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AMR Drug RepurposingSmart Screeningresearch prototype

Macitentan

FDA-approved product (tablet, oral), marketed as Macitentan, Opsumit.

Registered studies
50+
Lab records
0
Pathogens at ≥40%
1 of 4

Chemical structure

Chemical structure of Macitentan
A drawing shows what the molecule is, not what it does.

Existing / approved use

Documented · FDA, WHO, ChEMBL

Approved 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 evidence

Clinical

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.

Open Macitentan in ChEMBL Registered studies below

Docking

Computational · nothing measured

Dihydrofolate 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 measured

Other 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.

Registered studies

A registration describes a study; it does not establish a positive result.

  • A Study of Macitentan, in Healthy Japanese Male Participants

    NCT04500808 · start 2020-07-21

    Registered record
    Registry ID
    NCT04500808
    Conditions
    Healthy
    Interventions
    Macitentan Dose 1; Macitentan Dose 2; Macitentan Dose 3; Placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2020-07-21
    Completion
    2020-12-14
    Enrolment
    24

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHealthy
    InterventionMacitentan Dose 1; Macitentan Dose 2; Macitentan Dose 3; Placebo
    PhasePhase 1
    Registry statusCompleted

  • A Study to Evaluate Efficacy and Safety of Macitentan 75 mg in Inoperable or Persistent/Recurrent Chronic Thromboembolic Pulmonary Hypertension

    NCT04271475 · start 2020-07-07

    Registered record
    Registry ID
    NCT04271475
    Conditions
    Chronic Thromboembolic Pulmonary Hypertension
    Interventions
    Macitentan; Placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Terminated
    Start
    2020-07-07
    Completion
    2023-12-21
    Enrolment
    127

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionChronic Thromboembolic Pulmonary Hypertension
    InterventionMacitentan; Placebo
    PhasePhase 3
    Registry statusTerminated

  • A Study of Macitentan and Tadalafil as a Fixed Dose Combination and the Free Combination in Healthy Adult Participants

    NCT04235270 · start 2020-01-17

    Registered record
    Registry ID
    NCT04235270
    Conditions
    Healthy
    Interventions
    FDC of Macitentan and Tadalafil; Macitentan; Tadalafil
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2020-01-17
    Completion
    2020-07-17
    Enrolment
    62

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHealthy
    InterventionFDC of Macitentan and Tadalafil; Macitentan; Tadalafil
    PhasePhase 1
    Registry statusCompleted

  • Clinical Study to Compare the Efficacy and Safety of Macitentan and Tadalafil Monotherapies With the Corresponding Fixed-dose Combination Therapy in Subjects With Pulmonary Arterial Hypertension (PAH)

    NCT03904693 · start 2019-07-29

    Registered record
    Registry ID
    NCT03904693
    Conditions
    Pulmonary Arterial Hypertension (PAH) (WHO Group 1 PH)
    Interventions
    FDC macitentan/tadalafil; Macitentan 10 mg; Tadalafil 40 mg; Placebo FDC; Placebo macitentan; Placebo tadalafil
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Completed
    Start
    2019-07-29
    Completion
    2024-09-27
    Enrolment
    187

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionPulmonary Arterial Hypertension (PAH) (WHO Group 1 PH)
    InterventionFDC macitentan/tadalafil; Macitentan 10 mg; Tadalafil 40 mg; Placebo FDC +2 more
    PhasePhase 3
    Registry statusCompleted

  • A Long Term Study to Find Out if Macitentan is an Effective and Safe Treatment for Patients With Heart Failure With Preserved Ejection Fraction and Pulmonary Vascular Disease

    NCT03714815 · start 2018-12-07

    Registered record
    Registry ID
    NCT03714815
    Conditions
    Heart Failure With Preserved Ejection Fraction and Pulmonary Vascular Disease
    Interventions
    macitentan 10 mg
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Terminated
    Start
    2018-12-07
    Completion
    2021-10-12
    Enrolment
    91

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHeart Failure With Preserved Ejection Fraction and Pulmonary Vascular Disease
    Interventionmacitentan 10 mg
    PhasePhase 2
    Registry statusTerminated

  • CompRehensive Phenotypic Characterization of Patients With Scleroderma-Associated ILD and PH

    NCT03726398 · start 2018-09-01

    Registered record
    Registry ID
    NCT03726398
    Conditions
    Interstitial Lung Disease; Scleroderma; Pulmonary Hypertension
    Interventions
    Opsumit 10 Mg Tablet
    Study type
    INTERVENTIONAL
    Phase
    Phase 2 / Phase 3
    Registry status
    Withdrawn
    Start
    2018-09-01
    Completion
    2020-08-03
    Enrolment
    0

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionInterstitial Lung Disease; Scleroderma; Pulmonary Hypertension
    InterventionOpsumit 10 Mg Tablet
    PhasePhase 2 / Phase 3
    Registry statusWithdrawn

  • A Clinical Study to Investigate the Long-term Safety of the Drug Macitentan in Patients With Pulmonary Hypertension Who Were Previously Treated With Macitentan in Clinical Studies.

