Aprocitentan
TRYVIO
Pronunciation: a-proe-sye-TEN-tan (trye-VEE-oe)
What it isEndothelin-receptor antagonist; hypertension uncontrolled despite standard combination therapy.
Why this oneTargets endothelin vasoconstriction when conventional RAAS blockade, calcium blockade, and diuresis remain insufficient.
What limits itAdds only modest BP reduction; fluid retention, anemia and hepatotoxicity complicate use.
Pearls
- Check hemoglobin and liver enzymes.
- Contraception through 1 month after stopping.
- May lower sperm count.
Aprocitentan prescription history
Animated chart of estimated U.S. prescriptions per year, Antihypertensives (1953–2026). Aprocitentan enters in 2024 (estimated).
Classes and tags
Clinical profile
Legacy pregnancy categoryN/A (post-2015 labeling)
Defining liabilityEmbryofetal toxicity, fluid retention and anemia
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Hypertension not adequately controlled on other antihypertensives (studied in uncontrolled BP despite ≥3 drugs) | Adults | 12.5 mg QD | 12.5 mg QD | 12.5 mg QD |
Renal No adjustment for eGFR ≥15 mL/min (mild–severe); not recommended in kidney failure (eGFR <15) or on dialysis
Hepatic No adjustment in mild (Child-Pugh A); not recommended in moderate–severe (Child-Pugh B/C)
Do not take two doses on the same day
Instructions
- Swallow tablets whole; with or without food
- Missed dose: skip; do not take two doses on the same day
- Exclude pregnancy before initiation; effective contraception during and for 1 month after treatment
- Measure aminotransferases and total bilirubin before starting and periodically; do not initiate if ALT/AST >3x ULN or in moderate–severe hepatic impairment
- Measure hemoglobin before starting and periodically; initiation not recommended in severe anemia
Available strengths
- tab 12.5 mg
Contraindications
- Pregnancy
Cautions
- Hepatotoxicity (ERA class effect) — monitor LFTs; stop and evaluate for symptoms of hepatotoxicity; discontinue for sustained/clinically relevant elevations, bilirubin >2x ULN, or clinical symptoms
- Fluid retention/peripheral edema (9%) — risk higher with older age and CKD; not recommended in NYHA III–IV heart failure, unstable cardiac function, or NT-proBNP ≥500 pg/mL; may require diuretics; consider discontinuation if significant
- Hemoglobin decrease (>2 g/dL drop in 7%) — do not start in severe anemia; monitor hemoglobin
- Decreased sperm counts (ERA class) — counsel males on potential fertility effects
- Initial small eGFR decrease within first 6 weeks, then stabilizes
Adverse reactions
- Edema/fluid retention (9.1% vs 2.1% placebo)
- Anemia (3.7% vs 0)
- Hypersensitivity reactions (rash, erythema, allergic edema; 0.8%)
- Mean hemoglobin decrease ~0.8 g/dL
Pregnancy Contraindicated — can cause embryo-fetal toxicity incl. birth defects and fetal death (ERA-class teratogenicity in animals at all doses tested); discontinue as soon as pregnancy detected
Lactation Do not breastfeed during treatment (excreted in rat milk; potential for serious adverse reactions in breastfed infants)
Cost
| Strength | #/mo | generic $/mo | CostPlus | |
|---|---|---|---|---|
| 12.5 mg | tab | 30 qd | not offered |
Open Aprocitentan in the interactive console ↗
Self-check
- What hypertension setting is aprocitentan used for?
Uncontrolled despite standard combination therapy. - Which toxicity requires aprocitentan’s REMS?
Embryo-fetal toxicity.