Pharmacokinetics of Abiraterone Acetate Released from a Tablet Based on Lipid Matrix in Beagle Dogs
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Information for the User ZYTIGA 500 Mg Film-Coated Tablets Abiraterone
Package leaflet: Information for the user ZYTIGA 500 mg film-coated tablets abiraterone acetate Read all of this leaflet carefully before you start taking this medicine because it contains important information for you. - Keep this leaflet. You may need to read it again. - If you have any further questions, ask your doctor or pharmacist. - This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours. - If you get any side effects talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. See section 4. What is in this leaflet: 1. What ZYTIGA is and what it is used for 2. What you need to know before you take ZYTIGA 3. How to take ZYTIGA 4. Possible side effects 5. How to store ZYTIGA 6. Contents of the pack and other information 1. What ZYTIGA is and what it is used for ZYTIGA contains a medicine called abiraterone acetate. It is used to treat prostate cancer in adult men that has spread to other parts of the body. ZYTIGA stops your body from making testosterone; this can slow the growth of prostate cancer. When ZYTIGA is prescribed for the early stage of disease where it is still responding to hormone therapy, it is used with a treatment that lowers testosterone (androgen deprivation therapy ). When you take this medicine your doctor will also prescribe another medicine called prednisone or prednisolone. This is to lower your chances of getting high blood pressure, having too much water in your body (fluid retention), or having reduced levels of a chemical known as potassium in your blood. -
Abiraterone Acetate for Chemotherapy-Naive
Fan et al. BMC Urology (2018) 18:110 https://doi.org/10.1186/s12894-018-0416-6 RESEARCHARTICLE Open Access Abiraterone acetate for chemotherapy- naive metastatic castration-resistant prostate cancer: a single-centre prospective study of efficacy, safety, and prognostic factors Liancheng Fan†, Baijun Dong†, Chenfei Chi†, Yanqing Wang†, Yiming Gong†, Jianjun Sha, Jiahua Pan, Xun Shangguan, Yiran Huang, Lixin Zhou* and Wei Xue* Abstract Background: To evaluate the efficacy and safety of abiraterone acetate (AA) plus prednisone compared with prednisone alone in Asian patients with chemotherapy-naive metastatic castration-resistant prostate cancer (mCRPC), and to identify predictive factors. Methods: We reviewed the medical records of 60 patients with chemotherapy-naive mCRPC at Renji Hospital who were treated with AA plus prednisone (n = 43) or prednisone alone (n = 17). All patients were assessed for prostate- specific antigen (PSA) response, PSA progression-free survival (PSA PFS), radiographic progression-free survival (rPFS), and overall survival (OS). The ability of several parameters to predict PSA PFS, rPFS, and OS was studied. Results: The median follow-up time was 14.0 months (range 7.0–18.5 months), at which time 19 death events had been reported: 11 in the AA + prednisone group and 8 in the prednisone group. The AA + prednisone group had significantly longer median PSA PFS (10.3 vs 3.0 months, P < 0.001), rPFS (13.9 vs 3.9 months, P < 0.001), and OS (23. 3 vs 17.5 months, P = 0.016) than the prednisone-alone group. The most frequently reported grade 3 or 4 adverse event in both the AA + prednisone and prednisone-alone groups was elevated alanine aminotransferase level in 5 of 43 patients (11.6%) and 2 of 17 patients (11.8%), respectively. -
YONSA (Abiraterone Acetate) Tablets May Have Different Dosing and Food Effects Than Other Abiraterone Acetate Products
