Bosentan
TRACLEER
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.
FDA-approved for
- pulmonary arterial hypertension (2001)
FDA label
Read the full label on DailyMed ↗
| 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
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
⚠ BOXED WARNINGS
- Hepatotoxicity
- Embryo-fetal toxicity
Cost, est. cash$10–$300/month
Generic entry2019
Classes and tags
Clinical profile
Legacy pregnancy categoryX
Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.
Mechanism of action: Bosentan ballicule
Open Bosentan in the interactive console ↗
Memory aids: mascots and interaction avatars
