Page last updated: 2024-12-10

spirapril

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

Description

spirapril: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5311447
CHEMBL ID431
CHEBI ID135756
SCHEMBL ID17202
MeSH IDM0149125

Synonyms (43)

Synonym
setrilan
ti-211-950
sandopril
sch-33844
renormax
sch 33844
1,4-dithia-7-azaspiro(4,4)nonane-8-carboxylic acid, 7-(2-((1-(ethoxycarbonyl)-3-phenylpropyl)amino)-1-oxopropyl)-, (8s-(7(r*(r*)),8r*))-
espirapril [spanish]
brn 4277924
spiraprilum [latin]
spirapril [inn:ban]
spirapril
DB01348
CHEBI:135756
CHEMBL431 ,
83647-97-6
D08529
spirapril (inn)
7-[2-(1-ethoxycarbonyl-3-phenyl-propylamino)-propionyl]-1,4-dithia-7-aza-spiro[4.4]nonane-8-carboxylic acid (spirapiril)
bdbm50017124
7-[2-(1-ethoxycarbonyl-3-phenyl-propylamino)-propionyl]-1,4-dithia-7-aza-spiro[4.4]nonane-8-carboxylic acid
espirapril
spiraprilum
96u2k78i3v ,
unii-96u2k78i3v
AKOS016013943
spirapril [who-dd]
spirapril [inn]
spirapril [mi]
gtpl6575
(7s)-8-[(2s)-2-[[(2s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]-1,4-dithia-8-azaspiro[4.4]nonane-7-carboxylic acid
SCHEMBL17202
HRWCVUIFMSZDJS-SZMVWBNQSA-N
(s,s,s)-7-[2-[(1-ethoxycarbonyl-3-phenylpropyl)amino]-1-oxopropyl]-1,4-dithia-7-azaspiro[4.4]nonane-8-carboxylic acid
DTXSID1044300
(8s)-7-[(2s)-2-{[(2s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}propanoyl]-1,4-dithia-7-azaspiro[4.4]nonane-8-carboxylic acid
(s)-7-((s)-2-((s)-1-ethoxy-1-oxo-4-phenylbutan-2-ylamino)propanoyl)-1,4-dithia-7-azaspiro[4.4]nonane-8-carboxylic acid
(s)-7-((s)-2-(((s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1,4-dithia-7-azaspiro[4.4]nonane-8-carboxylic acid
Q835757
EN300-19766663
(8s)-7-[(2s)-2-[[(2s)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]-1,4-dithia-7-azaspiro[4.4]nonane-8-carboxylic acid
HY-A0230
CS-0017576

Research Excerpts

Overview

Spirapril is a prodrug that is converted by esterolysis to the active (but poorly absorbed) diacid spiraprilat. Spirapril proved to be a well tolerated ACE-inhibitor.

