Aliskiren

Synopsis, Chemistry

APIs // Active Pharmaceutical Ingredients

8 API Suppliers, 4 USDMF, 3 EU WC, 3 NDC API, 4 Listed Suppliers

PRICE INFORMATION

API Reference Price, API Exports, API Imports

INTERMEDIATES

5 Suppliers

5 Suppliers

DOSSIERs // Finished Dosage Formulations

22 Dossiers, 20 FDA Orange Book, 2 Europe

DRUG PRODUCT COMPOSITION

TABLET;ORAL - EQ 150MG BASE, TABLET;ORAL - EQ 300MG BASE, TABLET;ORAL - EQ 150MG BASE;12.5MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**, TABLET;ORAL - EQ 150MG BASE;25MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**, TABLET;ORAL - EQ 300MG BASE;12.5MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**, TABLET;ORAL - EQ 300MG BASE;25MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**

TABLET;ORAL - EQ 150MG BASE
TABLET;ORAL - EQ 300MG BASE
TABLET;ORAL - EQ 150MG BASE;12.5MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**
TABLET;ORAL - EQ 150MG BASE;25MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**
TABLET;ORAL - EQ 300MG BASE;12.5MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**
TABLET;ORAL - EQ 300MG BASE;25MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**

RELATED EXCIPIENT COMPANIES

Suppliers, 22 BASF, 16 Kerry, 10 Microlex e.U, 10 Roquette, 10 Corel Pharma Chem, 9 Sigachi Industries, 8 Gangwal Chemicals, 6 Anhui Sunhere Pharmaceutical Excipients Co.,Ltd, 6 Seppic, 6 Lonza Capsugel, 5 Gangwal Healthcare, 5 Boai NKY Pharmaceuticals Ltd, 5 Ideal Cures Pvt Ltd, 3 Shanghai Shenmei Pharmaceutical Technology Co., Ltd, 3 Actylis, 3 Pharmatrans-Sanaq, 3 Kima Chemical, 2 Ulanqab Kema New Material, 2 Vasa Pharmachem, 2 Nomisma Healthcare, 2 DFE Pharma, 2 Prachin Chemical, 2 Seqens, 2 The Dow Chemical Company, 1 Qianhao Chemical (Hebei) Co., Ltd, 1 ACG Worldwide, 1 Qualicaps, 1 DKSH, 1 Aeon Procare, 1 SPI Pharma, 1 Finar, 1 Alcedo Pharmachem

EXCIPIENTS BY APPLICATIONS

42 Coating Systems & Additives, 32 Fillers, Diluents & Binders, 28 Controlled & Modified Release, 22 Direct Compression, 21 Disintegrants & Superdisintegrants, 18 Thickeners and Stabilizers, 17 Granulation, 14 Solubilizers, 13 Lubricants & Glidants, 8 Film Formers & Plasticizers, 8 Co-Processed Excipients, 7 Topical, 6 Chewable & Orodispersible Aids, 5 Empty Capsules, 4 Vegetarian Capsules, 4 API Stability Enhancers, 4 Taste Masking, 4 Parenteral, 3 Emulsifying Agents, 2 Coloring Agents, 2 Rheology Modifiers

GLOBAL SALES INFORMATION

25 US Medicaid Prescriptions, 2 Finished Drug Prices

MARKET PLACE

1 APIs, 1 DOSSIERS // FDF

PATENTS

14 US Patents, 2 Health Canada Patents

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13 News

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API REF. PRICE (USD / KG)

9,349

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USA (Orange Book)

Europe

Canada

Australia

South Africa

Uploaded Dossiers

GLOBAL SALES (USD Million)

U.S. Medicaid

165.00

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EXCIPIENTS

152

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USFDA Orange Book Patents

USFDA Exclusivities

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Blog #PharmaFlow

News

REF STANDARD

EDQM

USP

Other Listed Suppliers

SERVICES

Also known as: 173334-58-2, Tekturna, Aliskiren fumarate, Aliskiren (hemifumarate), Enviage, Riprazo

