Macitentan
FDA-approved product (tablet, oral), marketed as Macitentan, Opsumit.
- Registered studies
- 50+
- Lab records
- 0
- Pathogens at ≥40%
- 1 of 4
Chemical structure
Existing / approved use
Documented · FDA, WHO, ChEMBLApproved for
- Hypertension
- Idiopathic and/or familial pulmonary arterial hypertension
- Pulmonary arterial hypertension
- Pulmonary hypertension
Indications ChEMBL records as approved, from FDA and DailyMed labels. Label ↗
- WHO therapeutic group
- Antihypertensives for pulmonary arterial hypertension
- FDA pharmacologic class
- Endothelin Receptor Antagonist FDA label ↗
- Anti-infective classification
- Not classified as an anti-infective.
Repurposing investigation
This medicine is being investigated here for AI-predicted antimicrobial activity against M. tuberculosis. It was surfaced computationally for further investigation; it is not an established treatment for this infection.
AI-predicted activity
AI prediction · nothing measured- MRSA39.8% AI-predicted activityBelow the ≥40% mark this site uses to surface candidates.
- E. coli29.5% AI-predicted activityBelow the ≥40% mark this site uses to surface candidates.
- K. pneumoniae27.8% AI-predicted activityBelow the ≥40% mark this site uses to surface candidates.
- M. tuberculosis55.0% AI-predicted activityAt or above the ≥40% mark this site uses to surface candidates.
A model’s estimate of laboratory activity against each pathogen species. It is not clinical effectiveness.
Evidence
Clinical and experimental
Documented evidenceClinical
50+registered studies name this medicine, for any condition. The registry search keeps the first 50, so there may be more. See them below.
Experimental
No evidence found
No laboratory measurement against the four pathogens in the ChEMBL records loaded here.
Docking
Computational · nothing measuredDihydrofolate reductase ↗ (E. coli)
Not yet docked: queued in the docking rundetails
KPC-2 carbapenemase ↗ (K. pneumoniae)
Not yet docked: queued in the docking rundetails
Enoyl-ACP reductase (InhA) ↗ (M. tuberculosis)
Not yet docked: queued in the docking rundetails
Dihydrofolate reductase ↗ (MRSA)
Not yet docked: queued in the docking rundetails
AutoDock Vina, one experimentally solved protein per pathogen. This project’s screening target is -7.0 kcal/mol, its own mark rather than a universal cutoff. A docking score is a structural hypothesis, not proof of binding, and requires experimental validation.
Other medicines to investigate
AI prediction · nothing measuredOther repurposing candidates: approved medicines besides Macitentan with AI-predicted activity ≥40% against the chosen pathogen, leaving out existing antimicrobials. They are computational candidates for further investigation, not alternatives and not recommendations.
Sorted by AI-predicted activity, high to low. The order is not a ranking of which medicine is better.
- FurazolidoneExisting use: Other antiinfectives and antiseptics91.4% AI-predicted activityagainst M. tuberculosisLab records exist49 registered studies
- TriflupromazineExisting use: Psychosis90.6% AI-predicted activityagainst M. tuberculosisNo documented evidence found
- ValdecoxibExisting use: Dysmenorrhea, Osteoarthritis, Rheumatic disease and 1 more88.6% AI-predicted activityagainst M. tuberculosisLab records exist31 registered studies
- CelecoxibExisting use: Ankylosing spondylitis, Cancer, Colorectal neoplasm and 15 more87.6% AI-predicted activityagainst M. tuberculosisLab records exist50+ registered studies
- Dorzolamide HydrochlorideExisting use: Glaucoma, Ocular hypertension, Open-angle glaucoma86.8% AI-predicted activityagainst M. tuberculosisLab records exist50+ registered studies
- MethazolamideExisting use: Glaucoma, Open-angle glaucoma85.6% AI-predicted activityagainst M. tuberculosisLab records exist11 registered studies
- AcetazolamideExisting use: Altitude sickness, Angle-closure glaucoma, Congestive heart failure and 5 more85.2% AI-predicted activityagainst M. tuberculosisLab records exist50+ registered studies
- Trifluoperazine HydrochlorideExisting use: Anxiety disorder, Mental or behavioural disorder, Psychosis and 1 more84.6% AI-predicted activityagainst M. tuberculosis1 registered study
- TriclosanExisting use: Phenol and derivatives, Medicated dressings with antiinfectives84.2% AI-predicted activityagainst M. tuberculosisLab records exist50+ registered studies
- NitrofurazoneExisting use: Eye infection, Leishmaniasis, Trypanosomiasis84.0% AI-predicted activityagainst M. tuberculosis8 registered studies
- BrinzolamideExisting use: Glaucoma, Ocular hypertension, Open-angle glaucoma83.8% AI-predicted activityagainst M. tuberculosisLab records exist50+ registered studies
- ZonisamideExisting use: Epilepsy, Focal-onset seizure, Partial epilepsy and 1 more82.8% AI-predicted activityagainst M. tuberculosisLab records exist50+ registered studies
Registered studies
A registration describes a study; it does not establish a positive result.
