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1. (2s)-n-((1s)-1-benzyl-2-(((1s)-3-methyl-1-(((2r)-2-methyloxiran-2-yl)carbonyl)butyl)amino)-2-oxoethyl)-4-methyl-2-(((2s)-2-((morpholin-4-ylacetyl)amino)-4-phenylbutanoyl)amino)pentanamide
2. Kyprolis
3. Pr-171
4. Pr171
1. 868540-17-4
2. Kyprolis
3. Carfilzomib (pr-171)
4. Pr-171
5. Carfilzomib (pr171)
6. Unii-72x6e3j5ar
7. Nsc-758252
8. 72x6e3j5ar
9. Chembl451887
10. Chebi:65347
11. Ncgc00249613-01
12. Dsstox_cid_28616
13. Dsstox_rid_82886
14. Dsstox_gsid_48690
15. (2s)-4-methyl-n-[(2s)-1-[[(2s)-4-methyl-1-[(2r)-2-methyloxiran-2-yl]-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[[(2s)-2-[(2-morpholin-4-ylacetyl)amino]-4-phenylbutanoyl]amino]pentanamide
16. (2s)-n-((1s)-1-benzyl-2-(((1s)-3-methyl-1-(((2r)-2-methyloxiran-2-yl)carbonyl)butyl)amino)-2-oxoethyl)-4-methyl-2-(((2s)-2-((morpholin-4-ylacetyl)amino)-4-phenylbutanoyl)amino)pentanamide
17. (alphas)-alpha-[[2-(4-morpholinyl)acetyl]amino]benzenebutanoyl-l-leucyl-n-[(1s)-3-methyl-1-[[(2r)-2-methyl-2-oxiranyl]carbonyl]butyl]-l-phenylalaninamide
18. (s)-4-methyl-n-((s)-1-(((s)-4-methyl-1-((r)-2-methyloxiran-2-yl)-1-oxopentan-2-yl)amino)-1-oxo-3-phenylpropan-2-yl)-2-((s)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamide
19. N-{(2s)-2-[(morpholin-4-ylacetyl)amino]-4-phenylbutanoyl}-l-leucyl-n-{(2s)-4-methyl-1-[(2r)-2-methyloxiran-2-yl]-1-oxopentan-2-yl}-l-phenylalaninamide
20. (s)-4-methyl-n-((s)-1-((s)-4-methyl-1-((r)-2-methyloxiran-2-yl)-1-oxopentan-2-ylamino)-1-oxo-3-phenylpropan-2-yl)-2-((s)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamide
21. Carfilzomib [usan]
22. Cas-868540-17-4
23. Carfilzomib [usan:inn]
24. Mfcd11040997
25. Kyprolis (tn)
26. Carfilzomib; Pr171
27. Carfilzomib [mi]
28. Carfilzomib [inn]
29. Carfilzomib [jan]
30. Carfilzomib [vandf]
31. Schembl85165
32. Carfilzomib [who-dd]
33. Mls006011102
34. Carfilzomib (jan/usan/inn)
35. Gtpl7420
36. Dtxsid4048690
37. Amy4357
38. Carfilzomib [orange Book]
39. Ex-a2037
40. Ono-7057
41. Tox21_113079
42. Bdbm50277889
43. Nsc756640
44. Nsc758252
45. S2853
46. Zinc49841054
47. Akos025401910
48. Tox21_113079_1
49. Ccg-270405
50. Cs-0984
51. Cs-w004540
52. Db08889
53. Nsc 758252
54. Nsc-756640
55. Ncgc00249613-02
56. Ncgc00249613-03
57. Ncgc00249613-08
58. Ncgc00249613-11
59. Ncgc00249613-13
60. Ac-27051
61. As-17059
62. Hy-10455
63. Smr004660024
64. Sw218090-2
65. D08880
66. Ab01565867_02
67. Sr-01000941582
68. J-501773
69. Sr-01000941582-1
70. Q15366934
71. (alphas)-alpha-((4-morpholinylacetyl)amino)benzenebutanoyl-l-leucyl-n-((1s)-3-methyl-1-(((2r)-2-methyloxiranyl)carbonyl)butyl)-l-phe Nylalaninamide
72. (s)-4-methyl-n-((s)-1-((s)-4-methyl-1-((r)-2- Methyloxiran-2-yl)-1 -oxopentan-2-ylamino)-1-oxo-3-phenylpropan-2-yl)-2-((s)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamide
73. L-phenylalaninamide, (.alpha.s)-.alpha.-((4-morpholinylacetyl)amino)benzenebutanoyl-l-leucyl-n-((1s)-3-methyl-1-(((2r)-2-methyloxiranyl)carbonyl)butyl)-
74. L-phenylalaninamide, (alphas)-alpha-((4-morpholinylacetyl)amino)benzenebutanoyl-l-leucyl-n-((1s)-3-methyl-1-(((2r)-2-methyloxiranyl)carbonyl)butyl)-
| Molecular Weight | 719.9 g/mol |
|---|---|
| Molecular Formula | C40H57N5O7 |
| XLogP3 | 4.7 |
| Hydrogen Bond Donor Count | 4 |
| Hydrogen Bond Acceptor Count | 8 |
| Rotatable Bond Count | 20 |
| Exact Mass | 719.42579917 g/mol |
| Monoisotopic Mass | 719.42579917 g/mol |
| Topological Polar Surface Area | 159 Ų |
| Heavy Atom Count | 52 |
| Formal Charge | 0 |
| Complexity | 1180 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 5 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
| 1 of 2 | |
|---|---|
| Drug Name | Kyprolis |
| PubMed Health | Carfilzomib (Injection) |
| Drug Classes | Antineoplastic Agent |
| Drug Label | KYPROLIS (carfilzomib) for Injection is an antineoplastic agent available for intravenous use only. KYPROLIS is a sterile, white to off-white lyophilized powder and is available as a single-use vial. Each vial of KYPROLIS contains 60mg of carfilzom... |
| Active Ingredient | Carfilzomib |
| Dosage Form | Powder |
| Route | Intravenous |
| Strength | 60mg/vial |
| Market Status | Prescription |
| Company | Onyx Pharms |
| 2 of 2 | |
|---|---|
| Drug Name | Kyprolis |
| PubMed Health | Carfilzomib (Injection) |
| Drug Classes | Antineoplastic Agent |
| Drug Label | KYPROLIS (carfilzomib) for Injection is an antineoplastic agent available for intravenous use only. KYPROLIS is a sterile, white to off-white lyophilized powder and is available as a single-use vial. Each vial of KYPROLIS contains 60mg of carfilzom... |
| Active Ingredient | Carfilzomib |
| Dosage Form | Powder |
| Route | Intravenous |
| Strength | 60mg/vial |
| Market Status | Prescription |
| Company | Onyx Pharms |
Carfilzomib is indicated for the treatment of adult patients with relapsed or refractory multiple myeloma who have received one to three lines of therapy in combination with lenalidomide and dexamethasone; or dexamethasone; or daratumumab and dexamethasone; or daratumumab and hyaluronidase-fihj and dexamethasone. It is also indicated as a single agent for the treatment of patients with relapsed or refractory multiple myeloma who have received one or more lines of therapy.
FDA Label
Kyprolis in combination with daratumumab and dexamethasone, with lenalidomide and dexamethasone, or with dexamethasone alone is indicated for the treatment of adult patients with multiple myeloma who have received at least one prior therapy.
Treatment of Multiple Myeloma
Treatment of acute lymphoblastic leukaemia
Intravenous carfilzomib administration resulted in suppression of proteasome chymotrypsin-like activity when measured in blood 1 hour after the first dose. On Day 1 of Cycle 1, proteasome inhibition in peripheral blood mononuclear cells (PBMCs) ranged from 79% to 89% at 15 mg/m2, and from 82% to 83% at 20 mg/m2. In addition, carfilzomib administration resulted in inhibition of the LMP2 and MECL1 subunits of the immunoproteasome ranging from 26% to 32% and 41% to 49%, respectively, at 20 mg/m2. Proteasome inhibition was maintained for 48 hours following the first dose of carfilzomib for each week of dosing. Resistance against carfilzomib has been observed and although the mechanism has not been confirmed, it is thought that up-regulation of P-glycoprotein may be a contributing factor. Furthermore, studies suggest that carfilzomib is more potent than bortezomib.
L01XX45
L01XX45
S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355
L - Antineoplastic and immunomodulating agents
L01 - Antineoplastic agents
L01X - Other antineoplastic agents
L01XG - Proteasome inhibitors
L01XG02 - Carfilzomib
Absorption
Cmax, single IV dose of 27 mg/m^2 = 4232 ng/mL; AUC, single IV dose of 27 mg/m^2 = 379 nghr/mL; Carfilzomib does not accumulation in the systemic. At doses between 20 and 36 mg/m2, there was a dose-dependent increase in exposure.
Volume of Distribution
Vd, steady state, 20 mg/m^2 = 28 L
Clearance
Systemic clearance = 151 - 263 L/hour. As this value exceeds hepatic blood flow, it suggests that carfilozmib is cleared extrahepatically.
Carfilzomib was rapidly and extensively metabolized by the liver. The predominant metabolites were the peptide fragments and the diol of carfilzomib which suggests that the main metabolic pathways are peptidase cleavage and epoxide hydrolysis. The cytochrome P450 enzyme system is minimally involved in the metabolism of carfilzomib. All metabolites are inactive.
Following intravenous administration of doses 15 mg/m^2, carfilzomib was rapidly cleared from the systemic circulation with a half-life of 1 hour on Day 1 of Cycle 1.
Carfilzomib is made up of four modified peptides and acts as a proteasome inhibitor. Carfilzomib irreversibly and selectively binds to N-terminal threonine-containing active sites of the 20S proteasome, the proteolytic core particle within the 26S proteasome. This 20S core has 3 catalytic active sites: the chymotrypsin, trypsin, and caspase-like sites. Inhibition of the chymotrypsin-like site by carfilzomib (5 and 5i subunits) is the most effective target in decreasing cellular proliferation, ultimately resulting in cell cycle arrest and apoptosis of cancerous cells. At higher doses, carfilzomib will inhibit the trypsin-and capase-like sites.
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