Page last updated: 2024-11-11

u 62840

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Description

U 62840: stereoisomeric benzindene prostaglandin analog; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6918140
CHEMBL ID1237119
CHEBI ID50861
SCHEMBL ID4349618
MeSH IDM0154586

Synonyms (81)

Synonym
L606 ,
tyvaso
ut-15
15au81
uniprost
lrx-15
81846-19-7
D06213
remodulin (tn)
treprostinil (jan/usan/inn)
CHEBI:50861 ,
treprostinilum
treprostinilo
({(1r,2r,3as,9as)-2-hydroxy-1-[(3s)-3-hydroxyoctyl]-2,3,3a,4,9,9a-hexahydro-1h-cyclopenta[b]naphthalen-5-yl}oxy)acetic acid
treprostinil
DB00374
u 62840
u-62,840
((1r,2r,3as,9as)-2-hydroxy-1-((3s)-3-hydroxyoctyl)-2,3,3a,4,9,9a-hexahydro-1h-cylopent(b)naphthalen-5-yl)oxy)acetate
treprostinil [usan:inn]
acetic acid, ((2,3,3a,4,9,9a-hexahydro-2-hydroxy-1-(3-hydroxyoctyl)-1h-benz(f)inden-5-yl)oxy)-, (1r-(1alpha(s*),2beta,3aalpha,9aalpha))-
lrx 15
acetic acid, (((1r,2r,3as,9as)-2,3,3a,4,9,9a-hexahydro-2-hydroxy-1-((3s)-3-hydroxyoctyl)-1h-benz(f)inden-5-yl)oxy)-
2-[[(1r,2r,3as,9as)-2,3,3a,4,9,9a-hexahydro-2-hydroxy-1-[(3s)-3-hydroxyoctyl]-1h-benz[f]inden-5-yl]oxy]acetic acid
SCHEMBL4349618
2-[[(1r,2r,3as,9as)-2-hydroxy-1-[(3s)-3-hydroxyoctyl]-2,3,3a,4,9,9a-hexahydro-1h-cyclopenta[g]naphthalen-5-yl]oxy]acetic acid
orenitram
unii-rum6k67esg
rum6k67esg ,
trevyent
15-au-81
rumodolin
lrx -15
tresprostinil
CHEMBL1237119
l-606
treprostinil [inn]
acetic acid,(((1r,2r,3as,9as)-2,3,3a,4,9,9a-hexahydro-2-hydroxy-1-((3s)-3-hydroxyoctyl)-1h-benz(f)inden-5-yl)oxy)-
treprostinil [vandf]
treprostinil [orange book]
treprostinil [usan]
treprostinil [mart.]
treprostinil [who-dd]
treprostinil [jan]
[(1r,2r,3as,9as)-2-hydroxy-1-((3s)-3-hydroxyoctyl)-2,3,3a,4,9,9a-hexahydro-1h-cylopent[b]naphthalen-5-yl]oxy]acetate
treprostinil phosphate [usan]
treprostinil [mi]
gtpl5820
2-[[(2r,3r,3as,9as)-2-hydroxy-3-[(3s)-3-hydroxyoctyl]-2,3,3a,4,9,9a-hexahydro-1h-cyclopenta[g]naphthalen-8-yl]oxy]acetic acid
BRD-K19706299-001-01-4
2-(((1r,2r,3as,9as)-2-hydroxy-1-((s)-3-hydroxyoctyl)-2,3,3a,4,9,9a-hexahydro-1h-cyclopenta[b]naphthalen-5-yl)oxy)acetic acid
[[(1r,2r,3as,9as)-2,3,4,9,9a-hexahydro-2-hydroxy-1-[(3s)-3-hydroxyoctyl]-1h-benz[f]inden-5-yl]oxy]acetic acid
AC-30207
HMS3648G07
2-{[(1r,2r,3as,9as)-2-hydroxy-1-[(3s)-3-hydroxyoctyl]-1h,2h,3h,3ah,4h,9h,9ah-cyclopenta[b]naphthalen-5-yl]oxy}acetic acid
[[(1r,2r,3as,9as)-2,3,3a,4,9,9a-hexahydro-2-hydroxy-1-[(s)-3-hydroxyoctyl]-1h-benzo[f]indene-5-yl]oxy]acetic acid
AKOS027470173
15au
CS-7872
HY-100441
2-((1r,2r,3as,9as)-2-hydroxy-1-((s)-3-hydroxyoctyl)-2,3,3a,4,9,9a-hexahydro-1h-cyclopenta[b]naphthalen-5-yloxy)acetic acid
Q3495231
81846-19-7 (free acid)
EX-A1414
treprostinil pound>>ut-15
mfcd00888847
sr-01000946210
SR-01000946210-1
BCP10253
AMY22230
treprostinil free acid
2-[[(1r,2r,3as,9as)-2,3,4,9,9a-hexahydro-2-hydroxy-1-[(3s)-3-hydroxyoctyl]-1h-benz[f]inden-5-yl]oxy]-acetic acid
AS-56364
NCGC00343944-03
EN300-19768672
bdbm50594971
tyvaso dpi
DTXSID901021654
treprostinil (mart.)
b01ac21
(((1r,2r,3as,9as)-2-hydroxy-1-((3s)-3-hydroxyoctyl)-2,3,3a,4,9,9a-hexahydro-1h-cyclopenta(b)naphthalen-5-yl)oxy)acetic acid

