102
Views
41
CrossRef citations to date
0
Altmetric
Review

Galeterone for the treatment of advanced prostate cancer: the evidence to date

&
Pages 2289-2297 | Published online: 15 Jul 2016

References

  • TorreLABrayFSiegelRLFerlayJLortet-TieulentJJemalAGlobal cancer statistics, 2012CA Cancer J Clin20156528710825651787
  • SiegelRLMillerKDJemalACancer statistics, 2016CA Cancer J Clin201666173026742998
  • BalkSPAndrogen receptor as a target in androgen-independent prostate cancerUrology2002603 Suppl 1132138 discussion 138–13912231070
  • ScherHISawyersCLBiology of progressive, castration-resistant prostate cancer: directed therapies targeting the androgen-receptor signaling axisJ Clin Oncol200523328253826116278481
  • RyanCJTindallDJAndrogen receptor rediscovered: the new biology and targeting the androgen receptor therapeuticallyJ Clin Oncol201129273651365821859989
  • KluetzPGNingYMMaherVEAbiraterone acetate in combination with prednisone for the treatment of patients with metastatic castration-resistant prostate cancer: U.S. Food and Drug Administration drug approval summaryClin Cancer Res201319246650665624150234
  • NingYMBraveMMaherVEU.S. Food and Drug Administration Approval Summary: Enzalutamide for the Treatment of Patients With Chemotherapy-Naive Metastatic Castration-Resistant Prostate CancerOncologist201520896096626070917
  • de BonoJSLogothetisCJMolinaAAbiraterone and increased survival in metastatic prostate cancerN Engl J Med2011364211995200521612468
  • RyanCJSmithMRde BonoJSAbiraterone in metastatic prostate cancer without previous chemotherapyN Engl J Med2013368213814823228172
  • ScherHIFizaziKSaadFIncreased survival with enzalutamide in prostate cancer after chemotherapyN Engl J Med2012367131187119722894553
  • BeerTMArmstrongAJRathkopfDEEnzalutamide in metastatic prostate cancer before chemotherapyN Engl J Med2014371542443324881730
  • EfstathiouETitusMTsavachidouDEffects of abiraterone acetate on androgen signaling in castrate-resistant prostate cancer in boneJ Clin Oncol201230663764322184395
  • EfstathiouETitusMWenSMolecular characterization of enzalutamide-treated bone metastatic castration-resistant prostate cancerEur Urol2015671536024882673
  • CarreiraSRomanelAGoodallJTumor clone dynamics in lethal prostate cancerSci Transl Med20146254254ra125
  • JosephJDLuNQianJA clinically relevant androgen receptor mutation confers resistance to second-generation antiandrogens enzalutamide and ARN-509Cancer Dis20133910201029
  • AzadAAVolikSVWyattAWAndrogen Receptor Gene Aberrations in Circulating Cell-Free DNA: Biomarkers of Therapeutic Resistance in Castration-Resistant Prostate CancerClin Cancer Res201521102315232425712683
  • NakazawaMAntonarakisESLuoJAndrogen receptor splice variants in the era of enzalutamide and abirateroneHorm Cancer20145526527325048254
  • AntonarakisESLuCWangHAR-V7 and resistance to enzalutamide and abiraterone in prostate cancerN Engl J Med2014371111028103825184630
  • AroraVKSchenkeinEMuraliRGlucocorticoid receptor confers resistance to antiandrogens by bypassing androgen receptor blockadeCell201315561309132224315100
  • SilbersteinJLTaylorMNAntonarakisESNovel Insights into Molecular Indicators of Response and Resistance to Modern Androgen-Axis Therapies in Prostate CancerCurr Urol Rep20161742926902623
  • MaughanBLAntonarakisESClinical Relevance of Androgen Receptor Splice Variants in Castration-Resistant Prostate CancerCurr Treat Options Oncol201516125726537882
  • de BonoJSOudardSOzgurogluMPrednisone plus cabazitaxel or mitoxantrone for metastatic castration-resistant prostate cancer progressing after docetaxel treatment: a randomised open-label trialLancet201037697471147115420888992
  • TannockIFde WitRBerryWRDocetaxel plus prednisone or mitoxantrone plus prednisone for advanced prostate cancerN Engl J Med2004351151502151215470213
  • LogothetisCJBaschEMolinaAEffect of abiraterone acetate and prednisone compared with placebo and prednisone on pain control and skeletal-related events in patients with metastatic castration-resistant prostate cancer: exploratory analysis of data from the COU-AA-301 randomised trialLancet Oncol201213121210121723142059
