Macitentan

Macitentan
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Gerald Chi

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Black Box Warning

WARNING: EMBRYO-FETAL TOXICITY See full prescribing information for complete Boxed Warning. * Do not administer OPSUMIT to a pregnant female because it may cause fetal harm. Females of reproductive potential: Exclude pregnancy before the start of treatment, monthly during treatment, and 1 month after stopping treatment. Prevent pregnancy during treatment and for one month after stopping treatment by using acceptable methods of contraception. For all female patients, OPSUMIT is available only through a restricted program called the OPSUMIT Risk Evaluation and Mitigation Strategy (REMS).

Overview

Macitentan is an endothelin receptor antagonist and antihypertensive that is FDA approved for the {{{indicationType}}} of pulmonary artery hypertension. There is a Black Box Warning for this drug as shown here. Common adverse reactions include anemia, influenza, headache, urinary tract infections, bronchitis, nasopharyngitis, and pharyngitis.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Pulmonary Arterial Hypertension

• OPSUMIT® is an endothelin receptor antagonist (ERA) indicated for the treatment of pulmonary arterial hypertension (PAH, WHO Group I) to delay disease progression. Disease progression included: death, initiation of intravenous (IV) or subcutaneous prostanoids, or clinical worsening of PAH (decreased 6-minute walk distance, worsened PAH symptoms and need for additional PAH treatment). OPSUMIT also reduced hospitalization for PAH.
• Effectiveness was established in a long-term study in PAH patients with predominantly WHO Functional Class II-III symptoms treated for an average of 2 years. Patients were treated with OPSUMIT monotherapy or in combination with phosphodiesterase-5 inhibitors or inhaled prostanoids. Patients had idiopathic and heritable PAH (57%), PAH caused by connective tissue disorders (31%), and PAH caused by congenital heart disease with repaired shunts (8%).

• Dosing Information

• The recommended dosage of OPSUMIT is 10 mg once daily for oral administration. Doses higher than 10 mg once daily have not been studied in patients with PAH and are not recommended.
• Initiate treatment with OPSUMIT in females of reproductive potential only after a negative pregnancy test. Obtain monthly pregnancy test during treatment.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Macitentan in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Macitentan in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding FDA-Labeled Use of Macitentan in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

• The safety and efficacy of OPSUMIT in children have not been established.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Macitentan in pediatric patients.

Contraindications

• Pregnancy

• OPSUMIT may cause fetal harm when administered to a pregnant woman. OPSUMIT is contraindicated in females who are pregnant. OPSUMIT was consistently shown to have teratogenic effects when administered to animals. If OPSUMIT is used during pregnancy, apprise the patient of the potential hazard to a fetus.

Warnings

WARNING: EMBRYO-FETAL TOXICITY See full prescribing information for complete Boxed Warning. * Do not administer OPSUMIT to a pregnant female because it may cause fetal harm. Females of reproductive potential: Exclude pregnancy before the start of treatment, monthly during treatment, and 1 month after stopping treatment. Prevent pregnancy during treatment and for one month after stopping treatment by using acceptable methods of contraception. For all female patients, OPSUMIT is available only through a restricted program called the OPSUMIT Risk Evaluation and Mitigation Strategy (REMS).

• Description

Precautions

• Description

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Clinical Trial Experience of Macitentan in the drug label.

Body as a Whole

Cardiovascular

Digestive

Endocrine

Hematologic and Lymphatic

Metabolic and Nutritional

Musculoskeletal

Neurologic

Respiratory

Skin and Hypersensitivy Reactions

Special Senses

Urogenital

Miscellaneous

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Macitentan in the drug label.

Body as a Whole

Cardiovascular

Digestive

Endocrine

Hematologic and Lymphatic

Metabolic and Nutritional

Musculoskeletal

Neurologic

Respiratory

Skin and Hypersensitivy Reactions

Special Senses

Urogenital

Miscellaneous

Drug Interactions

• Drug

• Description

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

• Pregnancy Category

Pregnancy Category (AUS):

• Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Macitentan in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Macitentan during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Macitentan with respect to nursing mothers.

Pediatric Use

There is no FDA guidance on the use of Macitentan with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Macitentan with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Macitentan with respect to specific gender populations.

Race

There is no FDA guidance on the use of Macitentan with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Macitentan in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Macitentan in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Macitentan in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Macitentan in patients who are immunocompromised.

Administration and Monitoring

Administration

• Oral

• Intravenous

Monitoring

There is limited information regarding Monitoring of Macitentan in the drug label.

• Description

IV Compatibility

There is limited information regarding IV Compatibility of Macitentan in the drug label.

Overdosage

Acute Overdose

Signs and Symptoms

• Description

Management

• Description

Chronic Overdose

There is limited information regarding Chronic Overdose of Macitentan in the drug label.

Pharmacology

Macitentan
Systematic (IUPAC) name
N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide
Identifiers
CAS number	441798-33-0
ATC code	C02KX04
PubChem	16004692
Chemical data
Formula	Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox
Mol. mass	588.273 g/mol
SMILES	eMolecules & PubChem
Synonyms	ACT-064992
Pharmacokinetic data
Bioavailability	?
Metabolism	Hydrolysis, oxidation (CYP3A4)
Half life	?
Excretion	2/3 urine, 1/3 faeces
Therapeutic considerations
Pregnancy cat.	X(US)
Legal status	[[Prescription drug|Template:Unicode-only]](US) FDA approved drug
Routes	Oral

Mechanism of Action

Structure

This image is provided by the National Library of Medicine.

Pharmacodynamics

There is limited information regarding Pharmacodynamics of Macitentan in the drug label.

Pharmacokinetics

There is limited information regarding Pharmacokinetics of Macitentan in the drug label.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Macitentan in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Macitentan in the drug label.

How Supplied

Storage

There is limited information regarding Macitentan Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Patient Counseling Information of Macitentan in the drug label.

Precautions with Alcohol

• Alcohol-Macitentan interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

• Opsumit®

Look-Alike Drug Names

• A® — B®

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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