Background: Platelet-derived Growth Factor Receptor (PDGFR) is a kind of Receptor Tyrosine Kinases
(RTKs). PDGFR Tyrosine Kinase Inhibitors (TKIs) which are small molecule inhibitors targeting PDGFR prevent
and block cell proliferation signal transduction pathways. Recently, there have been 11 TKIs (including imatinib,
sunitinib, regorafenib, sorafenib, pazopanib, axitinib, dasatinib, nilotinib, lenvatinib, cabozantinib and ponatinib)
targeting PDGFR approved by FDA for the treatment of chronic myelogenous leukemia, gastrointestinal stromal
tumors, renal cell carcinoma et al. Pharmacokinetics (PK) reflects the processes of drugs in body, while pharmacodynamics
(PD) reflects the efficacy. Genetic polymorphisms of metabolizers and transporters contribute to highly
inter-individual variability in PK and PD. This review aims to introduce the clinical applications, instruction and
usage, PK, PD and pharmacogenetics of these PDGFR TKIs.
Methods: In vivo and in vitro studies about PDGFR TKIs were searched from PubMed. Data and information were
analyzed and summarized.
Results: The overview of (1) general information on PDGFR kinase inhibitors; (2) PK parameters of PDGFR kinase
inhibitors; (3) metabolic enzymes and transporters of PDGFR kinase inhibitors; (4) main drug interactions of PDGFR
kinase inhibitors; (5) adverse events of PDGFR kinase inhibitors; and (6) genetic polymorphism on PK and PD of
PDGFR kinase inhibitors, was exhibited and discussed in this review.
Conclusion: This review summarized the general information, PK, metabolic enzymes and transporters, main drug
interactions, adverse events and pharmacogenetics of FDA approved PDGFR TKIs. Studies showed that Single nucleotide
polymorphisms of metabolic enzymes and transporters had influence on the PK and PD of PDGFR TKIs.