Kinase Inhibitors

A kinase inhibitor is more accurately called a protein kinase inhibitor. This is a special type of enzyme that blocks the action of one or more protein kinases. Protein kinases are enzymes that add a phosphate group to either a protein or other organic molecule; and phosphate groups can turn a protein off. In most cases, these phosphate groups are added to one of several amino acids that reside on the protein, typically the serine, threonine, or tyrosine amino acids. For this reason most of the kinase inhibitors (for proteins) are referred to by the amino acids they inhibit. In fact, most kinase inhibitors act on both serine and threonine. Tyrosine kinase inhibitors work on tyrosine and there are a number of these drugs that will work on all three.

Kinase Inhibitors Drugs

Below is a list of some of the drugs in the kinase inhibitor class.

  • Afatinib
  • Axitinib
  • Cetuximab
  • Dasatinib
  • Fostamatinib
  • Lapatinib
  • Imatinib
  • Sunitinib

Kinase Inhibitors Uses

Many different forms of cancer and inflammatory diseases will involve the addition of phosphate groups to proteins. Hence, these types of kinase inhibitors are able to help in the treatment of many cancers and inflammatory diseases.

Different kinase inhibitors work in slightly different ways, making them more valuable in the treatment of specific types of cancers and inflammations than others. Some will work by blocking a kinase gene from binding to ATP and preventing the formation and future rapid division and growth of a cancerous cell. Some of the common uses of kinase inhibitors are listed below.

  • Advanced non-small cell lung cancer
  • Advanced colorectal cancer
  • Wet macular degeneration
  • Renal cell carcinoma
  • Breast cancer
  • Thyroid cancer (certain types)

Kinase Inhibitors Side Effects

As is the case with most of the cancer medications currently available, there are a number of side effects that can occur from the use of kinase inhibitors. It is also important to remember that the specific side effects associated with kinase inhibitors must be matched up to the particular drug being used. Some are only meant to be used in very well-defined situations and conditions. Some of the side effects of kinase inhibitors are listed below.

  • Liver toxicity
  • Kidney failure
  • Electrolyte anomalies
  • interstitial lung disease
  • Thyroid dysfunction
  • Blood clots
  • GI problems
  • Congestive heart failure

Kinase Inhibitors Interactions

Some of the major drug interactions associated with kinase inhibitors are associated with over-the-counter drugs and medications like St. John's wort. Acid suppressive drugs like proton pump inhibitors and normal antacids can significantly alter the absorption of most types of tyrosine kinase inhibitors.

Some of the kinase inhibitors may also have drug interactions in the presence of citrus fruits. The most notable of these is grapefruit. This may actually lead to higher blood concentrations, resulting in too much of the medication being absorbed.

Main Kinase Inhibitors Drugs

Gleevec Xeljanz Sprycel

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