Page last updated: 2024-12-10

enprostil

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Enprostil: A synthetic PGE2 analog that has an inhibitory effect on gastric acid secretion, a mucoprotective effect, and a postprandial lowering effect on gastrin. It has been shown to be efficient and safe in the treatment of gastroduodenal ulcers. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5311225
CHEMBL ID2104194
SCHEMBL ID186877
MeSH IDM0025335

Synonyms (19)

Synonym
gtpl1918
methyl 7-[(1r,2r,3r)-3-hydroxy-2-[(e,3r)-3-hydroxy-4-(phenoxy)but-1-enyl]-5-oxocyclopentyl]hepta-4,5-dienoate
syngard
gardrine
gardrin
rs-84135
camleed
rs 84135-004
enprostil
camleed (tn)
73121-56-9
enprostil (jan/usan/inn)
D01891
AKOS016014109
CHEMBL2104194
SCHEMBL186877
methyl 7-((1r,2r,3r)-3-hydroxy-2-((r,e)-3-hydroxy-4-phenoxybut-1-en-1-yl)-5-oxocyclopentyl)hepta-4,5-dienoate
DTXSID401021647
EX-A6212

Research Excerpts

Overview

Enprostil is a synthetic dehydro-prostaglandin E2 with gastroduodenal ulcer-healing and mucosal-protective properties. It has gastric anti-secretory, cytoprotective, and gastrin lowering properties.

ExcerptReferenceRelevance
"Enprostil is a synthetic prostaglandin E2 analogue with gastric antisecretory and mucosal protective properties. "( Gastric ulcer healing: a comparison of enprostil versus ranitidine.
Bardhan, KD; Bose, K; Hinchliffe, RF; Miller, JP; Morris, P; Patrier, P; Thompson, M; Thompson, RP; Toivanen, E; Walker, R, 1991
)
1.99
"Enprostil is a prostaglandin E2 analogue characterized as a racemic mixture of four stereoisomers. "( The effects of enprostil and RS-86505-007 on in-vitro intestinal permeability of rabbit and monkey.
Bozarth, CA; Grass, GM; Sweetana, SA, 1990
)
2.07
"Enprostil is a synthetic dehydro-prostaglandin E2 with gastroduodenal ulcer-healing and mucosal-protective properties. "( Effect of enprostil on the gastroduodenal mucosa of healthy volunteers.
Basuk, PM; Isenberg, JI; Karlin, DA; Lanza, FL; Robinson, MG, 1990
)
2.12
"Enprostil is a synthetic prostaglandin E2 analogue with gastric anti-secretory, cytoprotective, and gastrin lowering properties. "( Treatment of duodenal ulcer with enprostil, a prostaglandin E2 analogue.
Bright-Asare, P, 1986
)
2
"Enprostil is a synthetic prostaglandin E2 analogue developed by Syntex. "( Treatment of duodenal ulcer with enprostil, a synthetic prostaglandin E2 analogue.
Thomson, AB, 1986
)
2
"Enprostil (E), is a semisynthetic E2 prostaglandin with wide-range antisecretory properties. "( [Effects of enprostil on changes in the gastric transepithelial potential differential induced by aspirin].
Bernier, JJ; Desaint, B; Florent, C; Joubert, M; Maurel, M, 1987
)
2.09
"Enprostil is a new synthetic prostaglandin E2 with antisecretory and mucosal-protective effects. "( A comparison of enprostil and ranitidine in treatment of duodenal ulcer.
Bardhan, KD; Bose, K; Colin, R; Hardman, M; Hinchliffe, RF; Lee, FI; Maxton, DG; Morris, P; Thompson, M; Whittaker, L, 1988
)
2.06

Actions

ExcerptReferenceRelevance
"Enprostil's apparent increase of gastric mucus secretion may contribute to its anti-ulcer activity and may promote gastric healing."( Stimulatory effect of enprostil, an anti-ulcer prostaglandin, on gastric mucus secretion.
Cohn, RG; Garay, GL; Mahoney, JM; Peak, TM; Waterbury, LD, 1986
)
1.31

Treatment

Pretreatment with enprostil (1 microgram/kg intragastrically) prevented most of the damaging effects of ethanol. Pretreatment withEnProstil antagonizes the increase in vascular permeability induced by histamine and presumably other inflammatory mediators.

