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AMR Drug RepurposingSmart Screeningresearch prototype

Aprocitentan

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

Registered studies
14
Lab records
0
Pathogens at ≥40%
1 of 4

Chemical structure

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

Existing / approved use

Documented · FDA, WHO, ChEMBL

Approved for

  • Hypertension

Indications ChEMBL records as approved, from FDA and DailyMed labels. Label ↗

WHO therapeutic group
Other antihypertensives
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
  • MRSA35.0% AI-predicted activityBelow the ≥40% mark this site uses to surface candidates.
  • E. coli23.0% AI-predicted activityBelow the ≥40% mark this site uses to surface candidates.
  • K. pneumoniae20.2% AI-predicted activityBelow the ≥40% mark this site uses to surface candidates.
  • M. tuberculosis59.5% 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

14registered studies name this medicine, for any condition. See them below.

Experimental

No evidence found

No laboratory measurement against the four pathogens in the ChEMBL records loaded here.

Open Aprocitentan in ChEMBL Registered studies below

Docking

Computational · nothing measured

Dihydrofolate reductase ↗ (E. coli)

-7.2 kcal/mol

0better fit →-12

KPC-2 carbapenemase ↗ (K. pneumoniae)

-7.6 kcal/mol

0better fit →-12

Enoyl-ACP reductase (InhA) ↗ (M. tuberculosis)

-7.6 kcal/mol

0better fit →-12

Dihydrofolate reductase ↗ (MRSA)

-7.0 kcal/mol

0better fit →-12

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 Aprocitentan 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 Evaluating Aprocitentan Tablets(SYH9108) for the Treatment of Resistant Hypertension

    NCT07635914 · start 2026-05-31

    Registered record
    Registry ID
    NCT07635914
    Conditions
    Resistant Hypertension
    Interventions
    Aprocitentan tablets(SYH9108); Placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Not yet recruiting
    Start
    2026-05-31
    Completion
    2030-05-31
    Enrolment
    382

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

    ConditionResistant Hypertension
    InterventionAprocitentan tablets(SYH9108); Placebo
    PhasePhase 3
    Registry statusNot yet recruiting

  • A Drug-drug Interaction Trial in Healthy Female Participants to Investigate the Effect of Aprocitentan on Combined Hormonal Contraceptives

    NCT06799884 · start 2025-01-18

    Registered record
    Registry ID
    NCT06799884
    Conditions
    Drug Drug Interaction
    Interventions
    Ethinyl Estradiol / Levonorgestrel Oral Tablet; Aprocitentan
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2025-01-18
    Completion
    2025-02-21
    Enrolment
    19

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

    ConditionDrug Drug Interaction
    InterventionEthinyl Estradiol / Levonorgestrel Oral Tablet; Aprocitentan
    PhasePhase 1
    Registry statusCompleted

  • Bioequivalence Study of Different Aprocitentan Tablet Formulations

    NCT05196399 · start 2022-02-02

    Registered record
    Registry ID
    NCT05196399
    Conditions
    Healthy Subjects
    Interventions
    Aprocitentan (Formulation A); Aprocitentan (Formulation B)
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2022-02-02
    Completion
    2022-04-07
    Enrolment
    36

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

    ConditionHealthy Subjects
    InterventionAprocitentan (Formulation A); Aprocitentan (Formulation B)
    PhasePhase 1
    Registry statusCompleted

  • The Effect of Hepatic Impairment on Aprocitentan Pharmacokinetics

    NCT04252495 · start 2020-06-26

    Registered record
    Registry ID
    NCT04252495
    Conditions
    Hepatic Impairment; Healthy Subjects
    Interventions
    Aprocitentan
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2020-06-26
    Completion
    2021-05-06
    Enrolment
    17

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

    ConditionHepatic Impairment; Healthy Subjects
    InterventionAprocitentan
    PhasePhase 1
    Registry statusCompleted

  • To Study the Effect of Aprocitentan on the Electrical Activity of the Heart in Healthy Men and Women

    NCT04281342 · start 2020-01-14

    Registered record
    Registry ID
    NCT04281342
    Conditions
    Healthy Subjects
    Interventions
    Aprocitentan 25 mg; Aprocitentan 100 mg; Matching placebo; Moxifloxacin control to establish assay sensitivity
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2020-01-14
    Completion
    2021-09-03
    Enrolment
    48

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

    ConditionHealthy Subjects
    InterventionAprocitentan 25 mg; Aprocitentan 100 mg; Matching placebo; Moxifloxacin control to establish assay sensitivity
    PhasePhase 1
    Registry statusCompleted

  • A Research Study to Show Aprocitentan is Efficacious and Safe to Treat Patients With Uncontrolled Blood Pressure and Chronic Kidney Disease.

