Selexipag
UPTRAVI
What it isSelective prostacyclin IP receptor agonist; pulmonary arterial hypertension.
Why this oneIts nonprostanoid active metabolite selectively targets IP and has outcomes evidence for delaying PAH progression.
What limits itHeadache, jaw pain, nausea and diarrhea during titration. Gemfibrozil is contraindicated.
FDA-approved for
- pulmonary arterial hypertension (2015)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Pulmonary arterial hypertension | Adults | 200 mcg BID | highest tolerated dose | 1600 mcg BID |
| Pulmonary arterial hypertension | Peds ≥2 yr (by body weight) | 100-200 mcg BID (weight-based) | highest tolerated dose | 800-1600 mcg BID (weight-based) |
Titration Increase at weekly intervals
Renal No adjustment if eGFR ≥15 mL/min; not studied in dialysis or eGFR <15
Hepatic Mild (Child-Pugh A): none; moderate (B): start once daily; severe (C): avoid
Instructions
- Swallow tablets whole; do not split or crush
- Taking with food may improve tolerability
- 100/150 mcg tablets may be dispersed in apple or orange juice or soft food if unable to swallow whole
- If a dose is missed, take ASAP unless next dose within 6 h
- If interrupted ≥3 days, restart at a lower dose and re-titrate
Contraindications
- Concomitant strong CYP2C8 inhibitors (e.g., gemfibrozil)
Cautions
- Pulmonary edema in patients with pulmonary veno-occlusive disease — if confirmed, discontinue
Adverse reactions
- Headache
- Diarrhea
- Jaw pain
- Nausea
- Myalgia
- Vomiting
- Pain in extremity
- Flushing
- Abdominal pain (pediatric)
Pregnancy No adequate human data; animal studies showed no clinically relevant embryofetal effects
Lactation Unknown in human milk; present in rat milk; discontinue nursing or drug
NO BOXED WARNINGS
Principal riskHeadache and jaw pain during titration
Cost, est. cash$1,000–$20,000/month
Generic entry2022
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.
Mechanism of action: Selexipag ballicule
Open Selexipag in the interactive console ↗
Memory aids: mascots and interaction avatars
pag ~ peg bag
