Seeley T, Langsetmo I, Stephenson R, Pacleb J, et al
Tumor progression studies and correction of anemia of chronic
disease in xenograft models.
ASN Annual Meeting -- Philadelphia
J Am Soc Nephrol
(Nov) 16:481A 2005

Anemia is a frequent complication of cancer in patients experiencing anemia
of chronic disease (also, Anemia of Cancer, AoC) and anemia associated with
cancer chemotherapy (Chemotherapy Induced Anemia, CIA). Patient response
rates to rHuEpo therapy have been reported in the 50% range in AoC and the
60% range in CIA. Factors adversely affecting erythropoietic response in AoC
are common to anemia of chronic disease (ACD) and include inflammatory
suppression of endogenous EPO production and erythroid progenitors, increased
iron retention, decreased iron absorption, and decreased iron bioavailability
in the bone marrow. FG-2216, a novel orally active inhibitor of HIF prolyl
hydroxylases designed to activate HIF2, up-regulates EPO and iron
mobilization genes, down-regulates hepcidin, and overcomes inflammatory
suppression of erythropoiesis. FG-2216 has also been shown to be efficacious
in treating anemic CKD patients.
Here, FG-2216 was administered to
animals for periods of 14 to 70 days in xenograft models of NSCLC. Key
hematology parameters (Hct, RBC, Hb) were suppressed in vehicle treated tumor
-bearing animals vs. controls, indicating the induction of ACD by xenograft
tumors. In tumor-bearing animals, FG-2216 treatment resulted in increases in
circulating EPO, RBC, Hb, and Hct, indicating that FG-2216 stimulated
erythropoiesis by overcoming functional iron deficiency and inflammatory
suppression.
As measured by final excised tumor weights, no
stimulation of tumor progression by FG-2216 treatment was observed. Similar
conclusions were obtained by caliper measurement of tumor volumes in
subcutaneous tumor studies. In these studies, FG-2216 treatment was
associated with a small to moderate inhibition of tumor development. In an
orthotopic model of lung tumor metastasis, FG-2216 treatment groups had
lowered incidence of tumor-induced morbidity and metastasis. FG-2216
treatment was well tolerated, with no reduction in mean body weights or
increase in frequency of animal deaths.
Together, this data supports
use of FG-2216 in AoC, CIA, and various other forms of EPO-hyporesponsive
ACD, such as uremic CKD patients.

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