Drug intelligence / Profile preview

imatinib + nilotinib

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Imatinib and nilotinib are small-molecule tyrosine kinase inhibitors (TKIs) that target the BCR-ABL fusion protein, the primary driver of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML). This specific entry refers to the TIKlet study (Tyrosine Kinase Inhibitors in chronic myeloid leukemia: Efficacy and Tolerability) conducted by the University of Pisa. The observational study evaluates the pharmacokinetics, pharmacogenetics, efficacy, and tolerability of these two drugs in CML patients. It specifically examines how genetic polymorphisms in transmembrane transporters, such as hOCT1, ABCB1, ABCG2, OCTN1, and OATP1A2, influence drug disposition and clinical outcomes, including Major Molecular Response (MMR) and Complete Cytogenetic Response (CCyR). While both drugs are used as standard-of-care therapies, the TIKlet study aims to optimize treatment by understanding interindividual variability in drug response.

Brand names
GleevecTasigna
Other names
Imatinib/Nilotinib
02

Targets

PDGFR (PDGFR family)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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