ExcerptReferenceRelevance
"Spirapril is a non-sulfhydryl angiotensin converting enzyme (ACE) inhibitor prodrug which is converted to the active metabolite spiraprilat following oral administration, and which has been evaluated primarily for the treatment of hypertension. "( Spirapril. A preliminary review of its pharmacology and therapeutic efficacy in the treatment of hypertension.
Noble, S; Sorkin, EM, 1995
)
3.18
"Spirapril is a new angiotensin-converting enzyme (ACE) inhibitor with a long duration of action. "( Effects of spirapril and captopril on regional blood flow in chronic congestive heart failure: a comparison between a short- and a long-acting angiotensin-converting enzyme inhibitor.
de Graeff, PA; Girbes, AR; Hillege, H; Lie, KI; Smit, AJ; van den Broek, SA; van Gilst, WH; van Veldhuisen, DJ; Wesseling, H, 1995
)
2.12
"Spirapril is a recent ACE inhibitor with a both renal and hepatic elimination pathway. "( [Kidney function in hypertensive patients with chronic renal failure treated with the dual eliminated ACE-inhibitor spirapril].
Haufe, CC; Jansa, U; Sierakowski, B; Stein, G, 1994
)
1.94
"Spirapril is a prodrug that is converted by esterolysis to the active (but poorly absorbed) diacid spiraprilat. "( Spirapril: pharmacokinetic properties and drug interactions.
Gerbeau, C; Grass, P; Kutz, K, 1994
)
3.17
"Spirapril proved to be a well tolerated ACE-inhibitor."( [Therapy of heart failure with spirapril--the open phase of the CASSIS study. Analysis of the 2nd year extension of the CASSIS study].
Jerie, P; Kremer, HJ; Nikodýmová, L; Uhlír, O; Widimský, J, 1997
)
1.3
"Spirapril is a new angiotensin-converting enzyme (ACE) inhibitor. "( Efficacy and safety of spirapril in mild-to-moderate hypertension.
Hayduk, K; Kraul, H, 1999
)
2.06
"Thus spirapril is seen to be an effective and well-tolerated antihypertensive drug whose efficacy is clearly related to baseline blood pressure and thus is also very effective in the treatment of severe forms of hypertension."( Clinical experience with spirapril in human hypertension.
Kraul, H; Schmidt, J, 1999
)
1.06
"Spirapril is a new non-sulphydryl angiotensin converting enzyme (ACE) inhibitor which is eliminated mainly through the liver. "( Comparison of the acute and chronic antihypertensive effect of two once-daily doses of spirapril by invasive twenty-four-hour ambulatory blood pressure monitoring.
Man in 't Veld, AJ; Ritsema van Eck, HJ; Schalekamp, MA; van den Meiracker, AH, 1989
)
1.94

Effects

ExcerptReferenceRelevance
"Spirapril has no relevant drug interactions."( Efficacy and safety of spirapril in mild-to-moderate hypertension.
Hayduk, K; Kraul, H, 1999
)
1.34

Treatment

Spirapril and enalapril treatment resulted in similar reductions in SBP at both peak and trough levels. Treatment with spirapril resulted in stable LV weight during the follow-up period of 32 days. The untreated group showed a significant steady increase in heart weight.

ExcerptReferenceRelevance
"Spirapril and enalapril treatment resulted in similar reductions in SBP at both peak and trough levels."( Comparison of efficacy of spirapril and enalapril in control of mild-to-moderate hypertension.
Alfiero, R; Alvisi, V; Guitard, C; Lohmann, FW; Ruina, M, 1997
)
1.32
"Treatment with spirapril resulted in stable LV weight during the follow-up period of 32 days, whereas the untreated group showed a significant steady increase in heart weight."( Effect of spirapril on left ventricular hypertrophy due to volume overload in rats.
Hof, RP; Novosel, D; Pedersen, B; Robertson, E; Rudin, M; Umemura, K; Zierhut, W, 1992
)
1.03
"Treatment with spirapril (2-2.5 mg.kg-1.d-1) or zofenopril (12-15 mg.kg-1.d-1) added to the drinking water was started immediately after myocardial infarction or sham operation and continued for six weeks."( Converting enzyme inhibition after experimental myocardial infarction in rats: comparative study between spirapril and zofenopril.
de Graeff, PA; de Langen, CD; Pinto, YM; van Gilst, WH; van Wijngaarden, J; Wesseling, H, 1991
)
0.83

Toxicity

ExcerptReferenceRelevance
" Reported adverse events were mostly not study drug-related and were similar to those with placebo except for headache, which was more frequent with spirapril than placebo (5."( A multicentre multidose study of the efficacy and safety of spirapril in mild-to-moderate essential hypertension. UK Study Group of Spirapril in Hypertension.
Fairhurst, GJ, 1994
)
0.73
" The most commonly reported adverse effects were cough (13-17%), dizziness, headache and insomnia."( Efficacy and safety of spirapril, a new ace-inhibitor, in elderly hypertensive patients.
Ekman, K; Honkanen, T; Järveläinen, V; Kantola, I; Kataja, M; Terént, A, 1996
)
0.6

Pharmacokinetics

The acute hemodynamic, hormonal, and pharmacokinetic responses to the oral angiotensin-converting enzyme (ACE) inhibitor spirapril were studied in 15 patients with moderate to severe congestive heart failure in a baseline controlled dose-ranging study. After intravenous infusion, the disposition of Spirapril is monophasic with a terminal half-life of 20-50 minutes.

ExcerptReferenceRelevance
"The acute hemodynamic, hormonal, and pharmacokinetic responses to the oral angiotensin-converting enzyme (ACE) inhibitor spirapril were studied in 15 patients with moderate to severe congestive heart failure in a baseline controlled dose-ranging study."( The acute hemodynamic, hormonal, and pharmacokinetic properties of oral spirapril in patients with moderate to severe heart failure.
de Graeff, PA; Hillege, H; Lie, KI; van Bruggen, A; van den Broek, SA; van Gilst, WH; Wesseling, H, 1991
)
0.72
" However, there was no evidence of accumulation of spiraprilat in any of the groups as determined by the pharmacokinetic parameters derived after single and multiple doses."( Pharmacokinetics of spirapril in renal impairment.
Elliott, HL; Grass, P; Guitard, C; Meredith, PA, 1994
)
0.86
" Regression analysis of pharmacokinetic parameters C(max)ss (the maximum steady-state drug concentration in plasma during a dosing interval), Cl/f (total plasma clearance) and k (elimination rate constant) of spirapril on creatinine clearance (Clcr) showed that the pharmacokinetics of spirapril were not significantly influenced by the degree of renal impairment."( Pharmacokinetics of spirapril and spiraprilat in patients with chronic renal failure.
Grass, P; Haufe, CC; Jansa, U; Sierakowski, B; Stein, G; Weidinger, G, 1994
)
0.8
" After intravenous infusion, the disposition of spirapril is monophasic with a terminal half-life of 20-50 minutes."( Spirapril: pharmacokinetic properties and drug interactions.
Gerbeau, C; Grass, P; Kutz, K, 1994
)
1.99
"00 h-1 in control subjects) while the elimination half-life of spiraprilat was not different."( Pharmacokinetics and haemodynamic effects of a single oral dose of the novel ACE inhibitor spirapril in patients with chronic liver disease.
Grass, P; Krähenbühl, S; Kutz, K; Reichen, J; Surve, A, 1993
)
0.75

Compound-Compound Interactions

quadropril (Spirapril, Pliva) was given for 2 months to patients with arterial hypertension combined with chronic obstructive pulmonary disease. Results suggest that hydrochlorothiazide does not interact in the fixed combination with the pharmacokinetics of spirapril.

ExcerptReferenceRelevance
" The results suggest that hydrochlorothiazide does not interact in the fixed combination with the pharmacokinetics of spirapril and vice versa."( Drug interaction of spirapril hydrochloride monohydrate and hydrochlorothiazide. A clinical study to compare the pharmacokinetics after administration of spirapril hydrochloride monohydrate tablets, hydrochlorothiazide tablets and fixed combination bi-lay
Amschler, S; Erb, K; Hermann, R; Junge, K; Krupp, S; Schäfer, HF; Schulz, HU; Schürer, M, 2003
)
0.85
"In this study quadropril (Spirapril, Pliva) was given for 2 months to patients with arterial hypertension combined with chronic obstructive pulmonary disease."( [Clinical application of spirapril in patients with arterial hypertension combined with chronic obstructive pulmonary disease].
Barbarash, OL; Kondrikova, NV; Smakotina, SA, 2006
)
0.94

Bioavailability

The bioavailability of orally administered spirapril was 50% whereas the bioavailability. of spirapilat was virtually zero. The metabolite responsible for the pharmacological action of Spirapril, was significantly reduced in patients.

ExcerptReferenceRelevance
" The bioavailability of orally administered spirapril was 50% whereas the bioavailability of orally administered spiraprilat was virtually zero."( Spirapril: pharmacokinetic properties and drug interactions.
Gerbeau, C; Grass, P; Kutz, K, 1994
)
1.99
" In contrast, the bioavailability of spiraprilat, the metabolite responsible for the pharmacological action of spirapril, was significantly reduced in patients (AUC 820 micrograms."( Pharmacokinetics and haemodynamic effects of a single oral dose of the novel ACE inhibitor spirapril in patients with chronic liver disease.
Grass, P; Krähenbühl, S; Kutz, K; Reichen, J; Surve, A, 1993
)
0.78

Dosage Studied

The pharmacokinetics of spirapril were not significantly influenced by the degree of renal impairment. There were statistically significant differences between all active-treatment groups (except the 24-mg dose group) and placebo. If, after 4 weeks of treatment, diastolic blood pressure (DBP) was still > 90 mm Hg, this dosage was doubled.

ExcerptRelevanceReference
"To investigate whether the compensatory rise in renin and plasma angiotensin I in response to repeated angiotensin converting enzyme (ACE) inhibitor treatment results in a partial escape of ACE inhibition over a 24-h dosing interval."( Partial escape of angiotensin converting enzyme (ACE) inhibition during prolonged ACE inhibitor treatment: does it exist and does it affect the antihypertensive response?
Admiraal, PJ; Boomsma, F; Derkx, FH; Man in 't Veld, AJ; Ritsema van Eck, HJ; Schalekamp, MA; van den Meiracker, AH, 1992
)
0.28
" At the end of dosing interval angiotensin II had returned to values seen under placebo with the 12."( Partial escape of angiotensin converting enzyme (ACE) inhibition during prolonged ACE inhibitor treatment: does it exist and does it affect the antihypertensive response?
Admiraal, PJ; Boomsma, F; Derkx, FH; Man in 't Veld, AJ; Ritsema van Eck, HJ; Schalekamp, MA; van den Meiracker, AH, 1992
)
0.28
" This escape also affects the antihypertensive response in the second half of the dosing interval."( Partial escape of angiotensin converting enzyme (ACE) inhibition during prolonged ACE inhibitor treatment: does it exist and does it affect the antihypertensive response?
Admiraal, PJ; Boomsma, F; Derkx, FH; Man in 't Veld, AJ; Ritsema van Eck, HJ; Schalekamp, MA; van den Meiracker, AH, 1992
)
0.28
" Systolic BP (SBP) and mean arterial pressure (MAP) were significantly lower in spirapril-treated rats, and the dose-response curve to ANGI was shifted to the right."( Effect of spirapril on left ventricular hypertrophy due to volume overload in rats.
Hof, RP; Novosel, D; Pedersen, B; Robertson, E; Rudin, M; Umemura, K; Zierhut, W, 1992
)
0.91
" Dosage of spirapril was increased from 12 mg to 48 mg once daily."( Digoxin pharmacokinetics and spirapril, a new ace inhibitor.
Flemming, J; Johnson, BF; Johnson, J; Wilson, J, 1991
)
0.96
" Systolic blood pressure and heart rate were recorded once a week just before dosing and at varying time intervals up to 6 hr thereafter."( Antihypertensive effect of spirapril and felodipine during repeated administration to spontaneously hypertensive rats.
Forlani, A; Milani, S; Monopoli, A; Ongini, E, 1988
)
0.57
" The dose-response curve for spirapril appears to be flat for doses of 6 to 24 mg once daily."( Spirapril. A preliminary review of its pharmacology and therapeutic efficacy in the treatment of hypertension.
Noble, S; Sorkin, EM, 1995
)
2.03
" The dosage was titrated if necessary after 4 weeks of treatment."( Sustained-release isradipine compared with spirapril in the treatment of elderly patients with isolated systolic hypertension.
