Protein / target

Prostacyclin receptor

PTGIRP43119Homo sapiensSwiss-Prot
UniProt: P43119Ensembl: ENSG00000160013HGNC: HGNC:9602NCBI Gene: 5739
Clinically validated
Therapeutic maturity
7
Approved medicines
20
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Guanyl-nucleotide exchange factor activity

Strongest disease association

adverse effect

Genetic evidence · score 0.52

Therapeutic maturity

Clinically validated target

7 approved medicines against this target

Druggability

Small molecule

Open Targets tractability · Approved Drug

Clinical development

7 approved · 3 in clinical development

20 linked trials

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function

Receptor for prostacyclin (prostaglandin I2 or PGI2). The activity of this receptor is mediated by G(s) proteins which activate adenylate cyclase

Subcellular location

Cell membrane
Domains and Gene Ontology detail (11)

Gene Ontology

  • Ccytosol
  • Cplasma membrane
  • Fguanyl-nucleotide exchange factor activity
  • Fprostacyclin receptor activity
  • Padenylate cyclase-activating G protein-coupled receptor signaling pathway
  • Pcell-cell signaling
  • PG protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger
  • Pinflammatory response
  • Pnegative regulation of platelet-derived growth factor receptor signaling pathway
  • Pnegative regulation of smooth muscle cell proliferation
  • Ppositive regulation of cytosolic calcium ion concentration

386 aa · 41 kDa

Biological roles

Reactome v97

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

G protein-coupled signallingGOImmune signallingGOHaemostasisGO
View supporting evidence

G protein-coupled signalling

  • ·adenylate cyclase-activating G protein-coupled receptor signaling pathway
  • ·G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messen…

Immune signalling

  • ·inflammatory response

Haemostasis

  • ·negative regulation of platelet-derived growth factor receptor signaling pathway
View underlying pathways (3)
Prostanoid ligand receptors
Prostacyclin signalling through prostacyclin receptor
G alpha (s) signalling events

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Interaction neighbourhood

STRING v12.0

Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.

GNASPTGISTBXA2RPTGS1GNG8PTGS2PDZK1SRCGNGT2CYSLTR2PTGIR

10 strongest partners — larger node and heavier line mean higher confidence

Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.

Drugs targeting this protein

1

Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.

selexipag
Narrow target profileApprovedAgonist

Prostanoid IP receptor agonist

Appears in clinical studies involving idiopathic pulmonary arterial hypertension, pulmonary arterial hypertension, Recurrent thrombophlebitis, pulmonary hypertension

Direct interaction with this protein · Only this protein recorded as a target

ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.

Translational evidence

Open Targets 26

Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.

Strongest genetic associations

Human genetic evidence — the most direct causal link between this target and a disease.

adverse effect0.52

Genetic · overall 0.31

Highest-confidence therapeutic associations

Diseases where a drug acting on this target has already reached clinical development.

pulmonary arterial hypertension0.99

Clinical · overall 0.61

pulmonary hypertension0.95

Clinical · overall 0.58

Recurrent thrombophlebitis0.87

Clinical · overall 0.53

idiopathic pulmonary arterial hypertension0.83

Clinical · overall 0.51

thromboangiitis obliterans0.61

Clinical · overall 0.37

Highest overall evidence

Remaining associations by Open Targets' aggregated evidence score.

neurodegenerative disease0.47

Pathway

idiopathic pulmonary fibrosis0.36

Clinical

pulmonary fibrosis0.33

Clinical

septic shock0.31

Clinical

Show all associations
pulmonary arterial hypertension0.61
pulmonary hypertension0.58
Recurrent thrombophlebitis0.53
idiopathic pulmonary arterial hypertension0.51
neurodegenerative disease0.47
thromboangiitis obliterans0.37
idiopathic pulmonary fibrosis0.36
pulmonary fibrosis0.33
adverse effect0.31
septic shock0.31

Open Targets ranks 189 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.

