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Macitentan/ tadalafil

Phase 1

Healthy Subjects | Small molecule | Other |Johnson & Johnson|Last Updated: Jun 22, 2025

Target and mechanism

Molecular targetEDNRB, EDNRA
Target classAntagonist
ModalitySmall molecule

Also known as Macitentan

Success Probability

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Market & Valuation

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Trial Design

RandomizedCONTROLLED
Total Trials2
Total Enrollment58

FDA Designations

No designations recorded

Clinical trial landscape

Macitentan/ tadalafil · 2 trials · 1 indication

Phase 1 2
NCT03359291Clinical Study to Investigate the Effect of Macitentan on the Concentrations of Rosuvastatin in the Blood of Healthy Male SubjectsHealthy Subjects
COMPLETED20 Analytics
NCT03215966A Study to Compare the Macitentan-tadalafil Fixed Dose Combination Tablet Relative to the Concomitant Administration of the Reference Tablets of Macitentan and Tadalafil in Healthy SubjectsHealthy Subjects
COMPLETED38 Analytics
PHASE1COMPLETED
Clinical Study to Investigate the Effect of Macitentan on the Concentrations of Rosuvastatin in the Blood of Healthy Male Subjects
Healthy SubjectsUnlock trial analytics
PHASE1COMPLETED
A Study to Compare the Macitentan-tadalafil Fixed Dose Combination Tablet Relative to the Concomitant Administration of the Reference Tablets of Macitentan and Tadalafil in Healthy Subjects
Healthy SubjectsUnlock trial analytics

Study Endpoints

Primary Endpoints

AUC(0-inf) of rosuvastatin following administration of rosuvastatin alone (treatment A) and in combination with macitentan (treatment B)
From Day1 to Day17 (treatment A: from Day1-Day5 and treatment B: from Day10-Day17)

AUC(0-inf) is the area under the plasma concentration-time curves of rosuvastatin, calculated from time zero to the extrapolated infinite time

Cmax of rosuvastatin following administration of rosuvastatin alone (treatment A) and in combination with macitentan (treatment B)
From Day1 to Day17 (treatment A: from Day1-Day5 and treatment B: from Day10-Day17)

Cmax is the maximum observed plasma concentration and is directly derived from the individual plasma concentration time curves of rosuvastatin

Maximum plasma concentration (Cmax) of macitentan and tadalafil
Blood samples for pharmacokinetic evaluations are collected at selected time points from Baseline (pre-dose) to 216 hours post-dose of each study period

The measured individual plasma concentrations of macitentan and tadalafil are used to directly obtain Cmax

Area under the plasma concentration-time curve from 0 to time t [AUC(0-t)] of macitentan and tadalafil
Blood samples for pharmacokinetic evaluations are collected at selected time points from Baseline (pre-dose) to 216 hours post-dose of each study period

AUC(0-t) is the area calculated from the concentration-time profile of macitentan and tadalafil, from time 0 to to time t of the last measured concentration above the limit of quantification

Area under the plasma concentration-time curve to infinitiy [AUC(0-inf)] of macitentan and tadalafil
Blood samples for pharmacokinetic evaluations are collected at selected time points from Baseline (pre-dose) to 216 hours post-dose of each study period

AUC(0-inf) is the area calculated from the concentration-time profile of macitentan and tadalafil, from time 0 to extrapolated infinite time

Secondary Endpoints

tmax of rosuvastatin following administration of rosuvastatin alone (treatment A) and in combination with macitentan (treatment B)
From Day1 to Day17 (treatment A: from Day1-Day5 and treatment B: from Day10-Day17)
t½ of rosuvastatin following administration of rosuvastatin alone (treatment A) and in combination with macitentan (treatment B)
From Day1 to Day17 (treatment A: from Day1-Day5 and treatment B: from Day10-Day17)
AUC(0-t) of rosuvastatin following administration of rosuvastatin alone (treatment A) and in combination with macitentan (treatment B)
From Day1 to Day17 (treatment A: from Day1-Day5 and treatment B: from Day10-Day17)
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Study Design & Arms

