Comparison of the Pharmacokinetic Properties of Two Tablet Formulations of Macitentan in Healthy Adults

NCT02476864 | Completed Phase 1

• 2 other identifiers: AC-055-1212015-001623-23
• Study Type: interventional
• Target: 12
• Locations: 0 countries
• Sites: N/A

Brief Summary

A study conducted in healthy adults to investigate if a new macitentan tablet leads to the same fate of macitentan in the body (time of onset, time of presence, amount in the blood) as the marketed macitentan tablet.

Conditions

Healthy Subjects

Keywords

macitentan; biocomparison; safety

Outcome Measures

Primary Outcomes (1)

• Plasma pharmacokinetic profile

  Pharmacokinetic profile will be determined by the following parameters: Cmax (Maximum plasma concentration), tmax (Time to reach Cmax), t1/2 (Terminal half-life), AUC(0-t) (Area under the plasma concentration-time curve from zero to time t of the last measured concentration above the limit of quantification), AUC(0-inf) (Area under the plasma concentration-time curve from zero to infinity)

  From pre-dose to 216 hours post-dose

Other Outcomes (2)

• Incidence of adverse events

  from baseline to Day 10-13 post-dose

• ECG abnormalities

  from baseline to to Day 10-13 post-dose

Study Arms (2)

Sequence AB

EXPERIMENTAL

Subjects receive treatment A in Period 1 followed by treatment B in Period 2 with a washout phase of 10 to 14 days between the two treatment periods

Drug: Treatment A (adult formulation); Drug: Treatment B (pediatric formulation)

Sequence BA

EXPERIMENTAL

Subjects receive treatment B in Period 1 followed by treatment A in Period 2 with a washout phase of 10 to 14 days between the two treatment periods

Drug: Treatment A (adult formulation); Drug: Treatment B (pediatric formulation)

Interventions

Treatment A (adult formulation) DRUG

Single oral administration of one film-coated tablet containing 10 mg of macitentan as active substance and lactose, magnesium stearate, microcrystalline cellulose, povidone, sodium starch glycolate type A, polysorbate as inactive ingredients.The film coat contains titanium dioxide, talc, xanthan gum, polyvinyl alcohol, and soy lecithin.

Also known as: Opsumit

Sequence AB; Sequence BA

Treatment B (pediatric formulation) DRUG

Single oral administration of two dispersible tablets, each containing 5 mg of macitentan as active ingredient and Mannitol delta polymorphic crystals, mannitol, isomalt, isomalt agglomerated, croscarmellose sodium, and magnesium stearate as inactive ingredients.

Sequence AB; Sequence BA

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Signed informed consent
• Healthy on the basis of the physical examination, vital signs (systolic and diastolic blood pressure, heart rate), 12-lead ECG, and laboratory tests performed at screening

You may not qualify if:

• History or clinical evidence of any disease and/or condition, which might interfere with the absorption, distribution, metabolism or excretion of the study drug
• Previous history of fainting, collapse, syncope, orthostatic hypotension, or vasovagal reactions
• History or clinical evidence of alcoholism or drug abuse within the 3 -year period prior to screening
• Excessive caffeine consumption
• Smoking within 3 months prior to screening and inability to refrain from smoking during the course of the study
• Previous treatment with any prescribed medications (including vaccines) or over-the counter medications within 2 weeks prior to first study drug administration
• Loss of 250 mL or more of blood within 3 months prior to screening
• Any circumstances or conditions, which, in the opinion of the investigator, may affect full participation in the study or compliance with the protocol

Sponsors & Collaborators

• Actelion: lead

MeSH Terms

Interventions

macitentan

Study Officials

• Patricia Sidharta, PharmD, PhD

  Actelion

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: OTHER
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: June 11, 2015
• First Posted: June 22, 2015
• Study Start: August 1, 2015
• Primary Completion: December 1, 2015
• Study Completion: December 1, 2015
• Last Updated: February 3, 2025

Record last verified: 2025-01