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"Intravenous epoprostenol is currently FDA approved for management of primary pulmonary hypertension, but it requires intravenous infusion and is associated with adverse effects."( Efficacy and safety of treprostinil: an epoprostenol analog for primary pulmonary hypertension.
Arneson, C; Badesch, DB; Barst, RJ; Blackburn, SD; Bourge, RC; Frost, A; Gaine, SP; McGoon, MD; McLaughlin, VV; Oudiz, RJ; Rich, S; Robbins, IM; Roscigno, R; Rubin, LJ; Sigman, J; Tapson, VF, 2003
)
0.32
"Long-term IV infusion of treprostinil is safe and appears to be effective for the treatment of patients with PAH."( Safety and efficacy of IV treprostinil for pulmonary arterial hypertension: a prospective, multicenter, open-label, 12-week trial.
Barst, RJ; Benza, RL; Gomberg-Maitland, M; Krichman, A; McLaughlin, VV; Tapson, VF; Widlitz, AC, 2006
)
0.33
"The addition of a long-acting prostacyclin analogue via the inhaled route might be a safe and effective strategy to optimize therapy in PAH patients on bosentan."( Safety and efficacy of inhaled treprostinil as add-on therapy to bosentan in pulmonary arterial hypertension.
Channick, RN; Olschewski, H; Rubin, LJ; Seeger, W; Staub, T; Voswinckel, R, 2006
)
0.33
" In the remaining 11 patients, inhaled treprostinil was safe and well tolerated."( Safety and efficacy of inhaled treprostinil as add-on therapy to bosentan in pulmonary arterial hypertension.
Channick, RN; Olschewski, H; Rubin, LJ; Seeger, W; Staub, T; Voswinckel, R, 2006
)
0.33
" Inhaled treprostinil has been shown to be safe and efficacious in adults."( Effectiveness and safety of inhaled treprostinil for the treatment of pulmonary arterial hypertension in children.
Calderbank, M; Coleman, E; Ivy, DD; Kerstein, J; Krishnan, U; Rosenzweig, EB; Takatsuki, S, 2012
)
0.38
" Oral treprostinil therapy was generally well tolerated; the most common adverse events (intent-to-treat) were headache (69%), nausea (39%), diarrhea (37%), and pain in jaw (25%)."( Efficacy and safety of oral treprostinil monotherapy for the treatment of pulmonary arterial hypertension: a randomized, controlled trial.
Allen, R; Arneson, C; Jerjes-Sanchez, C; Jing, ZC; Laliberte, K; Parikh, K; Pulido, T; Rubin, LJ; Torbicki, A; White, RJ; Xu, KF; Yehle, D, 2013
)
0.39
" Overall, iTRE taken at a higher dose than approved for use in PAH was safe and well-tolerated in our cohort of pulmonary hypertension patients."( Safety and Tolerability of High-dose Inhaled Treprostinil in Pulmonary Hypertension.
Fortin, T; Parikh, KS; Poms, AD; Rajagopal, S; Tapson, VF, 2016
)
0.43
"25), with no reported significant adverse hemodynamic events."( Rapid Inpatient Titration of Intravenous Treprostinil for Pulmonary Arterial Hypertension: Safe and Tolerable.
El-Kersh, K; Ruf, KM; Smith, JS,
)
0.13
"Subcutaneous treprostinil has dose-dependent beneficial effects in patients with severe pulmonary arterial hypertension, but adverse effects like infusion site pain can lead to treatment discontinuation."( Safety, Tolerability and Clinical Effects of a Rapid Dose Titration of Subcutaneous Treprostinil Therapy in Pulmonary Arterial Hypertension: A Prospective Multi-Centre Trial.
Benjamin, N; Egenlauf, B; Gerhardt, F; Grover, ER; Grünig, E; Halank, M; Held, M; Klose, H; Krueger, U; Lange, TJ; Neurohr, C; Pernow, M; Rosenkranz, S; Seyfarth, HJ; Traube, A; Viethen, T; Wilkens, H, 2016
)
0.43
" There were 82 complications/peri-procedural events in 60 patients; of these, 57 were serious adverse events (0."( Long-term safety and outcome of intravenous treprostinil via an implanted pump in pulmonary hypertension.
Bollmann, T; Classen, S; Ewert, R; Gall, H; Gerhardt Md, F; Ghofrani, HA; Grimminger, F; Grimminger, J; Grünig, E; Guth, S; Halank, M; Harutyunova, S; Heine, A; Hoeper, MM; Klose, H; Lange, TJ; Meyer, K; Neurohr, C; Nickolaus, K; Olsson, KM; Opitz, CF; Richter, MJ; Rosenkranz, S; Seyfarth, HJ; Warnke, C; Wiedenroth, C, 2018
)
0.48
"Our data suggest that intravenous treprostinil via the LENUS Pro pump in advanced PH is associated with a very low risk of bloodstream infections, but other serious adverse events may occur."( Long-term safety and outcome of intravenous treprostinil via an implanted pump in pulmonary hypertension.
Bollmann, T; Classen, S; Ewert, R; Gall, H; Gerhardt Md, F; Ghofrani, HA; Grimminger, F; Grimminger, J; Grünig, E; Guth, S; Halank, M; Harutyunova, S; Heine, A; Hoeper, MM; Klose, H; Lange, TJ; Meyer, K; Neurohr, C; Nickolaus, K; Olsson, KM; Opitz, CF; Richter, MJ; Rosenkranz, S; Seyfarth, HJ; Warnke, C; Wiedenroth, C, 2018
