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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.

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.

  • Efficacy and Mechanisms of Macitentan for Non-Coronary Obstructive Angina

    NCT07392281 · start 2025-09-01

    Registered record
    Registry ID
    NCT07392281
    Conditions
    Non-Coronary Obstructive Angina
    Interventions
    Macitentan 10 mg tablet, once daily.
    Study type
    INTERVENTIONAL
    Phase
    Early phase 1
    Registry status
    Recruiting
    Start
    2025-09-01
    Completion
    2027-08-31
    Enrolment
    40

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

    ConditionNon-Coronary Obstructive Angina
    InterventionMacitentan 10 mg tablet, once daily.
    PhaseEarly phase 1
    Registry statusRecruiting
  • Effects of Combination Medical Therapy Followed by BPA on Right Ventricular-PA Coupling and Hemodynamics in CTEPH

    NCT05140525 · start 2025-01-27

    Registered record
    Registry ID
    NCT05140525
    Conditions
    CTEPH
    Interventions
    Macitentan Tablets; Riociguat; balloon pulmonary angioplasty
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Terminated
    Start
    2025-01-27
    Completion
    2026-05-01
    Enrolment
    7

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

    ConditionCTEPH
    InterventionMacitentan Tablets; Riociguat; balloon pulmonary angioplasty
    PhasePhase 3
    Registry statusTerminated
  • Efficacy and Safety of Triple-targeted Drug Therapy in Treatment-naive Patients With Non-low-risk PAH: A Real-world, Multicenter Study

    NCT06753981 · start 2024-12-10

    Registered record
    Registry ID
    NCT06753981
    Conditions
    Arterial Pulmonary Hypertension (PAH)
    Interventions
    Endothelin receptor antagonist (ERA) combined with PDE5i/sGC agonist dual therapy prostacyclin drugs
    Study type
    OBSERVATIONAL
    Phase
    Not recorded
    Registry status
    Recruiting
    Start
    2024-12-10
    Completion
    2027-02-14
    Enrolment
    48

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

    ConditionArterial Pulmonary Hypertension (PAH)
    InterventionEndothelin receptor antagonist (ERA) combined with PDE5i/sGC agonist dual therapy prostacyclin drugs
    PhaseNot recorded
    Registry statusRecruiting
  • Bioequivalence Study of Macitentan and Tadalafil Film-coated Tablets 10 Mg/40 Mg and 'PrOpsynvi®' Macitentan and Tadalafil Film-coated Tablets 10 Mg/40 Mg

    NCT06553937 · start 2024-05-10

    Registered record
    Registry ID
    NCT06553937
    Conditions
    PAH
    Interventions
    Macitentan and Tadalafil; PrOpsynvi® Film-Coated Tablets
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2024-05-10
    Completion
    2024-07-31
    Enrolment
    30

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

    ConditionPAH
    InterventionMacitentan and Tadalafil; PrOpsynvi® Film-Coated Tablets
    PhasePhase 1
    Registry statusCompleted
  • Macitentan to Prevent PRVO

    NCT05946811 · start 2024-05-01

    Registered record
    Registry ID
    NCT05946811
    Conditions
    Pulmonary Embolism
    Interventions
    Macitentan 10mg
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Withdrawn
    Start
    2024-05-01
    Completion
    2028-06-01
    Enrolment
    0

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

    ConditionPulmonary Embolism
    InterventionMacitentan 10mg
    PhasePhase 3
    Registry statusWithdrawn
  • A Study of Macitentan in Japanese Pediatric Participants With Pulmonary Arterial Hypertension

    NCT05167825 · start 2022-11-14

    Registered record
    Registry ID
    NCT05167825
    Conditions
    Pulmonary Arterial Hypertension
    Interventions
    Macitentan
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Completed
    Start
    2022-11-14
    Completion
    2025-03-05
    Enrolment
    7

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

    ConditionPulmonary Arterial Hypertension
    InterventionMacitentan
    PhasePhase 3
    Registry statusCompleted
  • A Study of Two Macitentan Formulations in Healthy Adult Participants

    NCT05433675 · start 2022-06-22

    Registered record
    Registry ID
    NCT05433675
    Conditions
    Healthy
    Interventions
    Macitentan
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2022-06-22
    Completion
    2022-10-03
    Enrolment
    28

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

    ConditionHealthy
    InterventionMacitentan
    PhasePhase 1
    Registry statusCompleted
  • A Study of Two Different Test Formulations Compared to the Reference Formulation of Macitentan in Healthy Adult Participants

    NCT05392530 · start 2022-05-25

    Registered record
    Registry ID
    NCT05392530
    Conditions
    Healthy
    Interventions
    Macitentan
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2022-05-25
    Completion
    2022-09-14
    Enrolment
    23

