Aprocitentan

Class
Antihypertensives
Subclass
Endothelin receptor antagonists
Substance name
Aprocitentan
Brand names
Tryvio®
Common formulations
Film-coated tablet
Dosage and administration
Adults patients
Treatment of hypertension • Resistant
•
12.5 mg PO daily
Taken with or without food. Administered in combination with other antihypertensives.
Indications for use
Labeled indications
Adults
•
Treatment of hypertension (resistant)
Safety risks
Boxed warnings
Fetal toxicity
•
Obtain a negative pregnancy test before initiating aprocitentan in patients who can become pregnant, and advise them to use adequate methods of contraception and take monthly pregnancy tests throughout treatment and for one month after treatment.
Contraindications
Hypersensitivity to aprocitentan or its components
Severe anemia
Warnings and precautions
Anemia, decreased hematocrit
•
Maintain a high level of suspicion, as aprocitentan has been associated with an increased risk of these adverse events. Measure hemoglobin before and periodically during treatment as clinically indicated.
Decreased sperm concentration
•
Maintain a high level of suspicion, as aprocitentan, similar to other endothelin receptor antagonists, may have an adverse effect on spermatogenesis.
Fluid retention, peripheral edema, HF
•
Maintain a high level of suspicion in patients with older age or CKD. Monitor for signs and symptoms of fluid retention, weight gain, and worsening HF. Do not use aprocitentan in patients with HF (NYHA stage III-IV), unstable cardiac function, or with NT-proBNP ≥ 500 pg/mL, as aprocitentan has not been studied in these patients.
Increased serum transaminases
•
Maintain a high level of suspicion, as aprocitentan has been associated with an increased risk of elevated serum transaminases. Measure serum transaminases and TBIL before and periodically during treatment. Discontinue aprocitentan if sustained, clinically relevant aminotransferase elevations occur or when accompanied by an increase in bilirubin > 2× ULN.
Specific populations
Renal impairment
eGFR ≥ 15 mL/min/1.73 m²
•
Use acceptable. No dose adjustment required. Monitor for fluid retention.
eGFR < 15 mL/min/1.73 m²
•
Do not use.
Renal replacement therapy
Any modality
•
Do not use.
Hepatic impairment
Child-Pugh A (mild)
•
Use acceptable. No dose adjustment required. Monitor serum aminotransferases.
Child-Pugh B (moderate)
•
Do not use.
Child-Pugh C (severe)
•
Do not use.
Unexplained abnormality in LFTs
•
Use with caution. Do not use aprocitentan in patients with serum aminotransferase levels > 3× upper limit of normal.
Pregnancy and breastfeeding
Pregnancy
All trimesters
•
Do not use. Evidence of fetal harm in humans. Obtain a negative pregnancy test before initiating aprocitentan. Advise using effective contraception and taking monthly pregnancy tests throughout treatment and for one month after discontinuation. Discontinue aprocitentan when pregnancy is detected.
Breastfeeding
Do not use during breastfeeding.
Unknown amount excreted in breastmilk.
Unknown drug levels in breastfed infants.
May potentially cause adverse effects in breastfed infants.
Adverse reactions
Common 1-10%
•
Anemia, fluid retention
Unknown frequency
•
↓ GFR, ↓ hematocrit, ↓ sperm concentration, ↑ serum transaminases, hepatotoxicity, skin rash, skin erythema
Interactions
Drug(s)
Check Interactions
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