PMID- 28524738
OWN - NLM
STAT- MEDLINE
DCOM- 20170629
LR  - 20190109
IS  - 1751-2441 (Electronic)
IS  - 1751-2433 (Linking)
VI  - 10
IP  - 7
DP  - 2017 Jul
TI  - Selexipag, a selective prostacyclin receptor agonist in pulmonary arterial 
      hypertension: a pharmacology review.
PG  - 753-762
LID - 10.1080/17512433.2017.1322900 [doi]
AB  - Pulmonary hypertension is defined by a mean pulmonary artery pressure >/=25 mm Hg 
      at rest. Management of pulmonary arterial hypertension (PAH) includes specific 
      drug therapy with calcium channel blockers in vasoreactive patients, or drugs 
      approved for PAH in non-reactive patients that target the endothelin, 
      nitric-oxide and prostacyclin pathways. Areas covered: The review covers receptor 
      selectivity, pharmacokinetics, pharmacodynamics and adverse effects (AEs) of 
      intravenous (IV) epoprostenol (synthetic prostacyclin); the prostacyclin analogs 
      iloprost, beraprost, and treprostinil administered by IV, subcutaneous, inhaled 
      or oral routes; and the oral selective prostacyclin receptor agonist selexipag. 
      Expert commentary: Development of a selective prostacyclin receptor agonist has 
      aimed at identifying compounds with improved pharmacological properties. The high 
      selectivity of selexipag, and its active metabolite ACT-333679, for the 
      prostacyclin receptor, in conjunction with pharmacokinetic properties that reduce 
      peak-trough fluctuations and the up-titration regimen used at the start of 
      treatment, are collectively considered to minimize AEs associated with 
      prostacyclin use. In a large phase 3 study, selexipag-associated AEs were 
      consistent with those observed with drugs that target the prostacyclin pathway, 
      and mainly mild to moderate in severity. The dosing flexibility afforded by oral 
      selexipag may facilitate achieving the maximum therapeutic effect with acceptable 
      tolerability in patients with PAH.
FAU - Honorato Perez, Jesus
AU  - Honorato Perez J
AD  - a Medicina y Cirugia , Universidad Complutense de Madrid , Madrid , Spain.
AD  - b Medicina Interna y Farmacologia Clinica , Universidad de Navarra , Pamplona , 
      Spain.
AD  - c Servicio de Farmacologia Clinica , Clinica Universidad de Navarra , Pamplona , 
      Spain.
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20170519
PL  - England
TA  - Expert Rev Clin Pharmacol
JT  - Expert review of clinical pharmacology
JID - 101278296
RN  - 0 (Acetamides)
RN  - 0 (Acetates)
RN  - 0 (Antihypertensive Agents)
RN  - 0 (Pyrazines)
RN  - 0 (Receptors, Epoprostenol)
RN  - 5EXC0E384L (selexipag)
RN  - E9PC7N0DID ((4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid)
SB  - IM
MH  - Acetamides/*administration & dosage/adverse effects/pharmacology
MH  - Acetates/metabolism
MH  - Administration, Oral
MH  - Animals
MH  - Antihypertensive Agents/*administration & dosage/adverse effects/pharmacology
MH  - Drug Design
MH  - Humans
MH  - Hypertension, Pulmonary/*drug therapy/physiopathology
MH  - Pyrazines/*administration & dosage/adverse effects/metabolism/pharmacology
MH  - Receptors, Epoprostenol/agonists
OTO - NOTNLM
OT  - Pulmonary arterial hypertension
OT  - Selexipag
OT  - pharmacology
OT  - prostacyclin receptor agonists
EDAT- 2017/05/20 06:00
MHDA- 2017/07/01 06:00
CRDT- 2017/05/20 06:00
PHST- 2017/05/20 06:00 [pubmed]
PHST- 2017/07/01 06:00 [medline]
PHST- 2017/05/20 06:00 [entrez]
AID - 10.1080/17512433.2017.1322900 [doi]
PST - ppublish
SO  - Expert Rev Clin Pharmacol. 2017 Jul;10(7):753-762. doi: 
      10.1080/17512433.2017.1322900. Epub 2017 May 19.