selexipag: prostacyclin receptor agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
selexipag : A member of the class of pyrazines that is N-(methanesulfonyl)-2-{4-[(propan-2-yl)(pyrazin-2-yl)amino]butoxy}acetamide carrying two additional phenyl substituents at positions 5 and 6 on the pyrazine ring. An orphan drug used for the treatment of pulmonary arterial hypertension. It is a prodrug for ACT-333679 (the free carboxylic acid). [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 9913767 |
| CHEMBL ID | 238804 |
| CHEBI ID | 90844 |
| SCHEMBL ID | 674122 |
| MeSH ID | M0514408 |
| Synonym |
|---|
| ns-304 |
| act-293987 |
| CHEMBL238804 |
| selexipag |
| 2-{4-[n-(5,6-diphenylpyrazin-2-yl)-n-isopropylamino]butyloxy}-n-(methylsulfonyl)acetamide |
| selexipag (jan/usan/inn) |
| 475086-01-2 |
| uptravi (tn) |
| D09994 |
| ns 304 |
| act 293987 |
| 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)-n-(methylsulfonyl)acetamide |
| selexipag [usan:inn] |
| unii-5exc0e384l |
| 2-(4-((5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino)butoxy}-n-(methanesulfonyl)acetamide |
| 5exc0e384l , |
| uptravi |
| act293987 |
| S3726 |
| selexipag [orange book] |
| selexipag [inn] |
| selexipag [jan] |
| selexipag [who-dd] |
| 2-{4-[(5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}-n-(methanesulfonyl)acetamide |
| selexipag [mi] |
| selexipag [usan] |
| gtpl7552 |
| 2-[4-[[5,6-di(phenyl)pyrazin-2-yl]-propan-2-ylamino]butoxy]-n-methylsulfonylacetamide |
| SCHEMBL674122 |
| CS-3774 |
| CHEBI:90844 , |
| QXWZQTURMXZVHJ-UHFFFAOYSA-N |
| 2-[4-[(5,6-diphenyl-2-pyrazinyl)(1-methylethyl)amino]butoxy]-n-(methylsulfonyl)acetamide |
| HY-14870 |
| AC-30209 |
| AKOS024457572 |
| DB11362 |
| 2-{4-[(5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}-n-methanesulfonylacetamide |
| NCGC00370833-01 |
| ns-304(selexipag) |
| mfcd10567093 |
| BS-16872 |
| 2-(4-((5,6-diphenyl-2-pyrazinyl)(isopropyl)amino)butoxy)-n-(methylsulfonyl)acetamide |
| BCP09146 |
| bdbm50235383 |
| Q15424759 |
| AMY10851 |
| selexipag(ns-304) |
| SB17055 |
| 2-[4-[(5,6-diphenylpyrazin-2-yl)-propan-2-ylamino]butoxy]-n-methylsulfonylacetamide |
| CCG-269668 |
| ns-304;act-293987 |
| FT-0776043 |
| NCGC00370833-02 |
| A857156 |
| EN300-7378417 |
| DTXSID301027959 |
| 2-[4-[(5,6-diphenyl-2-pyrazinyl)(1-methylethyl)amino]butoxy]-n-(methylsulfonyl)acetamide; 2-[4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy]-n-(methylsulfonyl)acetamide; act 293987; ns 304; uptravi; |
| uptravi titration pack |
| selexipagum |
| 2-(4-((5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino)butoxy)-n-(methanesulfonyl)acetamide |
| b01ac27 |
| EX-A7991 |
Slexipag is a first-in-class, oral, long-acting, selective, non-prostanoid agonist of the prostacyclin receptor (IP receptor), indicated for the treatment of symptomatic adult pulmonary arterial hypertension (PAH)
| Excerpt | Reference | Relevance |
|---|---|---|
| "Selexipag has a high selectivity for the IP2-receptor and differs from conventional prostacyclin analogues in its chemical structure." | ( A Special Focus on Selexipag - Treatment of Pulmonary Arterial Hypertension. Grimm, D; Infanger, M; Kruger, M; Nassef, MZ; Simonsen, U; Sorensen, LM; Wehland, M, 2017) | 1.5 |
| "Selexipag has been approved and is used in the clinical treatment of PAH worldwide." | ( The selective PGI2 receptor agonist selexipag ameliorates Sugen 5416/hypoxia-induced pulmonary arterial hypertension in rats. Fuchikami, C; Honda, Y; Kosugi, K; Kuramoto, K; Kuwano, K; Numakura, Y, 2020) | 1.55 |
Oral selexipag was considered as a treatment which adds value, compared to iloprost, in the following MCDA quantitative criteria: comparative efficacy, patient reported outcomes, preventive benefit, therapeutic benefit, other medical costs and other non-medical costs. There were no significant differences in safety profile but with a higher acquisition cost than inhaled Iloprost.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Oral selexipag for PAH treatment was considered as a treatment which adds value, compared to iloprost, in the following MCDA quantitative criteria: comparative efficacy, patient reported outcomes, preventive benefit, therapeutic benefit, other medical costs and other non-medical costs, without significant differences in safety profile but with a higher acquisition cost than inhaled iloprost." | ( Determining the value contribution of selexipag for the treatment of pulmonary arterial hypertension (PAH) in Spain using reflective multi-criteria decision analysis (MCDA). Ais, A; Beaudet, A; Gil, A; Jiménez, A, 2018) | 1.27 |
| "Treatment with selexipag did not reduce the number of RP attacks compared with placebo. " | ( Efficacy and Safety of Selexipag in Adults With Raynaud's Phenomenon Secondary to Systemic Sclerosis: A Randomized, Placebo-Controlled, Phase II Study. Denton, CP; Frenoux, JM; Frey, A; Hachulla, É; Herrick, AL; Le Brun, FO; Riemekasten, G; Schwarting, A, 2017) | 1.12 |
Selexipag is a new drug with mild adverse reactions and is safe for the treatment of PAH. The adverse reactions were mild with headache, diarrhea and nausea reported as the main symptoms.
