Aprocitentan
Aprocitentan is an endothelin receptor antagonist (ERA) used for the treatment of hypertension, particularly in patients whose blood pressure is not adequately controlled with other medications. It works by blocking the binding of endothelin-1 (ET-1) to its receptors, thereby reducing ET-1-mediated harmful effects including vasoconstriction, inflammation, and fibrosis. This medication represents a novel approach to managing treatment-resistant hypertension.
Aprocitentan is a new antihypertensive drug that blocks endothelin receptors to lower blood pressure in patients with treatment-resistant hypertension.
This medication carries a boxed (black box) warning — the strongest type of FDA warning. Review the full prescribing information before use.
Key facts at a glance
- ATC
- C02KN01
- RxNorm
- 2679059
- Generic
- Aprocitentan
- Class
- atc-c02
- Brands
- Tryvio
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 12.5mg once daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- Not indicated for pediatric patients
- Maximum
- consult physician
- Frequency
- N/A
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 12.5mg once daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
10 groupspregnancy
first trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks; aprocitentan may cause fetal harm based on animal data showing embryofetal toxicity
regular fetal monitoring recommended if used
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
second trimesteravoid if possible
continue avoiding use; consider discontinuing if pregnancy detected
regular fetal monitoring
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
third trimesteravoid if possible
avoid use; discontinue if pregnancy detected
regular fetal monitoring and assessment of fetal well-being
Use of this medication in this population requires careful consideration of risks and benefits.
lactation
breastfeedingavoid breastfeeding
do not breastfeed during treatment with aprocitentan; it is unknown if aprocitentan is excreted in human milk
monitor infant for adverse effects if breastfeeding occurs
Use of this medication in this population requires careful consideration of risks and benefits.
geriatric
elderly 65 and olderno specific dose adjustment required based on age alone
use with caution; monitor blood pressure and renal function closely; start at lower end of dosing range
regular monitoring of blood pressure, renal function, and electrolytes
Use with caution and monitor for adverse effects.
pediatric_age
children under 18not established
safety and efficacy not established in pediatric patients; use only if benefits outweigh risks and under close supervision
closely monitor growth, development, blood pressure, and renal function
renal_impairment
mild renal impairmentno dose adjustment required
use with caution; monitor renal function regularly
monitor renal function (serum creatinine, eGFR) periodically
Use with caution and monitor for adverse effects.
renal_impairment
moderate to severe renal impairmentuse with caution; consider dose reduction in severe impairment
use with caution; not recommended in patients with severe renal impairment (eGFR <30 mL/min); monitor closely
frequent monitoring of renal function and electrolytes
Use with caution and monitor for adverse effects.
hepatic_impairment
mild hepatic impairmentno specific dose adjustment recommended
use with caution; limited data available
monitor liver function tests and blood pressure
Use with caution and monitor for adverse effects.
hepatic_impairment
moderate to severe hepatic impairmentnot recommended
avoid use in patients with moderate to severe hepatic impairment (Child-Pugh Class B and C); aprocitentan is primarily metabolized in liver
monitor liver function if used accidentally
Use of this medication in this population requires careful consideration of risks and benefits.
Statistics and clinical data
FDA approval year
FDA approval for treatment-resistant hypertension
Drug class
Dual endothelin (ETA and ETB) receptor antagonist
Indication
Used when blood pressure remains uncontrolled despite other antihypertensive medications
Mechanism of action
Blocks both ETA and ETB receptors to reduce vasoconstriction and lower blood pressure
Aprocitentan is indicated for the treatment of hypertension, specifically approved for patients whose blood pressure remains uncontrolled despite the use of other antihypertensive medications (treatment-resistant hypertension).
Aprocitentan is an endothelin receptor antagonist that inhibits the binding of endothelin-1 (ET-1) to both ET A and ET B receptors. By blocking these receptors, it prevents ET-1-mediated vasoconstriction, inflammation, fibrosis, and cell proliferation that contribute to elevated blood pressure.
As an endothelin receptor antagonist, aprocitentan may cause fluid retention and edema. Liver function should be monitored during treatment. It is contraindicated in pregnancy due to potential fetal harm. The medication should be used as part of a comprehensive antihypertensive regimen when other agents have proven insufficient.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 26, 2026. · Read our editorial policy