Molecular Formula

C₆₄H₁₁₀N₆O₁₆

Molecular Weight

1219.6 g/mol

InChI Key

KLRSDBSKUSSCGU-KRQUFFFQSA-N

FDA UNII

C8A0P8G029

Aliskiren Hemifumarate is an orally active nonpeptide renin inhibitor with antihypertensive activity. Aliskiren selectively binds to the S3 sub-pocket of renin, an enzyme in the renin-angiotensin-aldosterone system (RAAS) that is responsible for converting angiotensinogen to angiotensin I (AT I). By inhibiting the activity of renin, the conversion to AT I is prevented, which in turn prevents the conversion of AT I to AT II. This prevents arterial vasoconstriction by AT II and inhibits the production of aldosterone by AT II. As aldosterone causes re-uptake of sodium and water and eventually an increase in extracellular volume, aliskiren is able to prevent the effects that contribute to an increase in blood pressure.

1 2D Structure

Aliskiren

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

(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;(E)-but-2-enedioic acid

2.1.2 InChI

InChI=1S/2C30H53N3O6.C4H4O4/c2*1-19(2)22(14-21-10-11-26(38-8)27(15-21)39-13-9-12-37-7)16-24(31)25(34)17-23(20(3)4)28(35)33-18-30(5,6)29(32)36;5-3(6)1-2-4(7)8/h2*10-11,15,19-20,22-25,34H,9,12-14,16-18,31H2,1-8H3,(H2,32,36)(H,33,35);1-2H,(H,5,6)(H,7,8)/b;;2-1+/t2*22-,23-,24-,25-;/m00./s1

2.1.3 InChI Key

KLRSDBSKUSSCGU-KRQUFFFQSA-N

2.1.4 Canonical SMILES

CC(C)C(CC1=CC(=C(C=C1)OC)OCCCOC)CC(C(CC(C(C)C)C(=O)NCC(C)(C)C(=O)N)O)N.CC(C)C(CC1=CC(=C(C=C1)OC)OCCCOC)CC(C(CC(C(C)C)C(=O)NCC(C)(C)C(=O)N)O)N.C(=CC(=O)O)C(=O)O

2.1.5 Isomeric SMILES

CC(C)[C@@H](CC1=CC(=C(C=C1)OC)OCCCOC)C[C@@H]([C@H](C[C@@H](C(C)C)C(=O)NCC(C)(C)C(=O)N)O)N.CC(C)[C@@H](CC1=CC(=C(C=C1)OC)OCCCOC)C[C@@H]([C@H](C[C@@H](C(C)C)C(=O)NCC(C)(C)C(=O)N)O)N.C(=C/C(=O)O)\C(=O)O

2.2 Other Identifiers

2.2.1 UNII

C8A0P8G029

2.3 Synonyms

2.3.1 MeSH Synonyms

1. 2(s),4(s),5(s),7(s)-n-(2-carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-(4-methoxy-3-(3-methoxypropoxy)phenyl)octanamid Hemifumarate

2. Aliskiren

3. Cgp 060536b

4. Cgp-060536b

5. Cgp060536b

6. Rasilez

7. Spp100

8. Tekturna

2.3.2 Depositor-Supplied Synonyms

1. 173334-58-2

2. Tekturna

3. Aliskiren Fumarate

4. Aliskiren (hemifumarate)

5. Enviage

6. Riprazo

7. Sprimeo

8. Spp-100b

9. Chebi:53777

10. C8a0p8g029

11. Nsc-759185

12. Cgp 60536

13. Aliskirenfumarate

14. (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;(e)-but-2-enedioic Acid

15. Cgp60536b

16. Bis(2s,4s,5s,7s)-5-amino-n-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-7-(4-methoxy-3-(3-methoxypropoxy)benzyl)-8-methyl-2-(1-methylethyl)nonanamide) (2e)-but-2-enedioate

