Detailed description page of THPdb

Details of Th1148 which contains 5 entries.

Entry 1
(1) Primary information
ID 1648
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 Appearance 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.

Entry 2
(2) Primary information
ID 1649
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 150Â mg of aliskiren, and as a light-red biconvex ovaloid tablet containing 300Â mg of aliskiren.Â
Physcial Appearance 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://search.medscape.com/reference-search?newSearchHeader=1&queryText=aliskiren
PubMed ID 12927775
3-D Structure N.A.

Entry 3
(3) Primary information
ID 1650
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 Some 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).
Target Renin
Information of corresponding available drug in the market
Brand Name Tekturna HCT
Company Novartis Pharmaceuticals Corporation
Brand Discription Tekturna 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.Â
Prescribed for This 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 Name N.A.
Formulation TekturnaÂ HCT is supplied asÂ biconvex, ovaloid film-coated tablets.
Physcial Appearance 150Â mg/12.5Â 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 Administration Oral route
Recommended Dosage Â 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
Contraindication Do 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 Effects Dizziness 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 Link http://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=Aliskiren
PubMed ID 12927775
3-D Structure N.A.

Entry 4
(4) Primary information
ID 1651
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 Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): Increased risk of renal impairment and loss of antihypertensive effect, Simvastatin: Avoid doses greater than 20 mg daily. Â
Target Renin
Information of corresponding available drug in the market
Brand Name Tekamlo
Company Novartis Pharmaceuticals Corporation
Brand Discription Aliskiren: Renin inhibitor; blocks effect of increased renin levels, thereby decreasing feedback loop and reducing plasma renin activity, angiotensin I, and angiotensin II. Amlodipine: Calcium channel blocker; inhibits extracellular Ca ions across the membranes of myocardial cells and vascular smooth muscle cells, resulting in inhibition of cardiac and vascular smooth muscle contraction; this action causes dilation of the main coronary and systemic arteries.
Prescribed for TekamloÂ is a combination of aliskiren, a renin inhibitor, and amlodipine, a dihydropyridine calcium channel blocker, indicated for the treatment of hypertension, alone or with other antihypertensive agents, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.
Chemical Name N.A.
Formulation Tablets (aliskiren/amlodipine): 150 mg/5 mg, 150 mg/10 mg, 300 mg/5 mg, 300 mg/10 mg
Physcial Appearance 150 mg aliskiren/5Â mg amlodipine tablets: Non-scored light yellow, ovaloid convex shaped film-coated tablet with a beveled edgeÂ with debossing â€œT2â€ on one side and â€œNVRâ€ on the reverse side of the tablet, 150 mg aliskiren/10 mg amlodipine tablets: Non-scored yellow, ovaloid convex shaped f
Route of Administration Oral route
Recommended Dosage The recommended initial once-daily dose of Tekamlo is 150 mg/5 mg. Titrate as needed to a maximum of 300 mg/10 mg. The blood pressure lowering effects are largely attained within 1 to 2 weeks. If blood pressure remains uncontrolled after 2 to 4 weeks of therapy, titrate the dose to a maximum of Tekamlo 300 mg/10 mg once daily.
Contraindication Do not use with angiotensin receptor blockers (ARBs) or angiotensin-converting enzyme inhibitors (ACEIs) in patients with diabetes. Known hypersensitivity to any of the components.
Side Effects Swelling of lower legs, diarrhea,dizziness, cough, flu-like symptoms, tiredness, high levels of potassium in the blood (hyperkalemia)
Useful Link http://www.drugbank.ca/drugs/DB09026
PubMed ID 12927775
3-D Structure N.A.

Entry 5
(5) Primary information
ID 1652
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 Antidiabetic Drugs: Antidiabetic dosage adjustment may be required
Target Renin
Information of corresponding available drug in the market
Brand Name Amturnide
Company Novartis Pharmaceuticals Corporation
Brand Discription Amturnide is a combination of aliskiren, a renin inhibitor, amlodipine besylate, a dihydropyridine calcium channel blocker, and hydrochlorothiazide (HCTZ), a thiazide diuretic.Â
Prescribed for Amturnide 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.Â
Chemical Name N.A.
Formulation Tablets (aliskiren/ amlodipine/ HCTZ): 150/5/12.5,Â 300/5/12.5,Â 300/5/25, 300/10/12.5, 300/10/25 mg.Â
Physcial Appearance Tablets are convex ovaloid with a beveled edge, film-coated, and unscored.
Route of Administration Oral route
Recommended Dosage Dose once-daily.Â The dosage may be increased after 2Â weeks of therapy.Â The maximum recommended dose of Amturnide is 300/10/25 mg. High-fat meals decrease absorption of aliskiren substantially.
Contraindication Do not use with angiotensin receptor blockers (ARBs) or angiotensin-converting enzyme inhibitors (ACEIs) in patients with diabetes, Anuria, Hypersensitivity to sulfonamide derived drugs or to any of the components.
Side Effects Dizziness or lightheadedness as your body adjusts to the medication. Swelling hands/ankles/feet, flushing, headache, or diarrhea may also occur.
Useful Link http://pubchem.ncbi.nlm.nih.gov/compound/Aliskiren#section=FDA-Pharmacological-Classification
PubMed ID 12927775
3-D Structure N.A.