)
0.48
" During the study, 3 patients discontinued selexipag due to adverse events."( Safety and tolerability of transition from inhaled treprostinil to oral selexipag in pulmonary arterial hypertension: Results from the TRANSIT-1 study.
Benza, RL; Chin, KM; Eggert, M; Farber, HW; Fisher, M; Fortin, TA; Fritz, JS; Frost, A; Janmohamed, M; Kim, NH; McConnell, JW; McEvoy, C; McLaughlin, V; Miller, CE; Pfister, T; Poch, D; Shiraga, Y, 2019
)
0.51
" The first-line treatment is intravenous iloprost, but it induces dose-limiting adverse effects."( Treprostinil Hydrogel Iontophoresis in Systemic Sclerosis-Related Digital Skin Ulcers: A Safety Study.
Beau-Guillaumot, M; Blaise, S; Cracowski, C; Cracowski, JL; Guigui, A; Kotzki, S; Mazet, R; Roustit, M, 2020
)
0.56
" Seven patients withdrew due to intolerable adverse effects (n = 3), intercurrent unrelated illness (n = 2, cirrhosis, cancer), progressive SSc (n = 1) and personal reasons (n = 1)."( A pilot study to evaluate the safety and efficacy of treprostinil in the treatment of calcinosis in systemic sclerosis.
Catanese, B; Chung, L; Chung, MP; Fiorentino, D; Li, S; Stevens, K; Strand, V; Valenzuela, A, 2022
)
0.72
" Changes in clinical parameters, adverse events, and outcome were analyzed retrospectively."( Long-Term Safety, Outcome, and Clinical Effects of Subcutaneous and Intravenous Treprostinil Treatment in Patients with Severe Chronic Pulmonary Arterial Hypertension.
Benjamin, N; Egenlauf, B; Eichstaedt, C; Grünig, E; Harutyunova, S; Marra, AM; Nagel, C; Xanthouli, P, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic analysis of mean data indicated a biphasic decay of 15AU81 in plasma, with an initial half-life of approximately 2 min, and a terminal half-life of approximately 20 min."( The pharmacokinetics and pharmacodynamics of the prostacyclin analog 15AU81 in the anesthetized beagle dog.
McNulty, MJ; Sailstad, JM; Steffen, RP, 1993
)
0.29
" This report describes the development and validation of a radioimmunoassay for 15AU81, and its application to a pharmacokinetic study in the beagle dog."( Radioimmunoassay for the chemical stable prostacyclin analog, 15AU81: a preliminary pharmacokinetics study in the dog.
Chang, SY; Findlay, JW; McNulty, MJ; Page, TL; Sailstad, JM, 1993
)
0.29
"25, co-administration of oral treprostinil and bosentan did not result in a pharmacokinetic interaction for either agent."( Lack of a pharmacokinetic interaction between oral treprostinil and bosentan in healthy adult volunteers.
Dingemanse, J; Gotzkowsky, SK; Lai, A; Laliberte, K; Mottola, D, 2010
)
0.36
" Previous attempts at developing an oral prostanoid have been limited by rapid absorption and short plasma half-life; thus, the aim of this study was to characterize the pharmacokinetic profile of treprostinil diolamine in PAH patients after chronic dosing."( Pharmacokinetics of oral treprostinil sustained release tablets during chronic administration to patients with pulmonary arterial hypertension.
Allen, R; Howell, M; Jerjes, C; Laliberte, K; Marier, JF; Pulido, T; Tapson, VF; Torres, F; White, RJ; Yehle, D, 2013
)
0.39
" This study was designed to evaluate the presence of a pharmacokinetic drug interaction between treprostinil diolamine and sildenafil."( Lack of a pharmacokinetic interaction between treprostinil diolamine and sildenafil in healthy adult volunteers.
Gotzkowsky, SK; Kumar, P; Laliberte, K; Mottola, D, 2013
)
0.39
"Scleroderma patients with digital ulcers were enrolled in this dual-center, open-label, phase I pharmacokinetic study."( Open label study of escalating doses of oral treprostinil diethanolamine in patients with systemic sclerosis and digital ischemia: pharmacokinetics and correlation with digital perfusion.
Anderson, C; Boin, F; Hummers, LK; Phillips, K; Rollins, KD; Schiopu, E; Seibold, JR; Shah, AA; Wade, M; Wigley, F; Wise, R, 2013
)
0.39
" The objective of the current study was to develop a robust physiologically based pharmacokinetic (PBPK) model for treprostinil intravenous injection and extended-release tablet as the first step to optimize treprostinil pharmacotherapy in patients."( Physiologically based pharmacokinetic modelling of treprostinil after intravenous injection and extended-release oral tablet administration in healthy volunteers: An extrapolation to other patient populations including patients with hepatic impairment.
Shaik, IH; Venkataramanan, R; Wu, X; Xu, R; Zhang, X, 2022
)
0.72