17. Aliskiren Fumarate [usan]

18. Unii-c8a0p8g029

19. Aliskiren Fumarate [usan:jan]

20. Tekturna (tn)

21. Cgp-60536

22. Aliskiren Hemifumarate- Bio-x

23. Schembl187762

24. Aliskiren (as Fumarate)

25. Aliskiren Fumarate (jan/usan)

26. Aliskiren Fumarate [jan]

27. Chembl3545059

28. Cgp-60536b

29. Aliskiren Fumarate [mart.]

30. Aliskiren Hemifumarate [mi]

31. Aliskiren Fumarate [who-dd]

32. Mfcd10566724

33. S2199

34. Aliskiren Hemifumarate [vandf]

35. Akos015896419

36. Ccg-270658

37. Cs-0729

38. Ks-1395

39. Nsc 759185

40. S12129

41. (2s,4s,5s,7s)-5-amino-n-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-2-isopropyl-7-(4-methoxy-3-(3-methoxypropoxy)benzyl)-8-methylnonanamide Hemifumarate

42. Ba164146

43. Hy-12177

44. Aliskiren Hemifumarate [orange Book]

45. Sw222231-1

46. D06412

47. Rasitrio Component Aliskiren Hemifumarate

48. Tekamlo Component Aliskiren Hemifumarate

49. Valturna Component Aliskiren Hemifumarate

50. Amturnide Component Aliskiren Hemifumarate

51. Rasilamlo Component Aliskiren Hemifumarate

52. Aliskiren Hemifumarate Component Of Rasitrio

53. Aliskiren Hemifumarate Component Of Tekamlo

54. Aliskiren Hemifumarate Component Of Valturna

55. Raprazo-hct Component Aliskiren Hemifumarate

56. Rasilez-hct Component Aliskiren Hemifumarate

57. Sprimeo-hct Component Aliskiren Hemifumarate

58. Aliskiren Hemifumarate Component Of Amturnide

59. Aliskiren Hemifumarate Component Of Rasilamlo

60. Tekturna Hct Component Aliskiren Hemifumarate

61. Aliskiren Hemifumarate Component Of Raprazo-hct

62. Aliskiren Hemifumarate Component Of Rasilez-hct

63. Aliskiren Hemifumarate Component Of Sprimeo-hct

64. Q27124205

65. Aliskiren Hemifumarate Component Of Tekturna Hct

66. (?s,?s,?s,?s)-?-amino-n-(3-amino-2,2-dimethyl-3-oxopropyl)-?-hydroxy-4-methoxy-3-(3-methoxypropoxy)-?,?-bis(1-methylethyl)benzeneoctanamide Hemifumarate

67. 5-amino-n-(3-amino-2,2-dime-3-oxoprop)-4-oh-2-isoprop-7-[4-meo-3-(3-meo-propoxy)benzyl]-8-methylnonanamide Hemifumarate

68. Benzeneoctanamide, Delta-amino-n-(3-amino-2,2-dimethyl-3-oxopropyl)-gamma-hydroxy-4-methoxy-3-(3-methoxypropoxy)-alpha,zeta-bis(1-methylethyl)-, (alphas,gammas,deltas,zetas)-, (2e)-2-butenedioate (2:1) (salt)

69. Bis((2s,4s,5s,7s)-5-amino-n-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-2-isopropyl-7-(4-methoxy-3-(3-methoxypropoxy)benzyl)-8-methylnonanamide) Fumarate

70. Bis{(2s,4s,5s,7s)-5-amino-n-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-8-methyl-2-(propan-2-yl)nonanamide} (2e)-but-2-enedioate

2.4 Create Date

2006-07-28

3 Chemical and Physical Properties

Molecular Formula	C₆₄H₁₁₀N₆O₁₆
Molecular Weight	1219.6 g/mol
Hydrogen Bond Donor Count	10
Hydrogen Bond Acceptor Count	18
Rotatable Bond Count	40
Exact Mass	1218.79783144 g/mol
Monoisotopic Mass	1218.79783144 g/mol
Topological Polar Surface Area	367 Å²
Heavy Atom Count	86
Formal Charge	0
Complexity	836
Isotope Atom Count	0
Defined Atom Stereocenter Count	8
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	1
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	3