ExcerptReferenceRelevance
"Enprostil-treated and control rats were killed on day 3 (enprostil group, n = 5; control, n = 6) or day 10 (enprostil group, n = 5; control, n = 5) after TNBS treatment."( Effect of intrarectal prostaglandin E2 analogue (enprostil) on trinitrobenzenesulphonic acid-induced colitis in rats.
Furusu, H; Isomoto, H; Kohno, S; Makiyama, K; Mizuta, Y; Murase, K; Onizuka, Y; Takeshima, F, 2000
)
1.28
"One enprostil treated patient withdrew from the trial prematurely because of abdominal pain."( [Efficacy and tolerability of enprostil in the treatment of duodenal ulcer. Comparison with cimetidine].
Andrieu, J; Evreux, M; Frexinos, J; Guerre, J; Joubert, M; Michel, H; Vicari, F, 1989
)
1.05
"Six enprostil-treated patients and one ranitidine-treated patient withdrew from the trial prematurely because of adverse experiences."( Comparative clinical trial of enprostil and ranitidine in the treatment of gastric ulcer.
Dammann, HG; Hüttemann, W; Kalek, HD; Rohner, HG; Simon, B, 1986
)
1.04
"Pretreatment with enprostil (1 microgram/kg intragastrically) prevented most of the damaging effects of ethanol."( Protective effects of the synthetic prostaglandin enprostil on the gastric microvasculature after ethanol injury in the rat.
Browning, J; Gannon, B; O'Brien, P; Schultz, C, 1986
)
0.85
"Pretreatment with enprostil antagonizes the increase in vascular permeability induced by histamine and presumably other inflammatory mediators."( Effects of enprostil on platelets, endothelial cells, and other cell types, and second messenger systems by which these effects are mediated.
Allison, AC; Kowalski, WJ; Strulovici, B, 1986
)
0.98

Toxicity

ExcerptReferenceRelevance
" Patients recorded their drug compliance, antacid use, ulcer symptoms, and adverse experiences daily."( Enprostil and cimetidine: comparative efficacy and safety in patients with duodenal ulcer.
Almström, C; Carling, L; Cronstedt, J; Ekström, P; Hägg, S; Hansson, B; Unge, P, 1987
)
1.72
" Ratings of symptoms and adverse events were collated from patients' daily diaries, and endoscopy was repeated to verify healing after four weeks and, if appropriate, after six weeks."( Enprostil and ranitidine: comparative efficacy and safety in patients with duodenal ulcer.
Alp, M; Austad, WI; Byrnes, D; Cowen, A; Duggan, J; Mackinnon, M; Pirola, R; Thomas, M; Ward, M, 1987
)
1.72
" However, the combination of diclofenac and pirarubicin was more toxic than pirarubicin alone and induced centrolobular necrosis and sclerosing cholangitis."( Oral diclofenac combined with intra-portal pirarubicin: increased efficacy on liver VX2 tumour and hepatotoxicity in rabbits.
Ardouin, P; Bognel, C; Donatini, B; Munck, JN; Ramirez, L; Rougier, P, 1994
)
0.29

Dosage Studied

This study demonstrates the efficacy and safety of enprostil in the treatment of active duodenal ulcer at the dosage of 35 micrograms twice daily. The findings suggest that en Prostil can be given in a twice daily dosage to treat benign gastric ulcers.

ExcerptRelevanceReference
" This study demonstrates the efficacy and safety of enprostil in the treatment of active duodenal ulcer at the dosage of 35 micrograms twice daily."( [Efficacy and tolerability of enprostil in the treatment of duodenal ulcer. Comparison with cimetidine].
Andrieu, J; Evreux, M; Frexinos, J; Guerre, J; Joubert, M; Michel, H; Vicari, F, 1989
)
0.82
" The blood levels of non-volatile radioactivity at 1 h after each daily dosing were nearly constant."( Metabolic fate of the new anti-ulcer drug enprostil in animals. 3rd communication: tissue accumulation after consecutive oral administration of [3H]-enprostil in rats.
Chaplin, M; Kohno, M; Naito, K; Nakahara, M; Otsuka, M; Parnes, H; Takaiti, O; Yamada, Y, 1989
)
0.54
" One half of CONT and RAD groups were dosed orally with enprostil, 5 micrograms/kg body weight, and the other half of the CONT and RAD groups were dosed with placebo."( Lack of protective effect of oral enprostil, a synthetic prostaglandin E2, on intestinal transport and morphology following abdominal irradiation in the rat.
Cheeseman, CI; Clandinin, MT; Keelan, M; Lam, T; Tavernini, M; Thomson, AB; Walker, K, 1989
)
0.8
" This study was undertaken to assess the possible protective effect of oral dosing of enprostil, a synthetic E2 prostaglandin, on the BBM marker enzyme and lipid composition of non-irradiated control (CONT) animals and of rats exposed seven days perviously to a single dose of 600 cGy external abdominal irradiation (RAD)."( Effect of oral enprostil, a synthetic prostaglandin E2, on intestinal brush border membrane lipid composition following abdominal irradiation in the rat.
Cheeseman, CI; Clandinin, MT; Keelan, M; Tavernini, M; Thomson, AB; Walker, K, 1989
)
0.85
" Enprostil in a dosage of 35 or 70 micrograms BID had no effect on intragastric pH, but when enprostil was given in combination with ranitidine, postprandial and nocturnal intragastric alkalinity was accentuated along with a return of duodenal and antral G-cells and a loss of the antral D-cell hyperplasia."( Synergistic interaction between an H2-receptor antagonist and enprostil on 24-hour intragastric pH, serum gastrin concentration, and tissue immunoperoxidase staining for gastrin, somatostatin, and serotonin in a patient with metastatic gastrinoma.
Brunet, MK; Jewell, LD; Kirdeikis, P; Mahachai, V; Pinchbeck, B; Salkie, ML; Sherbaniuk, R; Walker, K; Yacoub, W; Zuk, L, 1986
)
1.42
" The findings suggest that enprostil can be given in a twice daily dosage in the treatment of benign gastric ulcers."( [Stomach ulcer healing with enprostil, an orally effective prostaglandin E2 analog: direct comparative study with ranitidine].
Beckenbach, HP; Daake, H; Dammann, HG; Hüttemann, W; Jancke, T; Kalek, HD; Kühn, V; Martens, W; Müller, P; Rohner, HG, 1986
)
0.86
"This study evaluated the efficacy of two dosage levels of enprostil in 129 patients with gastric ulcer disease."( Treatment of gastric ulcer with enprostil.
Navert, H, 1986
)
0.8
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID1346427Human EP4 receptor (Prostanoid receptors)2000British journal of pharmacology, Aug, Volume: 130, Issue:8
Pharmacological characterization of [(3)H]-prostaglandin E(2) binding to the cloned human EP(4) prostanoid receptor.
AID1346408Human EP1 receptor (Prostanoid receptors)2000Biochimica et biophysica acta, Jan-17, Volume: 1483, Issue:2
The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.
AID1346396Rat EP3 receptor (Prostanoid receptors)1997European journal of pharmacology, Dec-11, Volume: 340, Issue:2-3
Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
AID1346408Human EP1 receptor (Prostanoid receptors)2002The Journal of pharmacy and pharmacology, Apr, Volume: 54, Issue:4
Cloned human EP1 prostanoid receptor pharmacology characterized using radioligand binding techniques.
AID1346345Rat EP1 receptor (Prostanoid receptors)1997European journal of pharmacology, Dec-11, Volume: 340, Issue:2-3
Molecular cloning and characterization of the four rat prostaglandin E2 prostanoid receptor subtypes.
AID1346343Human EP3 receptor (Prostanoid receptors)1998The Journal of pharmacology and experimental therapeutics, Aug, Volume: 286, Issue:2
Pharmacology of [3H]prostaglandin E1/[3H]prostaglandin E2 and [3H]prostaglandin F2alpha binding to EP3 and FP prostaglandin receptor binding sites in bovine corpus luteum: characterization and correlation with functional data.
AID1346343Human EP3 receptor (Prostanoid receptors)2000Biochimica et biophysica acta, Jan-17, Volume: 1483, Issue:2
The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.
AID1346394Human FP receptor (Prostanoid receptors)2000Biochimica et biophysica acta, Jan-17, Volume: 1483, Issue:2
The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (160)

TimeframeStudies, This Drug (%)All Drugs %
pre-199093 (58.13)18.7374
1990's57 (35.63)18.2507
2000's8 (5.00)29.6817
2010's2 (1.25)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.57

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index29.57 (24.57)
Research Supply Index5.44 (2.92)
Research Growth Index3.97 (4.65)
Search Engine Demand Index42.09 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.57)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials64 (38.79%)5.53%
Reviews11 (6.67%)6.00%
Case Studies3 (1.82%)4.05%
Observational0 (0.00%)0.25%
Other87 (52.73%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]