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galeterone 6  (Tokai Pharmaceuticals)

 
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    Tokai Pharmaceuticals galeterone 6
    Galeterone 6, supplied by Tokai Pharmaceuticals, used in various techniques. Bioz Stars score: 90/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/product/galeterone/galeterone+6/pm40231807-31-0-4
    Average 90 stars, based on 1 article reviews
    galeterone 6 - by Bioz Stars, 2026-09
    90/100 stars

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    Related Articles

    other:

    Article Title: Industry Watch
    Article Snippet: Anda distributes generic, brand, specialty, and over-the-counter pharmaceutical products from more than 300 manufacturers to retail independent and chain pharmacies, nursing homes, mail-order pharmacies, hospitals, clinics, and physician offices across the U.S.. Through the acquisition, Teva said, it will gain 650 employees based at Anda’s centers in Olive Branch, MS; Weston, FL; and Groveport, OH.

    Article Title: [Splicing variant of androgen receptors (AR-V7): New paradigms].
    Article Snippet: L'épissage alternatif produit plus d'une vingtaine de variants du récepteur aux androgènes.. Parmi ces variants, certains sont tronqués du site de fixation du ligand et sont donc activés de manière constitutive.. Parmi ces variants activés de manière consécutive, ARV-7 est le variant le plus abondamment observé dans les cancers de la prostate métastatique [1].

    Article Title: Galeterone and its analogs inhibit Mnk-eIF4E axis, synergize with gemcitabine, impede pancreatic cancer cell migration, invasion and proliferation and inhibit tumor growth in mice
    Article Snippet: NOTE ADDED IN PROOF During the review of this manuscript, Tokai Pharmaceuticals announced discontinuation of Phase 3 ARMOR3-SV trial of galeterone in AR-V7 positive metastatic castration resistant cancer (mCRPC).

    Article Title: Abiraterone and Galeterone, Powerful Tools Against Prostate Cancer: Present and Perspective
    Article Snippet: These data enabled galeterone to be licensed to Tokai Pharmaceuticals Inc., Cambridge, MA, for further preclinical and clinical studies and granted it a new code name, TOK-001 [ ].

    Activity Assay:

    Article Title: Androgen receptor variant-driven prostate cancer: clinical implications and therapeutic targeting
    Article Snippet: .. Here we will highlight three of these agents, while others are summarized in . table ft1 table-wrap mode=article t1 caption a4 caption a8 Selected therapeutic trials using agents with potential activity against AR-V7-expressing CRPC The first drug is galeterone, manufactured by Tokai Pharmaceuticals, Boston, MA, USA. ..

    Article Title: Analytical Validation of Androgen Receptor Splice Variant 7 Detection in a Clinical Laboratory Improvement Amendments (CLIA) Laboratory Setting.
    Article Snippet: .. These include galeterone (Tokai Pharmaceuticals, Boston,MA), anAR-targeting agent that potentially can inhibit both AR-FLe and AR-V7emediated signaling31e33; the ESSA Pharmaceuticals Inc. (EPI, Vancouver, CA) family of small molecules (including EPI-506) that target the AR Nterminal domain34e36; agents targeting the bromodomain extraterminal family of proteins that bind with AR to facilitate its transcriptional activation37,38; and niclosamide, which can inhibit AR-FLe and AR-V7emediated transcriptional activity in preclinical models.39,40 In addition to the AR splice variants, several less common possible mechanisms of resistance to androgen-deprivation therapy have been documented in CRPC patients.41 These include AR gene amplification and overexpression, conversion of weak androgens to potent androgens, intratumoral androgen production, somatic point mutations in the N-terminal domain of AR, and stimulation of AR via androgen-independent pathways (reviewed by Maughan and Antonarakis22). ..

    Variant Assay:

    Article Title: 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.
    Article Snippet: .. During the review of this manuscript, Tokai Pharmaceuticals Inc. announced on June 24, 2015, the initiation of ARMOR3-SV, Tokai’s pivotal Phase 3 clinical trial of galeterone in men with metastatic castration-resistant prostate cancer (mCRPC) whose tumors express the AR-V7 splice variant that has been associated with non-responsiveness to commonly-used oral therapies for mCRPC. ..

