bedaquiline

Trade name: sirturo

Small moleculeapprovedOrphan Drug ^FDAFast Track ^FDA

Approved

Dec 28, 2012

Bedaquiline (trade name Sirturo, code names TMC207 and R207910) is a diarylquinoline anti-tuberculosis drug, which was discovered by a team led by Koen Andries at Janssen Pharmaceutica. When it was approved by the FDA on the 28th December 2012, it was the first new medicine to fight TB in more than forty years, and is specifically approved to treat multi-drug-resistant tuberculosis. Bedaquiline is a diarylquinoline antimycobacterial drug that inhibits the proton pump of mycobacterial ATP (adenosine 5'-triphosphate) synthase, an enzyme that is essential for the generation of energy in Mycobacterium tuberculosis. Bacterial death occurs as a result of bedaquiline. — NCATS

Clinical trial activity

88 trials · 146 clinical orgs · 1 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Mar 1, 2003 (NCT00042289)

Timeline

2000s

Jan 1, 2005
Earliest Phase 2 Sponsor(trial)
Jan 10, 2005
Orphan Drug Designation
Jan 1, 2009
Earliest Phase 1 Sponsor(trial)

2010s

Dec 28, 2012
Johnson and Johnson — Earliest FDA Approval
Dec 28, 2012
Johnson and Johnson — NDA Secondary Org
Dec 28, 2012
Johnson and Johnson — NDA Organization
Jan 1, 2014
Johnson and Johnson — Earliest Phase 3 Sponsor(trial)

Mechanism of action

ATP synthaseINHIBITOR
ATP synthase inhibitor
It has been shown that mutation in the atpE gene, which encodes the c subunit, of the mycobacterial ATP synthase, confers resistant to Bedaquiline, suggesting that Bedaquiline binds crucially to this target, inhibiting the proton pump of M. tuberculosis and therefore interfering with the rotation properties of the transmembrane disk, leading to ATP depletion (PMID: 15591164)

Approval history

approvedPriority reviewAcceleratedFast trackDec 28, 2012

Chemistry & pharmacology

Loading structure…

SMILES

COc1nc2ccc(Br)cc2cc1[C@@H](c1ccccc1)[C@@](O)(CCN(C)C)c1cccc2ccccc12

Mol. weight: 555.52 g/mol
Lipinski Ro5: 2 violation(s)
Rule of 3: No
Chirality: Single Stereoisomer
Inorganic: No
Polymer: No
Delivery: Oral
Availability: Prescription Only

Oral

Yes

Parenteral

Topical

Black box warningFirst in class

Sources

Also known as

1-(6-bromo-2-methoxy-quinolin-3-yl)-4-dimethylamino-2-(3-fluorophenyl)-1-phenyl-butan-2-ol
1-(6-bromo-2-methoxy-quinolin-3-yl)-4-dimethylamino-2-naphthalen-1-yl-1-phenyl-butan-2-ol
1-(6-bromo-2-methoxy-quinolin-3-yl)-4-dimethylamino-2-naphthalen-1-yl-1-phenyl-butan-2-ol
aids222088
aids-222089
bedaquilina
bedaquilina
bedaquiline
bedaquiline
bedaquiline
bedaquiline
bedaquiline
bedaquiline
bedaquiline
bedaquiline
bedaquiline
bedaquiline
bedaquiline fumarate
bedaquiline fumarate
bedaquiline fumarate
bedaquiline fumarate
bedaquiline fumarate
bedaquiline fumarate
bedaquilinum
bedaquilinum
r207910
r 207910
r 207910
r-207910
r-207910
r-403323
r-403323
sirturo
sirturo
sirturo
sirturo
tmc207
tmc207
tmc207
tmc207
tmc207
tmc207
tmc 207
tmc 207
tmc-207
tmc-207

