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Identification
NameRemikiren
Accession NumberDB00212  (APRD00163)
TypeSmall Molecule
GroupsApproved
DescriptionRemikiren is an orally active, high specificity renin inhibitor.
Structure
Thumb
SynonymsNot Available
External Identifiers
  • Ro 42-5892
  • RO-42-5892
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIILC7FBL96A4
CAS number126222-34-2
WeightAverage: 630.838
Monoisotopic: 630.345106042
Chemical FormulaC33H50N4O6S
InChI KeyUXIGZRQVLGFTOU-VQXQMPIVSA-N
InChI
InChI=1S/C33H50N4O6S/c1-33(2,3)44(42,43)20-25(16-22-10-6-4-7-11-22)31(40)37-28(18-26-19-34-21-35-26)32(41)36-27(17-23-12-8-5-9-13-23)30(39)29(38)24-14-15-24/h4,6-7,10-11,19,21,23-25,27-30,38-39H,5,8-9,12-18,20H2,1-3H3,(H,34,35)(H,36,41)(H,37,40)/t25-,27+,28+,29+,30-/m1/s1
IUPAC Name
(2S)-2-{[(2S)-2-benzyl-1-hydroxy-3-(2-methylpropane-2-sulfonyl)propylidene]amino}-N-[(2S,3R,4S)-1-cyclohexyl-4-cyclopropyl-3,4-dihydroxybutan-2-yl]-3-(1H-imidazol-5-yl)propanimidic acid
SMILES
[H][C@@](CC1=CC=CC=C1)(CS(=O)(=O)C(C)(C)C)C(O)=N[C@@]([H])(CC1=CN=CN1)C(O)=N[C@@]([H])(CC1CCCCC1)[C@@]([H])(O)[C@@]([H])(O)C1CC1
Pharmacology
IndicationFor the treatment of hypertension and heart failure
Structured Indications Not Available
PharmacodynamicsRemikiren is an orally available renin inhibitor with an established blood pressure-lowering effect in patients with essential hypertension. No data are available on the renal effects of remikiren in humans. In patients with essential hypertension, a single oral dose of remikiren can induce a renal vasodilation, without affecting the GFR and despite a significant decrease in blood pressure. This systemic and renal hemodynamic response is more pronounced in case of a more activated renin-angiotensin system.
Mechanism of actionSeveral in vivo experiments have shown that remikiren is specific for renin and does not decrease arterial pressure by an unrelated mechanism.
TargetKindPharmacological actionActionsOrganismUniProt ID
ReninProteinyes
inhibitor
HumanP00797 details
Related Articles
AbsorptionAbsorbed following oral administration.
Volume of distributionNot Available
Protein binding83%
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypotensive activities of Remikiren.Experimental
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Remikiren.Approved, Investigational
AcebutololRemikiren may increase the hypotensive activities of Acebutolol.Approved
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Remikiren.Approved, Investigational
AliskirenRemikiren may increase the hypotensive activities of Aliskiren.Approved, Investigational
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Remikiren.Approved, Illicit, Investigational
AlprenololRemikiren may increase the hypotensive activities of Alprenolol.Approved, Withdrawn
AmbrisentanRemikiren may increase the hypotensive activities of Ambrisentan.Approved, Investigational
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be decreased when it is combined with Remikiren.Experimental
AmifostineRemikiren may increase the hypotensive activities of Amifostine.Approved, Investigational
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Remikiren.Illicit, Withdrawn
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Remikiren.Approved
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Remikiren.Approved
AmlodipineRemikiren may increase the hypotensive activities of Amlodipine.Approved
AtenololRemikiren may increase the hypotensive activities of Atenolol.Approved
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Remikiren.Approved
BenazeprilRemikiren may increase the hypotensive activities of Benazepril.Approved, Investigational
BendroflumethiazideRemikiren may increase the hypotensive activities of Bendroflumethiazide.Approved
BenmoxinBenmoxin may increase the hypotensive activities of Remikiren.Withdrawn
BepridilRemikiren may increase the hypotensive activities of Bepridil.Approved, Withdrawn
BetaxololBetaxolol may increase the hypotensive activities of Remikiren.Approved
BethanidineRemikiren may increase the hypotensive activities of Bethanidine.Approved
BimatoprostRemikiren may increase the hypotensive activities of Bimatoprost.Approved, Investigational
BisoprololRemikiren may increase the hypotensive activities of Bisoprolol.Approved
BoceprevirThe serum concentration of Remikiren can be decreased when it is combined with Boceprevir.Approved
BosentanRemikiren may increase the hypotensive activities of Bosentan.Approved, Investigational
BretyliumRemikiren may increase the hypotensive activities of Bretylium.Approved
