Search results for "Pharmacologic Substance[C1909]|Hormone Therapy Agent[C147908]|Hormone Antagonist[C547]" in comments (approximate match)
Lilopristone (ZK 98.734) has a high affinity for progesterone receptors. The progesterone antagonistic effects of ZK 98.734 could be a result of the decrease in progesterone synthesis by the corpus luteum and/or placenta in addition to the interferen...
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Sufugolix (TAK-013 or 5-(N-benzyl-N-methylaminomethyl)-1-(2,6-difluorobenzyl)-6-[4-(3-methoxyureido)phenyl]-3-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione) is a highly potent and orally active non-peptide antagonist of luteinizing hormone-releasing...
Topilutamide is a non-steroidal anti-androgen. Topilutamide downregulated androgen receptor expression by 40% at 3 uM and up to 95% at 10 uM in LNCaP Cells After 48-h drug incubation. While highly hydrophobic and hydrolytically degradable, it is syst...
Turosteride [FCE 26073] is a selective 5α-reductase inhibitor being developed by Pharmacia Corporation. Turosteride inhibits human and rat prostatic 5 alpha-reductases with IC50 values of 55 and 53 nM, respectively. It was in phase II clinical trials...
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Asoprisnil (J867) is a novel selective steroid receptor modulator that shows unique pharmacodynamic effects in animal models and humans. Asoprisnil, its major metabolite J912, and other structurally related compounds represent a new class of progeste...
IZONSTERIDE, a benzoquinolinone, is a selective inhibitor of the 5-alpha reductase, with antagonistic effect on both the type I (liver, skin, hair follicles) and type II (prostate) isoforms of the enzyme. It is a competitive inhibitor of type I 5-alp...
Bifluranol (brand name Prostarex), a fluorinated bibenzyl anti-androgen was developed as a nonsteroidal estrogen and was studied for the treatment of benign prostatic hyperplasia. Besides, was shown that bifluranol inhibited 17 alpha-hydroxylase/C17-...
Retosiban is a small molecule oxytocin receptor antagonist that is under evaluation for treatment of premature labor. Retosiban was found to be safe in healthy non-pregnant volunteers in phase I studies. Intravenous retosiban also had good safety and...
Topterone is an anti-androgen agent. Topterone inhibited stimulation of flank organ development of castrated immature male hamsters by both testosterone and dihydrotestosterone. Topical application of topterone on the flank organs of the male hamster...