AllocationNA
MaskingNONE
ModelSINGLE_GROUP
PurposeOTHER

Treatment Arms

ArmTypeDescription
Sequence ABEXPERIMENTALSubjects participate in two study periods: During the first period (treatment A), they receive a single oral dose of rosuvastatin on Day 1. During the second period (treatment B), they receive a single oral loading dose of macitentan on Day 5 and oral doses of macitentan from Day 6 to Day 16 (i.e., 11 doses). Subjects receive a single oral dose of 10 mg rosuvastatin concomitantly with macitentan in the morning of Day 10.
Sequence A/BEXPERIMENTALSubjects receive one tablet of macitentan / tadalafil FDC (fixed dose combination) during Period 1, then after a washout period of at least 7 days they receive one tablet of macitentan (Opsumit®) and two tablets of tadalafil (Adcirca®) during Period 2
Sequence B/AEXPERIMENTALSubjects receive one tablet of macitentan (Opsumit®) and two tablets of tadalafil (Adcirca®) during Period 1, then after a washout period of at least 7 days, they receive one tablet of macitentan / tadalafil FDC (fixed dose combination) during Period 2

Interventions

NameTypeDescription
RosuvastatinDRUGSingle oral dose of 10 mg rosuvastatin (film-coated tablet) on Day 1 and Day 10
MacitentanDRUGSingle oral dose of 30 mg macitentan (film-coated tablet) on Day 5 and 10 mg macitentan administered orally from Day 6 to Day 16
Macitentan / tadalafil FDCCOMBINATION_PRODUCTTablets for oral administration containing 10 mg of macitentan and 40 mg of tadalafil
Macitentan (Opsumit®)DRUGFilm-coated tablets for oral administration formulated at a strength of 10 mg
Tadalafil (Adcirca®)DRUGFilm-coated tablets for oral administration formulated at a strength of 20 mg
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Eligibility Criteria

Age Range18 Years to 55 Years
SexMALE
Healthy VolunteersYes
Study Sites1

Principal Inclusion Criteria: * Signed informed consent in the local language prior to any study-mandated procedure. * Healthy male subjects aged between 18 and 55 years (inclusive) at screening. * No clinically significant findings on the physical examination at screening. * Body mass index of 18....

Countries:Germany
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Frequently asked questions about Macitentan/ tadalafil

What is Macitentan used for?

Macitentan is an investigational small molecule being studied for systemic sclerosis, pulmonary arterial hypertension (PAH, WHO Group 1 PH), congenital heart disease, and heart failure with preserved ejection fraction. It is also used in clinical trials involving healthy subjects. The drug is in Phase 2 development for these indications.

What does Macitentan target?

Macitentan is a small molecule being developed for cardiovascular conditions. It is being studied in patients with pulmonary arterial hypertension and heart failure with preserved ejection fraction. The drug's specific molecular target is not disclosed in the available information.

Who makes Macitentan?

Macitentan is developed by Johnson & Johnson, a company traded on the New York Stock Exchange under the ticker JNJ. The drug is currently in Phase 2 clinical development for cardiovascular indications.

What phase is Macitentan in?

Macitentan is in Phase 2 clinical development. It is an investigational drug and has not been approved by regulatory authorities. The drug is being studied for systemic sclerosis, pulmonary arterial hypertension, congenital heart disease, and heart failure with preserved ejection fraction.

What clinical trials is Macitentan in?

Macitentan has been studied in 10 clinical trials with a total enrollment of 3,395 participants. One trial is active, and nine are completed. Notable trials include NCT04273945, a Phase 3 study of a 75 mg dose in pulmonary arterial hypertension, and NCT03153111, a Phase 2 study in heart failure with preserved ejection fraction.

Is Macitentan the same as Macitentan 10 mg?

Yes, Macitentan is also known as Macitentan 10 mg. This alternative name refers to the 10 mg dosage form of the drug. The drug is being developed by Johnson & Johnson under the ticker JNJ.