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

    ConditionHealthy
    InterventionMacitentan
    PhasePhase 1
    Registry statusCompleted
  • A Study Providing Treatment Access in Participants With Pulmonary Hypertension Completing a Parent Study and Having no Other Option

    NCT05179876 · start 2022-05-04

    Registered record
    Registry ID
    NCT05179876
    Conditions
    Hypertension, Pulmonary
    Interventions
    Macitentan; Selexipag; Macitentan/Tadalafil FDC
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Recruiting
    Start
    2022-05-04
    Completion
    2030-09-30
    Enrolment
    280

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

    ConditionHypertension, Pulmonary
    InterventionMacitentan; Selexipag; Macitentan/Tadalafil FDC
    PhasePhase 3
    Registry statusRecruiting
  • A Study of Real-world Cohort of Pulmonary Arterial Hypertension (PAH) Participants

    NCT04955990 · start 2021-10-14

    Registered record
    Registry ID
    NCT04955990
    Conditions
    Pulmonary Arterial Hypertension
    Interventions
    PAH Therapies
    Study type
    INTERVENTIONAL
    Phase
    Phase 4
    Registry status
    Terminated
    Start
    2021-10-14
    Completion
    2022-12-20
    Enrolment
    232

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

    ConditionPulmonary Arterial Hypertension
    InterventionPAH Therapies
    PhasePhase 4
    Registry statusTerminated
  • Data Analysis for Drug Repurposing for Effective Alzheimer's Medicines (DREAM) - PDE5

    NCT05039086 · start 2021-09-01

    Registered record
    Registry ID
    NCT05039086
    Conditions
    Pulmonary Arterial Hypertension
    Interventions
    PDE5 inhibitor; Endothelin Receptor Antagonists
    Study type
    OBSERVATIONAL
    Phase
    Not recorded
    Registry status
    Completed
    Start
    2021-09-01
    Completion
    2022-10-04
    Enrolment
    13,021

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

    ConditionPulmonary Arterial Hypertension
    InterventionPDE5 inhibitor; Endothelin Receptor Antagonists
    PhaseNot recorded
    Registry statusCompleted
  • A Study of Two Macitentan Pediatric Formulations in Healthy Adult Participants

    NCT04963439 · start 2021-07-08

    Registered record
    Registry ID
    NCT04963439
    Conditions
    Healthy
    Interventions
    Macitentan
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2021-07-08
    Completion
    2021-10-05
    Enrolment
    16

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

    ConditionHealthy
    InterventionMacitentan
    PhasePhase 1
    Registry statusCompleted
  • Initial Dual Oral Combination Therapy Versus Standard-of-care Initial Oral Monotherapy Prior to Balloon Pulmonary Angioplasty in Patients With Inoperable Chronic Thromboembolic Pulmonary Hypertension

    NCT04780932 · start 2021-06-14

    Registered record
    Registry ID
    NCT04780932
    Conditions
    Thromboembolic Pulmonary Hypertension; Chronic Disease; Inoperable Disease
    Interventions
    Macitentan 10mg; Placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 2 / Phase 3
    Registry status
    Completed
    Start
    2021-06-14
    Completion
    2025-07-03
    Enrolment
    96

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

    ConditionThromboembolic Pulmonary Hypertension; Chronic Disease; Inoperable Disease
    InterventionMacitentan 10mg; Placebo
    PhasePhase 2 / Phase 3
    Registry statusCompleted
  • A Study of Macitentan/Tadalafil Combination Administered a Fixed-dose Combination Formulation Compared to the Reference Free Combination of Macitentan and Tadalafil

    NCT04540744 · start 2021-04-30

    Registered record
    Registry ID
    NCT04540744
    Conditions
    Healthy
    Interventions
    FDC of macitentan/tadalafil (10 mg/20 mg); Macitentan 10 mg; Tadalafil 20 mg
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2021-04-30
    Completion
    2021-08-30
    Enrolment
    18

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

    ConditionHealthy
    InterventionFDC of macitentan/tadalafil (10 mg/20 mg); Macitentan 10 mg; Tadalafil 20 mg
    PhasePhase 1
    Registry statusCompleted
  • A Study of Pulmonary Arterial Hypertension Participants Treated With Macitentan or Selexipag

    NCT04567602 · start 2020-10-06

    Registered record
    Registry ID
    NCT04567602
    Conditions
    Pulmonary Arterial Hypertension
    Interventions
    PAH medication
    Study type
    OBSERVATIONAL
    Phase
    Not recorded
    Registry status
    Completed
    Start
    2020-10-06
    Completion
    2024-03-05
    Enrolment
    372

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

    ConditionPulmonary Arterial Hypertension
    InterventionPAH medication
    PhaseNot recorded
    Registry statusCompleted