Interview
with Neil Love, MD from Breast Cancer Update for Medical Oncologists,
Program 4 2000
Play
Audio Below:
You
don’t affect the amount of messenger RNA, but what you do is
that you decrease the amount of estrogen receptor protein, and it
seems that you get increased degradation of the actual protein.
The second thing that we know about is that you shut down both AF-1
and AF-2 functions, whereas tamoxifen doesn’t do that and the
other SERMs don’t do that, too. The third thing we know is
that it appears not to have any estrogenic activity. For example,
with the other SERMs we know that they have an antiestrogen effect
on some tissues but they have an agonist effect on others. And that’s
why, for example, in the endometrium you see hyperplasia and sometimes
endometrial cancers, and that’s a negative agonistic effect,
whereas in another system, such as bone, that agonistic property
seems to be beneficial. And what we know about Faslodex is that
in the systems thus far tested it does not appear to have any agonistic
properties. That would clearly be beneficial in terms of the endometrium.
The question is, "Would it have a negative effect in terms of bone?"
And thus far from the studies that we have available, it doesn’t
appear to have any negative effect either in bone or in lipids.
It’s got no beneficial effect from what we can see, but it
has no negative effect either, so it seems to be neutral in those
sort of systems. Clearly we need more information about those systems
for long-term safety and efficacy, particularly in an adjuvant setting,
but it seems, as I said, that it’s got a different mechanism
of action both cellularly, but also in different tissues, too.
Similarities
and distinctions in the mode of action of different classes of antioestrogens
[Review]. Wakeling,
A. E. Endocrine-Related Cancer. 7(1):17-28, 2000 Mar. No abstract
Approaches
targeted to estrogen receptors for treatment of tamoxifen-resistant
breast cancer: A brief overview. Terakawa, N. (Reprint available from: Terakawa N Tottori Univ,
Sch Med, Dept Obstet & Gynecol Yonago Tottori 683 Japan)..
Oncology. 59(Suppl 1):3-4, 2000. No abstract
Treatment
with the pure antiestrogen faslodex (ICI 182780) induces tumor necrosis
factor receptor 1 (TNFR1) expression in MCF-7 breast cancer cells. Smolnikar,
K.; Loffek, S.; Schulz, T.; Michna, H., and Diel, P. (Reprint available
from: Smolnikar K DSHS Cologne, Inst Morphol & Tumor Res Carl
Diem Weg 6 D-50927 Cologne Germany). Breast Cancer Research &
Treatment. 63(3):249-259, 2000 Oct. In process
Symposium
overview: Estrogens and antiestrogens in managing the patient with
breast cancer. Newman,
L. A.; Wood, W. C.; Sellin, R. V.; Morrow, M.; Vogel, C., and Singletary,
S. E (Reprint available from: Singletary SE Univ Texas, MD Anderson
Canc Ctr, Dept Surg Oncol 1515 Holcombe Blvd,Box 106 Houston, TX
77030 USA).. Annals of Surgical Oncology. 7(8):568-574, 2000 Sep.
In process
