Selective Progesterone Receptor Modulators in Gynaecological Therapies
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(12) United States Patent (10) Patent No.: US 7,871,995 B2 Bunschoten Et Al
US00787 1995 B2 (12) United States Patent (10) Patent No.: US 7,871,995 B2 Bunschoten et al. (45) Date of Patent: *Jan. 18, 2011 (54) DRUG DELIVERY SYSTEM COMPRISINGA (52) U.S. Cl. ....................................... 514/171; 514/182 TETRAHYDROXYLATED ESTROGEN FOR (58) Field of Classification Search ................. 514/171, USE IN HORMONAL CONTRACEPTION 514f182 See application file for complete search history. (75) Inventors: Evert Johannes Bunschoten, Heesch (NL); Herman Jan Tijmen Coelingh (56) References Cited Bennink, Driebergen (NL); Christian U.S. PATENT DOCUMENTS Franz Holinka, New York, NY (US) 3,440,320 A 4, 1969 Sackler et al. O O 3,797.494. A 3, 1974 Zaffaroni (73) Assignee: Pantarhei Bioscience B.V., Al Zeist 4,460.372 A 7/1984 Campbell et al. (NL) 4,573.996 A 3/1986 Kwiatek et al. 4,624,665 A 1 1/1986 Nuwayser (*) Notice: Subject to any disclaimer, the term of this 4,722,941 A 2f1988 Eckert et al. patent is extended or adjusted under 35 4,762,717 A 8/1988 Crowley, Jr. U.S.C. 154(b) by 1233 days. 4.937,238 A 6, 1990 Lemon 5,063,507 A 1 1/1991 Lindsey et al. This patent is Subject to a terminal dis- 5,130,137 A 7/1992 Crowley, Jr. claimer. 5,211,952 A 5/1993 Spicer et al. 5,223,261 A 6/1993 Nelson et al. 5,340,584 A 8/1994 Spicer et al. (21) Appl. No.: 10/478,357 5,340,585 A 8/1994 Pike et al. 1-1. 5,340,586 A 8, 1994 Pike et al. -
Abnormal Uterine Bleeding: Strategies for Management”
PRE-CONGRESS COURSE 4 SIG Endometriosis & Endometrium “Abnormal uterine bleeding: strategies for management” CONTENTS Program overview p. 1 Speakers’ contributions • Abnormalities of menstrual bleeding: getting our terminologies right - I. Fraser (AUS) p. 3 • Abnormal uterine bleeding: the patient perspective - P. Warner (UK) p. 13 • Optimising strategies for evaluation and management of abnormal uterine bleeding - A. Prentice (UK) p. 32 • Unscheduled bleeding with exogenous hormone administration – P. Rogers (AUS) p. 33 • Strategies to control; endometrial bleeding - D. Archer (USA) p. 46 • Local mechanisms responsible for endometrial bleeding - H. Critchley (UK) p. 49 • Is there a role for selective progesterone receptor modulators in management of uterine bleeding? - K. Chwalisz (USA) p. 61 • Should menstruation be optional? – Health benefits of amenorrhoea – D. Baird (UK) p. 72 PRE-CONGRESS COURSE 4 - PROGRAMME SIG Endometriosis & Endometrium Abnormal uterine bleeding: strategies for management Course co-ordinators: H. Critchley (UK) & Th. D’Hooghe (B) Course description: Problematic uterine bleeding impairs quality of life for many women and often involves invasive treatments and significant cost. Agreement is needed on terminology and defi nitions in order to facilitate the establishment of multi-centre clinical trials evaluating the strategies for management. Contemporary management also requires an understanding of the patient’s perspective of her complaint and an understanding of acceptability to women of the available modes of investigation and treatment options. Optimal therapies will only be possible with a detailed understanding of the mechanisms involved in endometrial bleeding including unscheduled bleeding with exogenous hormone administration. Novel therapies need to be evaluated in the context of potential health benefits from therapies that reduce the number of menstrual cycles experienced by women. -
The Rising Phoenix-Progesterone As the Main Target of the Medical Therapy for Leiomyoma
