keyword
MENU ▼
Read by QxMD icon Read
search

Apalutamide

keyword
https://www.readbyqxmd.com/read/29734647/recent-advances-in-prostate-cancer-treatment-and-drug-discovery
#1
REVIEW
Ekaterina Nevedomskaya, Simon J Baumgart, Bernard Haendler
Novel drugs, drug sequences and combinations have improved the outcome of prostate cancer in recent years. The latest approvals include abiraterone acetate, enzalutamide and apalutamide which target androgen receptor (AR) signaling, radium-223 dichloride for reduction of bone metastases, sipuleucel-T immunotherapy and taxane-based chemotherapy. Adding abiraterone acetate to androgen deprivation therapy (ADT) in order to achieve complete androgen blockade has proven highly beneficial for treatment of locally advanced prostate cancer and metastatic hormone-sensitive prostate cancer (mHSPC)...
May 4, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29730201/androgen-receptor-targeted-treatments-for-prostate-cancer-35-years-progress-with-antiandrogens
#2
REVIEW
E David Crawford, Paul F Schellhammer, David G McLeod, Judd W Moul, Celestia S Higano, Neal Shore, Louis Denis, Peter Iversen, Mario A Eisenberger, Fernand Labrie
PURPOSE: Antiandrogens inhibit the androgen receptor (AR) and play an important role in the treatment of prostate cancer (PC). This review provides a historical perspective on the development and clinical benefit of antiandrogens in the treatment of PC. MATERIALS AND METHODS: We searched PubMed® for clinical trials with the search terms "antiandrogens" and "prostate cancer" combined with drug names for antiandrogens. This article represents a collaboration of clinical investigators who have made critical scientific contributions leading to the approval of antiandrogens for treating patients with PC...
May 3, 2018: Journal of Urology
https://www.readbyqxmd.com/read/29719365/pharmaceutical-approval-update
#3
Mary Choy
Vancomycin hydrochloride for oral solution (Firvanq) for C. difficile -associated diarrhea and enterocolitis caused by S. aureus ; dexamethasone intraocular suspension 9% (Dexycu) for the treatment of inflammation after eye surgery; and apalutamide (Erleada) for prostate cancer.
May 2018: P & T: a Peer-reviewed Journal for Formulary Management
https://www.readbyqxmd.com/read/29709784/validation-of-an-lc-ms-ms-method-for-simultaneous-quantitation-of-enzalutamide-n-desmethylenzalutamide-apalutamide-darolutamide-and-orm-15341-in-mice-plasma-and-its-application-to-a-mice-pharmacokinetic-study
#4
Suresh P Sulochana, Neeraj Kumar Saini, Prasanthi Daram, Sai Babu Polina, Ramesh Mullangi
A sensitive and rapid LC-MS/MS method was developed and validated for the simultaneous quantitation of enzalutamide, N-desmethylenzalutamide (active metabolite of enzalutamide), apalutamide, darolutamide and ORM-15341 (active metabolite of darolutamide) in mice plasma as per regulatory guidelines. The analytes and the internal standard (I.S.: apalutamide-d3 ) were extracted from 50 μL mice plasma by simple protein precipitation using acetonitrile, followed by chromatographic separation using an Atlantis C18 column with an isocratic mobile (0...
April 24, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29695920/profile-of-apalutamide-in-the-treatment-of-metastatic-castration-resistant-prostate-cancer-evidence-to-date
#5
REVIEW
Julio T Chong, William K Oh, Bobby C Liaw
Advances in therapies have led to the approval of six therapeutic agents since 2004, each demonstrating overall survival benefit in randomized studies, and these have significantly improved the outlook for men facing metastatic castration-resistant prostate cancer (CRPC). More recently, efforts have been directed at trying to effect change at earlier phases of the disease. Apalutamide (ARN-509), a second-generation androgen receptor antagonist, recently received approval in the nonmetastatic (M0) CRPC space...
2018: OncoTargets and Therapy
https://www.readbyqxmd.com/read/29691083/re-apalutamide-treatment-and-metastasis-free-survival-in-prostate-cancer
#6
Daniel Heinrich, Kjell Magne Russnes, Jan Oldenburg
No abstract text is available yet for this article.