4 Drug and Medication Information

4.1 Drug Information

1 of 2
Drug Name	Tekturna
PubMed Health	Aliskiren (By mouth)
Drug Classes	Antihypertensive
Drug Label	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-me...
Active Ingredient	Aliskiren hemifumarate
Dosage Form	Tablet
Route	Oral
Strength	eq 150mg base; eq 300mg base
Market Status	Prescription
Company	Novartis

2 of 2
Drug Name	Tekturna
PubMed Health	Aliskiren (By mouth)
Drug Classes	Antihypertensive
Drug Label	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-me...
Active Ingredient	Aliskiren hemifumarate
Dosage Form	Tablet
Route	Oral
Strength	eq 150mg base; eq 300mg base
Market Status	Prescription
Company	Novartis

4.2 Drug Indication

Treatment of essential hypertension.

Treatment of essential hypertension

5 Pharmacology and Biochemistry

5.1 FDA Pharmacological Classification

5.1.1 Pharmacological Classes

Renin Inhibitors [MoA]; Renin Inhibitor [EPC]

5.2 ATC Code

C09XA02

Find Aliskiren manufacturers, exporters & distributors on PharmaCompass

Aliskiren

Aliskiren

Synopsis

Chemistry

APIs // Active Pharmaceutical Ingredients

8 API Suppliers

4 USDMF

3 EU WC

3 NDC API

4 Listed Suppliers

PRICE INFORMATION

API Reference Price

API Exports

API Imports

INTERMEDIATES

5 Suppliers

DOSSIERs // Finished Dosage Formulations

22 Dossiers

20 FDA Orange Book

2 Europe

DRUG PRODUCT COMPOSITION

TABLET;ORAL - EQ 150MG BASE

TABLET;ORAL - EQ 300MG BASE

TABLET;ORAL - EQ 150MG BASE;12.5MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**

TABLET;ORAL - EQ 150MG BASE;25MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**

TABLET;ORAL - EQ 300MG BASE;12.5MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**

TABLET;ORAL - EQ 300MG BASE;25MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**

RELATED EXCIPIENT COMPANIES

Suppliers

22 BASF

16 Kerry

10 Microlex e.U

10 Roquette

10 Corel Pharma Chem

9 Sigachi Industries

8 Gangwal Chemicals

6 Anhui Sunhere Pharmaceutical Excipients Co.,Ltd

6 Seppic

6 Lonza Capsugel

5 Gangwal Healthcare

5 Boai NKY Pharmaceuticals Ltd

5 Ideal Cures Pvt Ltd

3 Shanghai Shenmei Pharmaceutical Technology Co., Ltd

3 Actylis

3 Pharmatrans-Sanaq

3 Kima Chemical

2 Ulanqab Kema New Material

2 Vasa Pharmachem

2 Nomisma Healthcare

2 DFE Pharma

2 Prachin Chemical

2 Seqens

2 The Dow Chemical Company

1 Qianhao Chemical (Hebei) Co., Ltd

1 ACG Worldwide

1 Qualicaps

1 DKSH

1 Aeon Procare

1 SPI Pharma

1 Finar

1 Alcedo Pharmachem

EXCIPIENTS BY APPLICATIONS

42 Coating Systems & Additives

32 Fillers, Diluents & Binders

28 Controlled & Modified Release

22 Direct Compression

21 Disintegrants & Superdisintegrants

18 Thickeners and Stabilizers

17 Granulation

14 Solubilizers

13 Lubricants & Glidants

8 Film Formers & Plasticizers

8 Co-Processed Excipients

7 Topical

6 Chewable & Orodispersible Aids

5 Empty Capsules

4 Vegetarian Capsules

4 API Stability Enhancers

4 Taste Masking

TABLET;ORAL - EQ 150MG BASE;12.5MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons

TABLET;ORAL - EQ 150MG BASE;25MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons

TABLET;ORAL - EQ 300MG BASE;12.5MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons

TABLET;ORAL - EQ 300MG BASE;25MG Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons