Targeted therapy

ARRAY is developing targeted therapies to inhibit molecular pathways involved in disease progression

Targeted therapies are designed to block or interfere with the part of an enzyme, protein or other molecule that is involved in the development or progression of a disease. In diseases such as cancer, targeted therapies can cause less harm to normal cells than conventional therapies like chemotherapy.

Attractive targets for potential therapies include

  • Targets that are found in diseased cells, but not healthy cells, or are found in a much higher quantity in diseased cells than in healthy cells, such as a protein that is overexpressed only in cancer cells

  • Abnormal chromosomes

  • Mutated proteins

Targeted therapies work by:

  • Lowering levels of the substance that fuels the growth or spread of disease;

  • Blocking the receptor on the surface of the cell that the enzyme, protein or molecule binds to; or

  • Preventing transmission of signals within the cell

Many targeted therapies are small molecules. Small molecule drugs can be taken orally, have the ability to enter cells to interfere with the target directly, have greater absorption in the body (bioavailability) than large molecule drugs and can be combined with other medications such as immunotherapy.

A key area of research for Array

Tyrosine kinases are enzymes, or chemical messengers, that play a central role in regulating cell growth, differentiation and survival by transmitting signals through a complex signaling network into the cell nucleus. In diseases such as cancer, tyrosine kinases in tumor cells can be mutated, expressed at high levels or sustain the signaling pathway in an activated state, making them an important therapeutic target. Tyrosine kinase inhibitors (TKIs) are drugs designed to block the activity of single or multiple tyrosine kinases.

The mitogen-activated protein kinase (MAPK) cascade is one of the most common cell-signaling pathways necessary for cell growth, proliferation and survival. Mutations in key tyrosine kinase genes involved in this signaling pathway can lead to uncontrolled cell proliferation, survival, invasion and metastasis. Dysregulated MAPK signaling is associated with numerous types of cancer. Key enzymes that use the MAPK pathway include RAS, RAF, MEK and ERK.

Tyrosine kinase inhibitors