April 21, 2018: European Urology
https://www.readbyqxmd.com/read/29626324/apalutamide-first-global-approval
#7
Zaina T Al-Salama
Apalutamide (ErleadaTM ) is a next-generation oral androgen receptor (AR) inhibitor that is being developed by Janssen for the treatment of prostate cancer (PC). It binds directly to the ligand-binding domain of the AR and blocks the effects of androgens. In February 2018, apalutamide received its first global approval in the USA for the treatment of non-metastatic castration-resistant PC (nmCRPC). Apalutamide is undergoing phase III investigation in chemotherapy-naive patients with metastatic CRPC (in combination with abiraterone acetate plus prednisone), patients with high-risk localized or locally advanced PC receiving primary radiation therapy, and in patients with metastatic hormone-sensitive PC and biochemically-relapsed PC...
April 6, 2018: Drugs
https://www.readbyqxmd.com/read/29606109/neoadjuvant-degarelix-with-or-without-apalutamide-followed-by-radical-prostatectomy-for-intermediate-and-high-risk-prostate-cancer-arneo-a-randomized-double-blind-placebo-controlled-trial
#8
Lorenzo Tosco, Annouschka Laenen, Thomas Gevaert, Isabelle Salmon, Christine Decaestecker, Elai Davicioni, Christine Buerki, Frank Claessens, Johan Swinnen, Karolien Goffin, Raymond Oyen, Wouter Everaerts, Lisa Moris, Gert De Meerleer, Karin Haustermans, Steven Joniau
BACKGROUND: Recent retrospective data suggest that neoadjuvant androgen deprivation therapy can improve the prognosis of high-risk prostate cancer (PCa) patients. Novel androgen receptor pathway inhibitors are nowadays available for treatment of metastatic PCa and these compounds are promising for early stage disease. Apalutamide is a pure androgen antagonist with a very high affinity with the androgen receptor. The combination of apalutamide with degarelix, an LHRH antagonist, could increase the efficacy compared to degarelix alone...
April 2, 2018: BMC Cancer
https://www.readbyqxmd.com/read/29518645/validation-of-an-lc-esi-ms-ms-method-for-the-determination-of-apalutamide-a-novel-non-steroidal-anti-androgen-in-mice-plasma-and-its-application-to-a-pharmacokinetic-study-in-mice
#9
Gurulingappa Hallur, Buchi Reddy Purra, Suresh P Sulochana, Neeraj Kumar Saini, Prasanthi Daram, Mohd Zainuddin, Ramesh Mullangi
A sensitive, specific, selective and rapid LC-ESI-MS/MS method has been developed and validated for the quantification of apalutamide in mice plasma using apalutamide-d3 as an internal standard (I.S.). Sample preparation was accomplished through a simple protein precipitation process. Chromatography of apalutamide and the I.S. was achieved on an Atlantis dC18 column using an isocratic mobile phase comprising 0.2% formic acid in water and acetonitrile (20:80, v/v) delivered at a flow rate of 0.8 mL/min. LC-MS/MS was operated under the multiple reaction-monitoring mode (MRM) using the electrospray ionization technique in positive ion mode and the transitions of m/z 478 → 450 and m/z 481 → 453 were used to measure the derivative of apalutamide and the I...
May 10, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29459439/apalutamide-ok-d-for-some-prostate-cancers
#10
(no author information available yet)
The FDA approved the antiandrogen apalutamide for the treatment of men with nonmetastatic, castration-resistant prostate cancer, the first drug for these patients greenlighted by the agency. Data from the definitive trial of apalutamide, presented at the 2018 Genitourinary Cancers Symposium, showed that the drug prolonged metastasis-free survival by more than 2 years compared with placebo. Data on the related drug enzalutamide, also presented at the symposium, showed that that drug led to dramatic improvements in metastasis-free survival, too...
April 2018: Cancer Discovery
https://www.readbyqxmd.com/read/29456088/apalutamide-shows-efficacy-in-prostate-cancer
#11
Elizabeth Gourd
No abstract text is available yet for this article.