Hindawi BioMed Research International Volume 2017, Article ID 4705164, 8 pages https://doi.org/10.1155/2017/4705164 Review Article The Rising Phoenix-Progesterone as the Main Target of the Medical Therapy for Leiomyoma H. H. Chill, M. Safrai, A. Reuveni Salzman, and A. Shushan Department of Obstetrics and Gynecology, Hadassah-Hebrew University Medical Center, Jerusalem, Israel Correspondence should be addressed to M. Safrai; [email protected] H. H. Chill and M. Safrai contributed equally to this work. Received 23 June 2017; Accepted 6 August 2017; Published 13 September 2017 Academic Editor: Markus Wallwiener Copyright © 2017 H. H. Chill et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. Leiomyomas, also known as uterine fibroids, are a common benign tumor in women of reproductive age. These lesions disrupt the function of the uterus causing menorrhagia and pelvic pressure as wellasreproductivedisorders.Thesewomenposeatruechallenge for clinicians in the attempt of choosing the suitable treatment for each patient. Patient’s age, interest in fertility preservation, and leiomyoma location and size are all factors to be taken into account when deciding upon the preferable therapeutic option. For the past few decades, surgical treatment was the only reliable long-term treatment available. A variety of surgical approaches have been developed over the years but these developments have come at the expense of other treatment options. The classical medical treatment includes gonadotropin-releasing hormone (GnRH) agonists and antagonists. These agents are well known for their limited clinical effect as well as their broad spectrum of side effects, inspiring a need for new pharmacological treatments. -
Quick-Starting After UPA Final
STATEMENT FROM THE CLINICAL EFFECTIVENESS UNIT September 2015 Faculty of Sexual and Reproductive Healthcare (FSRH) response to new data on quick- starting hormonal contraception after use of ulipristal acetate 30mg (ellaOne®) for emergency contraception. In 2010, the FSRH introduced guidelines supporting immediate commencement (“quick- start”) of hormonal contraception after administration of oral emergency contraception (EC).1 There is evidence that after oral EC, further episodes of unprotected intercourse in the same cycle put women at risk of pregnancy. 2 The advice applied to both levonorgestrel (LNG) and ulipristal acetate (UPA) given as EC. UPA is a selective progesterone-receptor modulator. Its primary mechanism of action as EC is to delay ovulation until sperm from an act of unprotected intercourse are no longer viable. In contrast to LNG, UPA can delay ovulation even after the start of the luteinising hormone (LH) surge,3 and meta-analysis of the available data concludes that UPA prevents significantly more pregnancies than LNG. 4 It has, however been postulated that: 1. The effectiveness of a progestogen-containing contraceptive method that is quick started immediately after administration of UPA might be reduced by UPA due to competition at the progesterone receptor site. 2. The effect of UPA in delaying ovulation might be reduced by quick-starting a progestogen-containing contraceptive. Regarding 1: Two recent studies suggest that UPA may not reduce the effectiveness of quick-started hormonal contraception.5,6 In their double-blind, randomised, placebo- controlled trial, Cameron et al . found no difference between the time taken for a combined oral contraceptive (COC) to induce ovarian quiescence when started immediately after UPA (n=39) and when the COC was taken after placebo ( n=37). -
Mifepristone
1. NAME OF THE MEDICINAL PRODUCT Mifegyne 200 mg tablets 2. QUALITATIVE AND QUANTITATIVE COMPOSITION Each tablet contains 200-mg mifepristone. For the full list of excipients, see section 6.1 3. PHARMACEUTICAL FORM Tablet. Light yellow, cylindrical, bi-convex tablets, with a diameter of 11 mm with “167 B” engraved on one side. 4. CLINICAL PARTICULARS For termination of pregnancy, the anti-progesterone mifepristone and the prostaglandin analogue can only be prescribed and administered in accordance with New Zealand’s abortion laws and regulations. 4.1 Therapeutic indications 1- Medical termination of developing intra-uterine pregnancy. In sequential use with a prostaglandin analogue, up to 63 days of amenorrhea (see section 4.2). 2- Softening and dilatation of the cervix uteri prior to surgical termination of pregnancy during the first trimester. 3- Preparation for the action of prostaglandin analogues in the termination of pregnancy for medical reasons (beyond the first trimester). 4- Labour induction in fetal death in utero. In patients where prostaglandin or oxytocin cannot be used. 4.2 Dose and Method of Administration Dose 1- Medical termination of developing intra-uterine pregnancy The method of administration will be as follows: • Up to 49 days of amenorrhea: 1 Mifepristone is taken as a single 600 mg (i.e. 3 tablets of 200 mg each) oral dose, followed 36 to 48 hours later, by the administration of the prostaglandin analogue: misoprostol 400 µg orally or per vaginum. • Between 50-63 days of amenorrhea Mifepristone is taken as a single 600 mg (i.e. 3 tablets of 200 mg each) oral dose, followed 36 to 48 hours later, by the administration of misoprostol. -
