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Marie Deguigne, Marion Brunet, Chadi Abbara, Alain Turcant, Gaël Le Roux, Bénédicte Lelièvre
OBJECTIVE: We report two cases of elevated digoxin plasma levels in patients receiving enzalutamide. Cases reported: The first patient, an 84-year-old male treated with enzalutamide, was hospitalized due to deterioration in his general state. Atrial fibrillation was discovered and treatment with digoxin was initiated. Supratherapeutic digoxin concentrations (4 µg/L and 3.5 µg/L 3 days later) led to treatment being stopped despite the lack of clinical or biological signs of overdose...
May 9, 2018: Clinical Toxicology
Xuedong Chen, Jieyang Lu, Liqun Xia, Gonghui Li
Understanding and targeting the mechanisms of resistance to enzalutamide in castration resistant prostate cancer. BACKGROUND: Enzalutamide (MDV3100, XTANDI) is a second generation androgen receptor inhibitor that is designed for the treatment of castration-resistant prostate cancer (CRPC) and has prolonged survival time. The mechanisms of mdv3100 resistance have not yet been clearly clarified and the majority of treated patients, innate or acquiring resistance invariably arises. OBJECTIVE: The purpose of this review is to summarize the main data available on the mechanisms of resistance to mdv3100...
2018: Current Drug Targets
Aditi Mridul Panditrao
No abstract text is available yet for this article.
January 2017: International Journal of Applied and Basic Medical Research
Chloé Alberto, Maria Polina Konstantinou, Catherine Martinage, Eline Casassa, Emilie Tournier, Haleh Bagheri, Vincent Sibaud, Loïc Mourey, Juliette Mazereeuw-Hautier, Nicolas Meyer, Carle Paul, Cristina Bulai Livideanu
INTRODUCTION: Enzalutamide (Xtandi®) is a new potent inhibitor of the signaling pathway for the androgen receptor with a half-life of 5.8 days. It has been on the market for the treatment of metastatic castration-resistant prostate cancer since November 2013. OBJECTIVE: We report the first case of acute generalized exanthematous pustulosis (AGEP) induced by enzalutamide. OBSERVATION: A 62-year-old male patient with no significant medical history, was diagnosed in April 2014 with metastatic prostatic adenocarcinoma...
November 13, 2016: Journal of Dermatological Case Reports
Trevor M Penning, Daniel Tamae
PURPOSE OF REVIEW: Androgen deprivation therapy is a cornerstone in the treatment of advanced prostate cancer and has extended the lives of countless patients. Unfortunately, many of these patients eventually succumb to metastatic castration-resistant prostate cancer (mCRPC). The efficacy of abiraterone acetate (AA, Zytiga) and enzalutamide (Enza, Xtandi) in the mCRPC setting prove that these tumors remain androgen-driven. We review recent studies that have shown that intratumoral androgen biosynthesis plays a significant role in the ever-evolving mCRPC tumor and we discuss the therapeutic implications of these findings...
June 2016: Current Opinion in Endocrinology, Diabetes, and Obesity
Thenappan Chandrasekar, Joy C Yang, Allen C Gao, Christopher P Evans
Despite advances in prostate cancer diagnosis and management, morbidity from prostate cancer remains high. Approximately 20% of men present with advanced or metastatic disease, while 29,000 men continue to die of prostate cancer each year. Androgen deprivation therapy (ADT) has been the standard of care for initial management of advanced or metastatic prostate cancer since Huggins and Hodges first introduced the concept of androgen-dependence in 1972, but progression to castration-resistant prostate cancer (CRPC) occurs within 2-3 years of initiation of ADT...