March 2018: Lancet Oncology
https://www.readbyqxmd.com/read/29420164/apalutamide-treatment-and-metastasis-free-survival-in-prostate-cancer
#12
RANDOMIZED CONTROLLED TRIAL
Matthew R Smith, Fred Saad, Simon Chowdhury, Stéphane Oudard, Boris A Hadaschik, Julie N Graff, David Olmos, Paul N Mainwaring, Ji Youl Lee, Hiroji Uemura, Angela Lopez-Gitlitz, Géralyn C Trudel, Byron M Espina, Youyi Shu, Youn C Park, Wayne R Rackoff, Margaret K Yu, Eric J Small
BACKGROUND: Apalutamide, a competitive inhibitor of the androgen receptor, is under development for the treatment of prostate cancer. We evaluated the efficacy of apalutamide in men with nonmetastatic castration-resistant prostate cancer who were at high risk for the development of metastasis. METHODS: We conducted a double-blind, placebo-controlled, phase 3 trial involving men with nonmetastatic castration-resistant prostate cancer and a prostate-specific antigen doubling time of 10 months or less...
April 12, 2018: New England Journal of Medicine
https://www.readbyqxmd.com/read/29381490/comparison-of-the-effect-of-the-antiandrogen-apalutamide-arn-509-versus-bicalutamide-on-the-androgen-receptor-pathway-in-prostate-cancer-cell-lines
#13
Michael I Koukourakis, Christos Kakouratos, Dimitra Kalamida, Achilleas Mitrakas, Stamatia Pouliliou, Erasmia Xanthopoulou, Evdokia Papadopoulou, Virginia Fasoulaki, Alexandra Giatromanolaki
Apalutamide (ARN-509) is an antiandrogen that binds selectively to androgen receptors (AR) and does not show antagonist-to-agonist switch like bicalutamide. We compared the activity of ARN versus bicalutamide on prostate cancer cell lines. The 22Rv1, PC3, and DU145 cell lines were used to study the effect of ARN and bicalutamide on the expression cytoplasmic/nuclear kinetics of AR, AR-V7 variant, phosphorylated AR, as well as the levels of the AR downstream proteins prostate-specific antigen and TMPRSS2, under exposure to testosterone and/or hypoxia...
April 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28636139/review-of-hplc-and-lc-ms-ms-assays-for-the-determination-of-various-nonsteroidal-anti-androgens-used-in-the-treatment-of-prostate-cancer
#14
REVIEW
P S Suresh, Nuggehally R Srinivas, Ramesh Mullangi
Prostate cancer is the most common cancer and one of the leading causes of cancer deaths in men. One of the commonly used approaches to treat metastatic prostate cancer was via first-generation nonsteroidal anti-androgens (NSAAs), namely flutamide, nilutamide, bicalutamide and topilutamide. Most prostate cancer patients who are initially responsive develop the most aggressive form of disease called castration-resistant prostate cancer. Second-generation NSAA receptor antagonists (enzalutamide, apalutamide and darolutamide) are emerging as additional new options to treat castration-resistant prostate cancer...
January 2018: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28633425/androgen-receptor-mutations-in-patients-with-castration-resistant-prostate-cancer-treated-with-apalutamide
#15
D E Rathkopf, M R Smith, C J Ryan, W R Berry, N D Shore, G Liu, C S Higano, J J Alumkal, R Hauke, R F Tutrone, M Saleh, E Chow Maneval, S Thomas, D S Ricci, M K Yu, C J de Boer, A Trinh, T Kheoh, R Bandekar, H I Scher, E S Antonarakis
Background: Mutations in the androgen receptor (AR) ligand-binding domain (LBD), such as F877L and T878A, have been associated with resistance to next-generation AR-directed therapies. ARN-509-001 was a phase I/II study that evaluated apalutamide activity in castration-resistant prostate cancer (CRPC). Here, we evaluated the type and frequency of 11 relevant AR-LBD mutations in apalutamide-treated CRPC patients. Patients and methods: Blood samples from men with nonmetastatic CRPC (nmCRPC) and metastatic CRPC (mCRPC) pre- or post-abiraterone acetate and prednisone (AAP) treatment (≥6 months' exposure) were evaluated at baseline and disease progression in trial ARN-509-001...
