Latanoprost a Promising New Glaucoma Drug
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CENTER FOR DRUG EVALUATION AND RESEARCH APPLICATION NUMBER: 202514Orig1s000 CLINICAL PHARMACOLOGY AND BIOPHARMACEUTICS REVIEW(S) OFFICE OF CLINICAL PHARMACOLOGY REVIEW NDA: 202-514 Submission Date(s): January 7, 2011 Proposed Brand Name TBD Generic Name Tafluprost Primary Reviewer Yongheng Zhang, Ph.D. Team Leader Philip M. Colangelo, Pharm.D., Ph.D. OCP Division DCP4 OND Division DTOP Applicant MERCK & CO., Inc. Relevant IND(s) 062690 Submission Type; Code 1S(NME) Formulation; Strength(s) Tafluprost 0.0015% Ophthalmic Solution Indication For the reduction of elevated intraocular pressure in open-angle glaucoma or ocular hypertension Dosage and Administration One drop of Tafluprost 0.0015% ophthalmic solution in the conjunctival sac of the affected eye(s) once daily in the evening TABLE OF CONTENTS 1. EXECUTIVE SUMMARY .................................................................................................................. 2 1.1. RECOMMENDATION ....................................................................................................................... 3 1.2. PHASE IV COMMITMENTS............................................................................................................. 3 1.3. SUMMARY OF IMPORTANT CLINICAL PHARMACOLOGY AND BIOPHARMACEUTICS FINDINGS.. 3 2. QUESTION BASED REVIEW ...........................................................................................................4 2.1. GENERAL ATTRIBUTES OF THE DRUG ......................................................................................... -
Differential Activity and Clinical Utility of Latanoprost in Glaucoma and Ocular Hypertension
Clinical Ophthalmology Dovepress open access to scientific and medical research Open Access Full Text Article REVIEW Differential activity and clinical utility of latanoprost in glaucoma and ocular hypertension Fernanda Pacella Background: The purpose of this study was to demonstrate the hypotensive efficacy and tolerability Paolo Turchetti of latanoprost when used as monotherapy and as polytherapy associated with antiglaucomatous Valentina Santamaria medication proven to be ineffective in keeping intraocular pressure under control. David Impallara Methods: Three hundred and thirty-seven patients (672 eyes) affected by primary open-angle Gianpaolo Smaldone glaucoma and intraocular hypertension were recruited over a period of 10 years from the Chiara Brillante Glaucoma Centre, Department of Ophthalmological Sciences, University of Rome “Sapienza”, and treated, subject to informed consent, with latanoprost 0.005% alone or in combination Aloisa Librando with other ocular hypotensive drugs. The patients were followed during this period at regular Angela Damiano intervals, with determination of visual field, fundus oculi, visual acuity, and eventual onset of Jose Pecori-Giraldi local and systemic side effects. Elena Pacella Results: Latanoprost used as monotherapy and as polytherapy renders possible optimal and Department of Sense Organs, durable control of intraocular pressure in the form of one antiglaucomatous drug because it can University of Rome “Sapienza”, substitute for one or more drugs and obtain the same hypotensive effect. Roma, -
Effect of Prostanoids on Human Platelet Function: an Overview
International Journal of Molecular Sciences Review Effect of Prostanoids on Human Platelet Function: An Overview Steffen Braune, Jan-Heiner Küpper and Friedrich Jung * Institute of Biotechnology, Molecular Cell Biology, Brandenburg University of Technology, 01968 Senftenberg, Germany; steff[email protected] (S.B.); [email protected] (J.-H.K.) * Correspondence: [email protected] Received: 23 October 2020; Accepted: 23 November 2020; Published: 27 November 2020 Abstract: Prostanoids are bioactive lipid mediators and take part in many physiological and pathophysiological processes in practically every organ, tissue and cell, including the vascular, renal, gastrointestinal and reproductive systems. In this review, we focus on their influence on platelets, which are key elements in thrombosis and hemostasis. The function of platelets is influenced by mediators in the blood and the vascular wall. Activated platelets aggregate and release bioactive substances, thereby activating further neighbored platelets, which finally can lead to the formation of thrombi. Prostanoids regulate the function of blood platelets by both activating or inhibiting and so are involved in hemostasis. Each prostanoid has a unique activity profile and, thus, a specific profile of action. This article reviews the effects of the following prostanoids: prostaglandin-D2 (PGD2), prostaglandin-E1, -E2 and E3 (PGE1, PGE2, PGE3), prostaglandin F2α (PGF2α), prostacyclin (PGI2) and thromboxane-A2 (TXA2) on platelet activation and aggregation via their respective receptors. Keywords: prostacyclin; thromboxane; prostaglandin; platelets 1. Introduction Hemostasis is a complex process that requires the interplay of multiple physiological pathways. Cellular and molecular mechanisms interact to stop bleedings of injured blood vessels or to seal denuded sub-endothelium with localized clot formation (Figure1). -
Effect of Latanoprost Or 8-Iso Prostaglandin E2 Alone and in Combination on Intraocular Pressure in Glaucomatous Monkey Eyes