Compound-Compound Interactions

ExcerptReferenceRelevance
" This retrospective, single-center, open-label study was designed to assess the efficacy of long-term, subcutaneously administered, treprostinil-based therapy alone or in combination with bosentan for the treatment of moderate-to-severe PAH."( Treprostinil-based therapy in the treatment of moderate-to-severe pulmonary arterial hypertension: long-term efficacy and combination with bosentan.
Benza, RL; Bourge, RC; Pamboukian, SV; Rayburn, BK; Tallaj, JA, 2008
)
0.35
"To investigate the effect of treprostinil on the early postoperative prognosis of patients with severe left heart valvular disease combined with severe pulmonary hypertension (PAH)."( Effect of Treprostinil on the Early Postoperative Prognosis of Patients with Severe Left Heart Valvular Disease Combined with Severe Pulmonary Hypertension.
Cao, H; Chen, Q; Huang, ST; Sun, KP; Xu, N, 2021
)
0.62
"A retrospective study including 55 patients with severe left heart valvular disease combined with severe PAH who underwent left heart valve replacement in our hospital between January 2019 and May 2019 was conducted."( Effect of Treprostinil on the Early Postoperative Prognosis of Patients with Severe Left Heart Valvular Disease Combined with Severe Pulmonary Hypertension.
Cao, H; Chen, Q; Huang, ST; Sun, KP; Xu, N, 2021
)
0.62
"Treprostinil can improve the early postoperative prognosis of patients with severe left heart valvular disease combined with severe PAH undergoing prosthetic valve replacement."( Effect of Treprostinil on the Early Postoperative Prognosis of Patients with Severe Left Heart Valvular Disease Combined with Severe Pulmonary Hypertension.
Cao, H; Chen, Q; Huang, ST; Sun, KP; Xu, N, 2021
)
0.62
"To investigate the midterm postoperative prognosis of patients with severe left heart valvular disease combined with moderate or severe pulmonary hypertension (PAH) using subcutaneous injection of treprostinil."( Midterm postoperative prognosis of patients with severe left heart valvular disease combined with moderate or severe pulmonary hypertension treated with treprostinil.
Cao, H; Chen, Q; Huang, ST; Sun, KP; Wang, ZC; Xu, N, 2020
)
0.56
"A retrospective study was conducted on 61 patients with severe left heart valvular disease combined with moderate or severe PAH who had undergone mechanical mitral and/or aortic valve replacement from April 2018 to October 2018."( Midterm postoperative prognosis of patients with severe left heart valvular disease combined with moderate or severe pulmonary hypertension treated with treprostinil.
Cao, H; Chen, Q; Huang, ST; Sun, KP; Wang, ZC; Xu, N, 2020
)
0.56
"Continuous subcutaneous infusion of treprostinil was not capable of decreasing pulmonary pressures in patients with severe left heart valvular disease combined with moderate or severe PAH during 1 year follow-up, although which some of our data suggest that might improve the symptoms and quality of life of these patients."( Midterm postoperative prognosis of patients with severe left heart valvular disease combined with moderate or severe pulmonary hypertension treated with treprostinil.
Cao, H; Chen, Q; Huang, ST; Sun, KP; Wang, ZC; Xu, N, 2020
)
0.56

Bioavailability

ExcerptReferenceRelevance
"8 min), while after intratracheal administration, clearance appeared to be somewhat slower and bioavailability was appreciable (mean, 46%), suggesting that this route of administration may be worthy of further evaluation."( Radioimmunoassay for the chemical stable prostacyclin analog, 15AU81: a preliminary pharmacokinetics study in the dog.
Chang, SY; Findlay, JW; McNulty, MJ; Page, TL; Sailstad, JM, 1993
)
0.29
"The objective of this study was to evaluate the absolute bioavailability and acute pharmacokinetics of treprostinil sodium administered by continuous, short-term subcutaneous infusion in normal subjects."( Absolute bioavailability and pharmacokinetics of treprostinil sodium administered by acute subcutaneous infusion.
Baker, FJ; DellaMaestra, W; Hunt, TL; Lai, AA; Roscigno, R; Wade, M, 2004
)
0.32
" Previous data have demonstrated that the oral bioavailability of treprostinil was improved when taken with a meal containing at least 500 calories."( The effect of different meal compositions on the oral bioavailability of treprostinil diolamine in healthy volunteers.
Kates, J; Kumar, P; Laliberte, K; Laurent, A; Lim, A; Wang-Smith, L, 2013
)
0.39
"As twice-daily intake of a high-fat, high-calorie meal may be undesirable or not feasible for some patients, this open-label, randomized, crossover study evaluated the effect of different meal compositions [a 500-calorie well-balanced meal (WB500), a 250-calorie well-balanced meal (WB250), a 250-calorie high-fat meal (HF250) and a 250-calorie well-balanced liquid meal (Ensure®)] on the relative bioavailability of oral treprostinil."( The effect of different meal compositions on the oral bioavailability of treprostinil diolamine in healthy volunteers.
Kates, J; Kumar, P; Laliberte, K; Laurent, A; Lim, A; Wang-Smith, L, 2013
)
0.39
"Overall, there were no clinically significant differences in the relative bioavailability of oral treprostinil when administered immediately after meals containing 250-500 calories and 30-50% fat."( The effect of different meal compositions on the oral bioavailability of treprostinil diolamine in healthy volunteers.
Kates, J; Kumar, P; Laliberte, K; Laurent, A; Lim, A; Wang-Smith, L, 2013
)
0.39
"We conducted comparative bioavailability analyses of treprostinil exposure from LIQ861 (79."( Comparative bioavailability of inhaled treprostinil administered as LIQ861 and Tyvaso® in healthy subjects.
Eldon, MA; Hunt, T; Parsley, E; Roscigno, RF; Rubin, LJ; Vaughn, T, 2021
)
0.62
"Results showed comparable bioavailability of treprostinil and similar tolerability for LIQ861 and Tyvaso® administered to healthy adults."( Comparative bioavailability of inhaled treprostinil administered as LIQ861 and Tyvaso® in healthy subjects.
Eldon, MA; Hunt, T; Parsley, E; Roscigno, RF; Rubin, LJ; Vaughn, T, 2021
)
0.62
"Given the comparable treprostinil bioavailability and similar safety profiles of LIQ861 and Tyvaso®, LIQ861 fulfills a significant unmet need for PAH patients by maximizing the therapeutic benefits of treprostinil by safely delivering doses to the lungs in 1 to 2 breaths using a discreet, convenient, easy-to-use inhaler."( Comparative bioavailability of inhaled treprostinil administered as LIQ861 and Tyvaso® in healthy subjects.
Eldon, MA; Hunt, T; Parsley, E; Roscigno, RF; Rubin, LJ; Vaughn, T, 2021
)
0.62
" In PAH model rats, GlcA-modified liposomes significantly improved TPS bioavailability and sustained its release over time."( Targeted treprostinil delivery inhibits pulmonary arterial remodeling.
Li, B; Liu, A; Shi, Y; Su, J; Yang, M, 2022
)
0.72

