Scher, HI.,
Fizazi, K.,
Saad, F.,
Taplin, ME.,
Sternberg, CN.,
Miller, K.,
de Wit, R.,
Mulders, P.,
Chi, KN.,
Shore, ND.,
et al.
(2012)
Increased survival with enzalutamide in prostate cancer after chemotherapy. N Engl J Med, Vol.367(13),
pp.1187-1197,
Full Text,
Show Abstract
Enzalutamide (formerly called MDV3100) targets multiple steps in the androgen-receptor-signaling pathway, the major driver of prostate-cancer growth. We aimed to evaluate whether enzalutamide prolongs survival in men with castration-resistant prostate cancer after chemotherapy.
de Bono, JS.,
Logothetis, CJ.,
Molina, A.,
Fizazi, K.,
North, S.,
Chu, L.,
Chi, KN.,
Jones, RJ.,
Goodman, OB.,
Saad, F.,
et al.
(2011)
Abiraterone and increased survival in metastatic prostate cancer. N Engl J Med, Vol.364(21),
pp.1995-2005,
Full Text,
Show Abstract
Biosynthesis of extragonadal androgen may contribute to the progression of castration-resistant prostate cancer. We evaluated whether abiraterone acetate, an inhibitor of androgen biosynthesis, prolongs overall survival among patients with metastatic castration-resistant prostate cancer who have received chemotherapy.
Yap, TA.,
Olmos, D.,
Brunetto, AT.,
Tunariu, N.,
Barriuso, J.,
Riisnaes, R.,
Pope, L.,
Clark, J.,
Futreal, A.,
Germuska, M.,
et al.
(2011)
Phase I trial of a selective c-MET inhibitor ARQ 197 incorporating proof of mechanism pharmacodynamic studies. J Clin Oncol, Vol.29(10),
pp.1271-1279,
Show Abstract
The hepatocyte growth factor/c-MET axis is implicated in tumor cell proliferation, survival, and angiogenesis. ARQ 197 is an oral, selective, non-adenosine triphosphate competitive c-MET inhibitor. A phase I trial of ARQ 197 was conducted to assess safety, tolerability, and target inhibition, including intratumoral c-MET signaling, apoptosis, and angiogenesis.
de Bono, JS.,
Oudard, S.,
Ozguroglu, M.,
Hansen, S.,
Machiels, JP.,
Kocak, I.,
Gravis, G.,
Bodrogi, I.,
Mackenzie, MJ.,
Shen, L.,
et al.
(2010)
Prednisone plus cabazitaxel or mitoxantrone for metastatic castration-resistant prostate cancer progressing after docetaxel treatment: a randomised open-label trial. Lancet, Vol.376(9747),
pp.1147-1154,
Show Abstract
Cabazitaxel is a novel tubulin-binding taxane drug with antitumour activity in docetaxel-resistant cancers. We aimed to compare the efficacy and safety of cabazitaxel plus prednisone with those of mitoxantrone plus prednisone in men with metastatic castration-resistant prostate cancer with progressive disease after docetaxel-based treatment.
Fong, PC.,
Boss, DS.,
Yap, TA.,
Tutt, A.,
Wu, P.,
Mergui-Roelvink, M.,
Mortimer, P.,
Swaisland, H.,
Lau, A.,
O'Connor, MJ.,
et al.
(2009)
Inhibition of poly(ADP-ribose) polymerase in tumors from BRCA mutation carriers. N Engl J Med, Vol.361(2),
pp.123-134,
Show Abstract
The inhibition of poly(adenosine diphosphate [ADP]-ribose) polymerase (PARP) is a potential synthetic lethal therapeutic strategy for the treatment of cancers with specific DNA-repair defects, including those arising in carriers of a BRCA1 or BRCA2 mutation. We conducted a clinical evaluation in humans of olaparib (AZD2281), a novel, potent, orally active PARP inhibitor.
Attard, G.,
Reid, AH.,
Yap, TA.,
Raynaud, F.,
Dowsett, M.,
Settatree, S.,
Barrett, M.,
Parker, C.,
Martins, V.,
Folkerd, E.,
et al.
(2008)
Phase I clinical trial of a selective inhibitor of CYP17, abiraterone acetate, confirms that castration-resistant prostate cancer commonly remains hormone driven. J Clin Oncol, Vol.26(28),
pp.4563-4571,
Show Abstract
Studies indicate that castration-resistant prostate cancer (CRPC) remains driven by ligand-dependent androgen receptor (AR) signaling. To evaluate this, a trial of abiraterone acetate-a potent, selective, small-molecule inhibitor of cytochrome P (CYP) 17, a key enzyme in androgen synthesis-was pursued.