==== 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.====

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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 InteractionSome products that may interact with this drug include: cisapride, dofetilide, lithium, drugs that may increase the level of potassium in the blood (including ACE inhibitors such as benazepril/lisinopril, ARBs such as candesartan/losartan, birth control pills containing drospirenone).
TargetRenin
Information of corresponding available drug in the market
Brand NameTekturna HCT
CompanyNovartis Pharmaceuticals Corporation
Brand DiscriptionTekturna HCT is indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. 
Prescribed forThis product is used to treat high blood pressure (hypertension). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. This product contains 2 medications: aliskiren and hydrochlorothiazide. Aliskiren works by relaxing blood vessels so blood can flow more easily. It belongs to a class of drugs known as direct renin inhibitors. Hydrochlorothiazide causes your body to get rid of extra salt and water by making more urine. It is called a water pill or diuretic.
Chemical NameN.A.
FormulationTekturna HCT is supplied as biconvex, ovaloid film-coated tablets.
Physcial Appearnce150 mg/12.5 mg tablets: white, biconvex ovaloid, film-coated tablets imprinted with NVR/LCI, 150 mg/25 mg tablets: pale yellow, biconvex ovaloid, film-coated tablets imprinted with NVR/CLL, 300 mg/12.5 mg tablets: violet white, biconvex ovaloid, film-coated tablets imprinted with NVR/CVI, 300 mg/2
Route of AdministrationOral route
Recommended Dosage Initiate with 12.5 mg/150 mg PO qDay; after 2-4 weeks, may increase dose if needed; not to exceed 25 mg/300 mg
ContraindicationDo not use aliskiren with ARBs or ACEIs in patients with diabetes. Tekturna HCT is contraindicated in patients with anuria or hypersensitivity to sulfonamide derived drugs like HCTZ or to any of the components. Hypersensitivity reactions may range from urticaria to anaphylaxis.
Side EffectsDizziness or lightheadedness may occur as your body adjusts to the medication. If either of these effects persists or worsens, tell your doctor or pharmacist promptly.
Useful Linkhttp://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=Aliskiren
PubMed ID12927775
3-D StructureN.A.