Inhibitors of Receptor Tyrosine Kinases Flashcards
RTK inhibitors
Imatinib
Ibrutinib
Afatinib
Ceritinib
Imatinib
Gleevec
for CML or GI stromal tumor
at ATP site (INACTIVE) to get phosphate. PO take rest of life. Causes naus/vomit, edema, myelosupr. Causes Cardiotoxicity (not really tho)
–inhibits BCR-ABL TK. Induces apoptosis in BCRABL positive lines.
–Doesn’t deplete leukemic stem cells.
–Resistance develops in Philly chromosome +, from point mutation. Affect binding site or mode.
Inhibits 3A4, take with food.
Ibrutinib
for mantle cell lymphoma or CLL, NHL (B-cell malignancies)
Bruton’s tyrosine kinase inhibitor
–Causes myelosuppression because need to kill B-cells
AEs: hemorrhage, myelosupr, infections, rash
Avoid CYP3A4 inh and ind
Afatinib
for metastatic NSCLC with EGFR mutations. Inhibits EGFR and HER2
Ceritinib
ALK+ MSCLC. Inhibits ALK and EML4-ALK+ nsclc that’s resistant to crizotinib.
–Inhibits angiogensis! Causes GI tox, hepatotox, cardiotox