OSDDlinux

Raghava's Group

IMTECH

CSIR

CRDD
CPPSITE 2.0

(1) Primary information
Entry 1
ID	1648
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 Appearance	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.

(2) Primary information
Entry 2
ID	1649
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 150Â mg of aliskiren, and as a light-red biconvex ovaloid tablet containing 300Â mg of aliskiren.Â
Physcial Appearance	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://search.medscape.com/reference-search?newSearchHeader=1&queryText=aliskiren
PubMed ID	12927775
3-D Structure	N.A.

(3) Primary information
Entry 3
ID	1650
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	Some 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).
Target	Renin
Information of corresponding available drug in the market
Brand Name	Tekturna HCT
Company	Novartis Pharmaceuticals Corporation
Brand Discription	Tekturna 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.Â
Prescribed for	This 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 Name	N.A.
Formulation	TekturnaÂ HCT is supplied asÂ biconvex, ovaloid film-coated tablets.
Physcial Appearance	150Â mg/12.5Â 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 Administration	Oral route
Recommended Dosage	Â 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
Contraindication	Do 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 Effects	Dizziness 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 Link	http://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=Aliskiren
PubMed ID	12927775
3-D Structure	N.A.

(4) Primary information
Entry 4
ID	1651
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	Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): Increased risk of renal impairment and loss of antihypertensive effect, Simvastatin: Avoid doses greater than 20 mg daily. Â
Target	Renin
Information of corresponding available drug in the market
Brand Name	Tekamlo
Company	Novartis Pharmaceuticals Corporation
Brand Discription	Aliskiren: Renin inhibitor; blocks effect of increased renin levels, thereby decreasing feedback loop and reducing plasma renin activity, angiotensin I, and angiotensin II. Amlodipine: Calcium channel blocker; inhibits extracellular Ca ions across the membranes of myocardial cells and vascular smooth muscle cells, resulting in inhibition of cardiac and vascular smooth muscle contraction; this action causes dilation of the main coronary and systemic arteries.
Prescribed for	TekamloÂ is a combination of aliskiren, a renin inhibitor, and amlodipine, a dihydropyridine calcium channel blocker, indicated for the treatment of hypertension, alone or with other antihypertensive agents, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.
Chemical Name	N.A.
Formulation	Tablets (aliskiren/amlodipine): 150 mg/5 mg, 150 mg/10 mg, 300 mg/5 mg, 300 mg/10 mg
Physcial Appearance	150 mg aliskiren/5Â mg amlodipine tablets: Non-scored light yellow, ovaloid convex shaped film-coated tablet with a beveled edgeÂ with debossing â€œT2â€ on one side and â€œNVRâ€ on the reverse side of the tablet, 150 mg aliskiren/10 mg amlodipine tablets: Non-scored yellow, ovaloid convex shaped f
Route of Administration	Oral route
Recommended Dosage	The recommended initial once-daily dose of Tekamlo is 150 mg/5 mg. Titrate as needed to a maximum of 300 mg/10 mg. The blood pressure lowering effects are largely attained within 1 to 2 weeks. If blood pressure remains uncontrolled after 2 to 4 weeks of therapy, titrate the dose to a maximum of Tekamlo 300 mg/10 mg once daily.
Contraindication	Do not use with angiotensin receptor blockers (ARBs) or angiotensin-converting enzyme inhibitors (ACEIs) in patients with diabetes. Known hypersensitivity to any of the components.
Side Effects	Swelling of lower legs, diarrhea,dizziness, cough, flu-like symptoms, tiredness, high levels of potassium in the blood (hyperkalemia)
Useful Link	http://www.drugbank.ca/drugs/DB09026
PubMed ID	12927775
3-D Structure	N.A.

(5) Primary information
Entry 5
ID	1652
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	Antidiabetic Drugs: Antidiabetic dosage adjustment may be required
Target	Renin
Information of corresponding available drug in the market
Brand Name	Amturnide
Company	Novartis Pharmaceuticals Corporation
Brand Discription	Amturnide is a combination of aliskiren, a renin inhibitor, amlodipine besylate, a dihydropyridine calcium channel blocker, and hydrochlorothiazide (HCTZ), a thiazide diuretic.Â
Prescribed for	Amturnide 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.Â
Chemical Name	N.A.
Formulation	Tablets (aliskiren/ amlodipine/ HCTZ): 150/5/12.5,Â 300/5/12.5,Â 300/5/25, 300/10/12.5, 300/10/25 mg.Â
Physcial Appearance	Tablets are convex ovaloid with a beveled edge, film-coated, and unscored.
Route of Administration	Oral route
Recommended Dosage	Dose once-daily.Â The dosage may be increased after 2Â weeks of therapy.Â The maximum recommended dose of Amturnide is 300/10/25 mg. High-fat meals decrease absorption of aliskiren substantially.
Contraindication	Do not use with angiotensin receptor blockers (ARBs) or angiotensin-converting enzyme inhibitors (ACEIs) in patients with diabetes, Anuria, Hypersensitivity to sulfonamide derived drugs or to any of the components.
Side Effects	Dizziness or lightheadedness as your body adjusts to the medication. Swelling hands/ankles/feet, flushing, headache, or diarrhea may also occur.
Useful Link	http://pubchem.ncbi.nlm.nih.gov/compound/Aliskiren#section=FDA-Pharmacological-Classification
PubMed ID	12927775
3-D Structure	N.A.