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1 Rochem International Inc, 13 SPI Pharma, 1 Faran Shimi Pharmaceutical, 1 Pfanstiehl, 1 BASF, 2 Gangwal Chemicals, 1 Ingredion Pharma Solutions, 2 Kerry, 2 Microlex e.U, 1 Pluviaendo, 3 Roquette, 1 Shanghai Shenmei Pharmaceutical Technology Co., Ltd, 1 Shijiazhuang Huaxu Pharmaceutical, 1 Sigachi Industries

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1 Rochem International Inc
13 SPI Pharma
1 Faran Shimi Pharmaceutical
1 Pfanstiehl
1 BASF
2 Gangwal Chemicals
1 Ingredion Pharma Solutions
2 Kerry
2 Microlex e.U
1 Pluviaendo
3 Roquette
1 Shanghai Shenmei Pharmaceutical Technology Co., Ltd
1 Shijiazhuang Huaxu Pharmaceutical
1 Sigachi Industries

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17 Fillers, Diluents & Binders
10 Chewable & Orodispersible Aids
9 Direct Compression
9 Taste Masking
4 Co-Processed Excipients
4 Parenteral
3 Granulation
3 Disintegrants & Superdisintegrants
1 API Stability Enhancers
1 Thickeners and Stabilizers
1 Solubilizers

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Synopsis

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Chemistry

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Also known as: Som 230, Som-230, Som230, 396091-73-9, Pasireotide free base, Chebi:72312

Molecular Formula

C₅₈H₆₆N₁₀O₉

Molecular Weight

1047.2 g/mol

InChI Key

VMZMNAABQBOLAK-DBILLSOUSA-N

FDA UNII

98H1T17066

Pasireotide is a synthetic long-acting cyclic peptide with somatostatin-like activity. Pasireotide activates a broad spectrum of somatostatin receptors, exhibiting a much higher binding affinity for somatostatin receptors 1, 3, and 5 than octreotide in vitro, as well as a comparable binding affinity for somatostatin receptor 2. This agent is more potent than somatostatin in inhibiting the release of human growth hormone (HGH), glucagon, and insulin.

Pasireotide is a Somatostatin Analog. The mechanism of action of pasireotide is as a Somatostatin Receptor Agonist.

1 2D Structure

Pasireotide

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

[(3S,6S,9S,12R,15S,18S,20R)-9-(4-aminobutyl)-3-benzyl-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-15-phenyl-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-(2-aminoethyl)carbamate

2.1.2 InChI

InChI=1S/C58H66N10O9/c59-27-13-12-22-46-52(69)64-47(30-38-23-25-42(26-24-38)76-36-39-16-6-2-7-17-39)53(70)66-49(31-37-14-4-1-5-15-37)57(74)68-35-43(77-58(75)61-29-28-60)33-50(68)55(72)67-51(40-18-8-3-9-19-40)56(73)65-48(54(71)63-46)32-41-34-62-45-21-11-10-20-44(41)45/h1-11,14-21,23-26,34,43,46-51,62H,12-13,22,27-33,35-36,59-60H2,(H,61,75)(H,63,71)(H,64,69)(H,65,73)(H,66,70)(H,67,72)/t43-,46+,47+,48-,49+,50+,51+/m1/s1

2.1.3 InChI Key

VMZMNAABQBOLAK-DBILLSOUSA-N

2.1.4 Canonical SMILES

C1C(CN2C1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C2=O)CC3=CC=CC=C3)CC4=CC=C(C=C4)OCC5=CC=CC=C5)CCCCN)CC6=CNC7=CC=CC=C76)C8=CC=CC=C8)OC(=O)NCCN

2.1.5 Isomeric SMILES

C1[C@H](CN2[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C2=O)CC3=CC=CC=C3)CC4=CC=C(C=C4)OCC5=CC=CC=C5)CCCCN)CC6=CNC7=CC=CC=C76)C8=CC=CC=C8)OC(=O)NCCN

2.2 Other Identifiers

2.2.1 UNII

98H1T17066

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Cyclo((4r)-4-(2-aminoethylcarbamoyloxy)-l-prolyl-l-phenylglycyl-d-tryptophyl-l-lysyl-4-o-benzyl-l-tyrosyl-l-phenylalanyl-)

2. Som 230

3. Som-230

4. Som230

2.3.2 Depositor-Supplied Synonyms

1. Som 230

2. Som-230

3. Som230

4. 396091-73-9

5. Pasireotide Free Base

6. Chebi:72312

7. Signifor Lar

8. Chembl3349607

9. 396091-73-9 (free Base)

10. 98h1t17066

11. Pasireotide Diaspartate

12. Cyclo((4r)-4-(2-aminoethylcarbamoyloxy)-l-prolyl-l-phenylglycyl-d-tryptophyl-l-lysyl-4-o-benzyl-l-tyrosyl-l- Phenylalanyl-)

13. Cyclo((4r)-4-(2-aminoethylcarbamoyloxy)-l-prolyl-l-phenylglycyl-d-tryptophyl-l-lysyl-4-o-benzyl-l-tyrosyl-l-phenylalanyl-)