The Efficacy and Safety of Initial Triple Versus Initial Dual Oral Combination Therapy in Patients With Newly Diagnosed Pulmonary Arterial Hypertension
NCT02558231 · start 2016-05-01
Registered record
- Registry ID
- NCT02558231
- Conditions
- Pulmonary Arterial Hypertension
- Interventions
- Macitentan; Tadalafil; Selexipag
- Study type
- INTERVENTIONAL
- Phase
- Phase 3
- Registry status
- Completed
- Start
- 2016-05-01
- Completion
- 2020-04-20
- Enrolment
- 247
As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.
ConditionPulmonary Arterial HypertensionInterventionMacitentan; Tadalafil; SelexipagPhasePhase 3Registry statusCompletedClinical Study Evaluating the Effects of First-line Oral cOmbination theraPy of maciTentan and tadalafIl in Patients With Newly Diagnosed pulMonary Arterial Hypertension (OPTIMA)
NCT02968901 · start 2015-09-01
Registered record
- Registry ID
- NCT02968901
- Conditions
- Pulmonary Arterial Hypertension
- Interventions
- macitentan; tadalafil
- Study type
- INTERVENTIONAL
- Phase
- Phase 4
- Registry status
- Terminated
- Start
- 2015-09-01
- Completion
- 2018-09-10
- Enrolment
- 46
As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.
ConditionPulmonary Arterial HypertensionInterventionmacitentan; tadalafilPhasePhase 4Registry statusTerminatedPORtopulmonary Hypertension Treatment wIth maCitentan - a randOmized Clinical Trial
NCT02382016 · start 2015-06-23
Registered record
- Registry ID
- NCT02382016
- Conditions
- Portopulmonary Hypertension
- Interventions
- Macitentan; Placebo
- Study type
- INTERVENTIONAL
- Phase
- Phase 4
- Registry status
- Completed
- Start
- 2015-06-23
- Completion
- 2018-10-31
- Enrolment
- 85
As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.
ConditionPortopulmonary HypertensionInterventionMacitentan; PlaceboPhasePhase 4Registry statusCompletedREPAIR: Right vEntricular Remodeling in Pulmonary ArterIal hypeRtension
NCT02310672 · start 2015-06-01
Registered record
- Registry ID
- NCT02310672
- Conditions
- Pulmonary Arterial Hypertension
- Interventions
- Macitentan
- Study type
- INTERVENTIONAL
- Phase
- Phase 4
- Registry status
- Completed
- Start
- 2015-06-01
- Completion
- 2019-09-10
- Enrolment
- 89
As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.
ConditionPulmonary Arterial HypertensionInterventionMacitentanPhasePhase 4Registry statusCompletedEffect of Pharmacologic Interaction Between ERAs and PDE-5 Inhibitors on Medication Serum Levels and Clinical Disease Status in Patients With PAH
NCT02484807 · start 2015-05
Registered record
- Registry ID
- NCT02484807
- Conditions
- Pulmonary Arterial Hypertension
- Interventions
- no intervention, only observation of different groups
- Study type
- OBSERVATIONAL
- Phase
- Not recorded
- Registry status
- Completed
- Start
- 2015-05
- Completion
- 2016-12
- Enrolment
- 125
As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.
ConditionPulmonary Arterial HypertensionInterventionno intervention, only observation of different groupsPhaseNot recordedRegistry statusCompletedClinical Study to Assess the Safety, Tolerability and Efficacy of Macitentan in Subjects With Inoperable Chronic Thromboembolic Pulmonary Hypertension
NCT02060721 · start 2015-02-03
Registered record
- Registry ID
- NCT02060721
- Conditions
- Chronic Thromboembolic Pulmonary Hypertension
- Interventions
- Macitentan
- Study type
- INTERVENTIONAL
- Phase
- Phase 2
- Registry status
- Completed
- Start
- 2015-02-03
- Completion
- 2022-03-21
- Enrolment
- 76
As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.
ConditionChronic Thromboembolic Pulmonary HypertensionInterventionMacitentanPhasePhase 2Registry statusCompletedChronic Thrombo-embolic Pulmonary Hypertension: Classification and Long Term Outcome
NCT02565030 · start 2015-02
Registered record
- Registry ID
- NCT02565030
- Conditions
- Chronic Thromboembolic Pulmonary Hypertension; Idiopathic Pulmonary Arterial Hypertension
- Interventions
- Not recorded
- Study type
- OBSERVATIONAL
- Phase
- Not recorded
- Registry status
- Completed
- Start
- 2015-02
- Completion
- 2021-10
- Enrolment
- 1,200
As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.
