KinasePro

Kinase Chemistry – Just a year and a half behind the times.

Tasigna Approved

Posted by kinasepro on October 30, 2007

aka nilotinib, AMN-107 is a Novartis‘ follow-on to Gleevec now approved for CML.

O=C(C1=CC=C(C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C)NC4=CC(C(F)(F)F)=CC(N5C=C(N=C5)C)=C4

wiki; clinic; WO/2002/022597

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4 Responses to “Tasigna Approved”

  1. Pablo said

    Someone knows why according to the label, “Patients with low blood potassium or magnesium should not use Tasigna”?

  2. pf01273 said

    Pablo,

    Tasigna also has a black-box warning about possible irregular heartbeat/sudden death. This is caused by long QT syndrome due to blockade of the hERG channel by the drug.

    If you have low potassium levels this can also affect the functioning of the hERG channel, increasing the likelihood of long QT syndrome occuring.

    Furthermore, correct levels of magnesium in the body are also required to to maintain healthy potassium levels, therefore the two are, I guess, directly linked.

  3. Pablo said

    Thanks pf01273. It makes me wonder that Novartis did not weed out that toxicity preclinically…the QT/hERG issue has been known forseveral years.

  4. pf01273 said

    Yes, it’s not ideal however as this is a second-line therapy for patients where Gleevec has not worked I guess you can get away with it?

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