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Pulmonary Arterial HypertensionEPICNCT02484807

Effect of Pharmacologic Interaction Between ERAs and PDE-5 Inhibitors on Medication Serum Levels and Clinical Disease Status in Patients With PAH

An observational study of Pulmonary Arterial Hypertension, run by Heidelberg University at 1 site in Germany.

Completed

Finished. The study has ended and is not enrolling. Results may be posted on the official record.

Official record
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Trial summary

The development of disease-targeted medication for the treatment of pulmonary arterial hypertension (PAH) has significantly improved within the last years, leading to the development of 10 approved agents. Read more about this study

Who is it for?
Ages 18 years and older
Conditions the study is for
Pulmonary Arterial Hypertension
How many people
125 participants
Where
1 siteGermany
Study dates
May 2015to Dec 2016
Phase
Observational
Are there results?
Yes, posted in the registrySummary in the doctors' view

Key requirements

Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.

  • Ages 18 years and older
  • All sexes
  • No healthy volunteers
  • Adult, Older adult

Study population: patients with pulmonary arterial hypertension receiving disease-targeted combination therapy

Who may be able to join

  • Men and women ≥ 18 years old
  • Diagnosis of PAH according to ESC/ERS-guidelines: patients with manifest pulmonary arterial hypertension, mean pulmonary arterial pressure ≥25mmHg, measured by right heart catheterization.
  • Combination treatment with ERA (Bosentan, Ambrisentan or Macitentan) and PDE-5-Inhibitor (Sildenafil or Tadalafil) for more than 3 months.

Who cannot join

  • Underage patients
  • Pregnancy or lactation

Trial locations and contacts

1 site in 1 country.

Germany1 site
  • Centre for pulmonary hypertension, Thoraxclinic at the University Hospital Heidelberg

    Heidelberg, 69126

Other trials in Germany

About this study

Official title: Effect of Pharmacologic Interaction Between Endothelin-Receptor-Antagonists and Phosphodiesterase-5 Inhibitors on Medication Serum Levels and Clinical Disease Status in Patients Wih Pulmonary Arterial Hypertension

The development of disease-targeted medication for the treatment of pulmonary arterial hypertension (PAH) has significantly improved within the last years, leading to the development of 10 approved agents. Combination treatment with Endothelin-Receptor-Antagonists (ERA) and Phosphodiesterase-Type-5-Inibitors (PDE-5-Inhibitor) has become increasingly important for the treatment of PAH. In a recent press release, the results of the AMBITION study reported that an upfront combination treatment immediately after diagnosis leads to a delayed disease progression [4]. Thus, the question if there is a clinically relevant pharmaco-dynamic drug-drug interaction is of rising interest.

Read the detailed description

Mechanisms of action Three ERAs have been approved for the treatment of PAH including the dual inhibitors Bosentan and Macitentan and the selective Endothelin Receptor type A inhibitor (ETA-Inhibitor) Ambrisentan. The dual antagonists inhibit both ETA- and the type B (ETB)-receptor, while the selective antagonist only affects the ETA-receptor [2]. The physiologic ligand of the receptors is Endothelin-1, which binds to the ETA-receptor and causes vasoconstriction and proliferation of the vascular smooth muscle cells. The binding to the ETB-receptor leads to an endogenous production of NO and prostacyclin in the endothelial cells.

PDE-5-Inhibitors include the two substances Sildenafil and Tadalafil. They inhibit the degradation of cyclic guanosine monophosphate (cGMPs), which triggers the vasodilative effect of endothelial NO.

Interaction There is evidence for the pharmacokinetic interaction (inhibition / induction of critical targets of drug metabolism and drug distribution) of both substance classes: the PDE-5-Inhibitors Sildenafil and Tadalafil are mainly eliminated in the liver by the hepatic enzyme Cytochrom-P450-Oxygenase type 3A4 (CYP3A4). The dual inhibitor Bosentan is both a substrate and an inductor of the Cytochrom-P450-Oxydase type 3A4 and type 2C9 [5,6].

It has already been shown in an in vivo-study, that simultaneous application of PDE-5-Inhibitors and Bosentan leads to a systemic reduction of the PDE-5-Inhibitor concentration of 40%, due to the CYP3A4-inducing effect of Bosentan [5]. Sildenafil, in contrast, leads to a decreased degradation of Bosentan in the liver with an approximately 50% increase in plasma leves. An anticipated result, especially when higher dosages of Sildenafil are applied, is the accumulation of Bosentan and reduction of Sildenafil levels.

A recent in vitro-study has shown that Tadalafil may also serve as CYP3A4-inductor, while this effect has not been detected for Sildenafil [7].

In contrast Macitentan which has been approved in 2013, has no clinically relevant CYP3A4-inducing effects. [8]. The in vitro-study has also detected a further interaction between ERAs and PDE-5-Inhibitors. Both PDE-5-Inhibitors Sildenafil and Tadalafil affect the transport molecules organic anion transporting polypeptides (OATPs), which are responsible for the hepatocellular intake of the dual ERA Bosentan. They also had a mild effect on the intake of Ambrisentan.

Sildenafil is a potent inhibitor of OATPs, whereas Tadalafil shows only minor inhibition of OATPs [7]. Both Sildenafil and Tadalafil significantly reduce the intracellular concentration of Bosentan in the liver, leading to a reduced degradation of Bosentan. For Ambrisentan this effect seemed to be less pronounced [7]. Consequently, this mechanisms of action lead to higher ERA-levels and to decreased PDE-5-Inhibitor plasma concentrations in patients receiving combination treatment. The most distinct interaction is expected for the combination of Sildenafil (PDE-5-Inhibitor) and Bosentan (ERA).

Up to now, the prevalence and role of this pharmacokinetic interaction for the clinical status and progression of the disease is not clear. Respective combination treatments have only been investigated in healthy male volunteers so far [5,9].

Being tested
no intervention, only observation of different groups
Medical subject headings
Pulmonary Arterial Hypertension

What participants receive

What participants receive. In a randomised study each person is assigned to one group by chance.

  • no intervention, only observation of different groupsOther

Study groups in NCT02484807
Study groupRoleWhat they receive
Bosentan + SildenafilCombination treatment with Bosentan + Sildenafil at baseline
Receives: Other: no intervention, only observation of different groups
Bosentan + TadalafilCombination treatment with Bosentan + Tadalafil at baseline
Receives: Other: no intervention, only observation of different groups
Ambrisentan + SildenafilCombination treatment with Ambrisentan + Sildenafil at baseline
Receives: Other: no intervention, only observation of different groups
Ambrisentan + TadalafilCombination treatment with Ambrisentan + Tadalafil at baseline
Receives: Other: no intervention, only observation of different groups
Macitentan + SildenafilCombination treatment with Macitentan + Sildenafil at baseline
Receives: Other: no intervention, only observation of different groups
Macitentan + TadalafilCombination treatment with Macitentan + Tadalafil at baseline
Receives: Other: no intervention, only observation of different groups

What is being measured

The primary outcome is the main question the study is designed to answer.

  1. Characterisation of Medication Levels

    comparison of different combination treatment arms (mean ± standard deviation), measurement of endothelin receptor antagonist plasma concentrations and PDE-5I plasma concentrations, results given es multiple of the expected mean plasma concentration (MOM). Due to technical setup measurement of plasma concentrations of macitentan was not possible.

    The expected mean concentration ranges (MOM) refer to data extracted from published plasma concentration-time profiles measured during monotherapy with sildenafil, tadalafil, bosentan, and ambrisentan and served as comparative values. Each individually measured drug concentration was set in proportion to the expected mean concentration and expressed as a multiple of the expected mean (MoM), with values <1 denoting lower and values >1 higher values than the expected mean.

    Measured: baseline vs. measurement after 3-6 months

Secondary outcomes (6)
  1. Impact of Medication Adjustment

    Change of medication serum levels after clinically indicated medication adaptation in patients who received Bosentan + Sildenafil in the beginning and changed the ERA to Macitentan

    1. change of mean levels ± standard deviation
    2. frequency of borderline medication serum levels or medication levels out of the therapeutic window The expected mean concentration ranges (MOM) refer to data extracted from published plasma concentration-time profiles measured during monotherapy with sildenafil, tadalafil, bosentan, and ambrisentan and served as comparative values. Each individually measured drug concentration was set in proportion to the expected mean concentration and expressed as a multiple of the expected mean (MoM), with values <1 denoting lower and values >1 higher values than the expected mean.

    Measured: baseline vs. measurement 3-6 months after switch

  2. Clinical Relevance 6 Minute Walking Distance

    • Changes of medication levels after adjustment of combination therapy if clinically indicated
    • correlation with clinical routine parameters indicating clinical disease status

    Measured: baseline vs. measurement 3-6 months after switch

  3. Clinical Relevance NTproBNP

    • Changes of medication levels after adjustment of combination therapy if clinically indicated
    • correlation with clinical routine parameters indicating clinical disease status

    Measured: baseline vs. measurement after 3-6 months

  4. Clinical Relevance Echocardiography Systolic Pulmonary Arterial Pressure (sPAP)

    • Changes of medication levels after adjustment of combination therapy if clinically indicated
    • correlation with clinical routine parameters indicating clinical disease status

    Measured: baseline vs. measurement after 3-6 months

  5. Clinical Relevance Echocardiography Tricuspid Annular Plane Systolic Excursion (TAPSE)

    • Changes of medication levels after adjustment of combination therapy if clinically indicated
    • correlation with clinical routine parameters indicating clinical disease status

    Measured: baseline vs. measurement after 3-6 months

  6. Clinical Relevance Blood Gas Analysis Oxygen Saturation

    • Changes of medication levels after adjustment of combination therapy if clinically indicated
    • correlation with clinical routine parameters indicating clinical disease status

    Measured: baseline vs. measurement after 3-6 months

Timeline

From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.

  1. First posted30 Jun 2015 (estimated)
  2. Study startMay 2015
  3. Primary completionDec 2016
  4. Study completionDec 2016

Resources

More details

For doctors and researchers: how the study is designed, who runs it, and its registry IDs.