Steady-state levels of selexipag and ACT-333679 after repeated doses of 400 μg selexIPag had no influence on the warfarin pharmacodynamic variables. The 90% CIs of the geometric mean ratios of AUC and Cmax for R- and S-warfarin were inside the reference range.
| Excerpt | Reference | Relevance |
|---|---|---|
| " However, due to its low dose and relatively low unbound exposure, selexipag has a low potential for causing drug-drug interactions." | ( The metabolism and drug-drug interaction potential of the selective prostacyclin receptor agonist selexipag. Äänismaa, P; de Kanter, R; Delahaye, S; Gnerre, C; Ichikawa, T; Pfeifer, T; Seeland, S; Segrestaa, J; Treiber, A; Yamada, T, 2018) | 0.93 |
The absolute oral bioavailability of selexipag (90% CI) was 49. The bioavailability after oral administration is approximately 50%.
Slexipag may enable earlier combination therapy targeting the three-molecular pathways of PAH with anticipated improvements in daily- and long-term clinical function and outcome in PAH. The dosing flexibility afforded by oral selexipags may facilitate achieving the maximum therapeutic effect.
| Role | Description |
|---|---|
| orphan drug | Any drug that has been developed specifically for treatment of a rare medical condition, the condition itself being known as an orphan disease. |
| prostacyclin receptor agonist | An agonist that binds to and activates prostacyclin receptors |
| platelet aggregation inhibitor | A drug or agent which antagonizes or impairs any mechanism leading to blood platelet aggregation, whether during the phases of activation and shape change or following the dense-granule release reaction and stimulation of the prostaglandin-thromboxane system. |
| vasodilator agent | A drug used to cause dilation of the blood vessels. |
| prodrug | A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| monocarboxylic acid amide | A carboxamide derived from a monocarboxylic acid. |
| ether | An organooxygen compound with formula ROR, where R is not hydrogen. |
| pyrazines | |
| aromatic amine | An amino compound in which the amino group is linked directly to an aromatic system. |
| tertiary amino compound | A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups. |
| N-sulfonylcarboxamide | A mixed diacylamine resulting from the formal condensation of the nitrogen of a carboxamide with a sulphonic acid. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 16.9330 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 23.9185 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 21.3174 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 23.9185 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 23.9185 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 23.9185 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 23.9185 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Prostacyclin receptor | Homo sapiens (human) | IC50 (µMol) | 0.0620 | 0.0084 | 0.0704 | 0.2880 | AID1437828 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Prostacyclin receptor | Homo sapiens (human) | EC50 (µMol) | 0.0060 | 0.0004 | 0.0545 | 0.3470 | AID1437825 |
| Prostacyclin receptor | Rattus norvegicus (Norway rat) | EC50 (µMol) | 0.2000 | 0.0007 | 0.1003 | 0.2000 | AID1437823 |
| Prostaglandin D2 receptor | Homo sapiens (human) | EC50 (µMol) | 0.1000 | 0.0006 | 0.4921 | 2.0590 | AID1437826 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1437822 | Intrinsic activity at recombinant rat IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level at 10 uM after 1 hr incubation by HTRF method relative to iloprost | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. |
| AID1437823 | Agonist activity at recombinant rat IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. |
| AID309972 | Hydrolytic rate in Sprague-Dawley rat plasma assessed as 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid production per mg of protein at 10 uM | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID1437907 | Selectivity ratio of EC50 for recombinant rat IP receptor expressed in CHO-K1 cells to EC50 for recombinant human IP receptor expressed in CHO-K1 cells | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. |
| AID301228 | Inhibition of ADP-induced platelet aggregation in human platelet rich plasma | 2007 | Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21 | Structure-activity studies on diphenylpyrazine derivatives: a novel class of prostacyclin receptor agonists. |
| AID309984 | Tmax in cynomolgus monkey assessed as 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid level at 1 mg/kg, po | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID1437906 | Ratio of IC50 for IP receptor in human primary platelets to EC50 for recombinant human IP receptor expressed in CHO-K1 cells | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. |
