Tyrosine kinase inhibitors with the indication: in Philadelphia chromosome-positive chronic myeloid leukemia.
Images (3)
Nilotinib
DefinitionThis section has been translated automatically.
General informationThis section has been translated automatically.
Nilotinib is a phenylamino-pyrimidine derivative that exhibits 20- to 30-fold higher affinity for the BCR-ABL oncoprotein than imatinib in vitro.
Like imatinib, nilotinib attaches only to the inactive conformation of BCR-ABL and binds with high affinity to the ATP-binding site. Attachment to the BCR-ABL binding pocket is possible even in the presence of mutations that cause resistance to imatinib. While nilotinib predominantly targets BCR-ABL, imatinib has a comparatively higher affinity for platelet derived growth factor receptor (PDGFR) tyrosine kinase. Listing the different tyrosine kinases by decreasing drug affinity, the tyrosine kinase preference for nilotinib is BCR-ABL > PDGFR > KIT and for imatinib PDGFR > KIT > BCR-ABL.
Complication(s)This section has been translated automatically.
A notable side effect of nilotinib therapy is the occurrence of ulerythema ophryogenes as well as generalized keratosis pilaris (Leong WM 2016; Tawil MH et al 2017).
LiteratureThis section has been translated automatically.
- Leong WM (2016). Nilotinib-induced keratosis pilaris. Case Rep Dermatol 8:91-96.
- Tawil MH et al (2017) Nilotinib-induced keratosis pilaris associated with alopecia areata and eyebrow thinning. Int J Trichology 9:87-89.