    NCT03422328 · start 2018-04-05

    Registered record
    Registry ID
    NCT03422328
    Conditions
    Pulmonary Arterial Hypertension; Chronic Thromboembolic Pulmonary Hypertension
    Interventions
    macitentan
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Completed
    Start
    2018-04-05
    Completion
    2023-12-27
    Enrolment
    151

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionPulmonary Arterial Hypertension; Chronic Thromboembolic Pulmonary Hypertension
    Interventionmacitentan
    PhasePhase 3
    Registry statusCompleted

  • (RIGHT HEART III Study - Right Ventricular Hemodynamic Evaluation and Response to Treatment)

    NCT03362047 · start 2018-03-01

    Registered record
    Registry ID
    NCT03362047
    Conditions
    Pulmonary Arterial Hypertension (PAH)
    Interventions
    Riciguat Group; Macitentan Group
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Completed
    Start
    2018-03-01
    Completion
    2024-08-14
    Enrolment
    7

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionPulmonary Arterial Hypertension (PAH)
    InterventionRiciguat Group; Macitentan Group
    PhasePhase 2
    Registry statusCompleted

  • A Study to Assess Whether Macitentan Delays Disease Progression in Children With Pulmonary Arterial Hypertension (PAH)

    NCT02932410 · start 2017-10-24

    Registered record
    Registry ID
    NCT02932410
    Conditions
    Pulmonary Arterial Hypertension
    Interventions
    Macitentan; Standard-of-care
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Completed
    Start
    2017-10-24
    Completion
    2025-11-27
    Enrolment
    165

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionPulmonary Arterial Hypertension
    InterventionMacitentan; Standard-of-care
    PhasePhase 3
    Registry statusCompleted

  • Clinical Study Assessing the Efficacy and Safety of Macitentan in Fontan-palliated Subjects

    NCT03153137 · start 2017-08-14

    Registered record
    Registry ID
    NCT03153137
    Conditions
    Congenital Heart Disease
    Interventions
    Macitentan 10 mg; Placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Completed
    Start
    2017-08-14
    Completion
    2021-07-26
    Enrolment
    142

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionCongenital Heart Disease
    InterventionMacitentan 10 mg; Placebo
    PhasePhase 3
    Registry statusCompleted

  • A Study to Compare the Macitentan-tadalafil Fixed Dose Combination Tablet Relative to the Concomitant Administration of the Reference Tablets of Macitentan and Tadalafil in Healthy Subjects

    NCT03215966 · start 2017-08-07

    Registered record
    Registry ID
    NCT03215966
    Conditions
    Healthy Subjects
    Interventions
    Macitentan / tadalafil FDC; Macitentan (Opsumit®); Tadalafil (Adcirca®)
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2017-08-07
    Completion
    2017-09-24
    Enrolment
    38

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHealthy Subjects
    InterventionMacitentan / tadalafil FDC; Macitentan (Opsumit®); Tadalafil (Adcirca®)
    PhasePhase 1
    Registry statusCompleted

  • Retrospective Chart Review of First-time Opsumit® (Macitentan) Users in the United States

    NCT03197688 · start 2017-08-03

    Registered record
    Registry ID
    NCT03197688
    Conditions
    Pulmonary Arterial Hypertension
    Interventions
    Notapplicable
    Study type
    OBSERVATIONAL
    Phase
    Not recorded
    Registry status
    Completed
    Start
    2017-08-03
    Completion
    2018-09-06
    Enrolment
    2,200

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionPulmonary Arterial Hypertension
    InterventionNotapplicable
    PhaseNot recorded
    Registry statusCompleted

  • A Study to Evaluate Whether Macitentan is an Effective and Safe Treatment for Patients With Heart Failure With Preserved Ejection Fraction and Pulmonary Vascular Disease

    NCT03153111 · start 2017-07-11

    Registered record
    Registry ID
    NCT03153111
    Conditions
    Heart Failure With Preserved Ejection Fraction
    Interventions
    Macitentan; Placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Completed
    Start
    2017-07-11
    Completion
    2021-03-12
    Enrolment
    143

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHeart Failure With Preserved Ejection Fraction
    InterventionMacitentan; Placebo
    PhasePhase 2
    Registry statusCompleted

  • Impact of Rehabilitation Program on PAH Patients Treated With Macitentan.

    NCT03045666 · start 2017-04-15

    Registered record
    Registry ID
    NCT03045666
    Conditions
    Pulmonary Arterial Hypertension
    Interventions
    Exercise program
    Study type
    INTERVENTIONAL
    Phase
    Not applicable
    Registry status
    Unknown
    Start
    2017-04-15
    Completion
    2018-05-01
    Enrolment
    48

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionPulmonary Arterial Hypertension
    InterventionExercise program
    PhaseNot applicable
    Registry statusUnknown

  • Macitentan in the Treatment of Organ Rejection After Lung Transplantation

    NCT02893176 · start 2016-09

    Registered record
    Registry ID
    NCT02893176
    Conditions
    Lung Transplant Rejection
    Interventions
    macitentan; placebo (for macitentan)
    Study type
    INTERVENTIONAL
    Phase
    Phase 4
    Registry status
    Withdrawn
    Start
    2016-09
    Completion
    2019-09-19
    Enrolment
    0

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionLung Transplant Rejection
    Interventionmacitentan; placebo (for macitentan)
    PhasePhase 4
    Registry statusWithdrawn