  • RyanCJSmithMRFizaziKAbiraterone acetate plus prednisone versus placebo plus prednisone in chemotherapy-naive men with metastatic castration-resistant prostate cancer (COU-AA-302): final overall survival analysis of a randomised, double-blind, placebo-controlled phase 3 studyLancet Oncol201516215216025601341
  • KantoffPWHiganoCSShoreNDSipuleucel-T immunotherapy for castration-resistant prostate cancerN Engl J Med2010363541142220818862
  • ParkerCNilssonSHeinrichDAlpha emitter radium-223 and survival in metastatic prostate cancerN Engl J Med2013369321322323863050
  • BaschELoblawDAOliverTKSystemic therapy in men with metastatic castration-resistant prostate cancer: American Society of Clinical Oncology and Cancer Care Ontario clinical practice guidelineJ Clin Oncol201432303436344825199761
  • GillessenSOmlinAAttardGManagement of patients with advanced prostate cancer: recommendations of the St Gallen Advanced Prostate Cancer Consensus Conference (APCCC) 2015Ann Oncol20152681589160426041764
  • LorenteDMateoJPerez-LopezRde BonoJSAttardGSequencing of agents in castration-resistant prostate cancerLancet Oncol2015166e279e29226065613
  • WatsonPAAroraVKSawyersCLEmerging mechanisms of resistance to androgen receptor inhibitors in prostate cancerNat Rev Cancer2015151270171126563462
  • EfstathiouETitusMWenSEnzalutamide (ENZA) in combination with abiraterone acetate (AA) in bone metastatic castration resistant prostate cancer (mCRPC)J Clin Oncol201432:5s suppl abstr 5000
  • RobinsonDVan AllenEMWuYMIntegrative clinical genomics of advanced prostate cancerCell201516151215122826000489
  • YuZChenSSowalskyAGRapid induction of androgen receptor splice variants by androgen deprivation in prostate cancerClin Cancer Res20142061590160024449822
  • ScherHILuDSchreiberNAAssociation of AR-V7 on circulating tumor cells as a treatment-specific biomarker with outcomes and survival in castration-resistant prostate cancerJAMA Oncol Epub201664
  • SprengerCUoTPlymateSAndrogen receptor splice variant V7 (AR-V7) in circulating tumor cells: a coming of age for AR splice variants?Ann Oncol20152691805180726199394
  • AntonarakisESLuCLuberBAndrogen Receptor Splice Variant 7 and Efficacy of Taxane Chemotherapy in Patients With Metastatic Castration-Resistant Prostate CancerJAMA Oncol20151558259126181238
  • OnstenkWSieuwertsAMKraanJEfficacy of Cabazitaxel in Castration-resistant Prostate Cancer Is Independent of the Presence of AR-V7 in Circulating Tumor CellsEur Urol201568693994526188394
  • NakazawaMLuCChenYSerial blood-based analysis of AR-V7 in men with advanced prostate cancerAnn Oncol20152691859186526117829
  • SmithMRAntonarakisESRyanCJPhase 2 Study of the Safety and Antitumor Activity of Apalutamide (ARN-509), a Potent Androgen Receptor Antagonist, in the High-risk Nonmetastatic Castration-resistant Prostate Cancer CohortEur Urol Epub201656
  • RomanelAGasi TandefeltDConteducaVPlasma AR and abiraterone-resistant prostate cancerSci Transl Med20157312312re310
  • WyattAWAzadAAVolikSVGenomic Alterations in Cell-Free DNA and Enzalutamide Resistance in Castration-Resistant Prostate CancerJAMA Oncol Epub201655
  • BeltranHTomlinsSAparicioAAggressive variants of castration-resistant prostate cancerClin Cancer Res201420112846285024727321
  • SmallEJHuangJYoungrenJCharacterization of neuroendocrine prostate cancer (NEPC) in patients with metastatic castration resistant prostate cancer (mCRPC) resistant to abiraterone (Abi) or enzalutamide (Enz): Preliminary results from the SU2C/PCF/AACR West Coast Prostate Cancer Dream Team (WCDT)J Clin Oncol201533suppl abstr 5003
  • BeltranHJendrisakALandersMThe Initial Detection and Partial Characterization of Circulating Tumor Cells in Neuroendocrine Prostate CancerClin Cancer Res20162261510151926671992
  • BoudadiKAntonarakisESResistance to Novel Antiandrogen Therapies in Metastatic Castration-Resistant Prostate CancerClin Med Insights Oncol201610Suppl 11927013902
  • BeltranHPrandiDMosqueraJMDivergent clonal evolution of castration-resistant neuroendocrine prostate cancerNat Med201622329830526855148
  • AparicioAMShenLTapiaELCombined Tumor Suppressor Defects Characterize Clinically Defined Aggressive Variant Prostate CancersClin Cancer Res20162261520153026546618
  • NjarVCKatoKNnaneIPGrigoryevDNLongBJBrodieAMNovel 17-azolyl steroids, potent inhibitors of human cytochrome 17 alpha-hydroxylase-C17,20-lyase (P450(17) alpha): potential agents for the treatment of prostate cancerJ Med Chem19984169029129526564