HIGHLIGHTS OF PRESCRIBING INFORMATION hypokalemia before treatment. Monitor blood pressure, serum These highlights do not include all the information needed to use YONSA potassium and symptoms of fluid retention at least monthly. (5.1) safely and effectively. See full prescribing information for YONSA. • Adrenocortical insufficiency: Monitor for symptoms and signs of adrenocortical insufficiency. Increased dosage of corticosteroids YONSA® (abiraterone acetate) tablets, for oral use may be indicated before, during and after stressful situations. (5.2) Initial U.S. Approval: 2011 • Hepatotoxicity: Can be severe and fatal. Monitor liver function and modify, interrupt, or discontinue YONSA dosing as recommended. ----------------------------INDICATIONS AND USAGE-------------------------- YONSA is a CYP17 inhibitor indicated in combination with (5.3) methylprednisolone for the treatment of patients with metastatic castration- resistant prostate cancer (CRPC). (1) ------------------------------ADVERSE REACTIONS------------------------------ The most common adverse reactions (≥ 10%) are fatigue, joint swelling or ----------------------DOSAGE AND ADMINISTRATION---------------------- discomfort, edema, hot flush, diarrhea, vomiting, cough, hypertension, To avoid medication errors and overdose, be aware that YONSA tablets may dyspnea, urinary tract infection and contusion. have different dosing and food effects than other abiraterone acetate products. Recommended dose: YONSA 500 mg (four 125 mg tablets) administered The most common laboratory -
Ep 3027638 B1
(19) TZZ¥Z ¥_T (11) EP 3 027 638 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: C07J 31/00 (2006.01) C07J 43/00 (2006.01) 27.12.2017 Bulletin 2017/52 (86) International application number: (21) Application number: 13771622.1 PCT/IB2013/056206 (22) Date of filing: 29.07.2013 (87) International publication number: WO 2015/015246 (05.02.2015 Gazette 2015/05) (54) PROCESS FOR THE PREPARATION OF ABIRATERONE AND ABIRATERONE ACETATE VERFAHREN ZUR HERSTELLUNG VON ABIRATERON ODER ABIRATERONACETAT PROCÉDÉ DE PRÉPARATION D’ABIRATÉRONE ET D’ACÉTATE D’ABIRATÉRONE (84) Designated Contracting States: (56) References cited: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB WO-A1-93/20097 WO-A1-2006/021777 GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO WO-A2-2014/207567 PL PT RO RS SE SI SK SM TR • SUN Q ET AL: "Pd(PPh3)4/AgOAc-catalyzed (43) Date of publication of application: coupling of 17-steroidal triflates and alkynes: 08.06.2016 Bulletin 2016/23 Highly efficient synthesis of D-ring unsaturated 17-alkynylsteroids", STEROIDS, ELSEVIER (73) Proprietor: Industriale Chimica S.R.L. SCIENCE PUBLISHERS, NEW YORK, NY, US, vol. 20145 Milano (IT) 75, no. 12, 1 December 2010 (2010-12-01), pages 936-943, XP027221112, ISSN: 0039-128X (72) Inventors: [retrieved on 2010-06-01] • LENNA, Roberto I-20010 S. Giorgio Su Legnano (IT) Remarks: • DI BRISCO, Riccardo Thefile contains technical information submitted after I-28069 Trecate (IT) the application was filed and not included in this specification (74) Representative: Palladino, Saverio Massimo et al Notarbartolo & Gervasi S.p.A. -
Therapies Targeted to Androgen Receptor Signaling Axis in Prostate Cancer: Progress, Challenges, and Hope
cancers Review Therapies Targeted to Androgen Receptor Signaling Axis in Prostate Cancer: Progress, Challenges, and Hope Sirin Saranyutanon 1,2, Sanjeev Kumar Srivastava 1,2,*, Sachin Pai 3, Seema Singh 1,2,4 and Ajay Pratap Singh 1,2,4,* 1 Department of Pathology, College of Medicine, University of South Alabama, Mobile, AL 36617, USA; [email protected] (S.S.); [email protected] (S.S.) 2 Department of Oncologic Sciences, Mitchell Cancer Institute, University of South Alabama, Mobile, AL 36604, USA 3 Department of Medical Oncology, Mitchell Cancer Institute, University of South Alabama, Mobile, AL 36604, USA; [email protected] 4 Department of Biochemistry and Molecular Biology, College of Medicine, University of South Alabama, Mobile, AL 36688, USA * Correspondence: [email protected] (S.K.S.); [email protected] (A.P.S.); Tel.: +1-251-445-9874 (S.K.S.); +1-251-445-9843 (A.P.S.) Received: 4 November 2019; Accepted: 18 December 2019; Published: 23 December 2019 Abstract: Prostate cancer is the mostly commonly diagnosed non-cutaneous malignancy and the second leading cause of cancer-related death affecting men in the United States. Moreover, it disproportionately affects the men of African origin, who exhibit significantly greater incidence and mortality as compared to the men of European origin. Since androgens play an important role in the growth of normal prostate and prostate tumors, targeting of androgen signaling has remained a mainstay for the treatment of aggressive prostate cancer. Over the years, multiple approaches have been evaluated to effectively target the androgen signaling pathway that include direct targeting of the androgens, androgen receptor (AR), AR co-regulators or other alternate mechanisms that impact the outcome of androgen signaling. -
Assessment Report for Zytiga (Abiraterone) Procedure
21 July 2011 EMA/CHMP/542871/2011 Committee for Medicinal Products for Human Use (CHMP) Assessment Report For Zytiga (abiraterone) Procedure No.: EMEA/H/C/002321 Assessment Report as adopted by the CHMP with all information of a commercially confidential nature deleted 7 Westferry Circus ● Canary Wharf ● London E14 4HB ● United Kingdom Telephone +44 (0)20 7418 8400 Facsimle +44 (0)20 7523 7455 E-mail [email protected] Website www.ema.europa.eu An agency of the European Union TABLE OF CONTENTS 1. Background information on the procedure .............................................. 5 1.1. Submission of the dossier .................................................................................... 5 1.2. Steps taken for the assessment of the product........................................................ 5 2. Scientific discussion................................................................................ 6 2.1. Introduction....................................................................................................... 6 2.2. Quality aspects .................................................................................................. 8 2.2.1. Introduction.................................................................................................... 8 2.2.2. Active Substance ............................................................................................. 9 2.2.3. Finished Medicinal Product .............................................................................. 10 2.2.4. Discussion on chemical, pharmaceutical -
Hikma Launches Abiraterone Acetate Tablets
Press Release Hikma launches Abiraterone Acetate Tablets London, 14 February 2019 – Hikma Pharmaceuticals PLC (Hikma, Group) (LSE: HIK) (NASDAQ Dubai: HIK) (OTC: HKMPY) (rated Ba1 Moody’s / BB+ S&P, both stable) announces that Hikma Pharmaceuticals USA Inc., formerly known as West-Ward Pharmaceuticals Corp., has launched Abiraterone Acetate Tablets, 250mg, the generic equivalent to Zytiga®.1 Abiraterone acetate tablets are a CYP17 inhibitor indicated in combination with prednisone for the treatment of patients with metastatic castration-resistant prostate cancer (CRPC). In October 2018, the United States District Court for the District of New Jersey’s invalidated a key Zytiga® patent. On 20 November 2018, the United States Court of Appeals for the Federal Circuit denied the patent holder’s request to prevent Hikma’s launching Abiraterone Acetate Tablets pending appeal. Hikma was one of the first ANDA applicants to submit an ANDA with a Paragraph IV certification challenging the validity of certain patents listed for Zytiga® tablets, 250mg, and therefore is eligible for 180 days of generic drug exclusivity. According to IQVIA, US sales of Abiraterone Acetate Tablets were approximately $1,793 million in the 12 months ending December 2018. Brian Hoffmann, President, Generics Division, said, “We are adding Abiraterone Acetate Tablets to our oncology portfolio, improving patients access to this life-saving product. This launch continues to demonstrate our ability to successfully litigate paragraph IV products, which is an important element of our portfolio strategy.” -- ENDS -- Enquiries Hikma Pharmaceuticals PLC Susan Ringdal +44 (0)20 7399 2760/ +44 7776 477050 EVP, Strategic Planning and Global Affairs [email protected] FTI Consulting Ben Atwell/Andrew Ward +44 (0)20 3727 1000 1 Zytiga® is a registered trademark of Janssen Biotech, Inc. -
2021 Formulary List of Covered Prescription Drugs
2021 Formulary List of covered prescription drugs This drug list applies to all Individual HMO products and the following Small Group HMO products: Sharp Platinum 90 Performance HMO, Sharp Platinum 90 Performance HMO AI-AN, Sharp Platinum 90 Premier HMO, Sharp Platinum 90 Premier HMO AI-AN, Sharp Gold 80 Performance HMO, Sharp Gold 80 Performance HMO AI-AN, Sharp Gold 80 Premier HMO, Sharp Gold 80 Premier HMO AI-AN, Sharp Silver 70 Performance HMO, Sharp Silver 70 Performance HMO AI-AN, Sharp Silver 70 Premier HMO, Sharp Silver 70 Premier HMO AI-AN, Sharp Silver 73 Performance HMO, Sharp Silver 73 Premier HMO, Sharp Silver 87 Performance HMO, Sharp Silver 87 Premier HMO, Sharp Silver 94 Performance HMO, Sharp Silver 94 Premier HMO, Sharp Bronze 60 Performance HMO, Sharp Bronze 60 Performance HMO AI-AN, Sharp Bronze 60 Premier HDHP HMO, Sharp Bronze 60 Premier HDHP HMO AI-AN, Sharp Minimum Coverage Performance HMO, Sharp $0 Cost Share Performance HMO AI-AN, Sharp $0 Cost Share Premier HMO AI-AN, Sharp Silver 70 Off Exchange Performance HMO, Sharp Silver 70 Off Exchange Premier HMO, Sharp Performance Platinum 90 HMO 0/15 + Child Dental, Sharp Premier Platinum 90 HMO 0/20 + Child Dental, Sharp Performance Gold 80 HMO 350 /25 + Child Dental, Sharp Premier Gold 80 HMO 250/35 + Child Dental, Sharp Performance Silver 70 HMO 2250/50 + Child Dental, Sharp Premier Silver 70 HMO 2250/55 + Child Dental, Sharp Premier Silver 70 HDHP HMO 2500/20% + Child Dental, Sharp Performance Bronze 60 HMO 6300/65 + Child Dental, Sharp Premier Bronze 60 HDHP HMO -
HSD3B1 and Response to a Nonsteroidal CYP17A1 Inhibitor in Castration-Resistant Prostate Cancer
Research JAMA Oncology | Brief Report HSD3B1 and Response to a Nonsteroidal CYP17A1 Inhibitor in Castration-Resistant Prostate Cancer Nima Almassi, MD; Chad Reichard, MD; Jianbo Li, PhD; Carly Russell, MS; Jaselle Perry, MS; Charles J. Ryan, MD; Terence Friedlander, MD; Nima Sharifi, MD Invited Commentary page 562 IMPORTANCE The HSD3B1 (1245C) germline variant encodes for a gain-of-function missense Related article page 558 in 3β-hydroxysteroid dehydrogenase isoenzyme 1 (3βHSD1) that results in increased dihydrotestosterone synthesis from extragonadal precursors and is predictive of more rapid progression to castration-resistant prostate cancer (CRPC). OBJECTIVE To determine whether the HSD3B1 (1245C) genotype is predictive of clinical response to extragonadal androgen ablation with nonsteroidal 17α-hydroxylase/17,20-lyase (CYP17A1) inhibition in men with metastatic CRPC. DESIGN, SETTING, AND PARTICIPANTS An observational study of men with metastatic CRPC treated with ketoconazole between June 1998 and December 2012 was conducted at the University of California, San Francisco. EXPOSURES Extragonadal androgen ablation with the nonsteroidal CYP17A1 inhibitor ketoconazole among men with metastatic CRPC. MAIN OUTCOMES AND MEASURES The primary end points of analysis were duration of ketoconazole therapy and time to disease progression stratified by HSD3B1 genotype. Disease progression was defined as either biochemical or radiographic progression, using the Prostate Cancer Working Group 3 and Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1 definitions, respectively. Kaplan-Meier analysis was used to estimate time on therapy and time to disease progression. A log-rank test for trend was used to compare outcomes by HSD3B1 genotype. RESULTS A total of 90 men (median [interquartile range] age, 61.5 [55.3-67.0] years) with metastatic CRPC were included in the analysis, with sufficient data to determine duration of ketoconazole therapy and time to disease progression in 88 and 81 patients, respectively. -
Zytiga Datasheet
ZYTIGA® abiraterone acetate NEW ZEALAND DATA SHEET 1. PRODUCT NAME ZYTIGA 250 mg tablets ZYTIGA 500 mg film-coated tablets 2. QUALITATIVE AND QUANTITATIVE COMPOSITION ZYTIGA tablets contain either 250 mg or 500 mg of abiraterone acetate. Excipients with known effects: Each 250 mg tablet contains 189 mg of lactose and 6.8 mg of sodium. Each 500 mg film-coated tablet contains 253.2 mg of lactose and 13.5 mg of sodium. For the full list of excipients, see section 6.1. 3. PHARMACEUTICAL FORM ZYTIGA 250 mg uncoated tablets are white to off-white, oval-shaped tablets, debossed with “AA250” on one side. ZYTIGA 500 mg film-coated tablets are purple, oval-shaped, film-coated tablets, debossed with “AA” on one side and “500” on the other. 