Info

Fibroids Miracle

Fibroids Treatment Diet

Get Instant Access

(single 15 pg/kg im dose)d

unchanged in urined

Indications: A, assisted reproduction (LH surge suppression for timing control); B, in oncology, to reduce the amount of testosterone made in patients with advanced symptomatic prostate cancer for which no other treatment options are available; said to overcome the need for anti-androgen coprescribing; C, hormone-sensitive cancers of the prostate; D, hormone-sensitive cancers of the breast (in premenopausal/perimenopausal women); E, certain benign gynecological disorders (endometriosis, uterine fibroids and endometrial thinning). "Cetrotide product information (FDA labeling approved 4-Apr-2008). hGanirelix Acetate (Organon) product information (30-June-2008 FDA labeling). cDegarelix Acetate (Ferring) product information (24-Dec-2008 FDA labeling). dWong, S. L., Lau, D. T., Baughman, S. A., et al.: J. Clin. Pharmacol. 44(5):495-502, 2004. iv, intravenous; im, intramuscular; NA, not available; sc, subcutaneous.

Indications: A, assisted reproduction (LH surge suppression for timing control); B, in oncology, to reduce the amount of testosterone made in patients with advanced symptomatic prostate cancer for which no other treatment options are available; said to overcome the need for anti-androgen coprescribing; C, hormone-sensitive cancers of the prostate; D, hormone-sensitive cancers of the breast (in premenopausal/perimenopausal women); E, certain benign gynecological disorders (endometriosis, uterine fibroids and endometrial thinning). "Cetrotide product information (FDA labeling approved 4-Apr-2008). hGanirelix Acetate (Organon) product information (30-June-2008 FDA labeling). cDegarelix Acetate (Ferring) product information (24-Dec-2008 FDA labeling). dWong, S. L., Lau, D. T., Baughman, S. A., et al.: J. Clin. Pharmacol. 44(5):495-502, 2004. iv, intravenous; im, intramuscular; NA, not available; sc, subcutaneous.

Figure 20.33 • Primary sequences and selected substructures for marketed GnRH antagonists.

placed in the antagonists with structural moieties that engage the receptor but do not allow receptor activation. Additional structure-activity information came from studies of cyclic peptides,138,139 which, together with information from protein structure modeling (see discussion that follows), indicated a relatively large binding pocket formed within the bundle of the transmembrane helices I to VII of the GnRH-R. (Although there are genes corresponding to GnRH-R1 and GnRH-R2 subtypes, the latter is apparently not expressed in humans.) Abarelix incorporates backbone n-methylation at Tyr5. All are decapeptides like GnRH itself, but unlike GnRH, incorporate alaninamide rather than glycinamide at the c-terminus. Rather than having a pyro-Glu at the N-terminus as in the native hormone, all are instead n-acetylated. Each has at least one strongly basic amino acid in its sequence, at residue 8, thus these peptides are formulated as salts. The counterion is acetate in all cases. Ganirelix is a diacetate, having an additional basic

Was this article helpful?

0 0
51 Tips for Dealing with Endometriosis

51 Tips for Dealing with Endometriosis

Do you have Endometriosis? Do you think you do, but aren’t sure? Are you having a hard time learning to cope? 51 Tips for Dealing with Endometriosis can help.

Get My Free Ebook


Post a comment