  • HandrattaVDVasaitisTSNjarVCNovel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft modelJ Med Chem20054882972298415828836
  • VasaitisTBelosayASchayowitzAAndrogen receptor inactivation contributes to antitumor efficacy of 17{alpha}-hydroxylase/17,20-lyase inhibitor 3beta-hydroxy-17-(1H-benzimidazole-1-yl)androsta-5,16-diene in prostate cancerMol Cancer Ther2008782348235718723482
  • PurushottamacharPGodboleAMGediyaLKSystematic 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 cancerJ Med Chem201356124880489823713567
  • SoiferHSSouleimanianNWuSDirect regulation of androgen receptor activity by potent CYP17 inhibitors in prostate cancer cellsJ Biol Chem201228763777378722174412
  • YuZCaiCGaoSSimonNIShenHCBalkSPGaleterone prevents androgen receptor binding to chromatin and enhances degradation of mutant androgen receptorClin Cancer Res201420154075408524874833
  • Al NakouziNWangCJacobyDGleaveMEZoubeidiAGaleterone suppresses castration-resistant and enzalutamide-resistant prostate cancer growth in vitroMol Cancer Ther20131211 SupplC89
  • NjarVCBrodieAMDiscovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancerJ Med Chem20155852077208725591066
  • LiBLuWChenZRegulation of Androgen Receptor by E3 Ubiquitin Ligases: for More or LessReceptors Clin Investig201415110
  • QiJFanLHussainAImplications of ubiquitin ligases in castration-resistant prostate cancerCurr Opin Oncol201527317217625811345
  • LinHKWangLHuYCAltuwaijriSChangCPhosphorylation-dependent ubiquitylation and degradation of androgen receptor by Akt require Mdm2 E3 ligaseEMBO J200221154037404812145204
  • RileyMFLozanoGThe Many Faces of MDM2 Binding PartnersGenes Cancer201233–422623923150756
  • MurataSMinamiYMinamiMChibaTTanakaKCHIP is a chaperone-dependent E3 ligase that ubiquitylates unfolded proteinEMBO Rep20012121133113811743028
  • LiBLuWYangQYuXMatusikRJChenZSkp2 regulates androgen receptor through ubiquitin-mediated degradation independent of Akt/mTOR pathways in prostate cancerProstate201474442143224347472
  • QiJTripathiMMishraRThe E3 ubiquitin ligase Siah2 contributes to castration-resistant prostate cancer by regulation of androgen receptor transcriptional activityCancer Cell201323333234623518348
  • XuKShimelisHLinnDERegulation of androgen receptor transcriptional activity and specificity by RNF6-induced ubiquitinationCancer Cell200915427028219345326
  • BurskaULHarleVJCoffeyKDeubiquitinating enzyme Usp12 is a novel co-activator of the androgen receptorJ Biol Chem201328845326413265024056413
  • McClurgULSummerscalesEEHarleVJGaughanLRobsonCNDeubiquitinating enzyme Usp12 regulates the interaction between the androgen receptor and the Akt pathwayOncotarget20145167081709225216524
  • Kwegyir-AffulAKRamalingamSPurushottamacharPRamamurthyVPNjarVCGaleterone 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 vivoOncotarget2015629274402746026196320
  • DransfieldDTNamdevNJacobyDBFerranteKGaleterone-induced degradation of the androgen receptor involves inhibition of deubiquitinating enzymesAACR Annual MeetingNew OrleansApril 18, 2016 Abstract 12342016
  • MontgomeryBEisenbergerMARettigMBAndrogen Receptor Modulation Optimized for Response (ARMOR) Phase I and II Studies: Galeterone for the Treatment of Castration-Resistant Prostate CancerClin Cancer Res20162261356136326527750
  • MontgomeryBEisenbergerMAHeathEIGaleterone in men with CRPC: Results in four distinct patient populations from the ARMOR2 studyJ Clin Oncol2014325s suppl; abstr 5029
  • TaplinMEChiKNChuFActivity of galeterone in castrate-resistant prostate cancer (CRPC) with C-terminal AR loss: Results from ARMOR2European Journal of Cancer20145068
  • McKayRRWernerLFiorilloMActivity of sequential therapies (txs) in patients (pts) with castration resistant prostate cancer (CRPC) previously treated with galeteroneJ Clin Oncol201533 suppl; abstr e16072
  • TaplinMEAntonarakisESDransfieldDTFerranteKJDe BonoJSAndrogen receptor modulation optimized for response: Splice variant (ARMOR3-SV)–Randomized, open-label, multicenter, controlled study of galeterone vs enzalutamide in men with metastatic castration-resistant prostate cancer (mCRPC) expressing AR-V7 splice variantJ Clin Oncol201533 suppl; abstr TPS5069