| AID309976 | Hydrolytic rate in human hepatic microsomes assessed as 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid production per mg of protein at 10 uM | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID309977 | Hydrolytic rate in cynomolgus monkey hepatic microsomes assessed as 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid production in presence of 10 uM PMSF relative to control | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID309986 | Half life in cynomolgus monkey assessed as 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid at 1 mg/kg, po | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID309983 | AUC (0 to 24 hrs) in cynomolgus monkey at 1 mg/kg, po | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID309985 | Cmax in cynomolgus monkey assessed as 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid level at 1 mg/kg, po | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID309975 | Hydrolytic rate in cynomolgus monkey hepatic microsomes assessed as 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid production per mg of protein at 10 uM | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID309973 | Hydrolytic rate in Sprague-Dawley rat hepatic microsomes assessed as 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid production per mg of protein at 10 uM | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID1437825 | Agonist activity at recombinant human IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. |
| AID309980 | Tmax in cynomolgus monkey at 1 mg/kg, po | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID1437830 | Half life in rat microsomes | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. |
| AID309979 | Hydrolytic rate in cynomolgus monkey hepatic microsomes assessed as 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid production in presence of 1000 uM PMSF relative to control | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID1437828 | Agonist activity at IP receptor in human primary platelets assessed as inhibition of ADP-induced platelet aggregation | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. |
| AID1437826 | Agonist activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. |
| AID309987 | AUC (0 to 24 hrs) in cynomolgus monkey assessed as 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid at 1 mg/kg, po | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID1437829 | Half life in human microsomes | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. |
| AID1437824 | Intrinsic activity at recombinant human IP receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level at 10 uM after 1 hr incubation by HTRF method relative to iloprost | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. |
| AID309978 | Hydrolytic rate in cynomolgus monkey hepatic microsomes assessed as 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid production in presence of 100 uM PMSF relative to control | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID309981 | Cmax in cynomolgus monkey at 1 mg/kg, po | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID309982 | Half life in cynomolgus monkey at 1 mg/kg, po | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID1437827 | Intrinsic activity at recombinant human DP1 receptor expressed in CHO-K1 cells assessed as increase in intracellular cAMP level after 1 hr incubation by HTRF method relative to prostaglandin D2 | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. |
| AID309974 | Hydrolytic rate in Beagle dog hepatic microsomes assessed as 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)acetic acid production per mg of protein at 10 uM | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346350 | Human IP receptor (Prostanoid receptors) | 2007 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 322, Issue:3 | 2-[4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy]-N-(methylsulfonyl)acetamide (NS-304), an orally available and long-acting prostacyclin receptor agonist prodrug. |
| AID1346331 | Rat IP receptor (Prostanoid receptors) | 2007 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 322, Issue:3 | 2-[4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy]-N-(methylsulfonyl)acetamide (NS-304), an orally available and long-acting prostacyclin receptor agonist prodrug. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 4 (2.88) | 29.6817 |
| 2010's | 83 (59.71) | 24.3611 |
| 2020's | 52 (37.41) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (72.12) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 32 (21.62%) | 5.53% |
| Reviews | 28 (18.92%) | 6.00% |
| Case Studies | 18 (12.16%) | 4.05% |
| Observational | 5 (3.38%) | 0.25% |
| Other | 65 (43.92%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| A Prospective, Open-label, Platform Study for Long-term Follow-up of Participants Using Study Intervention in Pulmonary Hypertension Parent Studies [NCT05179876] | Phase 3 | 230 participants (Anticipated) | Interventional | 2022-05-04 | Recruiting | ||
| A Multicenter, Single-arm, Open-label, Long-term Follow-up Safety Study of Selexipag in Participants Who Participated in a Previous Selexipag Study [NCT04565990] | Phase 3 | 43 participants (Actual) | Interventional | 2021-05-03 | Active, not recruiting | ||
| 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 Arte [NCT04175600] | Phase 3 | 138 participants (Actual) | Interventional | 2020-01-16 | Active, not recruiting | ||