Study design
Study type
Observational
Observational model
Cohort
Time perspective
Prospective
Enrolment
125 participants (actual)
IDs, dates and publications
ClinicalTrials.gov ID
NCT02484807
Sponsor's protocol ID
EPIC-01
Acronym
EPIC
Status last verified
Jan 2020
First submitted
24 Jun 2015
Last updated
5 Feb 2020
Data monitoring committee
No

Publications

  • Galie N, Hoeper MM, Humbert M, Torbicki A, Vachiery JL, Barbera JA, Beghetti M, Corris P, Gaine S, Gibbs JS, Gomez-Sanchez MA, Jondeau G, Klepetko W, Opitz C, Peacock A, Rubin L, Zellweger M, Simonneau G; ESC Committee for Practice Guidelines (CPG). Guidelines for the diagnosis and treatment of pulmonary hypertension: the Task Force for the Diagnosis and Treatment of Pulmonary Hypertension of the European Society of Cardiology (ESC) and the European Respiratory Society (ERS), endorsed by the International Society of Heart and Lung Transplantation (ISHLT). Eur Heart J. 2009 Oct;30(20):2493-537. doi: 10.1093/eurheartj/ehp297. Epub 2009 Aug 27. No abstract available.

    PubMed 19713419
  • Humbert M, Sitbon O, Simonneau G. Treatment of pulmonary arterial hypertension. N Engl J Med. 2004 Sep 30;351(14):1425-36. doi: 10.1056/NEJMra040291. No abstract available.

    PubMed 15459304
  • Voelkel NF, Gomez-Arroyo J, Abbate A, Bogaard HJ, Nicolls MR. Pathobiology of pulmonary arterial hypertension and right ventricular failure. Eur Respir J. 2012 Dec;40(6):1555-65. doi: 10.1183/09031936.00046612. Epub 2012 Jun 27.

    PubMed 22743666
  • Wrishko RE, Dingemanse J, Yu A, Darstein C, Phillips DL, Mitchell MI. Pharmacokinetic interaction between tadalafil and bosentan in healthy male subjects. J Clin Pharmacol. 2008 May;48(5):610-8. doi: 10.1177/0091270008315315. Epub 2008 Feb 27.

    PubMed 18305126
  • Paul GA, Gibbs JS, Boobis AR, Abbas A, Wilkins MR. Bosentan decreases the plasma concentration of sildenafil when coprescribed in pulmonary hypertension. Br J Clin Pharmacol. 2005 Jul;60(1):107-12. doi: 10.1111/j.1365-2125.2005.02383.x.

    PubMed 15963102
  • Weiss J, Theile D, Spalwisz A, Burhenne J, Riedel KD, Haefeli WE. Influence of sildenafil and tadalafil on the enzyme- and transporter-inducing effects of bosentan and ambrisentan in LS180 cells. Biochem Pharmacol. 2013 Jan 15;85(2):265-73. doi: 10.1016/j.bcp.2012.11.020. Epub 2012 Dec 5.

    PubMed 23219525
  • Weiss J, Theile D, Ruppell MA, Speck T, Spalwisz A, Haefeli WE. Interaction profile of macitentan, a new non-selective endothelin-1 receptor antagonist, in vitro. Eur J Pharmacol. 2013 Feb 15;701(1-3):168-75. doi: 10.1016/j.ejphar.2013.01.010. Epub 2013 Jan 23.

    PubMed 23353592
  • Burgess G, Hoogkamer H, Collings L, Dingemanse J. Mutual pharmacokinetic interactions between steady-state bosentan and sildenafil. Eur J Clin Pharmacol. 2008 Jan;64(1):43-50. doi: 10.1007/s00228-007-0408-z. Epub 2007 Nov 27.

    PubMed 18040672

Questions about this trial

What is this clinical trial studying?

An observational study of Pulmonary Arterial Hypertension, run by Heidelberg University at 1 site in Germany.

The full registered description is in the About this study section and the official record.

Who may be eligible to take part?

The sponsor lists 3 inclusion and 2 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.

Is this clinical trial currently recruiting?

The record says: finished, as of the sponsor's last update on 5 Feb 2020. Status can change between updates, so confirm with the study contact before making plans.

Where is the study taking place?

The record lists 1 site in Germany. Whether a site is taking part right now should be confirmed with that site. See every site.

What are the possible benefits and risks?

They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.

Are results available for this study?

Yes. Results are posted in the registry (first posted 5 Feb 2020). A summary is in the For doctors view, and the full results are on ClinicalTrials.gov.

How can a doctor refer a patient or contact the research team?

The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.

What does the primary outcome measure?

Characterisation of Medication Levels (time frame: baseline vs. measurement after 3-6 months). It is what the study was designed to measure, not a finding.

Where can I read the original study information?

On the ClinicalTrials.gov record for NCT02484807, which also lists 8 linked publications.

Does a listing mean the treatment is approved or proven to work?

No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.

How often is this information updated?

AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 5 Feb 2020.

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