IP Library › Granted Patent US 12,697,322
Granted Patent B2
US 12,697,322 · App. 17/771,180 · Granted Aug 4, 2026

Methods of treating cancer using androgen receptor antagonists

Inventors: Christine Chaffer (New South Wales, AU); Beatriz Pérez San Juan (New South Wales, AU)
Assignee: Garvan Institute of Medical Research
A61K31/4192A61K31/277A61K31/4166A61K31/58A61K45/06A61P35/00
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Quick Facts
Patent No.
US 12,697,322
App. No.
17/771,180
Filed
Apr 22, 2022
Granted
Aug 4, 2026
Kind
B2
Art Unit
1622
USPC
514/171
Abstract

The present disclosure generally relates to cancer and methods of treating and diagnosing cancer.

Claims (11)

1 . A method of sensitizing a cancer cell in a subject to an anti-cancer agent, comprising administering to the subject an androgen receptor antagonist, wherein the cell is a breast cancer cell, wherein the anti-cancer agent is docetaxel, paclitaxel, or doxorubicin, and wherein the androgen receptor antagonist is seviteronel.

2 . The method according to claim 1 wherein the cancer cell is a poorly tumourigenic cell or a highly tumourigenic cell.

3 . The method according to claim 1 , wherein the cancer cell is a CD44 Lo cell.

4 . The method according to claim 2 , wherein the method comprises impeding or preventing the development of resistance to the anti-cancer agent.

5 . The method according to claim 1 , wherein the cancer cell is a CD44 Hi cell.

6 . The method according to claim 5 , wherein the method comprises inhibiting proliferation of the CD44 Hi cell or increasing sensitivity of the CD44 Hi cell to an anti-cancer agent.

7 . The method according to claim 1 , wherein the method comprises determining the level of expression and/or activity of the androgen receptor and/or ZEB1 in the cell.

8 . The method according to claim 1 , wherein the method comprises determining the level of expression and/or activity of the androgen receptor and/or ZEB1 in the cytoplasm of the cell.

9 . A method of inhibiting the development of resistance to an anti-cancer agent in a cancer cell in a subject, the method comprising: determining the level of expression and/or activity of the androgen receptor and/or ZEB1 in the cancer cell; and administering to the subject an androgen receptor antagonist if the level of expression and/or activity of the androgen receptor and/or ZEB1 is low, wherein the cell is a breast cancer cell, wherein the anti-cancer agent is docetaxel, paclitaxel, or doxorubicin, and wherein the androgen receptor antagonist is seviteronel.

10 . A method of inhibiting the proliferation of a cancer cell in a subject, the method comprising: determining the level of expression and/or activity of the androgen receptor and/or ZEB1 in the cancer cell; and administering to the subject an androgen receptor antagonist if the level of expression and/or activity of the androgen receptor and/or ZEB1 is high, wherein the cell is a breast cancer cell, wherein the anti-cancer agent is docetaxel, paclitaxel, or doxorubicin, and wherein the androgen receptor antagonist is seviteronel.

11 . The method according to claim 9 , wherein the level of expression and/or activity of the androgen receptor and/or ZEB1 is determined in the cytoplasm of the cell.