| 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 Subjects [NCT03496506] | Phase 1 | 22 participants (Actual) | Interventional | 2018-03-05 | Completed | ||
| 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 Impacts [NCT03078907] | Phase 4 | 108 participants (Actual) | Interventional | 2017-11-08 | Completed | ||
| 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 Sclerosis [NCT02260557] | Phase 2 | 74 participants (Actual) | Interventional | 2014-10-31 | Completed | ||
| 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 Fem [NCT02206204] | Phase 1 | 159 participants (Actual) | Interventional | 2012-06-30 | Completed | ||
| 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) [NCT05825417] | Phase 4 | 40 participants (Anticipated) | Interventional | 2023-06-14 | Recruiting | ||
| 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 Tab [NCT02745860] | Phase 1 | 20 participants (Actual) | Interventional | 2016-06-30 | Completed | ||
| Pulmonary Arterial Hypertension Quality Enhancement Research Initiative Extension Program [NCT01389206] | 797 participants (Actual) | Observational [Patient Registry] | 2011-06-01 | Completed | |||
| A Single-center, Open-label, Randomized, Formulation Screening, Two-cohort, Four-period, Crossover Study for Selexipag Sustained Release in Healthy Male Subjects [NCT04266756] | Phase 1 | 24 participants (Actual) | Interventional | 2020-01-23 | Completed | ||
| 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 Subjects [NCT02791815] | Phase 1 | 20 participants (Actual) | Interventional | 2016-07-31 | Completed | ||
| A Prospective, Multicenter, Single-Arm, Open-Label, Phase 4 Study of the Effects of Selexipag on Right Ventricular Remodeling in Pulmonary Arterial Hypertension Assessed by Cardiac Magnetic Resonance Imaging [NCT04435782] | Phase 4 | 9 participants (Actual) | Interventional | 2021-07-07 | Terminated(stopped due to The Sponsor decided to prematurely terminate the study due to the lower-than-expected recruitment rate.) | ||
| 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 D [NCT02206295] | Phase 1 | 80 participants (Actual) | Interventional | 2012-09-30 | Completed | ||
| 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. [NCT03942211] | Phase 2 | 10 participants (Actual) | Interventional | 2021-02-26 | Completed | ||
| Selexipag for the Treatment of Schistosomiasis-Associated Pulmonary Arterial Hypertension [NCT04589390] | Phase 2 | 20 participants (Anticipated) | Interventional | 2020-10-15 | Recruiting | ||
| Single-center, Open-label, Phase 1 Study Consisting of a Single-dose Pilot Phase and a Randomized, Two-way Crossover, Single-dose Main Phase to Investigate the Absolute Bioavailability of a Single Oral Dose of Selexipag in Healthy Male Subjects [NCT02882425] | Phase 1 | 19 participants (Actual) | Interventional | 2015-01-31 | Completed | ||
| 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 Hypertension [NCT01106014] | Phase 3 | 1,156 participants (Actual) | Interventional | 2009-12-01 | Completed | ||
| 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. [NCT02770222] | Phase 1 | 40 participants (Actual) | Interventional | 2016-06-30 | Completed | ||
| A Prospective, Multicenter, Open Label, Single Arm, Phase 2 Study to Investigate the Safety, Tolerability and Pharmacokinetics of Selexipag in Children With Pulmonary Arterial Hypertension [NCT03492177] | Phase 2 | 63 participants (Actual) | Interventional | 2018-07-23 | Active, not recruiting | ||
| 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 Selexipag [NCT03187678] | Phase 3 | 20 participants (Actual) | Interventional | 2017-12-04 | Completed | ||
| 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 Wit [NCT03689244] | Phase 3 | 128 participants (Actual) | Interventional | 2019-01-23 | Terminated(stopped due to The study did not demonstrate efficacy on the primary endpoint, PVR vs. placebo at wk 20 at a planned interim analysis.) | ||
| A Multi-centre, Multinational, Open-label, Single-dose Acute Hemodynamic Study Followed by Multi-centre, Multinational, Randomized, Double-blind, Parallel-group, Placebo Controlled Study to Assess the Safety, Tolerability, Pharmacokinetics and Preliminary [NCT00993408] | Phase 2 | 43 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
| 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 Study [NCT02558231] | Phase 3 | 247 participants (Actual) | Interventional | 2016-05-01 | Completed | ||
| 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 Hypertension [NCT02471183] | Phase 3 | 34 participants (Actual) | Interventional | 2015-10-12 | Completed | ||
| Long-term Single-arm Open-label Study, to Assess the Safety and Tolerability of ACT-293987 in Patients With Pulmonary Arterial Hypertension [NCT01112306] | Phase 3 | 709 participants (Actual) | Interventional | 2010-07-07 | Completed | ||
| Individual Patient Expanded Access IND for Selexipag (Uptravi) in Participants With Non-healing Wound, Buerger's Disease [NCT04914247] | 0 participants | Expanded Access | Available | ||||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||