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galeterone
Known as:
Androsta-5,16-dien-3-ol, 17-(1h-benzimidazol-1-yl)-, (3beta)-
, Specific Androgen Receptor Modulator/CYP17 Lyase Inhibitor TOK-001
An orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits…
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National Institutes of Health
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2 relations
NCIt Antineoplastic Agent Terminology
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TOK-001
Papers overview
Semantic Scholar uses AI to extract papers important to this topic.
Review
2016
Review
2016
Emerging data on androgen receptor splice variants in prostate cancer.
Subing Cao
,
Y. Zhan
,
Yan Dong
Endocrine-Related Cancer
2016
Corpus ID: 5791724
Androgen receptor splice variants are alternatively spliced variants of androgen receptor, which are C-terminally truncated and…
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Review
2016
Review
2016
Galeterone for the treatment of advanced prostate cancer: the evidence to date
D. Bastos
,
E. Antonarakis
Drug Design, Development and Therapy
2016
Corpus ID: 4030802
Major advances have been achieved recently in the treatment of metastatic castration-resistant prostate cancer, resulting in…
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2016
2016
Specificity of anti-prostate cancer CYP17A1 inhibitors on androgen biosynthesis.
S. Udhane
,
B. Dick
,
Qingzhong Hu
,
R. Hartmann
,
A. Pandey
Biochemical and Biophysical Research…
2016
Corpus ID: 9647826
Highly Cited
2015
Highly Cited
2015
Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.
V. Njar
,
A. Brodie
Journal of Medicinal Chemistry
2015
Corpus ID: 25287488
In our effort to discover potent and specific inhibitors of 17α-hydroxylase/17,20-lyase (CYP17), the key enzyme which catalyzes…
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Highly Cited
2015
Highly Cited
2015
Galeterone and VNPT55 induce proteasomal degradation of AR/AR-V7, induce significant apoptosis via cytochrome c release and suppress growth of castration resistant prostate cancer xenografts in vivo
Andrew K. Kwegyir-Afful
,
S. Ramalingam
,
P. Purushottamachar
,
Vidya P Ramamurthy
,
V. Njar
OncoTarget
2015
Corpus ID: 8547302
Galeterone (Gal) is a first-in-class multi-target oral small molecule that will soon enter pivotal phase III clinical trials in…
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Review
2015
Review
2015
CYP17A1 inhibitors in castration-resistant prostate cancer
L. Gomez
,
J. Kovac
,
D. Lamb
Steroids
2015
Corpus ID: 23479200
Highly Cited
2014
Highly Cited
2014
Galeterone Prevents Androgen Receptor Binding to Chromatin and Enhances Degradation of Mutant Androgen Receptor
Ziyang Yu
,
Changmeng Cai
,
Shuai Gao
,
Nicholas I. Simon
,
Howard C. Shen
,
S. Balk
Clinical Cancer Research
2014
Corpus ID: 439862
Purpose: Galeterone inhibits the enzyme CYP17A1 and is currently in phase II clinical trials for castration-resistant prostate…
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Review
2013
Review
2013
Steroidal 5α-reductase and 17α-hydroxylase/17,20-lyase (CYP17) inhibitors useful in the treatment of prostatic diseases
J. Salvador
,
R. Pinto
,
S. Silvestre
Journal of Steroid Biochemistry and Molecular…
2013
Corpus ID: 31516382
Highly Cited
2013
Highly Cited
2013
Systematic structure modifications of multitarget prostate cancer drug candidate galeterone to produce novel androgen receptor down-regulating agents as an approach to treatment of advanced prostate…
P. Purushottamachar
,
Abhijit M. Godbole
,
+6 authors
V. Njar
Journal of Medicinal Chemistry
2013
Corpus ID: 10608886
As part of our program to explore the influence of small structural modifications of our drug candidate 3β-(hydroxy)-17-(1H…
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Review
2012
Review
2012
Targeting the androgen receptor in the management of castration-resistant prostate cancer: rationale, progress, and future directions.
R. Leibowitz-Amit
,
A. Joshua
Current Oncology
2012
Corpus ID: 7877138
Since the year 2000, tremendous progress has been made in the understanding of castration-resistant prostate cancer (crpc), a…
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