2-Methoxyestradiol disulfamate
2-Methoxyestradiol disulfamate (developmental code STX-140; also known as 2-methoxyestradiol 3,17β-"O","O"-"bis"(sulfamate)) is a synthetic, oral active anti-cancer medication which was previously under development for potential clinical use. It has improved potency, low metabolism, and good pharmacokinetic properties relative to 2-methoxyestradiol (2-MeO-E2). It is also a potent inhibitor of steroid sulfatase, the enzyme that catalyzes the desulfation of steroids such as estrone sulfate and dehydroepiandrosterone sulfate (DHEA-S).

2-Methoxyestradiol disulfamate exhibits anti-angiogenic activity and induction of cell cycle arrest and apoptosis in human tumor xenografts, with clinical potential for hormone–independent tumors. Some of this activity stems from tubulin binding at the colchicine site and disruption of interphase microtubules. 2-Methoxyestradiol disulfamate is highly active in tumors that are resistant to chemotherapy.

In xenograft models of breast and prostate cancer complete cures were achieved after oral treatment with 2-methoxyestradiol disulfamate and drug-resistant tumors also shrank in size after oral treatment. Conventional treatments for hormone-independent cancers targeting tubulin are associated with side effects, such as neurotoxicity, and can only be given infrequently and intravenously. 2-Methoxyestradiol disulfamate is more effective on the same tumors, blocks metastatic spread without the peripheral neuropathy associated with current clinical anticancer drugs.
Q174211
synthetic
Concept
Q285166
oral active
Concept
Q974135
anti-cancer medication
Concept
Q2066956
potency
Concept
Q1057
metabolism
Concept
Q323936
pharmacokinetic
Concept
Q4596897
2-methoxyestradiol
Concept
Q427492
inhibitor
Concept
Q17832124
steroid sulfatase
Concept
Q8047
enzyme
Concept
Q82264
catalyze
Concept
Q994559
desulfation
Concept
Q177911
steroid
Concept
Q5401864
estrone sulfate
Concept
Q2505402
dehydroepiandrosterone sulfate
UNK
Q574834
anti-angiogenic
Concept
Q422492
tubulin
Concept
Q55505
xenograft
Concept
Q945238
peripheral neuropathy
Concept
Q27097624
2-Methoxyestradiol disulfamate
UNK
Q27097624
2-Methoxyestradiol disulfamate
UNK
Q27097624
2-Methoxyestradiol disulfamate
UNK
Q27097624
2-Methoxyestradiol disulfamate
UNK
2020-03-17T00:00:00Z^^http://www.w3.org/2001/XMLSchema#dateTime
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molecular function
instance of