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

NCT ID: NCT02476864

Last Updated: 2025-02-03

Basic Information

• Recruitment Status: COMPLETED
• Clinical Phase: PHASE1
• Total Enrollment: 12 participants
• Study Classification: INTERVENTIONAL
• Study Start Date: 2015-08-31
• Study Completion Date: 2015-12-31

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.

Detailed Description

The purpose of this study is to establish biocomparison of 2 types of tablets containing macitentan: a pediatric dispersible tablet and the adult film-coated tablet. A single oral dose of each tablet will be given to healthy subjects on 2 different periods separated by a washout phase of 10 to 14 days.

Biocomparison will be based on the comparison of the pharmacokinetic parameters of macitentan with the two types of tablets using specific statistical methods. The pharmacokinetic parameters will be considered equivalent if specific criteria defined in the study protocol are met.

Conditions

Healthy Subjects

Study Design

• Allocation Method: RANDOMIZED
• Intervention Model: CROSSOVER
• Primary Study Purpose: OTHER
• Blinding Strategy: NONE

Study Groups

Sequence AB

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

Group Type: EXPERIMENTAL

Treatment A (adult formulation)

Intervention Type: 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.

Treatment B (pediatric formulation)

Intervention Type: 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 BA

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

Group Type: EXPERIMENTAL

Treatment A (adult formulation)

Intervention Type: 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.

Treatment B (pediatric formulation)

Intervention Type: 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.

Interventions

Treatment A (adult formulation)

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.

Intervention Type: DRUG

Treatment B (pediatric formulation)

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.

Intervention Type: DRUG

Other Intervention Names

Opsumit

Eligibility Criteria

Inclusion Criteria

• 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

Exclusion Criteria

• 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

• Minimum Eligible Age: 18 Years
• Maximum Eligible Age: 45 Years
• Eligible Sex: MALE
• Accepts Healthy Volunteers: Yes

Sponsors

Actelion

INDUSTRY

Sponsor Role: lead

Responsible Party

Responsibility Role: SPONSOR

Principal Investigators

Patricia Sidharta, PharmD, PhD

Role:

Actelion

Other Identifiers

2015-001623-23

Identifier Type: EUDRACT_NUMBER

Identifier Source: secondary_id

AC-055-121

Identifier Type: -

Identifier Source: org_study_id