Kinase inhibitors Flashcards
Abemaciclib
CDK4/6 inhibitor - breast cancer
Acalabrutinib
Bruton’s tyrosine kinase
Used in CLL, SLL, mantle cell lymphoma
ADR - AF/aflutter, transient lymphocytosis, increased bleeding from platelet dysfunction
Afatinib
EGFR, HER2, HER4 receptor inhibitor
Alectinib
ALK receptor
For ALK-positive NSCLC
Axitinib
VEGF receptor inhibitor
Baricitinib
JAK 1 and JAK2 inhibitor
Used for RA, atopic dermatitis, COVID
Do not use in severe renal impairment
Binimetinib
Mitogen-activated extracellular kinases (MEK) 1 + 2
Used in melanoma
Brigatinib
ALK receptor, ROS1
NSCLC
Carbozatinib
Hepatocyte growth factor receptor (HGFR, c-Met), VEGFR type 2, AXL
Used in HCC and advanced RCC
Ceritinib
ALK receptor
Cobimetinib
MEK1, MEK2
Crizotinib
ALK receptor, c-Met, ROS1
Dabrafinib
BRAF including V600E and V600K
Dasatinib
BCR-ABL1, Src family, stem cell factor receptor, PDGFR
Used in CML, phil chromosome positive ALL
Encorafenib
BRAF inhibitor
Entrectinib
Tropomysin receptor tyrosine kinase, ROS1, ALK receptor
Erlotinib
EGFR
Used in NSCLC, pancreatic Ca
Gefitinib
EGFR
Ibrutinib
BTK
Used for CLL, SLL, mantle cell lymphoma, Waldenstrom macoglobulinaemia
Idelalisib
PI3K inhibitor
Imatinib
BCR-ABL1, c-Kit, PDGFR
Used in CML, GIST, phil chromosome positive ALL, MDS
Lapatinib
EGFR, HER2
Lenvatinib
VEGFR types 1-3, fibroblast growth factor types 1-4, PDGFR, c-Kit, RET
Lorlatinib
ALK receptor, ROS1
Midostaurin
VEGFR type 2, PDGFR, c-Kit, FLT-3, protein kinase C
Used in AML, advanced systemic mastocytosis
Nilotinib
BCR-ABL1, c-Kit, ephrin receptor, PDGFR
Used in CML
Nintedanib
VEGFR types 1-3, PDGFR, FGFR types 1-3
Used in IPF
Osimertinib
EGFR including T790M mutation
Used in NSCLC
Palbociclib
CDK4/6 inhibtor
Pazopanib
VEGFR types 1-3, PDGFR, c-Kit
Ponatinib
BCR-ABL1, c-Kit, PLT-3, RET
Regorafenib
VEGFR types 1-3, PDGFR, c-Kit, RET
Ribociclib
CDK4/6 inhibitor
Used in advanced or metastatic breast cancer
Ruxolitinib
JAK 1, JAK2
Used in myelofibrosis, PCV
Sorafenib
VEGFR types 2-3, PDGFR, c-Kit, FLT-3
Used in RCC, HCC, thyroid carcinoma
Sunitinib
VEGFR types 1-3, PDGFR, c-Kit, FLT-3
Tofacitinib
JAK1, JAK2, JAK3
Trametinib
MEK1, MEK2
Upadacitinib
JAK1
Used in RA, psoriatic arthritis, ankylosing spondylitis
Vandetanib
VEGFR types 2-3, EGFR, RET
Vemurafenib
BRAF V600E and V600K
Used in metastatic melanoma with BRAF V600E mutation