REMS restricted

Bosentan

TRACLEER

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Pronunciation: boe-SEN-tan

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

Bosentan TRACLEER mascot mnemonic cartoon — Visual mnemonic: Bosentan mascot
**“Boss E.T., Track clearer”**

What it isEndothelin-A receptor antagonist; pulmonary arterial hypertension.

Why this oneIt was the first oral therapy for pulmonary arterial hypertension.

What limits itHepatotoxicity requires monthly liver tests, and it is teratogenic under a REMS. CYP3A4 and CYP2C9 induction can defeat contraception.

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

FDA-approved for

pulmonary arterial hypertension (2001)

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger1 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk4 / 4

Legacy pregnancy categoryX

Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Hepatotoxicity — measure aminotransferases before and monthly during treatment; embryo-fetal toxicity — contraindicated in pregnancy, exclude pregnancy before start; available only through a restricted REMS program.

FDA dosing	Population	Start	Target	Max
Pulmonary arterial hypertension (WHO Group 1)	>12 yr and >40 kg	62.5 mg BID	125 mg BID (after 4 wk)	125 mg BID
Pulmonary arterial hypertension	≤12 yr (weight-based per Table 1)	weight-based (Table 1)	weight-based (Table 1)	weight-based (Table 1)

Titration Increase to maintenance dose after 4 weeks

Renal No adjustment needed

Hepatic Not studied in severe impairment (Child-Pugh C); exposure increased in moderate (Child-Pugh B) — avoid in moderate-to-severe impairment; reduce dose or discontinue if aminotransferases >3× ULN

Instructions

Enroll in Bosentan REMS; monthly liver aminotransferase monitoring; exclude pregnancy before initiation
May be taken with or without food
Reduce dose and closely monitor if aminotransferases >3× ULN

Available strengths

tab 32, 62.5, 125 mg

Contraindications

Pregnancy
Concomitant cyclosporine A
Concomitant glyburide

Cautions

Hepatotoxicity (dose-dependent aminotransferase elevations)
Fluid retention (may require intervention)
Pulmonary veno-occlusive disease — consider if pulmonary edema occurs
Decreased sperm counts
Decreased hemoglobin/hematocrit — monitor at 1 and 3 months, then every 3 months

Adverse reactions

Respiratory tract infection
Anemia

Pregnancy Contraindicated — may cause fetal harm/birth defects (boxed); exclude pregnancy before start and use reliable contraception

Lactation Discontinue either breastfeeding or bosentan

Cost

Bosentan (TRACLEER)

Strength		#/mo	CostPlus
32 mg	tab	60 BID	not offered
62.5 mg	tab	60 BID	not offered
125 mg	tab	60 BID	not offered

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

Generic entry2019

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Memory aids: interaction avatars

CYP3A4 inducer (moderate)

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Self-check

How often are liver tests required with bosentan?
Monthly.
What can bosentan’s enzyme induction defeat?
Contraception.