==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

Detailed description page of THPdb

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1649 details
Primary information
ThPP IDTh1148
Therapeutic Peptide/Protein NameAliskiren
SequenceN.A. view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight551.75832
Chemical FormulaC30H53N3O6
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half Life24 hours
Description Aliskiren is an anti-hypertensive (blood pressure lowering) medicine. It works by decreasing substances in the body that narrow blood vessels and raise blood pressure. It is chemically, (2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methyl-2-propan-2-ylnonanamide.
Indication/DiseaseIt is used to treat hypertension, renal impairment and hepatic impairment
PharmacodynamicsAliskiren shows high specificity for human renin, with almost no inhibitory effect against other aspartic peptidases such as cathepsin D and pepsin. Although aliskiren also exhibits high affinity for primate renin, it is significantly less active against renin from dog, rat, rabbit, pig and cat. This high potency for human renin compensates for the relatively low oral bioavailability of the drug.
Mechanism of ActionRenin inhibitor that inhibits the conversion of angiotensinogen to angiotensin I. The decrease in antiotensin I causes a decrease in angiotensin II, a potent blood pressure elevating peptide.
ToxicityIt can cause injury and death to the developing fetus
MetabolismMetabolized by CYP3A4
AbsorptionPoorly absorbed; oral bioavailability is about 2.5%.
Volume of DistributionN.A.
ClearanceUrine (25% as parent compound in urine) 
CategoriesRenin inhibitor
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetRenin
Information of corresponding available drug in the market
Brand NameTekturna
CompanyNovartis Pharmaceuticals Corporation
Brand DiscriptionTekturna contains aliskiren hemifumarate, a renin inhibitor, that is provided as tablets for oral administration. Aliskiren hemifumarate is chemically described as (2S,4S,5S,7S)-N-(2-carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3-methoxypropoxy)phenyl]-octanamide hemifumarate. Aliskiren hemifumarate is a white to slightly yellowish crystalline powder with a molecular weight of 609.8. It is soluble in phosphate buffer, n-octanol, and highly soluble in water.
Prescribed forThis medication is used to treat high blood pressure (hypertension). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Aliskiren works by relaxing blood vessels so blood can flow more easily. It belongs to a class of drugs known as direct renin inhibitors.
Chemical Name(2S,4S,5S,7S)-N-(2-carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3-methoxypropoxy)phenyl]-octanamide hemifumarate
FormulationTekturna is supplied as a light-pink, biconvex round tablet containing 150 mg of aliskiren, and as a light-red biconvex ovaloid tablet containing 300 mg of aliskiren. 
Physcial Appearnce150 mg light pink biconvex round tablet, imprinted NVR/IL, 300 mg light red biconvex ovaloid round tablet, imprinted NVR/IU
Route of AdministrationOral route
Recommended DosageThe usual recommended starting dose of Tekturna is 150 mg once daily. In patients whose blood pressure is not adequately controlled, the daily dose may be increased to 300 mg. The antihypertensive effect of a given dose is substantially attained (85-90%) by 2 weeks.
ContraindicationNone
Side EffectsHives; vomiting, severe stomach pain; dizziness, diarrhea, difficult breathing; swelling of your face, lips, tongue, or throat.
Useful Linkhttp://search.medscape.com/reference-search?newSearchHeader=1&queryText=aliskiren
PubMed ID12927775
3-D StructureN.A.