    NCT04162366 · start 2020-01

    Registered record
    Registry ID
    NCT04162366
    Conditions
    Hypertension; Renal Insufficiency, Chronic
    Interventions
    Aprocitentan 25 mg; Placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Withdrawn
    Start
    2020-01
    Completion
    2021-07-15
    Enrolment
    0

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

    ConditionHypertension; Renal Insufficiency, Chronic
    InterventionAprocitentan 25 mg; Placebo
    PhasePhase 3
    Registry statusWithdrawn

  • A Study to Evaluate How Aprocitentan is Safe and How it is Absorbed and Broken Down in the Body of Japanese and Caucasian Subjects

    NCT03586570 · start 2018-07-17

    Registered record
    Registry ID
    NCT03586570
    Conditions
    Healthy Subjects
    Interventions
    Aprocitentan 25mg; Placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2018-07-17
    Completion
    2018-09-10
    Enrolment
    20

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

    ConditionHealthy Subjects
    InterventionAprocitentan 25mg; Placebo
    PhasePhase 1
    Registry statusCompleted

  • A Research Study to Show the Effect of Aprocitentan in the Treatment of Difficult to Control (Resistant) High Blood Pressure (Hypertension) and Find Out More About Its Safety

    NCT03541174 · start 2018-06-18

    Registered record
    Registry ID
    NCT03541174
    Conditions
    Resistant Hypertension
    Interventions
    Aprocitentan 12.5 mg; Aprocitentan 25 mg; Placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Completed
    Start
    2018-06-18
    Completion
    2022-04-25
    Enrolment
    730

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

    ConditionResistant Hypertension
    InterventionAprocitentan 12.5 mg; Aprocitentan 25 mg; Placebo
    PhasePhase 3
    Registry statusCompleted

  • A Study in Healthy Male Subjects to Investigate Whether Administration of ACT-132577 Can Affect Rosuvastatin's Fate in the Body (Amount and Time of Presence in the Blood)

    NCT03245229 · start 2017-08-10

    Registered record
    Registry ID
    NCT03245229
    Conditions
    Healthy Subjects
    Interventions
    Aprocitentan; Rosuvastatin
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2017-08-10
    Completion
    2017-09-18
    Enrolment
    20

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

    ConditionHealthy Subjects
    InterventionAprocitentan; Rosuvastatin
    PhasePhase 1
    Registry statusCompleted

  • A Study to Evaluate ACT-132577 in Healthy Subjects and in People With Severe Kidney Disease

    NCT03165071 · start 2017-06-03

    Registered record
    Registry ID
    NCT03165071
    Conditions
    Severe Renal Impairment; Healthy Subjects
    Interventions
    ACT-132577
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2017-06-03
    Completion
    2017-10-27
    Enrolment
    16

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

    ConditionSevere Renal Impairment; Healthy Subjects
    InterventionACT-132577
    PhasePhase 1
    Registry statusCompleted

  • A Study to Evaluate ACT-132577 in Healthy Male Subjects

    NCT03100591 · start 2017-03-28

    Registered record
    Registry ID
    NCT03100591
    Conditions
    Healthy Subjects
    Interventions
    14C-radiolabeled ACT-132577
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2017-03-28
    Completion
    2017-04-18
    Enrolment
    6

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

    ConditionHealthy Subjects
    Intervention14C-radiolabeled ACT-132577
    PhasePhase 1
    Registry statusCompleted

  • A Study to Investigate the Effect of ACT-132577 on the Pharmacokinetics of Midazolam and 1-hydroxy Midazolam in Healthy Male Subjects

    NCT02841761 · start 2016-07-01

    Registered record
    Registry ID
    NCT02841761
    Conditions
    Healthy Subjects
    Interventions
    Midalozam; Aprocitentan
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2016-07-01
    Completion
    2016-10-01
    Enrolment
    20

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

    ConditionHealthy Subjects
    InterventionMidalozam; Aprocitentan
    PhasePhase 1
    Registry statusCompleted

  • Clinical Study to Assess Body Fluid Homeostasis After Administration of ACT-132577 in Healthy Subjects

    NCT02708004 · start 2016-06-01

    Registered record
    Registry ID
    NCT02708004
    Conditions
    Healthy Subjects
    Interventions
    Aprocitentan; Placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2016-06-01
    Completion
    2016-12-01
    Enrolment
    24

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

    ConditionHealthy Subjects
    InterventionAprocitentan; Placebo
    PhasePhase 1
    Registry statusCompleted

  • Dose-finding Study With ACT-132577 (Aprocitentan) in Participants With Essential Hypertension

    NCT02603809 · start 2015-12-14

    Registered record
    Registry ID
    NCT02603809
    Conditions
    Essential Hypertension
    Interventions
    Aprocitentan 5 mg; Aprocitentan 10 mg; Aprocitentan 25 mg; Aprocitentan 50 mg; Lisinopril 20 mg; Placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Completed
    Start
    2015-12-14
    Completion
    2017-04-07
    Enrolment
    1,659

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

    ConditionEssential Hypertension
    InterventionAprocitentan 5 mg; Aprocitentan 10 mg; Aprocitentan 25 mg; Aprocitentan 50 mg +2 more
    PhasePhase 2
    Registry statusCompleted