Dosage Studied

ExcerptRelevanceReference
" Specificity was confirmed by comparative analysis by radioimmunoassay and by a quantitative GC/MS procedure of plasma samples from dogs dosed with 15AU81."( Radioimmunoassay for the chemical stable prostacyclin analog, 15AU81: a preliminary pharmacokinetics study in the dog.
Chang, SY; Findlay, JW; McNulty, MJ; Page, TL; Sailstad, JM, 1993
)
0.29
" The failure to enhance small bowel allograft survival may be explained by the inability at this low dosage of 15AU81 to influence the intense graft versus host reaction elicited by small bowel transplants."( 15AU81, a prostacyclin analog, enhances donor-specific hepatocytes to prolong the survival of rat heart but not small bowel allografts.
Boyle, MJ; Dumble, LJ,
)
0.13
" A symptom-limited, dose-escalation protocol was instituted, beginning with placebo and then with increasing dosage at 60-min intervals, followed by a 2-h period of maintenance dose at the maximum well-tolerated infusion rate."( Trial of a novel prostacyclin analog, UT-15, in patients with severe intermittent claudication.
Goldman, R; Kimmel, SE; Klugherz, B; Mohler, ER; Sehgal, CM; Wade, M, 2000
)
0.31
" Samples were also collected every 3 hours on Day 7 of each dosing period to evaluate diurnal variation over a 24-hour steady-state interval."( Pharmacokinetics of treprostinil sodium administered by 28-day chronic continuous subcutaneous infusion.
Arneson, CP; Baker, FJ; DellaMaestra, W; Hunt, TL; Lai, AA; Roscigno, R; Wade, M, 2004
)
0.32
" Each subject was dosed at 10 ng/kg/min for 72 hours by each route, with the infusions separated by a 4-day wash-out period."( Pharmacokinetics and steady-state bioequivalence of treprostinil sodium (Remodulin) administered by the intravenous and subcutaneous route to normal volunteers.
Arneson, C; Hunt, T; Jeffs, R; Laliberte, K; Wade, M, 2004
)
0.32
" The transition of treprostinil to epoprostenol is rare; however, in the event therapy change is needed, dosing information is minimal."( Staggered transition to epoprostenol from treprostinil in pulmonary arterial hypertension.
Bultsma, CJ; Coffman, PA; Floreani, AA; Olsen, KM; Reisbig, KA, 2005
)
0.33
"The model was a cost-minimization analysis, assuming clinical equivalence was achieved by proper dosing of both drugs, in terms of survival and surrogate measures."( Cost-minimization analysis of treprostinil vs. epoprostenol as an alternate to oral therapy non-responders for the treatment of pulmonary arterial hypertension.
Desjardins, O; Einarson, TR; Hague, LK; Iskedjian, M; Narine, L; Schilz, R; Vicente, C; Walker, JH, 2005
)
0.33
" We hypothesized that a rapid-escalation treprostinil dosing regimen would be as safe and effective as a slow-escalation dosing regimen."( A clinical comparison of slow- and rapid-escalation treprostinil dosing regimens in patients with pulmonary hypertension.
Gibbs, SJ; Harja, E; Kneussl, MP; Lang, IM; Sing, WG; Skoro-Sajer, N, 2008
)
0.35
" Currently, there are no universal recommendations for dosing delivery of inhaled prostanoids to intubated patients in the intensive care unit setting."( Prostacyclin in the intensive care setting.
Ivy, DD, 2010
)
0.36
" Dosing to achieve rapid onset of efficacy and proactively managing infusion site pain enhance the likelihood for a patient with PAH to maintain and derive benefit from SC treprostinil therapy."( Subcutaneous treprostinil in pulmonary arterial hypertension: Practical considerations.
Mathier, MA; McDevitt, S; Saggar, R, 2010
)
0.36
" Pilot clinical studies have elucidated the acute hemodynamic effects and relative pulmonary selectivity of this agent, as well as established target dosing in PAH and nonoperable chronic thromboembolic PAH."( Inhaled treprostinil: a therapeutic review.
Channick, RN; Rubin, LJ; Voswinckel, R, 2012
)
0.38
" At baseline, most patients (93%) were receiving 5 μg of iloprost per dose but 38% of patients reported a dosing frequency below the labeled rate of 6-9 times daily."( Rapid transition from inhaled iloprost to inhaled treprostinil in patients with pulmonary arterial hypertension.
Benza, RL; Bourge, RC; Channick, RN; Gotzkowsky, SK; McSwain, CS; Nelsen, AC; Rosenzweig, EB; Rubin, LJ; Safdar, Z; Shapiro, S; Tapson, VF; White, RJ, 2013
)
0.39
" After chronic twice-daily oral dosing of treprostinil diolamine, mean area under the curve (AUC0-12) of treprostinil increased from 5244 to 20,4086 pg·hr-·mL- and mean maximum observed plasma concentration (Cmax) increased from 1383 to 33588 pg/mL."( Pharmacokinetics of oral treprostinil sustained release tablets during chronic administration to patients with pulmonary arterial hypertension.
Allen, R; Howell, M; Jerjes, C; Laliberte, K; Marier, JF; Pulido, T; Tapson, VF; Torres, F; White, RJ; Yehle, D, 2013
)
0.39
" Relative to healthy subjects, mean area under the curve from time zero to 24 h after dosing interval (AUC0-24) values in subjects with mild, moderate and severe hepatic impairment increased by approximately 2·2-, 4·9- and 7·6-fold, respectively."( An evaluation of the pharmacokinetics of treprostinil diolamine in subjects with hepatic impairment.
