Exelixis, Inc. (Nasdaq: EXEL) has recently submitted an investigational new drug application (IND) to the USFDA for XL228, the company’s novel anticancer compound designed to inhibit the insulin-like growth factor type-1 receptor (IGF1R), Src and Abl tyrosine kinases – targets that play crucial roles in cancer cell proliferation, survival and metastasis.
XL228 is a potent inhibitor of the T315I mutant form of the Abl protein, which is associated with resistance to currently approved therapies like Gleevec® (imatinib mesylate) and Sprycel™ (dasatanib); administration of which in preclinical studies resulted in significant tumor growth inhibition and regression in xenograft tumor models.
According to George A. Scangos, president and chief executive officer of Exelixis:
Read the full press release."We believe that XL228 is the first compound to advance into the clinic with potent, low-nanomolar activity against both wild-type Abl and the T315I mutant form of Abl that is seen in a significant fraction of chronic myelogenous leukemia (CML) patients who have become resistant to treatment with Gleevec®.
"Targeting this mutation, in addition to potently inhibiting wild-type Abl and Src may address the increasing medical needs of CML patients who do not respond or develop resistance to Gleevec® or Sprycel™ and provides us with a potentially accelerated path through clinical development.”
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