    Amplification:

    Article Title: Analytical Validation of Androgen Receptor Splice Variant 7 Detection in a Clinical Laboratory Improvement Amendments (CLIA) Laboratory Setting.
    Article Snippet: .. These include galeterone (Tokai Pharmaceuticals, Boston,MA), anAR-targeting agent that potentially can inhibit both AR-FLe and AR-V7emediated signaling31e33; the ESSA Pharmaceuticals Inc. (EPI, Vancouver, CA) family of small molecules (including EPI-506) that target the AR Nterminal domain34e36; agents targeting the bromodomain extraterminal family of proteins that bind with AR to facilitate its transcriptional activation37,38; and niclosamide, which can inhibit AR-FLe and AR-V7emediated transcriptional activity in preclinical models.39,40 In addition to the AR splice variants, several less common possible mechanisms of resistance to androgen-deprivation therapy have been documented in CRPC patients.41 These include AR gene amplification and overexpression, conversion of weak androgens to potent androgens, intratumoral androgen production, somatic point mutations in the N-terminal domain of AR, and stimulation of AR via androgen-independent pathways (reviewed by Maughan and Antonarakis22). ..

    Over Expression:

    Article Title: Analytical Validation of Androgen Receptor Splice Variant 7 Detection in a Clinical Laboratory Improvement Amendments (CLIA) Laboratory Setting.
    Article Snippet: .. These include galeterone (Tokai Pharmaceuticals, Boston,MA), anAR-targeting agent that potentially can inhibit both AR-FLe and AR-V7emediated signaling31e33; the ESSA Pharmaceuticals Inc. (EPI, Vancouver, CA) family of small molecules (including EPI-506) that target the AR Nterminal domain34e36; agents targeting the bromodomain extraterminal family of proteins that bind with AR to facilitate its transcriptional activation37,38; and niclosamide, which can inhibit AR-FLe and AR-V7emediated transcriptional activity in preclinical models.39,40 In addition to the AR splice variants, several less common possible mechanisms of resistance to androgen-deprivation therapy have been documented in CRPC patients.41 These include AR gene amplification and overexpression, conversion of weak androgens to potent androgens, intratumoral androgen production, somatic point mutations in the N-terminal domain of AR, and stimulation of AR via androgen-independent pathways (reviewed by Maughan and Antonarakis22). ..

    Clinical Proteomics:

    Article Title: Azasteroidal mimics
    Article Snippet: .. Galeterone, developed by Tokai pharmaceutical company, has been in phase III clinical trials for castration-resistant prostate cancer. .. This company announced the discontinuation of its clinical trials on Jul.



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    Image Search Results


    Structures of abiraterone acetate ( 1 ), abiraterone ( 2 ), and galeterone ( 3 ).

    Journal: Pharmaceutics

    Article Title: Abiraterone and Galeterone, Powerful Tools Against Prostate Cancer: Present and Perspective

    doi: 10.3390/pharmaceutics16111401

    Figure Lengend Snippet: Structures of abiraterone acetate ( 1 ), abiraterone ( 2 ), and galeterone ( 3 ).

    Article Snippet: These data enabled galeterone to be licensed to Tokai Pharmaceuticals Inc., Cambridge, MA, for further preclinical and clinical studies and granted it a new code name, TOK-001 [ ].

    Techniques:

    Number of published papers by year from PubMed (results obtained using the “All” search field and keywords “abiraterone” ( A ) and “galeterone” ( C )) and Scopus (results obtained using the “Article title, Abstract, Keywords” field and keywords “abiraterone” ( B ) and “galeterone” ( D )).

    Journal: Pharmaceutics

    Article Title: Abiraterone and Galeterone, Powerful Tools Against Prostate Cancer: Present and Perspective

    doi: 10.3390/pharmaceutics16111401

    Figure Lengend Snippet: Number of published papers by year from PubMed (results obtained using the “All” search field and keywords “abiraterone” ( A ) and “galeterone” ( C )) and Scopus (results obtained using the “Article title, Abstract, Keywords” field and keywords “abiraterone” ( B ) and “galeterone” ( D )).

    Article Snippet: These data enabled galeterone to be licensed to Tokai Pharmaceuticals Inc., Cambridge, MA, for further preclinical and clinical studies and granted it a new code name, TOK-001 [ ].

    Techniques:

    Distribution of documents by type from Scopus (results obtained using keywords “abiraterone” or “galeterone” and the “Article title, Abstract, Keywords” field).

    Journal: Pharmaceutics

    Article Title: Abiraterone and Galeterone, Powerful Tools Against Prostate Cancer: Present and Perspective

    doi: 10.3390/pharmaceutics16111401

    Figure Lengend Snippet: Distribution of documents by type from Scopus (results obtained using keywords “abiraterone” or “galeterone” and the “Article title, Abstract, Keywords” field).

    Article Snippet: These data enabled galeterone to be licensed to Tokai Pharmaceuticals Inc., Cambridge, MA, for further preclinical and clinical studies and granted it a new code name, TOK-001 [ ].

    Techniques:

    Distribution of documents by subject area from Scopus (results obtained using keywords “abiraterone” or “galeterone” and the “Article title, Abstract, Keywords” field).