14. (3s,6r,9s,12s,15s,19r,20as)-6-((1h-indol-3-yl)methyl)-9-(4-aminobutyl)-15-benzyl-12-(4-(benzyloxy)benzyl)-1,4,7,10,13,16-hexaoxo-3-phenylicosahydropyrrolo[1,2-a][1,4,7,10,13,16]hexaazacyclooctadecin-19-yl (2-aminoethyl)carbamate

15. Cyclo[(2s)-2-phenylglycyl-d-tryptophyl-l-lysyl-o-benzyl-l-tyrosyl-l-phenylalanyl-(4r)-4-{[(2-aminoethyl)carbamoyl]oxy}-l-prolyl]

16. Pasireotide [inn]

17. Pasireotide [usan]

18. Pasireotide [usan:inn]

19. Pasireotida

20. Pasireotidum

21. Unii-98h1t17066

22. Pasireotide [mi]

23. Pasireotide [vandf]

24. Pasireotide [mart.]

25. Pasireotide [who-dd]

26. Gtpl2018

27. Schembl12462108

28. Som 320

29. Bdbm50474236

30. Db06663

31. Ncgc00378682-03

32. Hy-16381

33. Q3896970

34. [(3s,6s,9s,12r,15s,18s,20r)-9-(4-aminobutyl)-12-(1h-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-15-phenyl-6-[[4-(phenylmethoxy)phenyl]methyl]-3-(phenylmethyl)-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-(2-aminoethyl)carbamate

35. [(3s,6s,9s,12r,15s,18s,20r)-9-(4-aminobutyl)-3-benzyl-12-(1h-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-15-phenyl-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-(2-aminoethyl)carbamate

2.4 Create Date

2006-10-25

3 Chemical and Physical Properties

Molecular Formula	C₅₈H₆₆N₁₀O₉
Molecular Weight	1047.2 g/mol
XLogP3	4.7
Hydrogen Bond Donor Count	9
Hydrogen Bond Acceptor Count	11
Rotatable Bond Count	18
Exact Mass	1046.50142372 g/mol
Monoisotopic Mass	1046.50142372 g/mol
Topological Polar Surface Area	281 Å²
Heavy Atom Count	77
Formal Charge	0
Complexity	1940
Isotope Atom Count	0
Defined Atom Stereocenter Count	7
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Indication

For the treatment of Cushings disease, specifically for those patients whom pituitary surgery has not been curative or is not an option.

FDA Label

Signifor is indicated for the treatment of adult patients with Cushings disease for whom surgery is not an option or for whom surgery has failed.

Signifor is indicated for the treatment of adult patients with acromegaly for whom surgery is not an option or has not been curative and who are inadequately controlled on treatment with another somatostatin analogue.

Treatment of acromegaly and pituitary gigantism

Overproduction of pituitary ACTH, Pituitary dependant Cushing's disease, Pituitary dependant hyperadrenocorticism

5 Pharmacology and Biochemistry

5.1 Pharmacology

Signifor is an analogue of somatostatin that promotes reduced levels of cortisol secretion in Cushing's disease patients.

5.2 MeSH Pharmacological Classification

Hormones

Chemical substances having a specific regulatory effect on the activity of a certain organ or organs. The term was originally applied to substances secreted by various ENDOCRINE GLANDS and transported in the bloodstream to the target organs. It is sometimes extended to include those substances that are not produced by the endocrine glands but that have similar effects. (See all compounds classified as Hormones.)

5.3 FDA Pharmacological Classification

5.3.1 Active Moiety

PASIREOTIDE

5.3.2 FDA UNII

98H1T17066

5.3.3 Pharmacological Classes

Somatostatin Receptor Agonists [MoA]; Somatostatin Analog [EPC]

5.4 ATC Code

H01CB05

H - Systemic hormonal preparations, excl. sex hormones and insulins

H01 - Pituitary and hypothalamic hormones and analogues

H01C - Hypothalamic hormones

H01CB - Somatostatin and analogues

H01CB05 - Pasireotide

5.5 Absorption, Distribution and Excretion

Absorption

The peak plasma concentration of pasireotide occurs in 0.25-0.5 hours. After administration of single and multiple doses, there is dose-proportionoal increases in Cmax and AUC.

Route of Elimination

Pasireotide is eliminated mostly by hepatic clearance (biliary excretion)(about 48%) with some minor renal clearance (about 7.63%).

Volume of Distribution

Pasireotide is widely distributed and has a volume of distribution of >100L.

Clearance

The clearance in healthy patient is ~7.6 L/h and in Cushings disease patients is ~3.8 L/h.

5.6 Metabolism/Metabolites

Metabolism is minimal.

5.7 Biological Half-Life

The half-life is 12 hours.

5.8 Mechanism of Action

Pasireotide activates a broad spectrum of somatostatin receptors, exhbiting a much higher binding affinity for somatostatin receptors 1, 3, and 5 than octreotide in vitro, as well as a comparable binding affinity for somatostatin receptor 2. The binding and activation of the somatostatin receptors causes inhibition of ACTH secretion and results in reduced cortisol secretion in Cushing's disease patients. Also this agent is more potent than somatostatin in inhibiting the release of human growth hormone (HGH), glucagon, and insulin.

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