4. CLINICAL PARTICULARS 4.1 Therapeutic indications ZYTIGA is indicated in combination with prednisone or prednisolone and androgen deprivation therapy (ADT) for the treatment of high-risk metastatic hormone naïve prostate cancer (mHNPC) or newly diagnosed high-risk metastatic hormone sensitive prostate cancer (mHSPC) ZYTIGA is also indicated with prednisone or prednisolone for: • the treatment of patients with metastatic castration resistant prostate cancer (mCRPC) who are asymptomatic or mildly symptomatic after failure of androgen deprivation therapy (ADT) in whom chemotherapy is not yet clinically indicated (see Clinical Trials section). • the treatment of patients with metastatic advanced prostate cancer (castration resistant prostate cancer, mCRPC) who have received prior chemotherapy containing a taxane. 4.2 Dose and method of administration The recommended dosage of ZYTIGA is 1000 mg (either two 500 mg tablets or four 250 mg tablets) as a single daily dose that must not be taken with food. -
Slow Tight Binding Inhibition of CYP17A1 by Abiraterone Redefines Its Kinetic Selectivity and Dosing Regimen
JPET Fast Forward. Published on June 17, 2020 as DOI: 10.1124/jpet.120.265868 This article has not been copyedited and formatted. The final version may differ from this version. JPET # 265868 Slow tight binding inhibition of CYP17A1 by abiraterone redefines its kinetic selectivity and dosing regimen Eleanor Jing Yi Cheong1, Pramod C Nair2, Rebecca Wan Yi Neo1, Ho Thanh Tu1, Fu Lin3, Edmund Chiong4,5, Kesavan Esuvaranathan4,5, Hao Fan6, Russell Z. Szmulewitz7, Cody J. Peer8, William D. Figg8, Christina Li Lin Chai1, John O Miners2, Eric Chun Yong Chan1,9 1Department of Pharmacy, Faculty of Science, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore; 2Department of Clinical Pharmacology and Flinders Centre for Downloaded from Innovation in Cancer, College of Medicine and Public Health, Flinders University, Adelaide, Australia; 3Bioinformatics Institute, Biotransformation Innovation Platform (BioTrans), Agency for Science, Technology and Research (A*STAR), 30 Biopolis Street, Singapore 138671; 4Department of Surgery, jpet.aspetjournals.org National University Health System, 5 Lower Kent Ridge Road, Singapore 119074, Singapore; 5Department of Urology, National University Hospital, 5 Lower Kent Ridge Road, Singapore 119074; 6Bioinformatics Institute, Agency for Science, Technology and Research (A*STAR), 30 Biopolis Street, at ASPET Journals on September 27, 2021 Singapore 138671; Department of Biological Sciences, National University of Singapore, 14 Science 23 Drive 4, Singapore 117543; Centre for Computational Biology, DUKE-NUS Medical School, 8 College Road, Singapore 169857; 7The University of Chicago, Chicago, 8National Cancer Institute, Rockville, MD, 9National University Cancer Institute, Singapore (NCIS), NUH Medical Centre (NUHMC), 5 Lower Kent Ridge Road, Singapore 119074 1 | Page JPET Fast Forward. -
High Content Screening Using New U2OS Reporter Cell Models Identifies Harmol Hydrochloride As a Selective and Competitive Antago
cells Article High Content Screening Using New U2OS Reporter Cell Models Identifies Harmol Hydrochloride as a Selective and Competitive Antagonist of the Androgen Receptor 1,2, 1,2,3, 1,2 1,2 Hadjer Dellal y, Abdelhay Boulahtouf y, Elina Alaterre , Alice Cuenant , Marina Grimaldi 1,2, William Bourguet 2,4 ,Céline Gongora 1,2, Patrick Balaguer 1,2,* and Philippe Pourquier 1,2,* 1 IRCM, Institut de Recherche en Cancérologie de Montpellier, INSERM U1194, F-34298 Montpellier, France; [email protected] (H.D.); [email protected] (A.B.); [email protected] (E.A.); [email protected] (A.C.); [email protected] (M.G.); [email protected] (C.G.) 2 Université de Montpellier, F-34298 Montpellier, France; [email protected] 3 Institut régional du Cancer de Montpellier, F-34298 Montpellier, France 4 Centre de Biochimie Structurale, CNRS, INSERM, Université de Montpellier, F-34298 Montpellier, France * Correspondence: [email protected] (P.B.); [email protected] (P.P.); Tel.: +33-4-67-61-24-09 (P.B.); +33-4-66-68-32-31 (P.P.); Fax: +33-4-67-61-23-37 (P.B.); +33-4-66-68-37-02 (P.P.) H.D. and A.B. contributed equally. y Received: 6 May 2020; Accepted: 11 June 2020; Published: 16 June 2020 Abstract: Prostate cancer is the most commonly diagnosed malignancy in men. Its growth mainly relies on the activity of the androgen receptor (AR), justifying the use of androgen deprivation therapy as a gold standard treatment for the metastatic disease.