TKI

[Guest guest]

Karine, TKI's are the big 3 - Gleevec, Sprycel & Tasigna.

Tyrosine Kinase Inhibitor is an oral chemo, as opposed to intravenous chemos we

usually associate with tumor-like cancers. Since CML is a liquid tumor, it is

treated differently. These TKI's were developed to kill off the BCR ABL protein

that

causes the cancer. The oncogenes lead to the over-expression of the receptor

in the cancer cells that promote the tumor cell growth. In the case of CML, it

is the growth of the immature white cells (Ph+). If I am wrong, I am sure

someone

who is more proficient will correct me.

Since Beth will be receiving Dastinib, I thought of posting a little about it

here for the newcomers and those interested parties.

http://www.drugdevelopment-technology.com/projects/dasatinib/

[Guest guest]

>

> Karine, TKI's are the big 3 - Gleevec, Sprycel & Tasigna.

> Tyrosine Kinase Inhibitor is an oral chemo, as opposed to intravenous chemos

we usually associate with tumor-like cancers. Since CML is a liquid tumor, it

is treated differently. These TKI's were developed to kill off the BCR ABL

protein that

> causes the cancer.

___________________________

Hi Karine,

Just to add to what Lottie has written:

TKI does stand for tyrosine kinase inhibitor.

Tyrosine kinase is an enzyme found in the body and is actually involved in other

bodily functions also, but for us, it is the enzyme that allows the ph+ (cml)

cell to keep reproducing and creating more cml cells.

So, these drugs are blocking (inhibiting) the tyrosine kinase that the cml cell

needs and those cml cells die. To do this, the drug actually has to get into the

nucleus of the cell.

This is why these drugs are also called molecularly targeted drugs.....because

the specific defect in cml is known, it is possible to specifically target that

defect and keep the cell from continuing to survive.

This is the principle reason why Gleevec is hailed as a breakthrough in cancer

research and treatment. With the development of this drug, Dr. Druker

demonstrated (proved) that you could have a specific drug that targeted the

cancer cell and to a great extent spared other 'normal' cells. Prior to this,

and still with many cancers, the drugs used are called cytogenic drugs.....and

usually they target and kill off any rapidly reproducing cells....which is why

with traditional chemo, people lose their hair (which reproduces rapidly), often

lose fertility, etc.

CML was the ideal disease to work on creating a targeted drug because the

specific defect of CML (the Philadelphia chromosome) was known since about 1960

and pretty well understood. So, depending on the point of view that you wish to

take, this is why people would say that 'CML was the better leukemia' to get.

Prior to all this development it was not.

I know, because I am his patient and see him at least every 6 months, that Dr.

Druker is working in his lab to create similar targeted drugs for the other

forms of leukemia, but it is not as easy because there are more variables in the

other forms of leukemia. Genetically and molecularly, CML is a relatively simple

cancer in the chronic stage. 95% of early CML patients have the Philadelphia

chromosome as their only chromosomal defect. The disease becomes more

complicated and harder to control and treat as it progresses because other

chromosomal defects often develop.

All this is maybe more than you wanted to know, but someone might be interested?

I find it pretty fascinating.

Hooray for your Mom.........she is doing great on Gleevec!

C.