ConferenceJournal of Clinical Oncology · February 1, 2024
548Background: Interest in FGFR-targeted (FGFRi) therapies for UC or pan-tumor use is growing (ongoing clinical studies include erdafitinib (NCT05316155; NCT04172675; NCT03390504; NCT04083976), LOXO-435 (NCT05614739), and pemigatinib (NCT03914794) followin ...
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ConferenceJournal of Clinical Oncology · January 1, 2024
Background: Immune checkpoint inhibition (ICI) shows great promise, including approval of pembrolizumab, nivolumab and avelumab in urothelial cancer (UC). However, the overall percentage of UC patients with clinical benefit is relatively small, despite bio ...
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ConferenceJournal of Clinical Oncology · June 1, 2023
2044 Background: Lisavanbulin (BAL101553, prodrug of BAL27862) destabilizes microtubules and promotes tumor cell death by modulating the spindle assembly checkpoint. BAL27862 is a lipophilic small molecule shown in rodents to pen ...
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ConferenceJournal of Clinical Oncology · February 20, 2022
160 Background: Oral AA is a standard of care for metastatic prostate cancer. The recommended daily AA 1000 mg dose produces high peak and low trough plasma concentrations that are associated with safety issues (e.g., hepatotoxic ...
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ConferenceCancer Research · August 15, 2020
AbstractNew approaches are needed to overcome intrinsic therapy resistance in glioblastoma (GBM). Because GBMs exhibit sexual dimorphism and are reported to express steroid hormone receptors, we reasoned tha ...
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ConferenceCancer Research · February 15, 2019
AbstractBackground: Androgen receptor (AR) protein is expressed across breast cancer (BC) subtypes, including up to 50% of triple negative breast cancers (TNBC) and it is often maintained in metastases. Our ...
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ConferenceCancer Research · February 15, 2016
AbstractVT-464 is a lyase-selective inhibitor of the dual-activity CYP17A1 enzyme that is required for the synthesis of androgens and estrogens in the gonads, adrenals, and tumors. In addition to its role as ...
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ConferenceCancer Research · February 15, 2016
AbstractVT-464, an oral dual lyase-selective CYP17 inhibitor and AR antagonist (wild-type and mutated forms [e.g., F876L and T877A]), is in multiple Phase (Ph) 2 studies as treatment for men with castration- ...
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ConferenceJournal of Clinical Oncology · January 10, 2016
273 Background: VT-464 is an oral, CYP17-L inhibitor and non-clinically an antagonist of the AR and its variants associated with clinical resistance to enzalutamide (ENZ) and abiraterone (AA). The safety, tolerability and initial ...
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ConferenceJournal of Clinical Oncology · January 10, 2016
343 Background: VT-464 is an oral, CYP17-L inhibitor and non-clinically an antagonist of the AR and its variants associated with clinical resistance to enzalutamide (ENZ) and abiraterone (AA). The safety, tolerability and initial ...
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ConferenceJournal of Clinical Oncology · January 10, 2016
198 Background: VT-464 is a dual selective inhibitor of CYP17,20 lyase and an androgen receptor antagonist in development for the treatment of CRPC. In early clinical testing, several pts receiving VT-464 in 28-day cycles were no ...
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ConferenceJournal of Clinical Oncology · March 1, 2015
263 Background: MDV3100 inhibits binding of androgens to AR and abiraterone is known to block androgen production through CYP17 inhibition; both are effective treatments for castration-resistant prostate cancer (CRPC, yet cross-r ...
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ConferenceJournal of Clinical Oncology · March 1, 2015
187 Background: VT-464 is an oral, non-steroidal inhibitor of CYP17-L and an antagonist of androgen receptor (AR) variants F876L and T877A which are associated with resistance to enzalutamide (ENZ) and abiraterone/prednisone (AA) ...
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ConferenceJournal of Clinical Oncology · February 1, 2014
158 Background: CRPC typically responds to anti-androgen therapy but resistance is common. CYP17 inhibitors that block lyase (L) and not hydroxylase (H), do not require prednisone, and may delay tumor resistance are needed. VT-46 ...
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ConferenceCancer Research · April 15, 2013
AbstractCytochrome P450 17α-hydroxylase /17,20-lyase (CYP17) is a validated treatment target for metastatic castrate-resistant prostate cancer (mCRPC). Abiraterone acetate (AA; Zytiga) inhibits 17α-hydroxyla ...
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ConferenceJ Clin Endocrinol Metab · December 2004
Polycystic ovary syndrome (PCOS) is a familial disease. Affected males harbor some of the metabolic deficits seen in affected females. The prenatally androgenized (PA) female rhesus monkey, an animal model for PCOS, manifests glucoregulatory and reproducti ...
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