Inhibition of HSP90 with AUY922 induces synergy in HER2-amplified trastuzumab-resista

['lizbeth]

The above study is active, but not recruiting.

[donocco]

I didnt research AUY922 (I will) but a former post mentioned Dacomitinib so I printed some articles on this investigational drug.

Dacomitinib is an interesting drug. It is a Tyrosine Kinase Inhibitor. Tyrosine is an amino acid with an OH group at its end. Its a derivative of Phenylalanine. When you start reading about investigational drugs you often will run into the words Tyrosine Kinase Inhibitor or TKI for short. I don't
want to get too chemical but when a PO4 or phosphate group
attaches onto the OH group of Tyrosine the cancerous gene becomes activated. Its like turning on the ignition of a car. The molecule ATP goes into a special "pocket" of
the molecule and provides the phosphate group that activates the cancer inducing protein. TKI drugs push the ATP molecule out of the "pocket." The first drug that did this well was Geevec (Imatinib) for Chronic Granulocytic Leukemia.

Dacomitinib is also a TKI. It inhibits the Epidermal Growth Factor Receptor (EGFR), the Her2 Neu protein receptor and the HER4 receptor (don't know about this one).

There were some studies in non small cell carcinoma of the lung. The dosage of Dacomitinib was 45mg daily. The main side effects were diarrhea, fatigue, mouth sores, mouth dryness, rash and acne like eruptions.

Paul