Known drugs · 10 total

ESUBERAPROSTPhase 3

gout · pulmonary arterial hypertension

TREPROSTINILApproval

pulmonary arterial hypertension · Recurrent thrombophlebitis · idiopathic pulmonary arterial hypertension

RALINEPAGPhase 3

pulmonary arterial hypertension · pulmonary hypertension

ILOPROSTApproval

pulmonary arterial hypertension · Recurrent thrombophlebitis · pulmonary hypertension

EPOPROSTENOLApproval

Recurrent thrombophlebitis · pulmonary hypertension · pulmonary arterial hypertension

EPOPROSTENOL SODIUMApproval

pulmonary hypertension · pulmonary arterial hypertension · idiopathic pulmonary arterial hypertension

TREPROSTINIL SODIUMApproval

pulmonary hypertension · ischemia · chronic thromboembolic pulmonary hypertension

TREPROSTINIL DIOLAMINEPhase 3

pulmonary arterial hypertension · ischemia · scleroderma

ILOPROST TROMETHAMINEApproval

pulmonary hypertension

SELEXIPAGApproval

idiopathic pulmonary arterial hypertension · pulmonary arterial hypertension · Recurrent thrombophlebitis

Tractability

SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · GO CC high confAB · UniProt loc med confAB · UniProt SigP or TMHMMPR · Small Molecule Binder

Safety liabilities

aspirin-intolerant asthma

Clinical trials

20

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.

A Single-center, Open-label, Randomized, Two-period, Two-treatment, Crossover Study in Healthy Male Subjects to Demonstrate Bioequivalence of 1600 μg Selexipag Administered as Eight Tablets of 200 μg (Reference Drug) or as Single Tablet of 1600 μg (Test Drug)PHASE1

COMPLETED · via selexipag · NCT02206295

A Multicenter, Double-blind, Placebo-controlled Phase 3 Study Assessing the Safety and Efficacy of Selexipag on Morbidity and Mortality in Patients With Pulmonary Arterial HypertensionPHASE3

COMPLETED · via selexipag · NCT01106014

A Single-center, Open-label, Randomized, Two-part, Two-treatment, Two-period Crossover Study to Investigate the Effect of Gemfibrozil or Rifampicin on the Pharmacokinetics of Selexipag and Its Metabolite ACT-333679 in Healthy Male Subjects.PHASE1

COMPLETED · via selexipag · NCT02770222

Single-center, Open-label, Randomized, Two-way Crossover Study in Healthy Adult Male Subjects to Compare the Pharmacokinetics of Selexipag (ACT-293987) Following Single Oral Administration of 4 Film-coated Pediatric Tablets of 50 µg vs One Film-coated Tablet of 200 µg SelexipagPHASE1

COMPLETED · via selexipag · NCT02745860

A Multi-center, Double-blind, Placebo-controlled Phase 4 Study in Patients With Pulmonary Arterial Hypertension to Assess the Effect of Selexipag on Daily Life Physical Activity and Patient's Self-reported Symptoms and Their ImpactsPHASE4

COMPLETED · via selexipag · NCT03078907

A Single-center, Open-label, Randomized, Two-treatment Crossover Study to Investigate the Effect of Selexipag on the Pharmacokinetics of Midazolam and Its Metabolite 1-hydroxymidazolam in Healthy Male SubjectsPHASE1

COMPLETED · via selexipag · NCT02791815

Show remaining trials (14)
A Prospective, Multicenter, Open Label, Single Arm, Phase 2 Study to Investigate the Safety, Tolerability and Pharmacokinetics of Selexipag in Children With Pulmonary Arterial HypertensionPHASE2

ACTIVE_NOT_RECRUITING · via selexipag · NCT03492177

A Prospective, Open-label, Platform Study for Long-term Follow-up of Participants Using Study Intervention in Pulmonary Hypertension Parent StudiesPHASE3

RECRUITING · via selexipag · NCT05179876

A Multicenter, Single-arm, Open-label, Long-term Follow-up Safety Study of Selexipag in Participants Who Participated in a Previous Selexipag StudyPHASE3

COMPLETED · via selexipag · NCT04565990

A Multicentre Randomised Cross-over Trial of Disease Specific Therapy in Patients With Pulmonary Arterial Hypertension (PAH) Implanted With Pulmonary Artery Pressure and Cardiac Rhythm Monitoring Devices (CardioMEMS/ConfirmRx)PHASE4

RECRUITING · via selexipag · NCT05825417

A Single-center, Open-label, Two-treatment, One-sequence, Cross-over Study to Investigate the Effect of Clopidogrel on the Pharmacokinetics of Selexipag and Its Active Metabolite, ACT-333679, in Healthy Male SubjectsPHASE1

