Aprocitentan

TRYVIO

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Pronunciation: a-proe-sye-TEN-tan (trye-VEE-oe)

Aprocitentan ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Aprocitentan ballicule

What it isEndothelin-receptor antagonist; hypertension uncontrolled despite standard combination therapy.

Why this oneIt targets endothelin vasoconstriction when conventional RAAS blockade, calcium blockade, and diuresis remain insufficient.

What limits it⚑ Embryo-fetal toxicity requires a REMS; fluid retention and anemia can make resistant hypertension harder to manage.

Aprocitentan molecular structure (skeletal formula) — Molecular structure: Aprocitentan

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Embryo-fetal toxicity — contraindicated in pregnancy; exclude pregnancy before initiation; effective contraception before, during, and for 1 month after treatment; discontinue as soon as pregnancy is detected.

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

Aprocitentan (TRYVIO)

Strength		#/mo	generic $/mo	CostPlus
12.5 mg	tab	30 qd		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Aprocitentan is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

⚠ BOXED WARNING

Embryo-fetal toxicity

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger1 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk4 / 4

Legacy pregnancy categoryN/A (post-2015 labeling)

Defining liabilityEmbryofetal toxicity, fluid retention and anemia

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