Selexipag

UPTRAVI

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Pronunciation: se-LEX-i-pag (up-TRA-vee)

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

Selexipag UPTRAVI mascot mnemonic cartoon — Visual mnemonic: Selexipag mascot
**“Up-Travis Selects a pag”**
pag ~ peg bag

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.

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

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

Available strengths

tab 0.1, 0.15, 0.2, 0.4, 0.6, 0.8, 1, 1.2, 1.4, 1.6 mg
inj 1.8 mg

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

Cost

Selexipag (UPTRAVI)

Strength		#/mo	CostPlus
0.1 mg	tab	60 BID	not offered
0.15 mg	tab	60 BID	not offered
0.2 mg	tab	60 BID	not offered
0.4 mg	tab	60 BID	not offered
0.6 mg	tab	60 BID	not offered
0.8 mg	tab	60 BID	not offered
1 mg	tab	60 BID	not offered
1.2 mg	tab	60 BID	not offered
1.4 mg	tab	60 BID	not offered
1.6 mg	tab	60 BID	not offered
1.8 mg	inj	per unit	not offered

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

Generic entry2022

NO BOXED WARNINGS

Principal riskHeadache and jaw pain during titration

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4

Overdose danger1 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

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.

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Memory aids: interaction avatars

CYP2C8 substrate

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