    Journal: Pharmaceutics

    Article Title: Abiraterone and Galeterone, Powerful Tools Against Prostate Cancer: Present and Perspective

    doi: 10.3390/pharmaceutics16111401

    Figure Lengend Snippet: Distribution of documents by subject area from Scopus (results obtained using keywords “abiraterone” or “galeterone” and the “Article title, Abstract, Keywords” field).

    Article Snippet: These data enabled galeterone to be licensed to Tokai Pharmaceuticals Inc., Cambridge, MA, for further preclinical and clinical studies and granted it a new code name, TOK-001 [ ].

    Techniques:

    VOSviewer generated an overlay visualization graph with the co-occurrence of keywords related to galeterone.

    Journal: Pharmaceutics

    Article Title: Abiraterone and Galeterone, Powerful Tools Against Prostate Cancer: Present and Perspective

    doi: 10.3390/pharmaceutics16111401

    Figure Lengend Snippet: VOSviewer generated an overlay visualization graph with the co-occurrence of keywords related to galeterone.

    Article Snippet: These data enabled galeterone to be licensed to Tokai Pharmaceuticals Inc., Cambridge, MA, for further preclinical and clinical studies and granted it a new code name, TOK-001 [ ].

    Techniques: Generated

    Synthesis of galeterone ( 3 ) from dehydroepiandrosterone acetate ( 4 ). Reagents and conditions: (a) POCl 3 -DMF, CH 3 Cl, Ar, reflux; (b) benzimidazole, K 2 CO 3 , DMF, Ar, 80 °C; (c) 10% Pd on activated charcoal, PhCN, reflux; (d) 10% methanolic KOH, Ar, rt.

    Journal: Pharmaceutics

    Article Title: Abiraterone and Galeterone, Powerful Tools Against Prostate Cancer: Present and Perspective

    doi: 10.3390/pharmaceutics16111401

    Figure Lengend Snippet: Synthesis of galeterone ( 3 ) from dehydroepiandrosterone acetate ( 4 ). Reagents and conditions: (a) POCl 3 -DMF, CH 3 Cl, Ar, reflux; (b) benzimidazole, K 2 CO 3 , DMF, Ar, 80 °C; (c) 10% Pd on activated charcoal, PhCN, reflux; (d) 10% methanolic KOH, Ar, rt.

    Article Snippet: These data enabled galeterone to be licensed to Tokai Pharmaceuticals Inc., Cambridge, MA, for further preclinical and clinical studies and granted it a new code name, TOK-001 [ ].

    Techniques: Reflux

    In vitro and in vivo metabolism of galeterone.

    Journal: Pharmaceutics

    Article Title: Abiraterone and Galeterone, Powerful Tools Against Prostate Cancer: Present and Perspective

    doi: 10.3390/pharmaceutics16111401

    Figure Lengend Snippet: In vitro and in vivo metabolism of galeterone.

    Article Snippet: These data enabled galeterone to be licensed to Tokai Pharmaceuticals Inc., Cambridge, MA, for further preclinical and clinical studies and granted it a new code name, TOK-001 [ ].

    Techniques: In Vitro, In Vivo

    Galeterone derivatives 26 – 33 .

    Journal: Pharmaceutics

    Article Title: Abiraterone and Galeterone, Powerful Tools Against Prostate Cancer: Present and Perspective

    doi: 10.3390/pharmaceutics16111401

    Figure Lengend Snippet: Galeterone derivatives 26 – 33 .

    Article Snippet: These data enabled galeterone to be licensed to Tokai Pharmaceuticals Inc., Cambridge, MA, for further preclinical and clinical studies and granted it a new code name, TOK-001 [ ].

    Techniques:

    C-3-modified derivatives of galeterone.

    Journal: Pharmaceutics

    Article Title: Abiraterone and Galeterone, Powerful Tools Against Prostate Cancer: Present and Perspective

    doi: 10.3390/pharmaceutics16111401

    Figure Lengend Snippet: C-3-modified derivatives of galeterone.

    Article Snippet: These data enabled galeterone to be licensed to Tokai Pharmaceuticals Inc., Cambridge, MA, for further preclinical and clinical studies and granted it a new code name, TOK-001 [ ].

    Techniques: Modification

    Structures of galeterone analogs 40 – 46 .

    Journal: Pharmaceutics

    Article Title: Abiraterone and Galeterone, Powerful Tools Against Prostate Cancer: Present and Perspective

    doi: 10.3390/pharmaceutics16111401

    Figure Lengend Snippet: Structures of galeterone analogs 40 – 46 .

    Article Snippet: These data enabled galeterone to be licensed to Tokai Pharmaceuticals Inc., Cambridge, MA, for further preclinical and clinical studies and granted it a new code name, TOK-001 [ ].

    Techniques: