Identification

Name
Remikiren
Accession Number
DB00212  (APRD00163)
Type
Small Molecule
Groups
Approved
Description

Remikiren is an orally active, high specificity renin inhibitor.

Structure
Thumb
Synonyms
Not Available
External IDs
Ro 42-5892 / RO-42-5892
Categories
UNII
LC7FBL96A4
CAS number
126222-34-2
Weight
Average: 630.838
Monoisotopic: 630.345106042
Chemical Formula
C33H50N4O6S
InChI Key
UXIGZRQVLGFTOU-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

Indication

For the treatment of hypertension and heart failure

Pharmacodynamics

Remikiren 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 action

Several in vivo experiments have shown that remikiren is specific for renin and does not decrease arterial pressure by an unrelated mechanism.

TargetActionsOrganism
ARenin
inhibitor
Human
Absorption

Absorbed following oral administration.

Volume of distribution
Not Available
Protein binding

83%

Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not 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, Investigational
AcemetacinThe therapeutic efficacy of Remikiren can be decreased when used in combination with Acemetacin.Approved, Experimental, Investigational
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, Investigational
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
AmitriptylinoxideThe serum concentration of Amitriptylinoxide can be increased when it is combined with Remikiren.Approved, Investigational
AmlodipineRemikiren may increase the hypotensive activities of Amlodipine.Approved
AmoxapineThe serum concentration of Amoxapine can be increased when it is combined with Remikiren.Approved
AmphetamineAmphetamine may increase the hypotensive activities of Remikiren.Approved, Illicit, Investigational
AtenololRemikiren may increase the hypotensive activities of Atenolol.Approved
AvanafilAvanafil may increase the antihypertensive activities of Remikiren.Approved
BarnidipineRemikiren may increase the antihypertensive activities of Barnidipine.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, Investigational
BethanidineBethanidine may increase the hypotensive activities of Remikiren.Approved
BietaserpineBietaserpine may increase the hypotensive activities of Remikiren.Experimental
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, Withdrawn
BosentanBosentan may increase the hypotensive activities of Remikiren.Approved, Investigational
BQ-123Remikiren may increase the hypotensive activities of BQ-123.Investigational
BretyliumRemikiren may increase the hypotensive activities of Bretylium.Approved
BrimonidineBrimonidine may increase the antihypertensive activities of Remikiren.Approved
BrofaromineBrofaromine may increase the hypotensive activities of Remikiren.Experimental
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
ButriptylineThe serum concentration of Butriptyline can be increased when it is combined with Remikiren.Approved
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Remikiren.Approved
CadralazineCadralazine may increase the hypotensive activities of Remikiren.Experimental
CafedrineRemikiren may increase the hypotensive activities of Cafedrine.Investigational
CandesartanRemikiren may increase the hypotensive activities of Candesartan.Experimental
Candesartan cilexetilRemikiren may increase the hypotensive activities of Candesartan cilexetil.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
ChlorthalidoneRemikiren may increase the hypotensive activities of Chlorthalidone.Approved
CicletanineRemikiren may increase the hypotensive activities of Cicletanine.Investigational
CilazaprilRemikiren may increase the hypotensive activities of Cilazapril.Approved
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, Investigational, Vet Approved
ClonidineClonidine may increase the hypotensive activities of Remikiren.Approved
CloranololRemikiren may increase the hypotensive activities of Cloranolol.Experimental
CryptenamineRemikiren may increase the hypotensive activities of Cryptenamine.Approved
CyclopenthiazideRemikiren may increase the hypotensive activities of Cyclopenthiazide.Experimental
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
DebrisoquinDebrisoquin may increase the hypotensive activities of Remikiren.Approved, Investigational
DelaprilRemikiren may increase the hypotensive activities of Delapril.Investigational
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, Investigational
DiazoxideDiazoxide may increase the hypotensive activities of Remikiren.Approved
DibenzepinThe serum concentration of Dibenzepin can be increased when it is combined with Remikiren.Experimental
DiethylnorspermineRemikiren may increase the hypotensive activities of Diethylnorspermine.Investigational
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Remikiren.Approved, Investigational
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Remikiren.Approved
DihydralazineDihydralazine may increase the hypotensive activities of Remikiren.Approved, Investigational
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Remikiren.Approved, Investigational
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Remikiren.Approved, Investigational
DimetacrineThe serum concentration of Dimetacrine can be increased when it is combined with Remikiren.Approved, Withdrawn
DipyridamoleDipyridamole may increase the antihypertensive activities of 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
DoxazosinDoxazosin may increase the hypotensive activities of Remikiren.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Remikiren.Approved, Investigational
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Remikiren.Approved
EfonidipineRemikiren may increase the hypotensive activities of Efonidipine.Approved, Investigational
EnalaprilRemikiren may increase the hypotensive activities of Enalapril.Approved, Vet Approved
EnalaprilatRemikiren may increase the hypotensive activities of Enalaprilat.Approved
EndralazineEndralazine may increase the hypotensive activities of Remikiren.Experimental
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Remikiren.Approved, Investigational
EpanololRemikiren may increase the hypotensive activities of Epanolol.Experimental
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
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Remikiren.Approved, Investigational, Vet Approved
Estradiol cypionateThe serum concentration of Estradiol cypionate can be decreased when it is combined with Remikiren.Approved, Investigational, Vet Approved
Estradiol valerateThe serum concentration of Estradiol valerate can be decreased when it is combined with Remikiren.Approved, Investigational, Vet 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
Ferulic acidRemikiren may increase the hypotensive activities of Ferulic acid.Experimental
FosinoprilRemikiren may increase the hypotensive activities of Fosinopril.Approved
FostamatinibFostamatinib may increase the antihypertensive activities of Remikiren.Approved, Investigational
FurazolidoneFurazolidone may increase the hypotensive activities of Remikiren.Approved, Investigational, Vet Approved
GarlicThe serum concentration of Remikiren can be decreased when it is combined with Garlic.Approved, Nutraceutical
GuanabenzRemikiren may increase the hypotensive activities of Guanabenz.Approved, Investigational
GuanadrelRemikiren may increase the hypotensive activities of Guanadrel.Approved
GuanazodineRemikiren may increase the hypotensive activities of Guanazodine.Experimental
GuanethidineRemikiren may increase the hypotensive activities of Guanethidine.Approved
GuanfacineGuanfacine may increase the hypotensive activities of Remikiren.Approved, Investigational
GuanoclorRemikiren may increase the hypotensive activities of Guanoclor.Experimental
GuanoxabenzRemikiren may increase the hypotensive activities of Guanoxabenz.Experimental
GuanoxanRemikiren may increase the hypotensive activities of Guanoxan.Experimental
HarmalineHarmaline may increase the hypotensive activities of Remikiren.Experimental
HexamethoniumRemikiren may increase the hypotensive activities of Hexamethonium.Experimental
HydracarbazineHydracarbazine may increase the hypotensive activities of Remikiren.Experimental
HydralazineHydralazine may increase the hypotensive activities of Remikiren.Approved
HydrochlorothiazideRemikiren may increase the hypotensive activities of Hydrochlorothiazide.Approved, Vet Approved
HydroflumethiazideRemikiren may increase the hypotensive activities of Hydroflumethiazide.Approved, Investigational
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
IndoraminIndoramin may increase the hypotensive activities of Remikiren.Withdrawn
IprindoleThe serum concentration of Iprindole can be increased when it is combined with Remikiren.Experimental
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, Investigational
KetanserinKetanserin may increase the hypotensive activities of Remikiren.Investigational
LabetalolRemikiren may increase the hypotensive activities of Labetalol.Approved
LacidipineRemikiren may increase the hypotensive activities of Lacidipine.Approved, Investigational
LatanoprostRemikiren may increase the hypotensive activities of Latanoprost.Approved, Investigational
LercanidipineRemikiren may increase the hypotensive activities of Lercanidipine.Approved, Investigational
LinsidomineRemikiren may increase the hypotensive activities of Linsidomine.Experimental
LisinoprilRemikiren may increase the hypotensive activities of Lisinopril.Approved, Investigational
LofepramineThe serum concentration of Lofepramine can be increased when it is combined with Remikiren.Experimental
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, Investigational
MebanazineMebanazine may increase the hypotensive activities of Remikiren.Withdrawn
MecamylamineMecamylamine may increase the hypotensive activities of Remikiren.Approved, Investigational
MelitracenThe serum concentration of Melitracen can be increased when it is combined with Remikiren.Experimental, Investigational
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Remikiren.Approved
MethoserpidineRemikiren may increase the hypotensive activities of Methoserpidine.Experimental
MethyldopaRemikiren may increase the hypotensive activities of Methyldopa.Approved
Methylene blueMethylene blue may increase the hypotensive activities of Remikiren.Approved, Investigational
MethylergometrineThe serum concentration of Methylergometrine can be increased when it is combined with Remikiren.Approved
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.Investigational, 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
MinoxidilMinoxidil may increase the hypotensive activities of Remikiren.Approved, Investigational
MirodenafilMirodenafil may increase the antihypertensive activities of Remikiren.Investigational
MoclobemideMoclobemide may increase the hypotensive activities of Remikiren.Approved, Investigational
MoexiprilRemikiren may increase the hypotensive activities of Moexipril.Approved
MolsidomineMolsidomine may increase the hypotensive activities of Remikiren.Approved, Investigational
MoxonidineMoxonidine may increase the hypotensive activities of Remikiren.Approved, Investigational
MuzolimineRemikiren may increase the hypotensive activities of Muzolimine.Experimental
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, Investigational
NicorandilRemikiren may increase the hypotensive activities of Nicorandil.Approved, Investigational
NiguldipineRemikiren may increase the hypotensive activities of Niguldipine.Experimental
NilvadipineRemikiren may increase the hypotensive activities of Nilvadipine.Approved, Investigational
NimodipineRemikiren may increase the hypotensive activities of Nimodipine.Approved, Investigational
NisoldipineRemikiren may increase the hypotensive activities of Nisoldipine.Approved
NitrendipineRemikiren may increase the hypotensive activities of Nitrendipine.Approved, Investigational
NitroprussideNitroprusside may increase the hypotensive activities of Remikiren.Approved, Investigational
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Remikiren.Approved
ObinutuzumabRemikiren may increase the hypotensive activities of Obinutuzumab.Approved, Investigational
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
PinacidilPinacidil may increase the hypotensive activities of Remikiren.Approved
PindololRemikiren may increase the hypotensive activities of Pindolol.Approved, Investigational
PirlindolePirlindole may increase the hypotensive activities of Remikiren.Approved
PivhydrazinePivhydrazine may increase the hypotensive activities of Remikiren.Withdrawn
Platelet Activating FactorRemikiren may increase the hypotensive activities of Platelet Activating Factor.Experimental
PolythiazideRemikiren may increase the hypotensive activities of Polythiazide.Approved
PrazosinPrazosin may increase the hypotensive activities of Remikiren.Approved
ProcaineProcaine may increase the hypotensive activities of Remikiren.Approved, Investigational, Vet Approved
ProcarbazineProcarbazine may increase the hypotensive activities of Remikiren.Approved, Investigational
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, Investigational
RilmenidineRilmenidine may increase the hypotensive activities of Remikiren.Approved, 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
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
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.Approved, Investigational, Nutraceutical
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Remikiren.Approved, Investigational
TadalafilTadalafil may increase the antihypertensive activities of Remikiren.Approved, Investigational
TalinololRemikiren may increase the hypotensive activities of Talinolol.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
TetrahydropalmatineRemikiren may increase the hypotensive activities of Tetrahydropalmatine.Investigational
TheodrenalineRemikiren may increase the hypotensive activities of Theodrenaline.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, Investigational
TiboloneRemikiren may increase the hypotensive activities of Tibolone.Approved, Investigational
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
TolonidineRemikiren may increase the hypotensive activities of Tolonidine.Experimental
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
TranylcypromineTranylcypromine may increase the hypotensive activities of Remikiren.Approved, Investigational
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, Investigational
TrichlormethiazideRemikiren may increase the hypotensive activities of Trichlormethiazide.Approved, Vet Approved
TrimazosinTrimazosin may increase the hypotensive activities of Remikiren.Experimental
TrimethaphanTrimethaphan may increase the hypotensive activities of Remikiren.Approved, Investigational
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, Investigational
UrapidilUrapidil may increase the hypotensive activities of Remikiren.Investigational
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
VincamineRemikiren may increase the hypotensive activities of Vincamine.Experimental
VinpocetineRemikiren may increase the hypotensive activities of Vinpocetine.Investigational
XipamideRemikiren may increase the hypotensive activities of Xipamide.Experimental
XylometazolineRemikiren may increase the hypotensive activities of Xylometazoline.Approved, Investigational
YohimbineYohimbine may decrease the antihypertensive activities of Remikiren.Approved, Investigational, Vet Approved
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Remikiren.Approved
ZofenoprilRemikiren may increase the hypotensive activities of Zofenopril.Experimental
Food Interactions
Not Available

References

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
KEGG Compound
C07465
PubChem Compound
6324659
PubChem Substance
46507286
ChemSpider
4884377
BindingDB
50077669
ChEMBL
CHEMBL31601
Therapeutic Targets Database
DAP001220
PharmGKB
PA164774779
HET
REM
Wikipedia
Remikiren
ATC Codes
C09XA01 — Remikiren
PDB Entries
3d91

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
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 FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as histidine and derivatives. These are compounds containing cysteine or a derivative thereof resulting from reaction of cysteine at the amino group or the carboxy group, or from the replacement of any hydrogen of glycine by a heteroatom.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Carboxylic acids and derivatives
Sub Class
Amino acids, peptides, and analogues
Direct Parent
Histidine and derivatives
Alternative Parents
N-acyl-alpha amino acids and derivatives / Alpha amino acid amides / Benzene and substituted derivatives / Fatty amides / Sulfones / Imidazoles / Heteroaromatic compounds / Secondary carboxylic acid amides / Secondary alcohols / 1,2-diols
show 6 more
Substituents
Histidine or derivatives / N-acyl-alpha amino acid or derivatives / Alpha-amino acid amide / Monocyclic benzene moiety / Fatty amide / Fatty acyl / Benzenoid / Azole / Imidazole / Heteroaromatic compound
show 19 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
Not 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 b...
Gene Name
REN
Uniprot ID
P00797
Uniprot Name
Renin
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]

Drug created on June 13, 2005 07:24 / Updated on July 02, 2018 17:15