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT07227779	Phase 2	Feb 15, 2026	Makerere University, University of Minnesota
NCT07069582	Phase 1	Oct 1, 2025	McGill University, Padjadjaran University
NCT07198685	N/A	Sep 30, 2025	Huazhong University of Science and Technology
NCT07126639	N/A	Sep 1, 2025	Huazhong University of Science and Technology
NCT07129629	Phase 2	Aug 20, 2025	Fudan University, Huazhong University of Science and Technology
NCT07076225	Phase 3	Jul 25, 2025	Capital Medical University, Fudan University, Huazhong University of Science and Technology, Shenzhen Third People's Hospital, Sichuan University, Tsinghua University
NCT06905522	Phase 3	Apr 15, 2025	Shenyang Tenth People's Hospital, Shenzhen Third People's Hospital, Zhejiang University
NCT06568484	Phase 3	Nov 30, 2024	Elizabeth Glaser Pediatric AIDS Foundation, Johns Hopkins University, United States Agency for International Development
NCT06649721	Phase 3	Nov 15, 2024	Capital Medical University, Fudan University
NCT06441006	Phase 3	Nov 1, 2024	Johns Hopkins University, University of California, San Francisco
NCT06192160	Phase 2	Oct 15, 2024	National Institute of Allergy and Infectious Diseases (NIAID), TB Alliance, University of California, Berkeley, Vanderbilt University
NCT06114628	Phase 2	Dec 8, 2023	German Center for Infection Research, GlaxoSmithKline, Government of France, Janssen Pharmaceutica NV, KNCV Tuberculosis Foundation, Otsuka, Radboud University, Research Center Borstel, TASK Applied Science, TB Alliance, Tuberculosis Network European Trialsgroup, University of California, San Francisco, University of Cambridge, University of Hamburg, University of Liverpool, University of London, University of Milan, University of Oxford, University of Porto, University of St Andrews, Uppsala University, Vita-Salute University of Milano. Italy
NCT06081361	Phase 3	Nov 1, 2023	Capital Medical University
NCT06058299	Phase 2	Oct 31, 2023	Global Alliance for TB Drug Development, TB Alliance
NCT05926466	Phase 2	Sep 21, 2023	Ludwig Maximilians University, Radboud University, University of California, San Francisco, University of London
NCT05686356	Phase 2/Phase 3 (Phase 3)	Jul 28, 2023	Aurum Institute, Global Alliance for TB Drug Development, Government of Mozambique, Katholieke Universiteit Leuven, Ludwig Maximilians University, National Institute for Medical Research, Tanzania, Sequella, Inc., Stellenbosch University, Wits Health Consortium (Pty) Ltd
NCT05971602	Phase 2	Jul 26, 2023	Bill and Melinda Gates Foundation, Global Alliance for TB Drug Development, Janssen Pharmaceutica NV, Otsuka
NCT05807399	Phase 2	Apr 14, 2023	GlaxoSmithKline, LegoChem Biosciences, Inc, Ludwig Maximilians University, Radboud University, University of California, San Francisco, University of London
NCT05556746	Phase 2	Mar 31, 2023	Haitian Group for the Study of Kaposi's Sarcoma and Opportunistic, Harvard University, Stellenbosch University, University of California, Los Angeles, University of Cape Town
NCT05597280	Phase 3	Mar 1, 2023	Damien Foundation Bangladesh, Institute of Tropical Medicine, Belgium

Showing 20 of 88 trials

Page 1 / 5

Organizations

Research & Development (146)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Global Alliance for TB Drug Development	Academic/Hospital	13	9	3	2010
Janssen Pharmaceutica NV	For profit	11	2	4	2007
Johnson and Johnson	For profit	11	11	4	2007
University of California, San Francisco	Academic/Hospital	9	1	2	2019
National Institute of Allergy and Infectious Diseases (NIAID)	Government	8	7	4	2003
University of London	Academic/Hospital	8	2	2	2017
Capital Medical University	Academic/Hospital	7	4	3	2019
Fudan University	Academic/Hospital	6	3	4	2021
Medecins Sans Frontieres	Academic/Hospital	6	6	1	2016
Tibotec	For profit	6	6	2	2005
Huazhong University of Science and Technology	Academic/Hospital	5	4	4	2021
Johns Hopkins University	Academic/Hospital	5	1	3	2009
Ludwig Maximilians University	Academic/Hospital	5	3	2	2019
Radboud University	Academic/Hospital	5	0	1	2019
Stellenbosch University	Academic/Hospital	5	0	3	2015
University of Cape Town	Academic/Hospital	5	1	2	2014
Harvard University	Academic/Hospital	4	1	2	2016
Institute of Tropical Medicine, Belgium	Academic/Hospital	4	2	2	2016
Otsuka	For profit	4	1	2	2020
Pfizer	For profit	4	3	2	2010

146 organizations

Page 1 / 8

Marketing (2)

Organization	Org type	Relationship	Date
Johnson and Johnson	For profit	NDA2	Dec 28, 2012
Johnson and Johnson	For profit	NDA	Dec 28, 2012