BrimonidineRemikiren may increase the hypotensive activities of Brimonidine.Approved
BrimonidineBrimonidine may increase the antihypertensive activities of Remikiren.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Remikiren.Approved, Investigational
BupranololRemikiren may increase the hypotensive activities of Bupranolol.Approved
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Remikiren.Approved
CandesartanRemikiren may increase the hypotensive activities of Candesartan.Approved
CandoxatrilRemikiren may increase the hypotensive activities of Candoxatril.Experimental
CaptoprilRemikiren may increase the hypotensive activities of Captopril.Approved
CarbamazepineThe metabolism of Remikiren can be increased when combined with Carbamazepine.Approved, Investigational
CaroxazoneCaroxazone may increase the hypotensive activities of Remikiren.Withdrawn
CarteololRemikiren may increase the hypotensive activities of Carteolol.Approved
CarvedilolRemikiren may increase the hypotensive activities of Carvedilol.Approved, Investigational
CeliprololRemikiren may increase the hypotensive activities of Celiprolol.Approved, Investigational
ChlorothiazideRemikiren may increase the hypotensive activities of Chlorothiazide.Approved, Vet Approved
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Remikiren.Withdrawn
ChlorthalidoneRemikiren may increase the hypotensive activities of Chlorthalidone.Approved
CilazaprilRemikiren may increase the hypotensive activities of Cilazapril.Approved
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Remikiren.Approved, Investigational, Withdrawn
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Remikiren.Approved
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Remikiren.Approved, Vet Approved
ClonidineRemikiren may increase the hypotensive activities of Clonidine.Approved
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be decreased when it is combined with Remikiren.Approved
CryptenamineRemikiren may increase the hypotensive activities of Cryptenamine.Approved
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Remikiren.Approved
CyclophosphamideThe risk or severity of adverse effects can be increased when Remikiren is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Remikiren.Approved, Investigational, Vet Approved
CyclothiazideRemikiren may increase the hypotensive activities of Cyclothiazide.Approved
DebrisoquinRemikiren may increase the hypotensive activities of Debrisoquin.Approved
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Remikiren.Approved
DeserpidineRemikiren may increase the hypotensive activities of Deserpidine.Approved
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Remikiren.Approved
DiazoxideDiazoxide may increase the hypotensive activities of Remikiren.Approved
DienestrolThe serum concentration of Dienestrol can be decreased when it is combined with Remikiren.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Remikiren.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Remikiren.Approved
DihydralazineRemikiren may increase the hypotensive activities of Dihydralazine.Investigational
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Remikiren.Approved
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Remikiren.Approved
DorzolamideRemikiren may increase the hypotensive activities of Dorzolamide.Approved
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Remikiren.Approved
DoxazosinRemikiren may increase the hypotensive activities of Doxazosin.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Remikiren.Approved
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Remikiren.Approved
EfonidipineRemikiren may increase the hypotensive activities of Efonidipine.Approved
EnalaprilRemikiren may increase the hypotensive activities of Enalapril.Approved, Vet Approved
EnalaprilatRemikiren may increase the hypotensive activities of Enalaprilat.Approved
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Remikiren.Approved, Investigational
EpoprostenolRemikiren may increase the hypotensive activities of Epoprostenol.Approved
EprosartanRemikiren may increase the hypotensive activities of Eprosartan.Approved
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Remikiren.Approved
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Remikiren.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Remikiren.Approved
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Remikiren.Investigational
