A database of FDA approved therapeutic peptides and proteins
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1649 details |
Primary information | |
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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 | N.A. |
Target | Renin |
Information of corresponding available drug in the market | |
Brand Name | Tekturna |
Company | Novartis Pharmaceuticals Corporation |
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 150 mg of aliskiren, and as a light-red biconvex ovaloid tablet containing 300 mg of aliskiren. |
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 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. |
Contraindication | None |
Side Effects | Hives; vomiting, severe stomach pain; dizziness, diarrhea, difficult breathing; swelling of your face, lips, tongue, or throat. |
Useful Link | http://search.medscape.com/reference-search?newSearchHeader=1&queryText=aliskiren |
PubMed ID | 12927775 |
3-D Structure | N.A. |