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1. Pf 02341066
2. Pf 2341066
3. Pf-02341066
4. Pf-2341066
5. Pf02341066
6. Pf2341066
7. Xalkori
1. 877399-52-5
2. Xalkori
3. Pf-02341066
4. (r)-crizotinib
5. Pf-2341066
6. Pf 2341066
7. Crizotinib (pf-02341066)
8. (r)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1h-pyrazol-4-yl)pyridin-2-amine
9. 3-[(1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1h-pyrazol-4-yl]-2-pyridinamine
10. Pf 02341066
11. Pf2341066
12. Chembl601719
13. Crizotinib (pf-2341066)
14. Chebi:64310
15. 877399-52-5 (free Base)
16. 53ah36668s
17. Nsc-756645
18. 3-[(1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)-1h-pyrazol-4-yl]pyridin-2-amine
19. 2-pyridinamine, 3-((1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(4-piperidinyl)-1h-pyrazol-4-yl)-
20. 3-[(1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-yl-1h-pyrazol-4-yl)pyridin-2-amine
21. 3-[(1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-ylpyrazol-4-yl)pyridin-2-amine
22. 3-[(1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1h-pyrazol-4-yl]pyridin-2-amine
23. (r)-3-[1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1h-pyrazol-4-yl)-pyridin-2-ylamine
24. Xalkori (tn)
25. Crizotinib [usan]
26. Crizotinib [usan:inn]
27. Crizotinibum
28. Unii-53ah36668s
29. 3-((1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1h-pyrazol-4-yl)pyridin-2-amine
30. Vgh
31. Crizotinib- Bio-x
32. Crizotinib [mi]
33. Crizotinib [inn]
34. Crizotinib [jan]
35. Pf02341066
36. Crizotinib [vandf]
37. Crizotinib [mart.]
38. Crizotinib [who-dd]
39. Schembl93829
40. Pf-2341066,crizotinib
41. Crizotinib (jan/usan/inn)
42. Gtpl4903
43. Crizotinib [orange Book]
44. Crizotinib, >=98% (hplc)
45. Pf-2341066 - Crizotinib
46. Ex-a096
47. Bcpp000116
48. Dtxsid701009329
49. Amy10313
50. Bdbm50306682
51. Mfcd12407409
52. Nsc749005
53. Nsc749769
54. Nsc800080
55. Zinc35902489
56. Akos015901233
57. Akos015995207
58. Ccg-264803
59. Db08865
60. Gs-6178
61. Nsc 756645
62. Nsc-749005
63. Nsc-749769
64. Nsc-800080
65. Ncgc00250400-01
66. Ncgc00250400-02
67. Ncgc00250400-09
68. Ncgc00250400-12
69. Bc164334
70. Hy-50878
71. Bb 0261738
72. Sw202555-3
73. D09731
74. 399p525
75. J-510370
76. Q5186964
77. Brd-k78431006-001-01-1
78. Brd-k78431006-001-03-7
79. 877399-52-5, 877399-53-6 (acetate)
80. 3-(2,6-dichloro-3-fluorobenzyloxy)-5-(1-(piperidin-4-yl)-1h-pyrazol-4-yl)pyridin-2-amine
81. (r)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1h-pyrazol-4-yl)pyridin-2-am Ine
82. 3-(1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy-5-1-(4-piperidinyl)-1h-pyrazol-4-yl-2-pyridinamine
83. 3-[(r)-1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1h-pyrazol-4-yl)-pyridin-2-ylamine
| Molecular Weight | 450.3 g/mol |
|---|---|
| Molecular Formula | C21H22Cl2FN5O |
| XLogP3 | 3.7 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 5 |
| Exact Mass | 449.1185439 g/mol |
| Monoisotopic Mass | 449.1185439 g/mol |
| Topological Polar Surface Area | 78 Ų |
| Heavy Atom Count | 30 |
| Formal Charge | 0 |
| Complexity | 558 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 1 |
| 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 | Xalkori |
| PubMed Health | Crizotinib (By mouth) |
| Drug Classes | Antineoplastic Agent |
| Drug Label | XALKORI (crizotinib) is an oral receptor tyrosine kinase inhibitor. The molecular formula for crizotinib is C21H22Cl2FN5O. The molecular weight is 450.34 Daltons. Crizotinib is described chemically as (R)-3-[1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[... |
| Active Ingredient | Crizotinib |
| Dosage Form | Capsule |
| Route | Oral |
| Strength | 200mg; 250mg |
| Market Status | Prescription |
| Company | Pf Prism Cv |
| 2 of 2 | |
|---|---|
| Drug Name | Xalkori |
| PubMed Health | Crizotinib (By mouth) |
| Drug Classes | Antineoplastic Agent |
| Drug Label | XALKORI (crizotinib) is an oral receptor tyrosine kinase inhibitor. The molecular formula for crizotinib is C21H22Cl2FN5O. The molecular weight is 450.34 Daltons. Crizotinib is described chemically as (R)-3-[1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[... |
| Active Ingredient | Crizotinib |
| Dosage Form | Capsule |
| Route | Oral |
| Strength | 200mg; 250mg |
| Market Status | Prescription |
| Company | Pf Prism Cv |
Crizotinib is used for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) that is anaplastic-lymphoma kinase (ALK)-positive as detected by a FDA-approved test.
FDA Label
Xalkori is indicated for the first-line treatment of adults with anaplastic lymphoma kinase (ALK) positive advanced non-small cell lung cancer (NSCLC).
Xalkori is indicated for the treatment of adults with previously treated anaplastic lymphoma kinase (ALK) positive advanced non-small cell lung cancer (NSCLC).
Treatment of lung malignant neoplasms
Treatment of anaplastic large cell lymphoma, Treatment of inflammatory myofibroblastic tumours
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.)
L01ED01
L01XE16
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
L01E - Protein kinase inhibitors
L01ED - Anaplastic lymphoma kinase (alk) inhibitors
L01ED01 - Crizotinib
Absorption
The peak serum concentration was reached in 4 to 6 hours following an oral single-dose administration. Steady state was reached within 15 days when a dose of 250 mg twice daily was administered. The mean absolute bioavailability was 43% (range of 32% to 66%) following a single 250 mg oral dose. When taken with high-fat meal, AUC and Cmax were reduced.
Route of Elimination
Following the administration of a single 250 mg radiolabeled crizotinib dose to healthy subjects, 63% and 22% of the administered dose was recovered in feces and urine, respectively. Unchanged crizotinib represented approximately 53% and 2.3% of the administered dose in feces and urine, respectively.
Volume of Distribution
Mean volume of distribution (Vss) is 1772 L following intravenous administration of a 50 mg dose. This high volume of distribution suggest extensive distribution into tissue from plasma.
Clearance
The mean apparent clearance (CL/F) of crizotinib was lower at steady state (60 L/hr) after 250 mg twice daily than that after a single 250 mg oral dose (100 L/hr), which was likely due to autoinhibition of CYP3A by crizotinib after multiple dosing.
Crizotinib is metabolized by CYP3A4 and CYP3A5 in which these enzymes mediates the O-dealkylation of the drug.
Plasma terminal half-life, patients = 42 hours
Crizotinib is a tyrosine kinase receptor inhibitor. More specifically, it inhibits anaplastic lymphoma kinase (ALK), hepatocyte growth factor receptor (HGFR, c-MET), and Recepteur d'Origine Nantais (RON). Abnormalities in the ALK gene caused by mutations or translocations may lead to expression of oncogenic fusion proteins. In patients with NSCLC, they have the EML4-ALK gene. Crizotinib inhibits ALK tyrosine kinase which ultimately results in decreased proliferation of cells that carry the genetic mutation and tumour survivability.
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