COMPLETED · via selexipag · NCT03496506

The Efficacy and Safety of Initial Triple Versus Initial Dual Oral Combination Therapy in Patients With Newly Diagnosed Pulmonary Arterial Hypertension: A Multi-center, Double-blind, Placebo-controlled, Phase 3b StudyPHASE3

COMPLETED · via selexipag · NCT02558231

A Multi-center, Double-blind, Randomized, Placebo-controlled, Parallel Group, Exploratory Phase 2 Study to Assess Efficacy and Safety of Selexipag in Adult Subjects With Raynaud's Phenomenon Secondary to Systemic SclerosisPHASE2

COMPLETED · via selexipag · NCT02260557

A Multicenter, Randomized, Double-Blind, Placebo-Controlled Study in Participants With Sarcoidosis-Associated Pulmonary Hypertension (SAPH) to Assess the Efficacy and Safety of Oral Selexipag.PHASE2

TERMINATED · via selexipag · NCT03942211

Selexipag for the Treatment of Schistosomiasis-Associated Pulmonary Arterial HypertensionPHASE2

UNKNOWN · via selexipag · NCT04589390

Single-center, Double-blind, Randomized, Placebo- and Positive-controlled, Parallel-group With Nested Cross-over, Multiple-dose, Up-titration Study of the Effects of Selexipag and Its Metabolite ACT-333679 on Cardiac Repolarization in Healthy Male and Female SubjectsPHASE1

COMPLETED · via selexipag · NCT02206204

A Multicenter, Open-label, Single-sequence Cross-over Study to Assess Safety, Tolerability, and Pharmacokinetics of Intravenous Selexipag in Subjects With Stable Pulmonary Arterial Hypertension Switching From an Oral Stable Dose of SelexipagPHASE3

COMPLETED · via selexipag · NCT03187678

A Randomized, Multicenter, Double-Blind, Placebo-Controlled, Parallel-Group Study With Open-Label Extension Period to Assess the Efficacy and Safety of Selexipag as Add-On Treatment to Standard of Care in Children Aged >=2 to <18 Years With Pulmonary Arterial HypertensionPHASE3

ACTIVE_NOT_RECRUITING · via selexipag · NCT04175600

Multicenter, Open-label, Single-group Study to Assess the Tolerability and the Safety of the Transition From Inhaled Treprostinil to Oral Selexipag in Adult Patients With Pulmonary Arterial HypertensionPHASE3

COMPLETED · via selexipag · NCT02471183

A Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel-group, Group-sequential, Adaptive, Phase 3 Study With Open-label Extension Period to Assess the Efficacy and Safety of Selexipag as an add-on to Standard of Care Therapy in Subjects With Inoperable or Persistent/Recurrent After Surgical and/or Interventional Treatment Chronic Thromboembolic Pulmonary HypertensionPHASE3

TERMINATED · via selexipag · NCT03689244

ClinicalTrials.gov via the drug-target graph.

Forefront confidence

Synthesis

Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.

pulmonary arterial hypertensionWell supported
0.76
agreement 0.60–0.91
Clinical94%Literature6%

Open Targets aggregate 0.61 · 2 independent evidence families

pulmonary hypertensionModerately supported
0.72
agreement 0.57–0.88
Clinical97%Literature3%

Open Targets aggregate 0.58 · 2 independent evidence families

Recurrent thrombophlebitisModerately supported
0.65
agreement 0.48–0.81
Clinical100%

Open Targets aggregate 0.53 · 1 independent evidence family

idiopathic pulmonary arterial hypertensionModerately supported
0.63
agreement 0.48–0.79
Clinical97%Literature3%

Open Targets aggregate 0.51 · 2 independent evidence families

adverse effectModerately supported
0.52
agreement 0.40–0.64
Genetic100%

Open Targets aggregate 0.31 · 1 independent evidence family

The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.

What's happening now

2

Recent activity around this target, drawn from one canonical event stream. Every item is reached through a drug that targets this protein, so each event is news about that drug rather than about the protein directly.

  1. Regulatory approval2016-05-12

    Approval: Uptravi (EMA)

    ema · regulatory · ema · via selexipag

  2. New publication2015-12-01
    Selexipag for the Treatment of Pulmonary Arterial Hypertension.

    The New England journal of medicine · 2015 · 686 citations · Europe PMC · via selexipag

Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.