Abstract
LK or IGF1R: When selectivity hurts.
Highlights
The success of small molecule tyrosine kinase (TKI) inhibitors in cancer treatment and recent studies both in vitro and in vivo sparked interest in targeting the insulin-like growth factor receptor 1 (IGF1R)
Does this mean that inhibition of both receptors is better? Small molecule TKIs inhibit both IGF1R and insulin receptor (IR), including heterodimer and IR-IR homodimer conformations
In another phase I study in patients with solid tumors, an intermittent regimen of OSI-906 was associated with antitumor activity in two patients with adrenocortical carcinoma achieving partial responses
Summary
The success of small molecule tyrosine kinase (TKI) inhibitors in cancer treatment and recent studies both in vitro and in vivo sparked interest in targeting the insulin-like growth factor receptor 1 (IGF1R). Small molecule TKIs inhibit both IGF1R and IR, including heterodimer and IR-IR homodimer conformations. We conducted a phase I trial of OSI-906 (linsitinib), an IGF1R TKI, in patients with advanced solid tumors [4].
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