ConditionChronic Thromboembolic Pulmonary Hypertension; Idiopathic Pulmonary Arterial HypertensionInterventionNot recordedPhaseNot recordedRegistry statusCompletedClinical Study on Macitentan, RT and TMZ Concurrent Therapy Followed by Maintenance Macitentan and TMZ in Newly Diagnosed Glioblastoma
NCT02254954 · start 2015-01-08
Registered record
- Registry ID
- NCT02254954
- Conditions
- Glioblastoma
- Interventions
- Macitentan in combination with RT and TMZ
- Study type
- INTERVENTIONAL
- Phase
- Phase 1
- Registry status
- Terminated
- Start
- 2015-01-08
- Completion
- 2016-09-29
- Enrolment
- 30
As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.
ConditionGlioblastomaInterventionMacitentan in combination with RT and TMZPhasePhase 1Registry statusTerminatedExtension of the Psychometric Validation Study ORCHESTRA in Patients With PAH
NCT02112487 · start 2014-06-23
Registered record
- Registry ID
- NCT02112487
- Conditions
- Pulmonary Arterial Hypertension
- Interventions
- Macitentan
- Study type
- INTERVENTIONAL
- Phase
- Phase 3
- Registry status
- Completed
- Start
- 2014-06-23
- Completion
- 2018-09-19
- Enrolment
- 88
As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.
ConditionPulmonary Arterial HypertensionInterventionMacitentanPhasePhase 3Registry statusCompletedOPsumit USers Registry
NCT02126943 · start 2014-04-30
Registered record
- Registry ID
- NCT02126943
- Conditions
- Pulmonary Arterial Hypertension
- Interventions
- Opsumit (macitentan)
- Study type
- OBSERVATIONAL
- Phase
- Not recorded
- Registry status
- Completed
- Start
- 2014-04-30
- Completion
- 2020-04-24
- Enrolment
- 2,686
As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.
ConditionPulmonary Arterial HypertensionInterventionOpsumit (macitentan)PhaseNot recordedRegistry statusCompletedA Study of Tadalafil in Pediatric Participants With Pulmonary Arterial Hypertension (PAH)
NCT01824290 · start 2014-02-05
Registered record
- Registry ID
- NCT01824290
- Conditions
- Hypertension, Pulmonary
- Interventions
- Tadalafil; Placebo; ERA as specific PAH treatment
- Study type
- INTERVENTIONAL
- Phase
- Phase 3
- Registry status
- Completed
- Start
- 2014-02-05
- Completion
- 2021-03-10
- Enrolment
- 35
As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.
ConditionHypertension, PulmonaryInterventionTadalafil; Placebo; ERA as specific PAH treatmentPhasePhase 3Registry statusCompletedClinical Study to Assess the Long-term Safety, Tolerability, and Efficacy of Macitentan in Subjects With Eisenmenger Syndrome
NCT01739400 · start 2013-09-10
Registered record
- Registry ID
- NCT01739400
- Conditions
- Pulmonary Arterial Hypertension
- Interventions
- Macitentan 10 mg tablet, once daily.
- Study type
- INTERVENTIONAL
- Phase
- Phase 3
- Registry status
- Terminated
- Start
- 2013-09-10
- Completion
- 2018-01-12
- Enrolment
- 217
As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.
ConditionPulmonary Arterial HypertensionInterventionMacitentan 10 mg tablet, once daily.PhasePhase 3Registry statusTerminatedClinical Study of Macitentan in Patients With PAH to Psychometrically Validate PAH-SYMPACT Instrument
NCT01847014 · start 2013-09-01
Registered record
- Registry ID
- NCT01847014
- Conditions
- Pulmonary Arterial Hypertension
- Interventions
- Macitentan
- Study type
- INTERVENTIONAL
- Phase
- Phase 3
- Registry status
- Terminated
- Start
- 2013-09-01
- Completion
- 2017-11-30
- Enrolment
- 4
As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.
ConditionPulmonary Arterial HypertensionInterventionMacitentanPhasePhase 3Registry statusTerminatedClinical Study of Macitentan in Patients With Pulmonary Arterial Hypertension to Psychometrically Validate the PAH-SYMPACT Instrument
NCT01841762 · start 2013-04-01
Registered record
- Registry ID
- NCT01841762
- Conditions
- Pulmonary Arterial Hypertension
- Interventions
- Macitentan
- Study type
- INTERVENTIONAL
- Phase
- Phase 3
- Registry status
- Completed
- Start
- 2013-04-01
- Completion
- 2015-11-01
- Enrolment
- 284
As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.
ConditionPulmonary Arterial HypertensionInterventionMacitentanPhasePhase 3Registry statusCompletedClinical Study on the Safety and Tolerability of Macitentan in Combination With Dose-dense Temozolomide in Patients With Recurrent Glioblastoma
NCT01499251 · start 2012-01
Registered record
- Registry ID
- NCT01499251
- Conditions
- Glioblastoma
- Interventions
- Phase 1 Dose Escalation; Phase 1b; Ancillary Study
- Study type
- INTERVENTIONAL
- Phase
- Phase 1
- Registry status
- Terminated
- Start
- 2012-01
- Completion
- 2016-04
- Enrolment
- 75
As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.
ConditionGlioblastomaInterventionPhase 1 Dose Escalation; Phase 1b; Ancillary StudyPhasePhase 1Registry statusTerminated