Week 24	Week 104 (Stage 1 Trial End)
Placebo / BR (Stage 1)	8.7	65.2	43.5
TMC207 / BR (Stage 1)	47.6	81.0	52.4

Intervention	hours/day (Mean)
TMC207 100	6.9
TMC207 200	4.8
TMC207 300	5.9
TMC207 400	4.4
Rifafour e-275 mg	11.5

Intervention	ng*h/mL (Mean)
	AUC(0-24) Day 1	AUC(0-24) Day 14
TMC207 100	18995.57	18689.03
TMC207 200	26619.51	33314.07
TMC207 300	31357.35	50547.15
TMC207 400	53179.27	69069.64

Intervention	ng/mL (Mean)
	C(max) Day 1	C(max) Day 14
TMC207 100	1846.13	1553.27
TMC207 200	2700.73	2884.67
TMC207 300	3128.00	3902.31
TMC207 400	5386.67	5178.57

Intervention	hour (Mean)
	T(max) Day 1	T(max) Day 14
TMC207 100	5.33	5.13
TMC207 200	5.20	4.60
TMC207 300	5.53	5.15
TMC207 400	5.67	5.29

Intervention	log10CFU/ml/day (Mean)
TMC207 100	0.040
TMC207 200	0.056
TMC207 300	0.077
TMC207 400	0.104
Rifafour e-275 mg	0.112

Intervention	log10CFU/ml/day (Mean)
TMC207 100	0.004
TMC207 200	-0.033
TMC207 300	0.015
TMC207 400	0.093
Rifafour e-275 mg	0.413

Intervention	log10CFU/ml/day (Mean)
TMC207 100	0.047
TMC207 200	0.071
TMC207 300	0.088
TMC207 400	0.106
Rifafour e-275 mg	0.046

Intervention	log10CFU/ml/day (Mean)
TMC207 100	0.053
TMC207 200	0.086
TMC207 300	0.098
TMC207 400	0.107
Rifafour e-275 mg	0.046

Intervention	percentage change in TTP/day (Mean)
DS-TB: Bedaquiline (Loading Dose/t.i.w)+ PA-824 + Pyrazinamide	4.878
DS-TB: Bedaquiline (200 mg) + PA-824 + Pyrazinamide	5.182
DS-TB: HRZE (Isoniazid+Rifampicin+Pyrazinamide+Ethambutol)	4.046
MDR-TB: Bedaquiline (200 mg)+Moxifloxacin+PA-824+Pyrazinamide	5.194

Intervention	Participants (Count of Participants)
	Any TEAE	Drug-related TEAE	TEAE leading to death	Any serious TEAE	Drug-related serious TEAE	TEAE leading to discontinuation of study drug	TEAE leading to early withdrawal from study	Grade III TEAE	Grade IV TEAE
DS-TB: Bedaquiline (200 mg) + PA-824 + Pyrazinamide	45	29	1	3	0	5	5	17	7
DS-TB: Bedaquiline (Loading Dose/t.i.w)+ PA-824 + Pyrazinamide	50	38	1	4	2	6	5	19	8
DS-TB: HRZE (Isoniazid+Rifampicin+Pyrazinamide+Ethambutol)	44	29	1	4	1	2	2	14	2
MDR-TB: Bedaquiline (200 mg)+Moxifloxacin+PA-824+Pyrazinamide	57	46	0	4	2	2	2	13	1

Intervention	Participants (Count of Participants)
Regimen A (Long Regimen)	0
Regimen B (Control Regimen)	133
Regimen C (Oral Regimen)	162
Regimen D (6-month Regimen)	122

Intervention	milliseconds (ms) (Mean)
Arm 1: Bedaquiline	12.3
Arm 2: Delamanid	8.6
Arm 3: Bedaquiline and Delamanid	20.7

bedaquiline

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Clinical Trials (61)

Trial Overview

Trial Outcomes

Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs

Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs

PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs

PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs

PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of ARVs and TB Drugs

PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs

PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (Range) for ARVs and TB Drugs

Plasma Concentration for Contraceptives

PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs

Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms

Area Under the Curve From 0 to 24 Hours (AUC24) of ARVs for Contraceptive Arms

Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs

PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs

PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs

PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs

PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs

PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs

PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs

PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs

PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) for ARVs and TB Drugs

PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) for ARVs and TB Drugs

PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs

PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs

PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs

PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs

The Percentage of Participants With Sputum Culture Conversion (Stage 2)

The Percentage of Participants With Sputum Culture Conversion (Stage 1)

The Time to Sputum Culture Conversion at Week 8 (Stage 1)

The Time to Sputum Culture Conversion at Week 72 (Stage 2)

The Time to Sputum Culture Conversion at Week 24 (Stage 2)

The Time to Sputum Culture Conversion at Week 24 (Stage 1)

The Percentage of Participants With Sputum Culture Conversion

The Median Time to Sputum Culture Conversion

Rate of Change in Time to Sputum Culture Positivity (TTP)(Hours) in Liquid Culture Media (Days 7-14)

Summary of Statistical Analysis of TMC207 Area Under the Concentration-time Curve Over the Dose Interval of 0 to 24 h (AUC(0-24)) on Day 1 and Day 14

Summary of Statistical Analysis of TMC207 Maximum Plasma Concentration Following Dosing (C(Max)) on Days 1 and 14

Summary of Statistical Analysis of TMC207 Time of Maximum Plasma Concentration (T(Max)) on Days 1 and 14

Rate of Change in Time to Sputum Culture Positivity (TTP)(Hours) in Liquid Culture Media (Days 0-2)

Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 0-14).

Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 0-2).

Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 2-14).

Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 7-14).

Rate of Change in Time to Sputum Culture Positivity (TTP)(Hours) in Liquid Culture Media (Days 0-14)

Rate of Change in Time to Sputum Culture Positivity (TTP)(Hours) in Liquid Culture Media (Days 2-14)

Rate of Change in Time to Sputum Culture Positivity (TTP) Over 8 Weeks in the Mycobacterial Growth Indicator Tube (MGIT) System

Number of Participants With Treatment Emergent Adverse Events (TEAEs)

STREAM Stage 2 Primary Outcome Measure (the Proportion of Patients With a Favourable Outcome at Week 76)

Proportion of Patients With Acquired Drug Resistance

Intervention	ng/mL (Mean)
	Week 2	Week 8	Week 24
Arm 2: Delamanid	224.8	198.2	220.9
Arm 3: Bedaquiline and Delamanid	206.8	217.2	182.2

Intervention	milliseconds (ms) (Median)
	Change from baseline to Week 2	Change from baseline to Week 4	Change from baseline to Week 6	Change from baseline to Week 8	Change from baseline to Week 10	Change from baseline to Week 12	Change from baseline to Week 14	Change from baseline to Week 16	Change from baseline to Week 18	Change from baseline to Week 20	Change from baseline to Week 22	Change from baseline to Week 24	Change from baseline to Week 28
Arm 1: Bedaquiline	16.70	15.00	15.30	12.00	10.30	9.30	12.70	15.35	17.65	9.30	12.00	11.70	13.30
Arm 2: Delamanid	4.15	8.70	9.30	7.00	7.80	10.30	5.30	7.35	11.70	13.65	9.00	13.00	6.00
Arm 3: Bedaquiline and Delamanid	13.15	14.30	15.30	20.30	18.30	20.30	21.30	21.00	12.70	21.00	20.85	24.00	17.65

Intervention	milliseconds (ms) (Least Squares Mean)
	Baseline	Post-baseline
Arm 1: Bedaquiline	397.4	409.7
Arm 2: Delamanid	404.9	413.4
Arm 3: Bedaquiline and Delamanid	391.7	412.4

Intervention	Percentage of participants (Number)
	Grade 3 adverse event	Grade 4 adverse event
Arm 1: Bedaquiline	36	4
Arm 2: Delamanid	11	11
Arm 3: Bedaquiline and Delamanid	19	19

Intervention	weeks (Median)
1200mg L x 26 Weeks + Pa + B	4
1200 mg L x 9 Weeks + Pa + B	4
600 mg L x 26 Weeks + Pa + B	6
600 mg L x 9 Weeks + Pa + B	6
Total	6

Intervention	weeks (Median)
Drug Sensitive-TB BPaMZ	6
Drug Sensitive-TB 2HRZE/4HR	11
Drug Resistant-TB BPaMZ	5