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Also known as: 120685-11-2, Pkc-412, Pkc412, Cgp 41251, 4'-n-benzoylstaurosporine, Pkc 412
Molecular Formula
C35H30N4O4
Molecular Weight
570.6  g/mol
InChI Key
BMGQWWVMWDBQGC-IIFHNQTCSA-N
FDA UNII
ID912S5VON

Midostaurin
Midostaurin is a synthetic indolocarbazole multikinase inhibitor with potential antiangiogenic and antineoplastic activities. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors.
Midostaurin is a Kinase Inhibitor. The mechanism of action of midostaurin is as a Receptor Tyrosine Kinase Inhibitor.
1 2D Structure

Midostaurin

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
N-[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]-N-methylbenzamide
2.1.2 InChI
InChI=1S/C35H30N4O4/c1-35-32(42-3)25(37(2)34(41)19-11-5-4-6-12-19)17-26(43-35)38-23-15-9-7-13-20(23)28-29-22(18-36-33(29)40)27-21-14-8-10-16-24(21)39(35)31(27)30(28)38/h4-16,25-26,32H,17-18H2,1-3H3,(H,36,40)/t25-,26-,32-,35+/m1/s1
2.1.3 InChI Key
BMGQWWVMWDBQGC-IIFHNQTCSA-N
2.1.4 Canonical SMILES
CC12C(C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)N(C)C(=O)C9=CC=CC=C9)OC
2.1.5 Isomeric SMILES
C[C@@]12[C@@H]([C@@H](C[C@@H](O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)N(C)C(=O)C9=CC=CC=C9)OC
2.2 Other Identifiers
2.2.1 UNII
ID912S5VON
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 4'-n-benzoyl Staurosporine

2. 4'-n-benzoylstaurosporine

3. Benzamide, N-(2,3,9,10,11,12-hexahydro-9-methoxy-8-methyl-1-oxo-8,12-epoxy-1h,8h-2,7b,12a-triazadibenzo(a,g)cyclonona(cde)trinden-10-yl)-n-methyl-, (8alpha,9beta,10beta,12alpha)-

4. Benzoylstaurosporine

5. Cgp 41 251

6. Cgp 41251

7. Cgp-41251

8. N-((9s,10r,11r,13r)-10-methoxy-9-methyl-1-oxo-2,3,10,11,12,13-hexahydro-9,13-epoxy-1h,9h-diindolo(1,2,3-gh:3',2',1'-lm)pyrrolo(3,4-j)(1,7)benzodiazonin-11-yl)-n-methylbenzamide

9. Pkc 412

10. Pkc-412

11. Pkc412

12. Rydapt

2.3.2 Depositor-Supplied Synonyms

1. 120685-11-2

2. Pkc-412

3. Pkc412

4. Cgp 41251

5. 4'-n-benzoylstaurosporine

6. Pkc 412

7. Rydapt

8. Cgp-41251

9. Benzoylstaurosporine

10. N-benzoylstaurosporine

11. Id912s5von

12. Nvp-pkc412

13. Chembl608533

14. Chebi:63452

15. Nsc-656576

16. N-((9s,10r,11r,13r)-10-methoxy-9-methyl-1-oxo-2,3,10,11,12,13-hexahydro-9,13-epoxy-1h,9h-diindolo(1,2,3-gh:3',2',1'-lm)pyrrolo(3,4-j)(1,7)benzodiazonin-11-yl)-n-methylbenzamide

17. N-[(5s,6r,7r,9r)-6-methoxy-5-methyl-14-oxo-6,7,8,9,15,16-hexahydro-5h,14h-5,9-epoxy-4b,9a,15-triazadibenzo[b,h]cyclonona[1,2,3,4-jkl]cyclopenta[e]-as-indacen-7-yl]-n-methylbenzamide

18. Midostaurin [inn]

19. Cgp 41 251

20. Midostaurin [usan:inn]

21. Unii-id912s5von

22. Cgp41251

23. Cgp 41231

24. Rydapt (tn)

25. Midostaurin(pkc412)

26. 4-n-benzoylstaurosporine

27. Midostaurin [mi]

28. Staurosporine, N-benzoyl

29. Midostaurin [jan]

30. Midostaurin [usan]

31. Midostaurin [mart.]

32. Midostaurin [who-dd]

33. Midostaurin (jan/usan/inn)

34. Gtpl5702

35. Schembl8295379

36. Midostaurin [orange Book]

37. Hms3229k17

38. Ex-a1741

39. Bdbm50326053

40. Cgp-41521

41. Mfcd00871372

42. Nsc800791

43. S8064

44. Akos024457372

45. Zinc100013130

46. Ccg-101288

47. Cs-3331

48. Db06595

49. Nsc 656576

50. Nsc-800791

51. Ncgc00241102-01

52. Ncgc00241102-02

53. Ncgc00241102-05

54. Ncgc00484987-03

55. Ac-31929

56. Benzamide, N-(2,3,9,10,11,12-hexahydro-9-methoxy-8-methyl-1-oxo-8,12-epoxy-1h,8h-2,7b,12a-triazadibenzo(a,g)cyclonona(cde)trinden-10-yl)-n-methyl-, (8alpha,9beta,10beta,12alpha)-

57. Hy-10230

58. C71714

59. D05029

60. J-004379

61. Q6842945

62. Brd-k13646352-001-01-2

63. [9s-(9?,10?,11?,13?)]-n-(2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1h,9h-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl)-n-methylbenzamide

64. Benzamide, N-((9s,10r,11r,13r)-2,3,9,10,11,12-hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1h,9h-diindolo(1,2,3-gh:3',2',1'-lm)pyrrolo(3,4-j)(1,7)benzodiazonin-11-yl)-n-methyl-

65. N-[(2s,3r,4r,6r)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8,10,12,14(28),15(19),20(27),21,23,25-nonaen-4-yl]-n-methylbenzamide

66. N-[(2s,3r,4r,6r)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8(13),9,11,14,19,21(26),22,24,27-nonaen-4-yl]-n-methyl-benzamide

67. N-[(2s,3r,4r,6r)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]-n-methylbenzamide

2.4 Create Date
2006-10-25
3 Chemical and Physical Properties
Molecular Weight 570.6 g/mol
Molecular Formula C35H30N4O4
XLogP34.8
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count4
Rotatable Bond Count3
Exact Mass570.22670545 g/mol
Monoisotopic Mass570.22670545 g/mol
Topological Polar Surface Area77.7 Ų
Heavy Atom Count43
Formal Charge0
Complexity1140
Isotope Atom Count0
Defined Atom Stereocenter Count4
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Information
1 of 1  
Drug NameRYDAPT
Active IngredientMIDOSTAURIN
CompanyNOVARTIS PHARMS CORP (Application Number: N207997. Patents: 7973031, 8222244, 8575146)

4.2 Drug Indication

Investigated for use/treatment in adult patients with high-risk acute myeloid leukemia (AML) who are FLT3 mutation-positive, agressive systemic mastocytosis (ASM), systemic mastocytosis with associated hematological neoplasm (SM-AHN), or mast cell leukemia (MCL).


FDA Label


Rydapt is indicated:

- in combination with standard daunorubicin and cytarabine induction and high dose cytarabine consolidation chemotherapy, and for patients in complete response followed by Rydapt single agent maintenance therapy, for adult patients with newly diagnosed acute myeloid leukaemia (AML) who are FLT3 mutation positive (see section 4. 2);

- as monotherapy for the treatment of adult patients with aggressive systemic mastocytosis (ASM), systemic mastocytosis with associated haematological neoplasm (SM AHN), or mast cell leukaemia (MCL).


5 Pharmacology and Biochemistry
5.1 Pharmacology

It targets multiple WT and mutated kinases that, when activated, constitutively stimulate aberrant signalling cascades that lead to malignancies such as AML and ASM. Alternative pharmacodynamic effect of midostaurin in prolonging QTc intervals was not clinically significant in patients with advanced SM or AML when compared to placebo. Midostaurin is therapeutically beneficial as a combination therapy for patients undergoing chemotherapy.


5.2 MeSH Pharmacological Classification

Antineoplastic Agents

Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)


Protein Kinase Inhibitors

Agents that inhibit PROTEIN KINASES. (See all compounds classified as Protein Kinase Inhibitors.)


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety
MIDOSTAURIN
5.3.2 FDA UNII
ID912S5VON
5.3.3 Pharmacological Classes
Receptor Tyrosine Kinase Inhibitors [MoA]; Kinase Inhibitor [EPC]
5.4 ATC Code

L01XE


L - Antineoplastic and immunomodulating agents

L01 - Antineoplastic agents

L01E - Protein kinase inhibitors

L01EX - Other protein kinase inhibitors

L01EX10 - Midostaurin


5.5 Absorption, Distribution and Excretion

Absorption

The time to reach maximum concentration ranges from 1-3 hrs in fasting patients. The maximum concentration and the time it takes to reach this concentration is reduced up to 20% in presence of a standard meal.


Route of Elimination

Accounting for 95% of recovered dose eliminated through fecal excretion, 91% was determined as metabolites and 4% as unchanged parent drug. Remaining 5% of the recovered dose is eliminated via renal excretion.


Volume of Distribution

The Vd of midostaurin is 95.2L. The parent drug and its main metabolites (CGP62221, CGP52421) are distributed in plasma in vitro.


Clearance

The clearance values of during the initial formation of metabolites are 1.47 L/h for CGP62221 metabolite and 0.501 L/h for CGP52421. 28 days following the oral administration of midostaurin, the clearance of CGP52421 may increase up to 5.2 fold in a recommended dose of 25 mg, resulting in a 2.1- to 2.5-fold increase in total clearance of midostaurin.


5.6 Metabolism/Metabolites

Midostaurin is primarily metabolized into CGP62221 and CGP52421 via hepatic CYP3A4 enzymatic activity. The metabolism of CGP62221 takes place initially in a linear relationship whereas CGP52421 formation is an inducible process.


5.7 Biological Half-Life

Elimination half life is approximately 21 hrs for midostaurin, 32 hrs for CGP62221 and 482 hrs for CGP52421.


5.8 Mechanism of Action

It potently inhibits multiple receptor tyrosine kinases. Midostaurin and its major active metabolites CGP62221 and CGP52421 inhibit the activity of protein kinase C alpha (PKCalpha), VEGFR2, KIT, PDGFR and WT and/or mutant FLT3 tyrosine kinases. Inhibition of FLT3 receptor signalling cascades induces apoptosis of target leukemia cells expressing target receptors and mast cells, in addition to its antiproliferative activity toward multiple cancer cell lines. Midostaurin also interacts with organic anion transporter (OATP) 1A1 and multidrug resistance protein (MRP)-2 according to preliminary in vitro studies.


API Reference Price

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07-Apr-2022
18-Sep-2024
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