Chan, TY; Critchley, JA; Or, KK; Sanderson, JE; Tomlinson, B; Woo, J, 1994
)
0.55
" If, after 4 weeks of treatment, CR-determined diastolic blood pressure (DBP) was still > 90 mm Hg, this dosage was doubled (n = 327) and, at week 8, pindolol at 5 mg or spirapril at 3 mg daily was added if necessary for blood pressure control."( A multicenter study using causal readings, self-recordings, and ambulatory blood pressure monitoring to assess isradipine effects. AMICUS Study Group.
Fitscha, P; Magometschnigg, D; Meisner, W, 1994
)
0.48
" Regression analysis of pharmacokinetic parameters C(max)ss (the maximum steady-state drug concentration in plasma during a dosing interval), Cl/f (total plasma clearance) and k (elimination rate constant) of spirapril on creatinine clearance (Clcr) showed that the pharmacokinetics of spirapril were not significantly influenced by the degree of renal impairment."( Pharmacokinetics of spirapril and spiraprilat in patients with chronic renal failure.
Grass, P; Haufe, CC; Jansa, U; Sierakowski, B; Stein, G; Weidinger, G, 1994
)
0.8
" There were statistically significant differences between all active-treatment groups (except the 24-mg dose group) and placebo, but not among the spirapril groups at the end of the +24-hour dosing interval."( A multicentre multidose study of the efficacy and safety of spirapril in mild-to-moderate essential hypertension. UK Study Group of Spirapril in Hypertension.
Fairhurst, GJ, 1994
)
0.73
" When blood pressures were measured at the end of the dosing interval (trough), all spirapril regimens had produced similar reductions in sitting systolic and diastolic blood pressures (siSBP/siDBP) which were significantly greater than those observed in placebo-treated patients."( Placebo-controlled comparison of spirapril at 6, 12 and 24 mg/day in mild to severe essential hypertension.
Alvisi, V; Boxho, G; Cocco, G; Franck, J; Guitard, C; Maibach, E; Mellein, B; Waite, R, 1994
)
0.79
" In contrast, the single dosing of all agents failed to show antinociceptive effect."( Antinociceptive effects of angiotensin-converting enzyme inhibitors and an angiotensin II receptor antagonist in mice.
Miyazaki, M; Okunishi, H; Song, K; Takai, S; Tanaka, T, 1996
)
0.29
" In patients whose blood pressure was not normalized (defined as DBP< or =90 mmHg) after 6 weeks of treatment, the dosage of either medication was doubled or, in the placebo group, was switched to the fixed combination."( Evaluation of the efficacy and tolerability of a low-dose combination of isradipine and spirapril in the first-line treatment of mild to moderate essential hypertension.
Antlsperger, A; Pittrow, DB; Schardt, W; Wambach, G; Weidinger, G; Welzel, D, 1997
)
0.52
"The administration of most angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin receptor blockers (ARBs) at bedtime results in a greater reduction of nighttime blood pressure (BP) than dosing upon awakening."( Administration-time-dependent effects of spirapril on ambulatory blood pressure in uncomplicated essential hypertension.
Alonso, I; Ayala, DE; Fernández, JR; Fontao, MJ; Hermida, RC; Mojón, A, 2010
)
0.63
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
prodrugA compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitorAn EC 3.4.15.* (peptidyl-dipeptidase) inhibitor that interferes with the action of peptidyl-dipeptidase A (EC 3.4.15.1).
antihypertensive agentAny drug used in the treatment of acute or chronic vascular hypertension regardless of pharmacological mechanism.
[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 (8)

ClassDescription
dipeptideAny molecule that contains two amino-acid residues connected by peptide linkages.
dithioketalA dithioacetal of formula R2C(SR')2, R =/= H, R' =/= H.
azaspiro compoundAn azaspiro compound is a spiro compound in which at least one of the cyclic components is a nitrogen heterocyle.
dicarboxylic acid monoesterA monoester of a dicarboxylic acid.
ethyl esterAny carboxylic ester resulting from the formal condensation of the carboxy group of a carboxylic acid with ethanol.
tertiary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a secondary amine; formula RC(=O)NHR(1)R(2).
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
pyrrolidinecarboxylic 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 Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Angiotensin-converting enzymeRattus norvegicus (Norway rat)IC50 (µMol)0.06700.00090.33223.0300AID38879
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID182326% Inhibition of angiotensin-I induced pressor response in normotensive rats after peroral dosing of 0.5 umol/kg1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines.
AID39748Compound was tested for inhibitory activity against Angiotensin I converting enzyme when administered intraperitoneally to anesthetized dogs1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Angiotensin converting enzyme inhibitors: spirapril and related compounds.
AID25872The acid dissociation constant, pKa was determined.'a' represents value of C-terminus carboxylic acid.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Design, synthesis, and physicochemical properties of a novel, conformationally restricted 2,3-dihydro-1,3,4-thiadiazole-containing angiotensin converting enzyme inhibitor which is preferentially eliminated by the biliary route in rats.
AID38879Compound tested in vitro for inhibition of Angiotensin I converting enzyme1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Angiotensin converting enzyme inhibitors: spirapril and related compounds.
AID38110Compound tested in vivo for inhibition of Angiotensin I converting enzyme in rat1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Angiotensin converting enzyme inhibitors: spirapril and related compounds.
AID182325% Inhibition of angiotensin-I induced pressor response in normotensive rats after peroral dosing of 0.15 umol/kg1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines.
AID60351Compound was tested for its efficacy in dog1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Angiotensin converting enzyme inhibitors: spirapril and related compounds.
AID38463Compound was tested for inhibitory activity against angiotensin converting enzyme when administered intraperitoneally to anesthetized dogs1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Angiotensin converting enzyme inhibitors: spirapril and related compounds.
AID26306Logarithm of the ratio of anionic to unionized species at pH 7.41991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Design, synthesis, and physicochemical properties of a novel, conformationally restricted 2,3-dihydro-1,3,4-thiadiazole-containing angiotensin converting enzyme inhibitor which is preferentially eliminated by the biliary route in rats.
AID38464Compound tested in vivo for inhibition of angiotensin converting enzyme in rat1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Angiotensin converting enzyme inhibitors: spirapril and related compounds.
AID182327% Inhibition of angiotensin-I induced pressor response in normotensive rats after peroral dosing of 1.5 umol/kg1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Angiotensin-converting enzyme inhibitors. Mercaptan, carboxyalkyl dipeptide, and phosphinic acid inhibitors incorporating 4-substituted prolines.
AID640615Clearance in human liver microsomes at 1 uM measured after 60 mins by HPLC analysis2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Capture hydrolysis signals in the microsomal stability assay: molecular mechanisms of the alkyl ester drug and prodrug metabolism.
AID26526Compound was tested for its maximum lipophilicity.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Design, synthesis, and physicochemical properties of a novel, conformationally restricted 2,3-dihydro-1,3,4-thiadiazole-containing angiotensin converting enzyme inhibitor which is preferentially eliminated by the biliary route in rats.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (120)

TimeframeStudies, This Drug (%)All Drugs %
pre-19909 (7.50)18.7374
1990's78 (65.00)18.2507
2000's29 (24.17)29.6817
2010's4 (3.33)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: 28.37

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 Index28.37 (24.57)
Research Supply Index5.21 (2.92)
Research Growth Index5.23 (4.65)
Search Engine Demand Index36.71 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.37)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials59 (47.97%)5.53%
Reviews6 (4.88%)6.00%
Case Studies1 (0.81%)4.05%
Observational0 (0.00%)0.25%
Other57 (46.34%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
NT-proBNP Selected PreventiOn of Cardiac eveNts in a populaTion of dIabetic Patients Without A History of Cardiac Disease: a Prospective Randomized Trial [NCT02817360]Phase 42,400 participants (Anticipated)Interventional2016-02-29Recruiting
Prognostic Value of Ambulatory Blood Pressure Monitoring in the Prediction of Cardiovascular Events and Effects of Chronotherapy in Relation to Risk (the MAPEC Study). [NCT00295542]Phase 43,344 participants (Actual)Interventional2000-03-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]