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Sutent/Sunitinib (Cheer up!)

Category: Drugs
Posted on: March 12, 2009 8:42 AM, by Molecule of the Day

Ready for some good news? Just now, Pfizer announced it was stopping Phase 3 trials of a new cancer treatment, Sutent, early - because it was working so well. Typically, stopping clinical trials of a drug early is bad news - your drug is hurting people, or it doesn't work. Once in awhile, if a drug is working especially well, the trials are stopped early and the placebo group is allowed to switch to the trial drug. That's what just happened here. The other good news? It was for pancreatic cancer. Pancreatic cancer is often hard to treat, because it often does not present many symptoms early on, so patients are often diagnosed very late. Another treatment for this is very good news.


Sutent inhibits a class of enzyme called tyrosine kinases. These enzymes hang a phosphate off of tyrosine amino acids in certain proteins. These phosphate groups act to send signals to the rest of the cell: "make some more of yourself," "shut yourself down," etc. Inhibiting some of these enzymes is proving to be a useful way of targeting cancer: Gleevec is another such drug.


Disclosure statement: the author holds no PFE position.

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Comments

1

Bilirubinesque?

Posted by: Uncle Al | March 12, 2009 11:31 AM

2

Do we know how they find this molecule ?

Posted by: Bjonnh | March 12, 2009 4:53 PM

3

Hooray! That IS good news!

(And a good tie-in to my current Cell Bio class in which I have a test including tyrosine kinase signaling tomorrow.)

Posted by: katie | March 12, 2009 6:43 PM

4

A short story goes this: a startup kinase biotech named SUGEN in Bay area in-licensed in tyrphostins from acedemic group in Israel and continued working on them for several more years. (Tyrphostins are simple Knoevagel condensation product of aromatic aldehydes with oxindoles). First two SUGEN compouns from this class failed to show efficacy in the clinic (SU 5416: poor solubility, SU 6668: too high human protein plasma binding). The third clinical compound SU 11248 eventually became Sutent. The compound was almost dropped because of worrisome organ toxicity in animals but with help of Pharmacia that acquired SUGEN the clinical trials went ahead. Improved back-up to Sutent with reduced organ accumulation and cardiotoxicity SU 14813 eventually went to phase I before being canned by Pfizer who bought Pharmacia. Pfizer then summarily fired everyone in SUGEN and transferred its unfinished projects and several pre-clinical anti-cancer compounds to Agouron Pfizer site in San Diego where they all died quietly.

Posted by: milkshake | March 13, 2009 5:25 AM

5

Correct me if I am wrong, but Sutent was found to be effective in Neuroendocrine tumors of the pancreas and not "pancreas cancer." Pancreas cancer is still without any breakthrough medications (although Gemcitibine has some capacity to fight pancreatic cancer.)

Neuro-endocrine tumors tend to be slower growing and do not necessarily start in the pancreas. Both sutent and the upcoming drug Afinitor (Everlimus, by Novartis) seem to help the neuro-endocrine tumors regress.

Posted by: David Young | March 27, 2009 2:53 PM

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