Transplantation and Immunology 1
Transplantation and Immunology 1 Transplantation and Immunology บรรยายโดย อ.นพ.สมชัย ลิ้มศรีจ าเริญ เรียบเรียง นพ.กิตติ์รวี จิรธานีเรืองกิจ อาจารย์ที่ปรึกษา อ.นพ.ราวิน วงษ์สถาปนาเลิศ Outline 1. Immunology 2. Immunosuppression: drug use in transplantation 3. Clinical transplant: liver pancreas intestine and kidney transplant ในอเมริกา ท า Transplant เยอะมาก และ resident ศัลยกรรมทุกคนต้องผ่าน rotation transplant ดังนั้น ในอนาคต บ้านเรา จะท ากันมากขึ้น และอาจจะบรรจุ เป็น requirement ให้ resident ต้องผ่าน • Immunology ประวัติศาสตร์ เริ่มจาก Jensen reported in 1902 - มีการทดลอง ศึกษาเกี่ยวกับ tumor และ immunology ของ tumor พบว่า สามารถน าเอา tumor จากหนูไป transplant ให้ตัวอื่นได้ ( ท าใน 19 successive generation) - พบว่าหนูบางส่วนจะ reject tumor ไม่ให้เติบโต (50% of mice) - โดยจะ reject ทุกครั้ง ที่น า tumor มา transplant ใหม่ (มี resistant to subsequent challenge) และ หากน า เอา normal tissue ใส่ไปก่อน และเอา tumor มา transplant ก็จะ reject ได้เร็วขึ้น - เกิด Theory อธิบายเหตุการณ์นี้ คือ Athrepsia theory (เกี่ยวกับ nutrition) เพราะ เวลาใส่ tumor เข้าไปแรกๆ จะยังเจริญได้ช่วงหนึ่งจากนั้น จึงตายไป เชื่อว่าเกิดจากการขาด สารอาหาร หลังจาก tumor ใช้สารอาหารหมด มันก็จะตายไป นับเป็นจุดเริ่มต้นที่ใช้ tumor ในการศึกษาหลักการเรื่อง Transplantation Medawar reported in 1943 (Nobel prize) - เมื่อมี rejection เกิดขึ้น หากเราใช้ graft ครั้งที่ 2 จาก donor เดิม จะเกิดการ reject เร็วขึ้น ซึ่งคิดว่าเกิดจาก Actively acquired immune reaction จากนั้นมีการศึกษาอีกหลายอย่างเพื่อศึกษา transplant immunology Owen reported in 1947 - ถ้าน าสัตว์เช่น ลูกวัว ที่เป็น dizygotic -
Effects of a Novel Estrogen-Free, Progesterone Receptor Modulator
Edinburgh Research Explorer Effects of a novel estrogen-free, progesterone receptor modulator contraceptive vaginal ring on inhibition of ovulation, bleeding patterns and endometrium in normal women Citation for published version: Brache, V, Sitruk-Ware, R, Williams, A, Blithe, D, Croxatto, H, Kumar, N, Kumar, S, Tsong, Y-Y, Sivin, I, Nath, A, Sussman, H, Cochon, L, Miranda, MJ, Reyes, V, Faundes, A & Mishell, D 2012, 'Effects of a novel estrogen-free, progesterone receptor modulator contraceptive vaginal ring on inhibition of ovulation, bleeding patterns and endometrium in normal women', Contraception, vol. 85, no. 5, pp. 480-8. https://doi.org/10.1016/j.contraception.2011.10.003 Digital Object Identifier (DOI): 10.1016/j.contraception.2011.10.003 Link: Link to publication record in Edinburgh Research Explorer Document Version: Peer reviewed version Published In: Contraception Publisher Rights Statement: NIH Public access author manuscript General rights Copyright for the publications made accessible via the Edinburgh Research Explorer is retained by the author(s) and / or other copyright owners and it is a condition of accessing these publications that users recognise and abide by the legal requirements associated with these rights. Take down policy The University of Edinburgh has made every reasonable effort to ensure that Edinburgh Research Explorer content complies with UK legislation. If you believe that the public display of this file breaches copyright please contact [email protected] providing details, and we will remove access to the work immediately and investigate your claim. Download date: 26. Sep. 2021 NIH Public Access Author Manuscript Contraception. Author manuscript; available in PMC 2013 May 01. -
Areas of Future Research in Fibroid Therapy