June 2015: Translational Andrology and Urology
Frank dela Rama, Caroline Pratz
BACKGROUND: Treatment of metastatic castration-resistant prostate cancer (mCRPC) has evolved rapidly. In particular, five new treatments that extend survival in mCRPC have been approved since 2010, including the chemotherapy cabazitaxel (Jevtana®), hormonal agents abiraterone (Zytiga®) and enzalutamide (Xtandi®), vaccine sipuleucel-T (Provenge®), and radiopharmaceutical radium-223 (Xofigo®); all have different indications and toxicity profiles. OBJECTIVES: This review discusses treatment advances in mCRPC, including considerations for side-effect management and treatment sequencing...
December 2015: Clinical Journal of Oncology Nursing
Wijdan H Ramadan, Wissam K Kabbara, Hiba S Al Basiouni Al Masri
OBJECTIVE: To review and evaluate current literature on the US Food and Drug Administration (FDA)-approved drug enzalutamide (XTANDI(®)) in metastatic castration-resistant prostate cancer. DATA SOURCES: Literature search was done through PubMed using the terms enzalutamide, MDV3100, abiraterone, and castration-resistant prostate cancer. Data from FDA product labels were also used. STUDY SELECTION AND DATA EXTRACTION: Recent and relevant studies were included in the review...
2015: OncoTargets and Therapy
Gillian M Keating
Enzalutamide (Xtandi(®)) is an androgen receptor inhibitor that blocks several steps in the androgen receptor signalling pathway. This article reviews the clinical efficacy and tolerability of oral enzalutamide in chemotherapy-naïve men with metastatic castration-resistant prostate cancer (CRPC), as well as summarizing its pharmacological properties. In the randomized, double-blind, multinational PREVAIL trial, enzalutamide significantly improved both radiographic progression-free survival and overall survival versus placebo in chemotherapy-naïve men with metastatic CRPC who were asymptomatic or mildly symptomatic...
March 2015: Drugs & Aging
Tian Zhang, Jason Zhu, Daniel J George, Andrew J Armstrong
INTRODUCTION: Over the past decade, treatment options for men with metastatic castration-resistant prostate cancer (CRPC) have expanded with the addition of abiraterone acetate (AA), enzalutamide, sipuleucel-T, radium-223, docetaxel and cabazitaxel. The optimal sequencing of therapies in the context of efficacy and known cross-resistance remains uncertain. AREAS COVERED: We review the development of enzalutamide (MDV3100, Xtandi), a novel second-generation androgen receptor (AR), and AA (Zytiga), a selective, irreversible inhibitor of cytochrome P17...
March 2015: Expert Opinion on Pharmacotherapy
Alexandre V Ivachtchenko, Oleg D Mitkin, Elizaveta V Kudan, Alexey A Rjahovsky, Anton A Vorobiev, Andrey S Trifelenkov, Natalia A Shevkun, Oxana V Proskurina, Dmitry V Kravchenko, Ruben N Karapetian
Recently new drugs targeting androgen-dependent axis have been approved for the treatment of castration-resistant prostate cancer (CRPC) - Zytiga and Xtandi (formerly MDV3100), several other candidates (for example, ARN-509) are in early phases of clinical trials. However despite significant improvement in overall survival with new treatments it is evident that resistance to these drugs develops. One of the approaches to overcome it is combination therapy and from this point of view some potential for drug-drug interactions can limit the application of the drug...
2014: Journal of Cancer
Lunawati L Bennett, April Ingason
OBJECTIVE: To review the pharmacology and pharmacokinetics, and to evaluate the clinical efficacy, safety, and place in therapy of enzalutamide for the treatment of castration-resistant prostate cancer (CRPC). DATA SOURCES: A literature search through PubMed (1984 to November 2013; English language) was performed using the following keywords: MDV3100, androgen deprivation therapy, enzalutamide, CRPC, and androgen receptor antagonist. Searches were limited to published studies in humans...
