Crizotinib

Crizotinib
Image illustrative de l’article Crizotinib
Identification
Nom UICPA 3-[(1R)-1-(2,6-dichloro-3-fluorophényl)éthoxy]-5-(1-pipéridin-4-ylpyrazol-4-yl)pyridin-2-amine
No CAS 877399-52-5
No ECHA 100.166.440
Code ATC L01ED01
PubChem 11626560
SMILES
InChI
Propriétés chimiques
Formule C21H22Cl2FN5O
Masse molaire[1] 450,337 ± 0,024 g/mol
C 56,01 %, H 4,92 %, Cl 15,74 %, F 4,22 %, N 15,55 %, O 3,55 %,
Données pharmacocinétiques
Biodisponibilité 43%
Liaison protéique 91%
Métabolisme hépatique (CYP3A4/CYP3A5)
Demi-vie d’élim. 42 heures
Excrétion

fèces (63%), urine (22%)

Unités du SI et CNTP, sauf indication contraire.
modifier 

Le crizotinib est une molécule inhibitrice de plusieurs tyrosine kinases, en cours de développement dans le traitement de certains cancers.

Cibles

Il inhibe l'ALK (« Anaplastic lymphoma kinase »), le MET (« Mesenchymal-Epithelial Transition »)[2] et le ROS1[3]. Il existe cependant des formes résistantes correspondant à des mutations sur ALK[4] ou sur ROS1[5].

Évaluations

Dans les cancers pulmonaires non à petites cellules, dits « ALK+ » et résistants aux autres traitements, le crizotinib améliore les symptômes et la qualité de vie sans modifier la mortalité[6]. Il a également une activité tumorale dans ces mêmes cancers comportant un ré-arrangement du gène ROS1[7].

Voir aussi

Notes et références

  1. ↑ Masse molaire calculée d’après « Atomic weights of the elements 2007 », sur www.chem.qmul.ac.uk.
  2. ↑ Ou SH, Kwak EL, Siwak-Tapp C et al. Activity of crizotinib (PF02341066), a dual mesenchymal-epithelial transition (MET) and anaplastic lymphoma kinase (ALK) inhibitor, in a non-small cell lung cancer patient with de novo MET amplification, J Thorac Oncol, 2011;6:942-946
  3. ↑ Davies KD, Le AT, Theodoro MF et al. Identifying and targeting ROS1 gene fusions in non-small cell lung cancer, Clin Cancer Res, 2012;18:4570-4579
  4. ↑ Doebele RC, Pilling AB, Aisner DL et al. Mechanisms of resistance to crizotinib in patients with ALK gene rearranged non-small cell lung cancer, Clin Cancer Res, 2012;18:1472-1482
  5. ↑ Awad MM, Katayama R, McTigue M et al. Acquired resistance to crizotinib from a mutation in CD74–ROS1, N Engl J Med, 2013;368:2395-2401
  6. ↑ Shaw AT, Kim DW, Nakagawa K et al. Crizotinib versus chemotherapy in advanced ALK-Positive lung cancer, N Engl J Med, 2013;368:2385-2394
  7. ↑ Shaw AT, Ou SHI, Bang YJ et al. Crizotinib in ROS1-rearranged non–small-cell lung cancer, N Engl J Med, 2014;371:1963-1971

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