Oncology Drugs: Kinase Inhibitors

Vocabulary and drug profiles for kinase inhibitors in oncology, including specific generations of EGFR inhibitors and key intracellular signaling targets.

Kinases

Enzymes such as tyrosine, serine, or lipid kinases that phosphorylate a residue of another protein or lipid, thereby changing its enzymatic activity, location, or conformation.

Phosphatases

Proteins that are often paired with kinases to act as on/off switches within cellular signaling pathways.

EGFR (Epidermal Growth Factor Receptor)

A receptor tyrosine kinase also known as $HER1$, which is a target for drugs indicated for Non-Small Cell Lung Cancer (NSCLC).

Erlotinib

A Generation $1$ EGFR inhibitor that reversibly binds to the ATP binding site of the receptor.

Afatinib

A Generation $2$ EGFR inhibitor that provides irreversible inhibition via covalent modification and also inhibits $HER2$.

Osimertinib

A Generation $3$ EGFR inhibitor that provides irreversible inhibition and can inhibit EGFR with the $T790M$ mutation.

Lapatinib

A prototype $HER2$ inhibitor indicated for $HER2$-positive Breast Cancer; it carries warnings for hepatotoxicity and cardiotoxicity.

Crizotinib

A prototype ALK (anaplastic lymphoma kinase) inhibitor indicated for anaplastic large cell lymphoma (ALCL) and NSCLC.

Vemurafenib

A prototype BRAF inhibitor indicated for melanoma in patients with $V600E$ or $V600K$ mutations.

Trametinib

A prototype MEK inhibitor indicated for melanoma service, often used in combination with BRAF inhibitors.

BCR-ABL

An abnormal fusion tyrosine kinase resulting from the translocation of chromosome $9$ ($ABL$) and chromosome $22$ ($BCR$).

Philadelphia chromosome

The name for the $t(9;22)$ translocation seen in approximately $95$ percent of Chronic Myeloid Leukemia (CML) cases.

Imatinib

The prototype inhibitor for BCR-ABL used to treat Chronic Myeloid Leukemia (CML).

Everolimus

A prototype mTOR (mammalian target of rapamycin) inhibitor indicated for advanced renal cell carcinoma.

Sunitinib

A multi-tyrosine kinase inhibitor that targets vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), and stem cell factor receptor (c-KIT).

Sorafenib

A multi-tyrosine kinase inhibitor that targets VEGFR, PDGFR, c-KIT, and Fms-like tyrosine kinase $3$ (FLT$3$).

PTEN

An intracellular inhibitory phosphatase that suppresses kinase signaling; it can be defective in cancer through mutation, gene deletion, or promoter methylation.

-ciclib

The naming suffix for small-molecule inhibitors in the category of Cyclin-dependent kinase $4$ and $6$.

-lisib

The naming suffix for small-molecule inhibitors in the category of PI$3$K.

-rafenib

The naming suffix for small-molecule inhibitors in the category of BRAF.