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Remikiren.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Estramustine can be decreased when it is combined with Remikiren.Approved
Estrogens, esterifiedThe serum concentration of Estrogens, esterified can be decreased when it is combined with Remikiren.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be decreased when it is combined with Remikiren.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Remikiren.Approved
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Remikiren.Approved
FelodipineRemikiren may increase the hypotensive activities of Felodipine.Approved, Investigational
FenoldopamRemikiren may increase the hypotensive activities of Fenoldopam.Approved
FosinoprilRemikiren may increase the hypotensive activities of Fosinopril.Approved
FurazolidoneFurazolidone may increase the hypotensive activities of Remikiren.Approved, Vet Approved
GarlicThe serum concentration of Remikiren can be decreased when it is combined with Garlic.Approved
GuanabenzRemikiren may increase the hypotensive activities of Guanabenz.Approved
GuanadrelRemikiren may increase the hypotensive activities of Guanadrel.Approved
GuanethidineRemikiren may increase the hypotensive activities of Guanethidine.Approved
GuanfacineRemikiren may increase the hypotensive activities of Guanfacine.Approved, Investigational
HexamethoniumRemikiren may increase the hypotensive activities of Hexamethonium.Experimental
HexestrolThe serum concentration of Hexestrol can be decreased when it is combined with Remikiren.Withdrawn
HydracarbazineHydracarbazine may increase the hypotensive activities of Remikiren.Approved
HydralazineRemikiren may increase the hypotensive activities of Hydralazine.Approved
HydrochlorothiazideRemikiren may increase the hypotensive activities of Hydrochlorothiazide.Approved, Vet Approved
HydroflumethiazideRemikiren may increase the hypotensive activities of Hydroflumethiazide.Approved
IloprostIloprost may increase the hypotensive activities of Remikiren.Approved, Investigational
ImidaprilRemikiren may increase the hypotensive activities of Imidapril.Investigational
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Remikiren.Approved
IndapamideRemikiren may increase the hypotensive activities of Indapamide.Approved
IndenololRemikiren may increase the hypotensive activities of Indenolol.Withdrawn
IndoraminRemikiren may increase the hypotensive activities of Indoramin.Withdrawn
IproclozideIproclozide may increase the hypotensive activities of Remikiren.Withdrawn
IproniazidIproniazid may increase the hypotensive activities of Remikiren.Withdrawn
IrbesartanRemikiren may increase the hypotensive activities of Irbesartan.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Remikiren.Approved
IsradipineRemikiren may increase the hypotensive activities of Isradipine.Approved
KetanserinRemikiren may increase the hypotensive activities of Ketanserin.Investigational
LabetalolRemikiren may increase the hypotensive activities of Labetalol.Approved
LacidipineRemikiren may increase the hypotensive activities of Lacidipine.Approved
LatanoprostRemikiren may increase the hypotensive activities of Latanoprost.Approved, Investigational
LercanidipineRemikiren may increase the hypotensive activities of Lercanidipine.Approved, Investigational
LisinoprilRemikiren may increase the hypotensive activities of Lisinopril.Approved, Investigational
LofexidineRemikiren may increase the hypotensive activities of Lofexidine.Approved, Investigational
LosartanRemikiren may increase the hypotensive activities of Losartan.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Remikiren.Approved, Investigational
MacitentanRemikiren may increase the hypotensive activities of Macitentan.Approved
ManidipineRemikiren may increase the hypotensive activities of Manidipine.Approved
MebanazineMebanazine may increase the hypotensive activities of Remikiren.Withdrawn
MecamylamineRemikiren may increase the hypotensive activities of Mecamylamine.Approved
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Remikiren.Approved
MethallenestrilThe serum concentration of Methallenestril can be decreased when it is combined with Remikiren.Experimental
MethyldopaRemikiren may increase the hypotensive activities of Methyldopa.Approved
Methylene blueMethylene blue may increase the hypotensive activities of Remikiren.Investigational
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Remikiren.Approved, Investigational
MetipranololRemikiren may increase the hypotensive activities of Metipranolol.Approved
MetolazoneRemikiren may increase the hypotensive activities of Metolazone.Approved
MetoprololRemikiren may increase the hypotensive activities of Metoprolol.Approved, Investigational
MetyrosineRemikiren may increase the hypotensive activities of Metyrosine.Approved
MibefradilRemikiren may increase the hypotensive activities of Mibefradil.Withdrawn
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Remikiren.Approved, Illicit
MinaprineMinaprine may increase the hypotensive activities of Remikiren.Approved
MinoxidilRemikiren may increase the hypotensive activities of Minoxidil.Approved
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Remikiren.Approved
MoclobemideMoclobemide may increase the hypotensive activities of Remikiren.Approved
MoexiprilRemikiren may increase the hypotensive activities of Moexipril.Approved
MolsidomineMolsidomine may increase the hypotensive activities of Remikiren.Approved
MoxonidineRemikiren may increase the hypotensive activities of Moxonidine.Approved
NadololRemikiren may increase the hypotensive activities of Nadolol.Approved
NaftopidilRemikiren may increase the hypotensive activities of Naftopidil.Investigational
NebivololRemikiren may increase the hypotensive activities of Nebivolol.Approved, Investigational
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Remikiren.Approved, Withdrawn
NialamideNialamide may increase the hypotensive activities of Remikiren.Withdrawn
NicardipineRemikiren may increase the hypotensive activities of Nicardipine.Approved
NicorandilRemikiren may increase the hypotensive activities of Nicorandil.Approved
NiguldipineRemikiren may increase the hypotensive activities of Niguldipine.Experimental
NilvadipineRemikiren may increase the hypotensive activities of Nilvadipine.Approved
NimodipineRemikiren may increase the hypotensive activities of Nimodipine.Approved
NisoldipineRemikiren may increase the hypotensive activities of Nisoldipine.Approved
NitrendipineRemikiren may increase the hypotensive activities of Nitrendipine.Approved
NitroprussideRemikiren may increase the hypotensive activities of Nitroprusside.Approved
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Remikiren.Approved
ObinutuzumabRemikiren may increase the hypotensive activities of Obinutuzumab.Approved
OctamoxinOctamoxin may increase the hypotensive activities of Remikiren.Withdrawn
OlmesartanRemikiren may increase the hypotensive activities of Olmesartan.Approved, Investigational
OmapatrilatRemikiren may increase the hypotensive activities of Omapatrilat.Investigational
OpipramolThe serum concentration of Opipramol can be increased when it is combined with Remikiren.Investigational
OxprenololRemikiren may increase the hypotensive activities of Oxprenolol.Approved
PargylinePargyline may increase the hypotensive activities of Remikiren.Approved
PenbutololRemikiren may increase the hypotensive activities of Penbutolol.Approved, Investigational
PentoliniumRemikiren may increase the hypotensive activities of Pentolinium.Approved
PentoxifyllinePentoxifylline may increase the hypotensive activities of Remikiren.Approved, Investigational
PerindoprilRemikiren may increase the hypotensive activities of Perindopril.Approved
PethidineThe risk or severity of adverse effects can be increased when Remikiren is combined with Pethidine.Approved
PhenelzinePhenelzine may increase the hypotensive activities of Remikiren.Approved
PheniprazinePheniprazine may increase the hypotensive activities of Remikiren.Withdrawn
PhenoxybenzamineRemikiren may increase the hypotensive activities of Phenoxybenzamine.Approved
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Remikiren.Withdrawn
PhentolamineRemikiren may increase the hypotensive activities of Phentolamine.Approved
PimozideThe serum concentration of Pimozide can be increased when it is combined with Remikiren.Approved
PinacidilRemikiren may increase the hypotensive activities of Pinacidil.Withdrawn
PindololRemikiren may increase the hypotensive activities of Pindolol.Approved
PirlindolePirlindole may increase the hypotensive activities of Remikiren.Approved
PivhydrazinePivhydrazine may increase the hypotensive activities of Remikiren.Withdrawn
PolythiazideRemikiren may increase the hypotensive activities of Polythiazide.Approved
PrazosinRemikiren may increase the hypotensive activities of Prazosin.Approved
PropranololRemikiren may increase the hypotensive activities of Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Remikiren.Approved
QuinaprilRemikiren may increase the hypotensive activities of Quinapril.Approved, Investigational