September 1, 2017: Annals of Oncology: Official Journal of the European Society for Medical Oncology
https://www.readbyqxmd.com/read/28604629/androgen-receptor-dependent-and-independent-mechanisms-involved-in-prostate-cancer-therapy-resistance
#16
REVIEW
Daniel J Crona, Young E Whang
Despite the initial efficacy of androgen deprivation in prostate cancer, virtually all patients progress to castration-resistant prostate cancer (CRPC). Androgen receptor (AR) signaling is critically required for CRPC. A new generation of medications targeting AR, such as abiraterone and enzalutamide, has improved survival of metastatic CRPC (mCRPC) patients. However, a significant proportion of patients presents with primary resistance to these agents, and in the remainder, secondary resistance will invariably develop, which makes mCRPC the lethal form of the disease...
June 12, 2017: Cancers
https://www.readbyqxmd.com/read/28478926/design-synthesis-and-biological-evaluation-of-deuterated-apalutamide-with-improved-pharmacokinetic-profiles
#17
Xuehai Pang, Yingwei Wang, Yuanwei Chen
A series of deuterated apalutamide were designed and prepared. Compared to its prototype compound 18, deuterated analogues 19 and 21 showed obviously higher plasma concentrations and better PK parameters after oral administration in mice. In rats, N-trideuteromethyl compound 19 displayed 1.8-fold peak concentration (Cmax ), and nearly doubled its drug exposure in plasma (AUC0-∞ ) compared to compound 18. Unsurprisingly, compounds 18 and 19 had similar affinity for AR in vitro. In summary, the deuteration strategy could obviously improve PK parameters of apalutamide...
June 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28213364/safety-and-antitumor-activity-of-apalutamide-arn-509-in-metastatic-castration-resistant-prostate-cancer-with-and-without-prior-abiraterone-acetate-and-prednisone
#18
Dana E Rathkopf, Emmanuel S Antonarakis, Neal D Shore, Ronald F Tutrone, Joshi J Alumkal, Charles J Ryan, Mansoor Saleh, Ralph J Hauke, Rajesh Bandekar, Edna Chow Maneval, Carla J de Boer, Margaret K Yu, Howard I Scher
Purpose: To evaluate the efficacy of apalutamide before or after treatment with abiraterone acetate and prednisone (AAP) in patients with progressive metastatic castration-resistant prostate cancer (mCRPC). Experimental Design: Two cohorts were studied: AAP-naïve and post-AAP patients who had received ≥6 months of AAP. Patients had progressive mCRPC per rising prostate-specific antigen (PSA) and/or imaging, without prior chemotherapy exposure. All received apalutamide 240 mg/day. Primary endpoint was ≥50% decline in 12-week PSA according to Prostate Cancer Working Group 2 criteria...
July 15, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28144693/-phase%C3%A2-iii-study-for-local-or-locally-advanced-prostate-cancer-randomized-double-blind-placebo-controlled-phase%C3%A2-3-study-of-apalutamide-in-patients-with-local-high-risk-prostate-cancer-or-locally-advanced-prostate-cancer-receiving-primary-radiotherapy-atlas
#19
RANDOMIZED CONTROLLED TRIAL
https://www.readbyqxmd.com/read/27979426/nuclear-specific-ar-v7-protein-localization-is-necessary-to-guide-treatment-selection-in-metastatic-castration-resistant-prostate-cancer
#20
Howard I Scher, Ryon P Graf, Nicole A Schreiber, Brigit McLaughlin, David Lu, Jessica Louw, Daniel C Danila, Lyndsey Dugan, Ann Johnson, Glenn Heller, Martin Fleisher, Ryan Dittamore
BACKGROUND: Circulating tumor cells (CTCs) expressing AR-V7 protein localized to the nucleus (nuclear-specific) identify metastatic castration-resistant prostate cancer (mCRPC) patients with improved overall survival (OS) on taxane therapy relative to the androgen receptor signaling inhibitors (ARSi) abiraterone acetate, enzalutamide, and apalutamide. OBJECTIVE: To evaluate if expanding the positivity criteria to include both nuclear and cytoplasmic AR-V7 localization ("nuclear-agnostic") identifies more patients who would benefit from a taxane over an ARSi...
June 2017: European Urology
keyword
keyword
110246
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"