Laliberte, K; Marbury, T; Marier, J; Peterson, L, 2013
)
0.39
"Based on these results, dosage adjustments should be performed in subjects with hepatic impairment."( An evaluation of the pharmacokinetics of treprostinil diolamine in subjects with hepatic impairment.
Laliberte, K; Marbury, T; Marier, J; Peterson, L, 2013
)
0.39
" Dosing downadjustment was needed in some patients who were switched over from SQ to IV prostacyclin analogs."( Subcutaneous to intravenous prostacyclin analog transition in pulmonary hypertension.
Alkukhun, L; Bair, ND; Dweik, RA; Tonelli, AR, 2014
)
0.4
" This study aimed to evaluate the pharmacokinetics (PK), safety, and tolerability of 3 times daily (TID) dosing of oral treprostinil."( Pharmacokinetics of 3 times a day dosing of oral treprostinil in healthy volunteers.
Jones, A; Laliberte, K; Pham, T; Wang-Smith, L, 2014
)
0.4
" Treprostinil PK after TID dosing of oral treprostinil follows linear kinetics and can be predicted based on PK data after a single dose."( Pharmacokinetics of 3 times a day dosing of oral treprostinil in healthy volunteers.
Jones, A; Laliberte, K; Pham, T; Wang-Smith, L, 2014
)
0.4
"From a pharmacological point of view, it appears that with sustained blood concentrations for 8 - 10 h after a single dose, twice or thrice daily dosing is possible."( Pharmacokinetic evaluation of treprostinil (oral) for the treatment of pulmonary arterial hypertension.
Bhattacharya, S; Farber, HW; Hellawell, JL, 2014
)
0.4
" However, their use can be complicated by potential drug interactions, adverse effects, dosing complexity, and cost."( Perspectives on oral pulmonary hypertension therapies recently approved by the U.S. Food and Drug Administration.
Badesch, D; Benza, RL; D'Eletto, TA; Farber, HW; Gomberg-Maitland, M; Hassoun, PM; Hill, NS; Preston, I, 2015
)
0.42
"The objective of this study was to evaluate safety, tolerability and clinical effects of a rapid up-titration dosing regimen of subcutaneous treprostinil using proactive infusion site pain management."( Safety, Tolerability and Clinical Effects of a Rapid Dose Titration of Subcutaneous Treprostinil Therapy in Pulmonary Arterial Hypertension: A Prospective Multi-Centre Trial.
Benjamin, N; Egenlauf, B; Gerhardt, F; Grover, ER; Grünig, E; Halank, M; Held, M; Klose, H; Krueger, U; Lange, TJ; Neurohr, C; Pernow, M; Rosenkranz, S; Seyfarth, HJ; Traube, A; Viethen, T; Wilkens, H, 2016
)
0.43
"Effects of rapid up-titration dosing regimen on tolerability and clinical parameters were evaluated in this 16-week, open-label multi-centre study."( Safety, Tolerability and Clinical Effects of a Rapid Dose Titration of Subcutaneous Treprostinil Therapy in Pulmonary Arterial Hypertension: A Prospective Multi-Centre Trial.
Benjamin, N; Egenlauf, B; Gerhardt, F; Grover, ER; Grünig, E; Halank, M; Held, M; Klose, H; Krueger, U; Lange, TJ; Neurohr, C; Pernow, M; Rosenkranz, S; Seyfarth, HJ; Traube, A; Viethen, T; Wilkens, H, 2016
)
0.43
" Patients achieved a median treprostinil dosage of 35."( Safety, Tolerability and Clinical Effects of a Rapid Dose Titration of Subcutaneous Treprostinil Therapy in Pulmonary Arterial Hypertension: A Prospective Multi-Centre Trial.
Benjamin, N; Egenlauf, B; Gerhardt, F; Grover, ER; Grünig, E; Halank, M; Held, M; Klose, H; Krueger, U; Lange, TJ; Neurohr, C; Pernow, M; Rosenkranz, S; Seyfarth, HJ; Traube, A; Viethen, T; Wilkens, H, 2016
)
0.43
" The impact of the route of delivery and the optimal dosing for transitioning inhaled treprostinil to oral treprostinil or selexipag is unknown."( Different efficacy of inhaled and oral medications in pulmonary hypertension.
AbuHalimeh, BJ; Parambil, JG; Tonelli, AR,
)
0.13
" The use of these medications is challenging due to complexity in dosing and their side effect profiles which limit patient tolerability and acceptance."( What Is the Role of Oral Prostacyclin Pathway Medications in Pulmonary Arterial Hypertension Management?
El Yafawi, R; Wirth, JA, 2017
)
0.46
"SMT-101, a novel, proprietary, water-resistant wearable infusion pump prefilled with a preset dosage of treprostinil, was designed to address many of the administration-related shortcomings of existing parenteral therapy for pulmonary arterial hypertension (PAH)."( Human factors and usability engineering in the development of SMT-101 for the treatment of pulmonary arterial hypertension.
Newell, K; Noymer, P; Shaked, A, 2018
)
0.48
"Treprostinil diolamine is the first oral dosage preparation of a prostacyclin analogue for use in treatment naive pulmonary arterial hypertension (PAH)."( Transitioning Parenteral or Inhaled Treprostinil to Oral Treprostinil Diolamine: Case Series and Review of the Literature.
Awdish, RL; Hegab, S; Kelly, B; Smith, ZR, 2019
)
0.51
" However, these trials were limited by subtherapeutic dosing owing to intolerable adverse effects."( Extended-release oral treprostinil in the management of pulmonary arterial hypertension: clinical evidence and experience.
Coons, JC; Miller, T,
)
0.13
"Treprostinil (TRE), a prostanoid analogue approved in the USA for the treatment of pulmonary arterial hypertension, requires continuous infusion or multiple dosing sessions per day for inhaled and oral routes of administration due to its short half-life."( Inhaled Treprostinil-Prodrug Lipid Nanoparticle Formulations Provide Long-Acting Pulmonary Vasodilation.
Chapman, RW; Chen, KJ; Corboz, MR; Konicek, DM; Laurent, CE; Leifer, FG; Li, Z; Perkins, WR; Plaunt, AJ; S Malinin, V; Salvail, D, 2018
)
0.48
"There is a paucity of published data on how to safely transition patients to oral therapy in the event of complications and problems during parenteral administration of prostacyclins, which can include bloodstream infections, injection-site pain (with use of subcutaneous treprostinil), infusion pump malfunction, and dosing errors due to incorrect dose preparation."( Transition from treprostinil to selexipag in patients with pulmonary arterial hypertension: Case series.
Fanous, SM; Janmohamed, M, 2018
)
0.48
" The safety of midodrine dosing at greater than 30 mg daily has not been established to date."( Midodrine treatment in a patient with treprostinil-induced hypotension receiving hemodialysis.
Alobaidi, A; Bielnicka, P; Drambarean, B, 2019
)
0.51
" In the next 24 hours, we adjusted the dosage to a median maximum dose of 15 ng/kg/min (interquartile range, 15-20 ng/kg/min) over a median uptitration period of 34 hours (interquartile range, 24-41 hours) for 17 parturients with severe pulmonary hypertension."( Rapid Titration of Intravenous Treprostinil to Treat Severe Pulmonary Arterial Hypertension Postpartum: A Retrospective Observational Case Series Study.
Chen, Y; Gao, J; Huang, J; Li, Q; Lu, J; Wang, T; Yang, D; Ye, Q; Zhang, J; Zhao, L, 2019
)
0.51
" Oral TRE was dosed 3 times daily."( Pharmacokinetics of Oral Treprostinil in Children With Pulmonary Arterial Hypertension.
Austin, ED; Deng, CQ; Feinstein, JA; Fineman, J; Hanna, BD; Hirsch, R; Hopper, RK; Ivy, DD; Kirkpatrick, E; Mullen, MP; Solum, D; Yung, D, 2020
)
0.56
" Consensus was also achieved on recommendations for adverse event management, including reassurance, administration of oral treprostinil 3 times daily with food, and dosing inhaled treprostinil at intervals ≥3 hours apart."( An expert panel delphi consensus statement on patient selection and management for transitioning between oral and inhaled treprostinil.
Allen, RP; Balasubramanian, VP; Chakinala, MM; Elwing, JM; Feldman, J; Leary, PJ; Oudiz, RJ; Rahaghi, FF; Rischard, F; Safdar, Z; Sood, N, 2021
)
0.62
" In humans, tachyphylaxis is frequently observed with continuous intravenous (IV) or subcutaneous (SC) infusion of TRE and requires dosage escalation to maintain activity."( Treprostinil palmitil, an inhaled long-acting pulmonary vasodilator, does not show tachyphylaxis with daily dosing in rats.
Chapman, RW; Chun, D; Cipolla, D; Corboz, MR; Gauani, H; Li, Z; Malinin, V; Perkins, WR; Plaunt, AJ, 2021
)
0.62
" In studies involving consecutive daily administrations of TPIS, the delivered TP dosage was 140."( Treprostinil palmitil, an inhaled long-acting pulmonary vasodilator, does not show tachyphylaxis with daily dosing in rats.
Chapman, RW; Chun, D; Cipolla, D; Corboz, MR; Gauani, H; Li, Z; Malinin, V; Perkins, WR; Plaunt, AJ, 2021
)
0.62
"05) inhibition of the increase of RVPP due to hypoxia over the full duration of the dosing periods."( Treprostinil palmitil, an inhaled long-acting pulmonary vasodilator, does not show tachyphylaxis with daily dosing in rats.
Chapman, RW; Chun, D; Cipolla, D; Corboz, MR; Gauani, H; Li, Z; Malinin, V; Perkins, WR; Plaunt, AJ, 2021
)
0.62
" Epoprostenol, iloprost and treprostinil have all been used intravenously in PAH, but titration, dosing and dose escalation in long-term therapy are not standardized."( Intravenous prostacyclin-analogue therapy in pulmonary arterial hypertension - A review of the past, present and future.
Ewert, R; Habedank, D; Halank, M; Opitz, CF; Stubbe, B, 2021
)
0.62
"Prostacyclin infusion for pulmonary arterial hypertension (PAH) is an effective therapy with varied dosing requirements and clinical response."( Two polymorphic gene loci associated with treprostinil dose in pulmonary arterial hypertension.
Benza, RL; Cox, NJ; Friedman, P; Gamazon, ER; Gomberg-Maitland, MI; Konkashbaev, A; Kubo, M; Maitland, ML; Nakamura, Y; Psotka, MA; Ratain, MJ; Thomeas-McEwing, V, 2022
)
0.72
" These data support the early initiation and uptitration of therapy to a dosage of at least 9 bps four times daily in patients with PH resulting from ILD."( Inhaled Treprostinil Dosage in Pulmonary Hypertension Associated With Interstitial Lung Disease and Its Effects on Clinical Outcomes.
Broderick, M; Deng, C; DuBrock, HM; Elwing, J; King, CS; Nathan, SD; Rajagopal, S; Rischard, F; Sahay, S; Shen, E; Smith, P; Tapson, VF; Waxman, AB, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (6)

RoleDescription
platelet aggregation inhibitorA 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 agentA drug used to cause dilation of the blood vessels.
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
cardiovascular drugA drug that affects the rate or intensity of cardiac contraction, blood vessel diameter or blood volume.
vitamin K antagonistA class of anticoagulants which act by inhibiting the action of vitamin K.
human blood serum metaboliteAny metabolite (endogenous or exogenous) found in human blood serum samples.
[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]

Drug Classes (2)

ClassDescription
carboxylic acidA carbon oxoacid acid carrying at least one -C(=O)OH group and having the structure RC(=O)OH, where R is any any monovalent functional group. Carboxylic acids are the most common type of organic acid.
carbotricyclic compoundA carbopolyclic compound comprising of three carbocyclic rings.
[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 Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GVesicular stomatitis virusPotency9.52210.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency9.52210.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Prostaglandin E2 receptor EP1 subtypeHomo sapiens (human)EC50 (µMol)0.28500.00030.32480.7600AID1872475
Prostaglandin E2 receptor EP2 subtypeHomo sapiens (human)EC50 (µMol)0.00620.00190.96657.8000AID1872474
Prostacyclin receptorHomo sapiens (human)EC50 (µMol)0.00190.00040.05450.3470AID1872473
Prostaglandin D2 receptorHomo sapiens (human)EC50 (µMol)0.00060.00060.49212.0590AID1872472
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (64)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
response to lipopolysaccharideProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
inflammatory responseProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
response to nematodeProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
response to lipopolysaccharideProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
response to progesteroneProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
regulation of cell population proliferationProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
cellular response to prostaglandin E stimulusProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
inflammatory responseProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerProstacyclin receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayProstacyclin receptorHomo sapiens (human)
cell-cell signalingProstacyclin receptorHomo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathwayProstacyclin receptorHomo sapiens (human)
response to lipopolysaccharideProstacyclin receptorHomo sapiens (human)
negative regulation of smooth muscle cell proliferationProstacyclin receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstacyclin receptorHomo sapiens (human)
inflammatory responseProstacyclin receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin D2 receptorHomo sapiens (human)
male sex determinationProstaglandin D2 receptorHomo sapiens (human)
sleepProstaglandin D2 receptorHomo sapiens (human)
mast cell degranulationProstaglandin D2 receptorHomo sapiens (human)
adenosine metabolic processProstaglandin D2 receptorHomo sapiens (human)
cellular response to prostaglandin D stimulusProstaglandin D2 receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationProstaglandin D2 receptorHomo sapiens (human)
inflammatory responseProstaglandin D2 receptorHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
D1 dopamine receptor bindingProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
prostaglandin E receptor activityProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
prostaglandin E receptor activityProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
guanyl-nucleotide exchange factor activityProstacyclin receptorHomo sapiens (human)
prostacyclin receptor activityProstacyclin receptorHomo sapiens (human)
prostaglandin J receptor activityProstaglandin D2 receptorHomo sapiens (human)
prostaglandin D receptor activityProstaglandin D2 receptorHomo sapiens (human)
protein bindingProstaglandin D2 receptorHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP1 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
plasma membraneProstaglandin E2 receptor EP2 subtypeHomo sapiens (human)
cytosolProstacyclin receptorHomo sapiens (human)
plasma membraneProstacyclin receptorHomo sapiens (human)
plasma membraneProstacyclin receptorHomo sapiens (human)
plasma membraneProstaglandin D2 receptorHomo sapiens (human)
membraneProstaglandin D2 receptorHomo sapiens (human)
plasma membraneProstaglandin D2 receptorHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (25)

Assay IDTitleYearJournalArticle
AID419528Volume of distribution at steady state in human at 15 ng/kg/min, iv administered 150 mins infusion2009Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
In silico prediction of volume of distribution in human using linear and nonlinear models on a 669 compound data set.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1872474Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis2022European journal of medicinal chemistry, Mar-05, Volume: 231Building on endogenous lipid mediators to design synthetic receptor ligands.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1872475Agonist activity at human EP1 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis2022European journal of medicinal chemistry, Mar-05, Volume: 231Building on endogenous lipid mediators to design synthetic receptor ligands.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1872473Agonist activity at human IP expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis2022European journal of medicinal chemistry, Mar-05, Volume: 231Building on endogenous lipid mediators to design synthetic receptor ligands.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1872472Agonist activity at human DP1 expressed in human 1321N1 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis2022European journal of medicinal chemistry, Mar-05, Volume: 231Building on endogenous lipid mediators to design synthetic receptor ligands.
AID1346350Human IP receptor (Prostanoid receptors)2012Biochemical pharmacology, Jul-01, Volume: 84, Issue:1
Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonist.
AID1346377Human DP1 receptor (Prostanoid receptors)2012Biochemical pharmacology, Jul-01, Volume: 84, Issue:1
Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonist.
AID1346427Human EP4 receptor (Prostanoid receptors)2012Biochemical pharmacology, Jul-01, Volume: 84, Issue:1
Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonist.
AID1346308Human EP2 receptor (Prostanoid receptors)2012Biochemical pharmacology, Jul-01, Volume: 84, Issue:1
Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonist.
AID1346408Human EP1 receptor (Prostanoid receptors)2012Biochemical pharmacology, Jul-01, Volume: 84, Issue:1
Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonist.
AID1346343Human EP3 receptor (Prostanoid receptors)2012Biochemical pharmacology, Jul-01, Volume: 84, Issue:1
Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (424)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (0.24)18.7374
1990's6 (1.42)18.2507
2000's104 (24.53)29.6817
2010's218 (51.42)24.3611
2020's95 (22.41)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials79 (17.67%)5.53%
Reviews79 (17.67%)6.00%
Case Studies66 (14.77%)4.05%
Observational9 (2.01%)0.25%
Other214 (47.87%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]