QuinineQuinine may increase the hypotensive activities of Remikiren.Approved
RamiprilRamipril may increase the hypotensive activities of Remikiren.Approved
RasagilineRasagiline may increase the hypotensive activities of Remikiren.Approved
RescinnamineRemikiren may increase the hypotensive activities of Rescinnamine.Approved
ReserpineReserpine may increase the hypotensive activities of Remikiren.Approved
RilmenidineRemikiren may increase the hypotensive activities of Rilmenidine.Investigational
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Remikiren.Approved
RituximabRemikiren may increase the hypotensive activities of Rituximab.Approved
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Remikiren.Approved
SafrazineSafrazine may increase the hypotensive activities of Remikiren.Withdrawn
SaprisartanRemikiren may increase the hypotensive activities of Saprisartan.Experimental
SelegilineSelegiline may increase the hypotensive activities of Remikiren.Approved, Investigational, Vet Approved
SelexipagRemikiren may increase the hypotensive activities of Selexipag.Approved
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Remikiren.Approved, Investigational
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Remikiren.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Remikiren.Approved
SitaxentanRemikiren may increase the hypotensive activities of Sitaxentan.Approved, Investigational, Withdrawn
SpiraprilRemikiren may increase the hypotensive activities of Spirapril.Approved
St. John's WortThe metabolism of Remikiren can be increased when combined with St. John's Wort.Nutraceutical
Synthetic Conjugated Estrogens, AThe serum concentration of Synthetic Conjugated Estrogens, A can be decreased when it is combined with Remikiren.Approved
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Remikiren.Approved, Investigational
TadalafilTadalafil may increase the antihypertensive activities of Remikiren.Approved, Investigational
TelmisartanRemikiren may increase the hypotensive activities of Telmisartan.Approved, Investigational
TemocaprilRemikiren may increase the hypotensive activities of Temocapril.Experimental, Investigational
TemsirolimusThe risk or severity of adverse effects can be increased when Remikiren is combined with Temsirolimus.Approved
TerlipressinRemikiren may increase the hypotensive activities of Terlipressin.Approved, Investigational
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Remikiren.Approved
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Remikiren.Approved
TiboloneRemikiren may increase the hypotensive activities of Tibolone.Approved
TicrynafenRemikiren may increase the hypotensive activities of Ticrynafen.Withdrawn
TimololRemikiren may increase the hypotensive activities of Timolol.Approved
TipranavirThe serum concentration of Remikiren can be decreased when it is combined with Tipranavir.Approved, Investigational
TolazolineRemikiren may increase the hypotensive activities of Tolazoline.Approved, Vet Approved
ToloxatoneToloxatone may increase the hypotensive activities of Remikiren.Approved
TorasemideRemikiren may increase the hypotensive activities of Torasemide.Approved
TrandolaprilRemikiren may increase the hypotensive activities of Trandolapril.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Remikiren.Experimental
TranylcypromineTranylcypromine may increase the hypotensive activities of Remikiren.Approved
TravoprostRemikiren may increase the hypotensive activities of Travoprost.Approved
TreprostinilRemikiren may increase the hypotensive activities of Treprostinil.Approved, Investigational
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Remikiren.Approved
TrichlormethiazideRemikiren may increase the hypotensive activities of Trichlormethiazide.Approved, Vet Approved
TrimazosinRemikiren may increase the hypotensive activities of Trimazosin.Experimental
TrimethaphanRemikiren may increase the hypotensive activities of Trimethaphan.Approved
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Remikiren.Approved
UdenafilUdenafil may increase the antihypertensive activities of Remikiren.Approved, Investigational
UnoprostoneRemikiren may increase the hypotensive activities of Unoprostone.Approved
Valproic AcidThe serum concentration of Valproic Acid can be decreased when it is combined with Remikiren.Approved, Investigational
ValsartanValsartan may increase the hypotensive activities of Remikiren.Approved, Investigational
VardenafilVardenafil may increase the antihypertensive activities of Remikiren.Approved
VerapamilThe metabolism of Verapamil can be decreased when combined with Remikiren.Approved