9/18/18 Cumulative Incidence of Fibroids over Reproductive Lifespan RFTS Areas of Future Research Blacks Blacks UFS Whites in Fibroid Therapy CARDIA Age 33-46 William H. Catherino, MD, PhD Whites Professor and Chair, Research Division Seveso Italy Uniformed Services University Blacks Whites Associate Program Director Sweden/Whites (Age 33-40) Division of REI, PRAE, NICHD, NIH The views expressed in this article are those of the author(s) and do not reflect the official policy or position of the Department of the Army, Department of Defense, or the US Government. Laughlin Seminars Reprod Med 2010;28: 214 Fibroids Increase Miscarriage Rate Obstetric Complications of Fibroids Complication Fibroid No Fibroid OR Abnormal labor 49.6% 22.6% 2.2 Cesarean Section 46.2% 23.5% 2.0 Preterm delivery 13.8% 10.7% 1.5 BreecH position 9.3% 4.0% 1.6 pp Hemorrhage 8.3% 2.9% 2.2 PROM 4.2% 2.5% 1.5 Placenta previa 1.7% 0.7% 2.0 Abruption 1.4% 0.7% 2.3 Guben Reprod Biol Odds of miscarriage decreased with no myoma comparedEndocrinol to myoma 2013;11:102 Biderman-Madar ArcH Gynecol Obstet 2005;272:218 Ciavattini J Matern Fetal Neonatal Med 2015;28:484-8 Not Impacting the Cavity Coronado Obstet Gynecol 2000;95:764 Kramer Am J Obstet Gynecol 2013;209:449.e1-7 Navid Ayub Med Coll Abbottabad 2012;24:90 Sheiner J Reprod Med 2004;49:182 OR = 0.737 [0.647, 0.840] Stout Obstet Gynecol 2010;116:1056 Qidwai Obstet Gynecol 2006;107:376 1 9/18/18 Best Studied Therapies Hysterectomy Option over Time Surgical Radiologic Medical >100 years of study Hysterectomy Open myomectomy GnRH agonists 25-34 years of study Endometrial Ablation GnRH agonists 20-24 years of study Laparoscopic myomectomy Uterine artery embolization Retinoic acid 10-19 years of study Uterine artery obstruction SPRMs: Mifepristone, ulipristal Robotic myomectomy GnRH antagonists 5-9 years of study Cryomyolysis MRI-guided high frequency ultrasound SPRMs: Asoprisnil, Telapristone, Laparoscopic ablation Vilaprisan SERMs: Tamoxifen, Raloxifene, Letrozole, Genistein Pitter MC, Simmonds C, Seshadri-Kreaden U, Hubert HB. -
Stems for Nonproprietary Drug Names
USAN STEM LIST STEM DEFINITION EXAMPLES -abine (see -arabine, -citabine) -ac anti-inflammatory agents (acetic acid derivatives) bromfenac dexpemedolac -acetam (see -racetam) -adol or analgesics (mixed opiate receptor agonists/ tazadolene -adol- antagonists) spiradolene levonantradol -adox antibacterials (quinoline dioxide derivatives) carbadox -afenone antiarrhythmics (propafenone derivatives) alprafenone diprafenonex -afil PDE5 inhibitors tadalafil -aj- antiarrhythmics (ajmaline derivatives) lorajmine -aldrate antacid aluminum salts magaldrate -algron alpha1 - and alpha2 - adrenoreceptor agonists dabuzalgron -alol combined alpha and beta blockers labetalol medroxalol -amidis antimyloidotics tafamidis -amivir (see -vir) -ampa ionotropic non-NMDA glutamate receptors (AMPA and/or KA receptors) subgroup: -ampanel antagonists becampanel -ampator modulators forampator -anib angiogenesis inhibitors pegaptanib cediranib 1 subgroup: -siranib siRNA bevasiranib -andr- androgens nandrolone -anserin serotonin 5-HT2 receptor antagonists altanserin tropanserin adatanserin -antel anthelmintics (undefined group) carbantel subgroup: -quantel 2-deoxoparaherquamide A derivatives derquantel -antrone antineoplastics; anthraquinone derivatives pixantrone -apsel P-selectin antagonists torapsel -arabine antineoplastics (arabinofuranosyl derivatives) fazarabine fludarabine aril-, -aril, -aril- antiviral (arildone derivatives) pleconaril arildone fosarilate -arit antirheumatics (lobenzarit type) lobenzarit clobuzarit -arol anticoagulants (dicumarol type) dicumarol -
(12) United States Patent (10) Patent No.: US 7,723,320 B2 Bunschoten Et Al
US007723320B2 (12) United States Patent (10) Patent No.: US 7,723,320 B2 Bunschoten et al. (45) Date of Patent: May 25, 2010 (54) USE OF ESTROGEN COMPOUNDS TO DE 23,36434. A 4, 1975 INCREASE LIBDO IN WOMEN WO WO96 O3929 A 2, 1996 (75) Inventors: Evert Johannes Bunschoten, Heesch OTHER PUBLICATIONS (NL); Herman Jan Tijmen Coelingh Bennink, Driebergen (NL); Christian Holinka CF et al: “Comparison of Effects of Estetrol and Taxoxifen Franz Holinka, New York, NY (US) with Those of Estriol and Estradiol on the Immature Rat Uterus'; Biology of Reproduction; 1980; pp. 913-926; vol. 22, No. 4. (73) Assignee: Pantarhei Bioscience B.V., Al