April 2014: Annals of Pharmacotherapy
Yangmin M Ning, William Pierce, V Ellen Maher, Stella Karuri, Sheng-Hui Tang, Haw-Jyh Chiu, Todd Palmby, Jeanne Fourie Zirkelbach, Dhananjay Marathe, Nitin Mehrotra, Qi Liu, Debasis Ghosh, Christy L Cottrell, John Leighton, Rajeshwari Sridhara, Amna Ibrahim, Robert Justice, Richard Pazdur
This article summarizes the regulatory evaluation that led to the full approval of enzalutamide (XTANDI, Medivation Inc.) by the U.S. Food and Drug Administration (FDA) on August 31, 2012, for the treatment of patients with metastatic castration-resistant prostate cancer who have previously received docetaxel. This approval was based on the results of a randomized, placebo-controlled trial which randomly allocated 1,199 patients with mCRPC who had received prior docetaxel to receive either enzalutamide, 160 mg orally once daily (n = 800), or placebo (n = 399)...
November 15, 2013: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
Mark Sanford
Enzalutamide (MDV3100, XTANDI(®)) is an androgen receptor inhibitor that is indicated for the treatment of metastatic, castration-resistant, prostate cancer (mCRPC) that has progressed despite treatment with docetaxel. This article reviews the pharmacology, efficacy and tolerability of enzalutamide relevant to this indication. In a randomized, double-blind, placebo-controlled, multinational, phase III trial in patients with mCRPC progressing after docetaxel therapy, enzalutamide significantly prolonged overall survival (OS), delayed prostate specific antigen progression and prolonged radiographic progression-free survival and time to the first skeletal event...
October 2013: Drugs
Javier Guerrero, Iván E Alfaro, Francisco Gómez, Andrew A Protter, Sebastián Bernales
BACKGROUND: Enzalutamide (formerly MDV3100 and available commercially as Xtandi), a novel androgen receptor (AR) signaling inhibitor, blocks the growth of castration-resistant prostate cancer (CRPC) in cellular model systems and was shown in a clinical study to increase survival in patients with metastatic CRPC. Enzalutamide inhibits multiple steps of AR signaling: binding of androgens to AR, AR nuclear translocation, and association of AR with DNA. Here, we investigate the effects of enzalutamide on AR signaling, AR-dependent gene expression and cell apoptosis...
September 2013: Prostate
Richa Dhingra, Tina Sharma, Sukhminder Singh, Shivani Sharma, Prince Tomar, Manav Malhotra, T R Bhardwaj
Prostate cancer is the most common malignancy among men found to be the second leading cause of male cancer-related mortality due to development of resistance against androgen deprivation therapy (ADT). With the advancement in understanding of prostate cancer, numbers of agents have been emerged to target Androgen-Receptor (AR) signaling for the treatment of castration resistant prostate cancer (CRPC). Food and Drug Administration (FDA) has recently approved enzalutamide (XTANDI) for the treatment of CRPC. Androgen receptor promotes the prostate cancer progression after transformation...
August 2013: Mini Reviews in Medicinal Chemistry
(no author information available yet)
No abstract text is available yet for this article.
March 4, 2013: Medical Letter on Drugs and Therapeutics
Jean Hoffman-Censits, Wm Kevin Kelly
Enzalutamide (MDV3100, Xtandi, Medivation\Astellas) is an oral inhibitor of androgen receptor signaling that blocks androgen receptor interaction, inhibits translocation of the androgen receptor to the nucleus, impairs androgen receptor binding to DNA, and inhibits coactivator recruitment and receptor-mediated DNA transcription. In a phase III randomized study comparing enzalutamide with placebo in men with progressive castration-resistant prostate cancer (CRPC) who were previously treated with docetaxel, enzalutamide showed an improvement in overall survival (18...
March 15, 2013: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
Marvin M Goldenberg
Truvada for HIV prevention, Xtandi for metastatic castration-resistant prostate cancer, and Marqibo, a vincristine liposome injection for acute myelogenous leukemia.
October 2012: P & T: a Peer-reviewed Journal for Formulary Management
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