VinpocetineRemikiren may increase the hypotensive activities of Vinpocetine.Investigational
XylometazolineRemikiren may increase the hypotensive activities of Xylometazoline.Approved
YohimbineYohimbine may decrease the antihypertensive activities of Remikiren.Approved, Vet Approved
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Remikiren.Approved
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Clozel JP, Fischli W: Discovery of remikiren as the first orally active renin inhibitor. Arzneimittelforschung. 1993 Feb;43(2A):260-2. [PubMed:8498974 ]
  2. Richter WF, Whitby BR, Chou RC: Distribution of remikiren, a potent orally active inhibitor of human renin, in laboratory animals. Xenobiotica. 1996 Mar;26(3):243-54. [PubMed:8730917 ]
External Links
ATC CodesC09XA01
AHFS CodesNot Available
PDB Entries
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.8744
Blood Brain Barrier-0.8746
Caco-2 permeable-0.8957
P-glycoprotein substrateSubstrate0.7043
P-glycoprotein inhibitor INon-inhibitor0.6427
P-glycoprotein inhibitor IINon-inhibitor0.9732
Renal organic cation transporterNon-inhibitor0.8832
CYP450 2C9 substrateNon-substrate0.5243
CYP450 2D6 substrateNon-substrate0.7775
CYP450 3A4 substrateSubstrate0.5695
CYP450 1A2 substrateNon-inhibitor0.8245
CYP450 2C9 inhibitorNon-inhibitor0.6456
CYP450 2D6 inhibitorNon-inhibitor0.8548
CYP450 2C19 inhibitorNon-inhibitor0.6534
CYP450 3A4 inhibitorInhibitor0.8648
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6298
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.7601
BiodegradationNot ready biodegradable0.9754
Rat acute toxicity2.5600 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9958
hERG inhibition (predictor II)Non-inhibitor0.5881
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP3.9Not Available
Caco2 permeability-6.13ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.0128 mg/mLALOGPS
logP3.56ALOGPS
logP3.22ChemAxon
logS-4.7ALOGPS
pKa (Strongest Acidic)5.47ChemAxon
pKa (Strongest Basic)6.49ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count9ChemAxon
Hydrogen Donor Count5ChemAxon
Polar Surface Area168.46 Å2ChemAxon
Rotatable Bond Count16ChemAxon
Refractivity170.64 m3·mol-1ChemAxon
Polarizability68.82 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzene and substituted derivatives. These are aromatic compounds containing one monocyclic ring system consisting of benzene.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassNot Available
Direct ParentBenzene and substituted derivatives
Alternative Parents
Substituents
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Sulfonyl
  • Sulfone
  • Imidazole
  • Azole
  • Secondary alcohol
  • 1,2-diol
  • Azacycle
  • Organoheterocyclic compound
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Carboximidic acid derivative
  • Carboximidic acid
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Alcohol
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Receptor binding
Specific Function:
Renin is a highly specific endopeptidase, whose only known function is to generate angiotensin I from angiotensinogen in the plasma, initiating a cascade of reactions that produce an elevation of blood pressure and increased sodium retention by the kidney.
Gene Name:
REN
Uniprot ID:
P00797
Molecular Weight:
45057.125 Da
References
  1. van Paassen P, Navis GJ, De Jong PE, De Zeeuw D: Pretreatment renal vascular tone predicts the effect of specific renin inhibition on natriuresis in essential hypertension. Eur J Clin Invest. 1999 Dec;29(12):1019-26. [PubMed:10583449 ]
  2. MacFadyen RJ, Jones CR, Doig JK, Birnbock H, Reid JL: Responses to an orally active renin inhibitor, remikiren (Ro 42-5892), after controlled salt depletion in humans. J Cardiovasc Pharmacol. 1995 Mar;25(3):347-53. [PubMed:7769797 ]
  3. Kiowski W, Beermann J, Rickenbacher P, Haemmerli R, Thomas M, Burkart F, Meinertz T: Angiotensinergic versus nonangiotensinergic hemodynamic effects of converting enzyme inhibition in patients with chronic heart failure. Assessment by acute renin and converting enzyme inhibition. Circulation. 1994 Dec;90(6):2748-56. [PubMed:7994817 ]
  4. Hilgers KF, Fischli W, Veelken R, Mann JF: Vascular renin in the guinea pig. Suppression by the renin inhibitor remikiren. Hypertension. 1994 Jun;23(6 Pt 2):861-4. [PubMed:8206619 ]
  5. Clozel JP, Fischli W: Comparative effects of three different potent renin inhibitors in primates. Hypertension. 1993 Jul;22(1):9-17. [PubMed:8319997 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23