Zeist Holinka CF et al; "In-Vivo Effects of Estetrol on the Immature Rat (NL) Uterus'; Biology of Reproduction; 1979: pp. 242-246; vol. 20, No. 2. Albertazzi Paola et al.; "The Effect of Tibolone Versus Continuous Combined Norethisterone Acetate and Oestradiol on Memory, (*) Notice: Subject to any disclaimer, the term of this Libido and Mood of Postmenopausal Women: A pilot study': Data patent is extended or adjusted under 35 base Biosis "Online!; Oct. 31, 2000: pp. 223-229; vol. 36, No. 3; U.S.C. 154(b) by 1072 days. Biosciences Information Service.: Philadelphia, PA, US. Visser et al., “In vitro effects of estetrol on receptor binding, drug (21) Appl. No.: 10/478,264 targets and human liver cell metabolism.” Climacteric (2008) 11(1) Appx. II: 1-5. (22) PCT Filed: May 17, 2002 Visser et al., “First human exposure to exogenous single-dose oral estetrol in early postmenopausal women.” Climacteric (2008) 11(1): (86). -
Durham E-Theses
Durham E-Theses Elemental Fluorine for the Greener Synthesis of Life-Science Building Blocks HARSANYI, ANTAL How to cite: HARSANYI, ANTAL (2016) Elemental Fluorine for the Greener Synthesis of Life-Science Building Blocks, Durham theses, Durham University. Available at Durham E-Theses Online: http://etheses.dur.ac.uk/11705/ Use policy The full-text may be used and/or reproduced, and given to third parties in any format or medium, without prior permission or charge, for personal research or study, educational, or not-for-prot purposes provided that: • a full bibliographic reference is made to the original source • a link is made to the metadata record in Durham E-Theses • the full-text is not changed in any way The full-text must not be sold in any format or medium without the formal permission of the copyright holders. Please consult the full Durham E-Theses policy for further details. Academic Support Oce, Durham University, University Oce, Old Elvet, Durham DH1 3HP e-mail: [email protected] Tel: +44 0191 334 6107 http://etheses.dur.ac.uk 2 Durham University A thesis entitled Elemental Fluorine for the Greener Synthesis of Life-Science Building Blocks by Antal Harsanyi (College of St. Hild and St. Bede) A candidate for the degree of Doctor of Philosophy Department of Chemistry, Durham University 2016 Antal Harsanyi: Elemental fluorine for the greener synthesis of life-science building blocks Abstract Fluorinated organic compounds are increasingly important in many areas of our modern lives, especially in pharmaceutical and agrochemical applications where the incorporation of this element can have a major influence on biochemical properties. -
22474 Ella Clinical PREA
Clinical Review Ronald J. Orleans, M.D. NDA 22-474 Ella (ulipristal acetate 30 mg) CLINICAL REVIEW Application Type NDA Application Number(s) 22-474 Priority or Standard Standard Submit Date(s) October 14, 2009 Received Date(s) October 15, 2009 PDUFA Goal Date August 15, 2010 Division / Office Reproductive and Urologic Drugs/ODE III Reviewer Name(s) Ronald J. Orleans, M.D. Review Completion Date July 27, 2010 Established Name Ulipristal acetate (Proposed) Trade Name Ella Therapeutic Class Progesterone agonist/antagonist Applicant HRA Pharma Formulation(s) 30 mg tablet Dosing Regimen One tablet by mouth Indication(s) Emergency contraception Intended Population(s) Women of reproductive age at risk for pregnancy August 5, 2010 (Final) 1 Clinical Review Ronald J. Orleans, M.D. NDA 22-474 Ella (ulipristal acetate 30 mg) Table of Contents 1 RECOMMENDATIONS/RISK BENEFIT ASSESSMENT......................................... 6 1.1 Recommendation on Regulatory Action ............................................................. 6 1.2 Risk Benefit Assessment.................................................................................... 6 1.3 Recommendations for Postmarket Risk Evaluation and Mitigation Strategies ... 7 1.4 Recommendations for Postmarket Requirements and Commitments ................ 7 2 INTRODUCTION AND REGULATORY BACKGROUND ........................................ 7 2.1 Product Information ............................................................................................ 7 Tables of Currently Available Treatments for