Generic
Selexipag
2 brands available in the market
At a glance
Selexipag is a selective non-prostanoid IP prostacyclin receptor agonist used for the treatment of pulmonary arterial hypertension (PAH, WHO Group I). It delays disease progression and reduces the risk of hospitalization.
Description
Selexipag is an oral prostacyclin receptor (IP receptor) agonist structurally distinct from prostacyclin. It is hydrolyzed by carboxylesterase 1 to yield an active metabolite that is approximately 37-fold more potent than selexipag. Selexipag and its active metabolite are selective for the IP receptor over other prostanoid receptors, inducing vasodilation and inhibiting vascular smooth muscle cell proliferation.
Indications
- Pulmonary Arterial Hypertension (PAH, WHO Group I)
Therapeutic class
Non-prostanoid IP Prostacyclin Receptor Agonist
Pharmacological class
IP Receptor Agonist
Pharmacology
Selexipag activates the IP receptor, inducing vasodilation and inhibiting vascular smooth muscle cell proliferation. It is selective for the IP receptor over other prostanoid receptors (EP1-4, DP, FP, TP) unlike prostacyclin analogs.
Mechanism of action
Activates IP receptors to induce vasodilation and inhibit vascular cell proliferation.
Dosage
Adult Dose (Oral):
- Starting: 200 mcg twice daily
- Titration: Increase by 200 mcg twice daily at weekly intervals to the highest tolerated dose (max 1600 mcg twice daily)
- Moderate hepatic impairment (Child-Pugh B): Start 200 mcg/day; increase by 200 mcg/day weekly
- Severe hepatic impairment (Child-Pugh C): Avoid use
Administration
- Swallow tablet whole; do not split, crush, or chew
- Tolerability may be improved when taken with food
- Take at the same time each day
Missed dose
- Missed dose: Take as soon as possible unless within 6 hours of next dose; if within 6 hours, skip
- If missed for ≥3 days, restart at a lower dose and re-titrate
Side effects
Common Side Effects (>10%):
- Headache (65%)
- Diarrhea (42%)
- Jaw pain (26%)
- Nausea (33%)
- Vomiting (18%)
- Pain in extremity (17%)
- Myalgia (16%)
- Flushing (12%)
- Arthralgia (11%)
- Rash (11%)
1-10%:
- Hemoglobin <10 g/dL (8.6%)
- Anemia (8%)
- Decreased appetite (6%)
Precautions & warnings
- If signs of pulmonary edema occur, consider PVOD; discontinue if confirmed
- Avoid use in severe hepatic impairment (Child-Pugh C)
- Do not use with strong CYP2C8 inhibitors
Contraindications
- Concomitant use of strong CYP2C8 inhibitors (e.g., gemfibrozil)
Drug interactions
- Strong CYP2C8 inhibitors: Significantly increase exposure to selexipag and active metabolite; avoid
- CYP2C8 inducers (rifampin): Halve active metabolite exposure; double dose with rifampin; reduce dose when rifampin stopped
Food interactions
Caution is advised when consuming alcohol with Selexipag; consult your doctor.
Use in pregnancy
Use in Pregnancy: No adequate controlled studies in pregnant women; use only if clearly needed; consult your doctor.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Unknown if secreted in human milk; discontinue selexipag or breastfeeding; consult your doctor.
Pediatric use
Safety and effectiveness not established in pediatric patients
Geriatric use
No overall differences observed between elderly and younger patients
Renal / hepatic impairment
Renal Impairment: No dosage adjustment needed; consult your doctor.
Hepatic Impairment: Mild (Child-Pugh A): no dose adjustment; Moderate (Child-Pugh B): start 200 mcg/day; Severe (Child-Pugh C): avoid use; consult your doctor.
Overdose effects
Isolated cases of overdose up to 3200 mcg reported; mild transient nausea was the only consequence; provide supportive measures.
Storage conditions
Store in a dry place, away from light and heat; keep out of reach of children.
Chemical structure
Selexipag