Priority Claims (1)
AU 2019904027 · Oct 25, 2019 · national
Continuity (1)
Related Publication 20220387394A1 · Dec 8, 2022
References Cited (33)
US 10391173B2 · Abazeed · 2019 [cited by examiner]
US 20080051380A1 · Auerbach · 2008 [cited by applicant]
US 20150209359A1 · Yaffe · 2015 [cited by applicant]
US 20170319692A1 · Abazeed · 2017 [cited by applicant]
WO 2011064663A1 · 2011 [cited by applicant]
WO WO2016179002A1 · 2016 [cited by examiner]
WO 2019113301 · 2019 [cited by applicant]
Lokeshwar, B. L., V. B. Lokeshwar, and N. L. Block. “Expression of CD44 in prostate cancer cells: association with cell proliferation and invasive potential.” Anticancer research 15, No. 4 (1995): 1191-1198 (Year: 1995). [cited by examiner]
Chen, M. E., Lin, S. H., Chung, L. W., & Sikes, R. A. (1998). Isolation and Characterization of p. 1 andGage-7: New Genes Expressed in The LNCaP Prostate Cancer Progression Model That Share Homology With Melanoma-Associ… [cited by examiner]
Kawada, Manabu, Hiroyuki Inoue, Ihomi Usami, Kozo Takamoto, Tohru Masuda, Yoko Yamazaki, and Daishiro Ikeda. “Establishment of a highly tumorigenic LNCaP cell line having inflammatory cytokine resistance.” Cancer letter… [cited by examiner]
Baskar, Rajamanickam, Kuo Ann Lee, Richard Yeo, and Kheng-Wei Yeoh. “Cancer and radiation therapy: current advances and future directions.” International journal of medical sciences 9, No. 3 (2012): 193. (Year: 2012). [cited by examiner]
Al Ssadh et al. “Measurements of heterotypic associations between cluster of differentiation CD74 and CD44 in human breast cancer-derived cells.” Oncotarget 8, No. 54 (2017): 92143 (Year: 2017). [cited by examiner]
Gordon, Michael A., Nicholas C. D'Amato, Haihua Gu, Beatrice Babbs, Julia Wulfkuhle, Emanuel F. Petricoin, Isela Gallagher et al. “Synergy between androgen receptor antagonism and inhibition of mTOR and HER2 in breast c… [cited by examiner]
Gupta et al “Phase I study of seviteronel, a selective CYP17 lyase and androgen receptor inhibitor, in men with castration-resistant prostate cancer.” Clinical Cancer Research 24, No. 21 (2018): 5225-5232. (Year: 2018). [cited by examiner]
Shiota, Masaki, Takashi Dejima, Yoshiaki Yamamoto, Ario Takeuchi, Kenjiro Imada, Eiji Kashiwagi, Junichi Inokuchi et al. “Collateral resistance to taxanes in enzalutamide-resistant prostate cancer through aberrant andro… [cited by examiner]
Vikram, Rajeev, Wen Cheng Chou, Shih-Chieh Hung, and Chen-Yang Shen. “Tumorigenic and metastatic role of CD44−/low/CD24−/low cells in luminal breast cancer.” Cancers 12, No. 5 (2020): 1239 (Year: 2020). [cited by examiner]
Su, Chen-Ying, Gwo-Che Huang, I-Cheng Chen, Pei-Yu Chen, Yu-Jen Chen, and Hsu-Wei Fang. “Distinct expression of surface and genetic biomarkers in prostate cancer cell lines.” in vivo 37, No. 1 (2023): 242-246 (Year: 202… [cited by examiner]
National Cancer Institute Dictionary of Cancer Terms, “anticancer therapy,” https://www.cancer.gov/publications/dictionaries/cancer-terms/def/anticancer-therapy, Accessed: Jul. 23, 2025) (Year: 2025). [cited by examiner]
Altogen Labs, “BT474 Xenograft Model,” Accessed: Jul. 29, 2025, https://altogenlabs.com/xenograft-models/breast-cancer-xenograft/bt474-xenograft-model/#:~:text=BT474%20is%20a%20well%2Destablished,therapies%2C%20and%20no… [cited by examiner]
Altogen Labs, “MDA-MB-453 Xenograft Model,” Accessed: Jul. 29, 2025, https://altogenlabs.com/xenograft-models/breast-cancer-xenograft/mda-mb-453-xenograft-model/#:~:text=Metastatic%20MDA%2DMB%2D453%20Xenograft%20Model&t… [cited by examiner]
National Center for Biotechnology Information. PubChem Compound Summary for CID 132971, Abiraterone. https://pubchem.ncbi.nlm.nih.gov/compound/Abiraterone. Accessed Jul. 29, 2025 (Year: 2025). [cited by examiner]
National Center for Biotechnology Information. PubChem Compound Summary for CID 78357816, Seviteronel. https://pubchem.ncbi.nlm.nih.gov/compound/Seviteronel. Accessed Jul. 30, 2025 (Year: 2025). [cited by examiner]
Barton, V. N., et al., “Androgen Receptor Supports an Anchorage-Independent, Cancer Stem Cell-like Population in Triple-Negative Breast Cancer,” Cancer Research, vol. 77, No. 13 (2017), pp. 3455-3466. [cited by applicant]
Fushimi, C., et al., “A prospective phase II study of combined androgen blockade in patients with androgen receptor-positive metastatic or locally advanced unresectable salivary gland carcinoma,” Annals of Oncology, vol… [cited by applicant]
Gerratana, L., et al., “Androgen receptor in triple negative breast cancer: A potential target for the targetless subtype,” Cancer Treatment Reviews, vol. 68 (2018), pp. 102-110. [cited by applicant]
Gordon, M. A., et al., “Synergy between Androgen Receptor Antagonism and Inhibition of mTOR and HER2 in Breast Cancer,” Molecular Cancer Therapeutics, vol. 16, No. 7 (2017), pp. 1389-1400. [cited by applicant]
Goscinski, M. A., et al., “Nuclear, cytoplasmic, and stromal expression of ZEB1 in squamous and small cell carcinoma of the esophagus,” APMIS, vol. 123, No. 12 (2015), pp. 1040-1047. [cited by applicant]
Kuasne, H., et al., “Nuclear loss and cytoplasmic expression of androgen receptor in penile carcinomas: role as a driver event and as a prognostic factor,” Virchows Archiv, vol. 473 (2018), pp. 607-614. [cited by applicant]
Morris, M. J., et al., “Phase Ib Study of Enzalutamide in Combination with Docetaxel in Men with Metastatic Castration-Resistant Prostate Cancer,” Clinical Cancer Research, vol. 22, No. 15 (2016), pp. 3774-3781. [cited by applicant]
Naderi, A., et al., “Synergy between inhibitors of androgen receptor and MEK has therapeutic implications in estrogen receptor-negative breast cancer,” Breast Cancer Research, vol. 13, No. 2(2011), R36. [cited by applicant]
Speers, C., et al., “Androgen receptor as a mediator and biomarker of radioresistance in triple-negative breast cancer,” NPJ Breast Cancer, vol. 3 (2017), Article 29. [cited by applicant]
Wardell, S. E., et al. “Abstract 1588: Effects of the selective CYP17-lyase and androgen receptor (AR) inhibitor, seviteronel, and the cyclin-dependent kinase (CDK) 4/6 inhibitor, G1T38, on tumor growth in an AR-V7+ cas… [cited by applicant]
Rahim, B., et al., “AR Signaling in Breast Cancer,” Cancers, vol. 9, No. 3 (2017), Article 21, 26 pages. [cited by applicant]