Released on = March 6, 2006, 7:20 am

Press Release Author = La Merie Business Intelligence

Industry = Biotech

Press Release Summary = At least six fully human or humanized antibodies against
insulin-like growth factor-1 receptor (IGF-1R) are in early clinical development or
close to phase I


Press Release Body = BARCELONA, Spain | March 6, 2006 | The Business Intelligence
firm La Merie S.L. reported today that antibodies are at the forefront of novel
cancer therapeutics targeting the insulin-like growth factor-1 receptor (IGF-1R).
Pfizer is leading the field with the fully human IgG2 antibody CP-751,871 under
investigation for multiple myeloma and advanced non-small cell lung cancer. Five
other companies are closely following with antibody projects. Only six companies are
currently visible with small molecule inhibitors targeting the IGF-1R tyrosine
kinase which are not always selective for IGF-1R. INSM-18 from Insmed and the
University of California San Francisco is a dual inhibitor of IGF-1R and Her2/neu
and is the only clinical stage IGF-1R small molecule antagonist (phase I/II in
prostate cancer). These results and more were found in a search conducted by La
Merie Business Intelligence published in the March 6 issue of R&D Pipeline News,
edited by La Merie. The competitor analysis of CB1 antagonists can be acquired at
www.pipelinereview.com, La Merie's News Center and Online Store.

Although the IGF-1 receptor was first cloned in 1986, it was the success of targeted
drugs such as trastuzumab and imatinib that tyrosine kinase inhibitors and growth
factor receptor blockers became hot targets. Now companies are aggressively pursuing
compounds that target IGF-1R. Other reasons for the long delay in bringing compounds
against IGF-1R into the clinic may be: 1) the fear that blocking IGF-1R in cancer
therapy would also block the insulin receptor and signaling (70 % homology with
IGF-1R) and, thus might be diabetogenic; and 2) the expression of IGF-1R in normal
tissue throughout the body. Aventis selected an antibody which does not bind to the
closely related insulin receptor. However, preclinical data indicate a limited
spectrum of tumor cell lines against which the antibody was effective.

While antibodies are exquisitely selective inhibitors of the IGF-1R function by
inducing rapid internalization and down regulation of the receptor, small molecule
tyrosine kinase inhibitors suffer from a lack of selectivity because of binding to a
well conserved site. In fact, several of the IGF-1R tyrosine kinase inhibitors in
development are dual inhibitors, and in general do not lead to internalization and
downregulation. Nevertheless, small molecule IGF-1R inhibitors offer the advantage
of the ability to control the duration of drug exposure in contrast to long-acting
antibodies.

Apart from antibodies and small molecules, there are individual approaches using
peptides, proteins or antisense oligonucleotides to antagonize IGF-1R. The latter
one has been evaluated as a topical cream to treat patients with psoriasis, but
needs further dose optimization.

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About La Merie

La Merie S.L. is a Business Intelligence enterprise fully dedicated to provide high
quality R&D information to the biopharmaceutical industry. La Merie offers
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information visit www.lamerie.com.

SOURCE: La Merie Business Intelligence

Web Site = http://www.pipelinereview.com/joomla/content/view/1424/1/

Contact Details = Jorge Márquez
La Merie Business Intelligence
C/ Caspe, 33B, 4º, 2ª
E-08010 Barcelona
Tel +34-93-342 91 97
Fax +34-93-342 91 98
e-mail: jorge.marquez@lamerie.com
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