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1648 details

Primary information
ThPP ID	Th1148
Therapeutic Peptide/Protein Name	Aliskiren
Sequence	N.A. view full sequnce in fasta
Functional Classification	IIa
Molecular Weight	551.75832
Chemical Formula	C30H53N3O6
Isoelectric Point	N.A.
Hydrophobicity	N.A.
Melting Point (℃)	N.A.
Half Life	24 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/Disease	It is used to treat hypertension, renal impairment and hepatic impairment
Pharmacodynamics	Aliskiren 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 Action	Renin 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.
Toxicity	It can cause injury and death to the developing fetus
Metabolism	Metabolized by CYP3A4
Absorption	Poorly absorbed; oral bioavailability is about 2.5%.
Volume of Distribution	N.A.
Clearance	Urine (25% as parent compound in urine)Â
Categories	Renin inhibitor
Patents Number	N.A.
Date of Issue	N.A.
Date of Expiry	N.A.
Drug Interaction	Cyclosporine, Itraconazole: Avoid concomitant use
Target	Renin
Information of corresponding available drug in the market
Brand Name	Tekturna
Company	Physicians Total Care, Inc.
Brand Discription	Tekturna 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 for	This 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
Formulation	Tekturna is supplied as a light-pink, biconvex round tablet containing 150Â mg of aliskiren, and as a light-red biconvex ovaloid tablet containing 300Â mg of aliskiren.Â
Physcial Appearnce	150Â mg light pink biconvex round tablet, imprinted NVR/IL, 300 mg light red biconvex ovaloid round tablet, imprinted NVR/IU
Route of Administration	Oral route
Recommended Dosage	The usual recommended starting dose of Tekturna is 150Â mg once daily.Â In patients whose blood pressure is not adequately controlled, the daily dose may be increased to 300Â mg. The antihypertensive effect of a given dose is substantially attained (85-90%) by 2 weeks.
Contraindication	None
Side Effects	Hives; vomiting, severe stomach pain; dizziness, diarrhea, difficult breathing; swelling of your face, lips, tongue, or throat.
Useful Link	http://www.drugs.com/mtm/aliskiren.html
PubMed ID	12927775
3-D Structure	N.A.