LABORATORY SCIENCES Effect of Latanoprost or 8-iso Prostaglandin E2 Alone and in Combination on Intraocular Pressure in Glaucomatous Monkey Eyes Rong-Fang Wang, MD; Steven M. Podos, MD; Janet B. Serle, MD; Thomas W. Mittag, PhD; F. Ventosa, MD; Bernard Becker, MD Objective: To evaluate the possible additivity of the ef- duction of IOP of 4.0 ± 0.6 mm Hg was produced when fects of latanoprost and 8-iso prostaglandin E2 (8-iso PGE2) 8-iso PGE2 was added to latanoprost and of 3.0 ± 0.7 on intraocular pressure (IOP) in monkey eyes with laser- mm Hg was produced when latanoprost was added to 8-iso induced glaucoma. PGE2 on day 13 before the morning dosing. Combina- tion therapy with both agents caused maximum IOP re- Methods: The IOP was measured hourly for 6 hours be- ductions from baseline of 11.3 ± 3.0 mm Hg (33%) (P,.05) ginning at 9:30 AM on day 1 (baseline day), days 6 and 7 (latanoprost with 8-iso PGE2 added) and of 9.8 ± 1.3 , (single-agent therapy), and days 13 and 14 (combination mm Hg (31%) (P .01) (8-iso PGE2 with latanoprost added) therapy with both agents). Following 1 day of baseline mea- on day 14. surement, 4 monkeys with unilateral glaucoma received monotherapy twice daily with either 1 drop of 0.005% la- Conclusion: Latanoprost and 8-iso PGE2 have an addi- tanoprost, or 0.1% 8-iso PGE2, 25 µL, at 9:30 AM and 3:30 tive effect on IOP in glaucomatous monkey eyes. -
Efficacy and Safety of the Fixed Combinations of Tafluprost/Timolol
www.nature.com/scientificreports OPEN Efcacy and safety of the fxed combinations of tafuprost/timolol and latanoprost/carteolol Received: 4 February 2019 Masahiro Fuwa, Atsushi Shimazaki, Masafumi Mieda, Naoko Yamashita, Takahiro Akaishi, Accepted: 7 May 2019 Takazumi Taniguchi & Masatomo Kato Published: xx xx xxxx In this study, we made a comparative efcacy and safety assessment of two diferent fxed combinations of drugs, viz., tafuprost/timolol (TAF/TIM) and latanoprost/carteolol (LAT/CAR), by determining their efects on intraocular pressure (IOP) in ocular normotensive monkeys and examining their toxic efects on ocular surface using human corneal epithelial cells. TAF/TIM was found to be more efective in lowering IOP for a longer duration compared to LAT/CAR. We found that the diference in the intensity of IOP-lowering efect was because of the diferences in the strength of timolol compared with that of carteolol as a beta-adrenergic antagonist and strength of tafuprost compared with that of latanoprost as a prostaglandin analogue. In addition, TAF/TIM showed much less cytotoxic efects compared to LAT/CAR on the human corneal epithelial cells. Our fndings showed that TAF/TIM is better than LAT/CAR with regard to the IOP-lowering efect in monkeys and toxicity on ocular surface. Glaucoma is a neurodegenerative disease of the eyes characterised by selective retinal ganglion cell loss, fol- lowed by progressive defects in visual feld, resulting in the principal cause of irreversible blindness worldwide1–4. Elevated intraocular pressure (IOP) is an important contributor for the progression of glaucoma, for which the current treatment primarily involves IOP reduction1,5–8. -
Prostaglandin Analogs for Glaucoma
Prostaglandin Analogs Company Brand Generic Name Name Akorn Inc. Zioptan™ Tafluprost ophthalmic solution 0.0015% (PF) Allergan Inc. Durysta™ Bimatoprost 10 mcg implant Allergan Inc. Lumigan® Bimatoprost 0.01%, 0.03% Bausch & Lomb, Vyzulta™ Latanoprostene bunod 0.024% Inc. Novartis Travatan® Z Travaprost 0.004% Pfizer Inc. Xalatan® Latanoprost 0.005% Sun Ophthalmics Xelpros™ Latanoprost ophthalmic emulsion 0.005% Prostaglandin analogs work by increasing the outflow of intraocular fluid from the eye. They have few systemic side effects but are associated with changes to the eye itself, including change in iris color and growth of eyelashes. Depending on the individual, one brand of this type of medication may be more effective and produce fewer side effects. Prostaglandin analogs are taken as eye drops (except Durysta™ which is an implant). They are effective at reducing intraocular pressure in people who have open-angle glaucoma. Latanoprost and some formulations of bimatoprost and travoprost are available in generic form. Tafluprost is a preservative-free prostaglandin analog. Side Effects Side effects can include eye color change, darkening of eyelid skin, eyelash growth, droopy eyelids, sunken eyes, stinging, eye redness, and itching. Follow these steps to make it easier to put in eye drops: Preparing the Drops ● Always wash your hands before handling your eye drops or touching your eyes. ● If you’re wearing contact lenses, take them out — unless your ophthalmologist has told you to leave them in. ● Shake the drops vigorously before using them. ● Remove the cap of the eye drop medication. ○ Do not touch the dropper tip. Putting in Eye Drops ● Tilt your head back slightly and look up. -
(12) United States Patent (10) Patent No.: US 9,155.716 B2 Chang Et Al
US009 155716B2 (12) United States Patent (10) Patent No.: US 9,155.716 B2 Chang et al. (45) Date of Patent: *Oct. 13, 2015 (54) ENHANCED BIMATOPROST OPHTHALMIC (56) References Cited SOLUTION U.S. PATENT DOCUMENTS (71) Applicant: ALLERGAN, INC. Irvine, CA (US) 4,055,602 A 10, 1977 Nelson 4,100,192 A 7, 1978 Morozowich (72) Inventors: Chin-Ming Chang, Tustin, CA (US); 4,122.282 A 10, 1978 Nelson James N. Chang, Newport Beach, CA 4,123,441 A 10, 1978 Johnson 4,128,577 A 12/1978 Nelson (US); Rhett M. Schiffman, Laguna 4,171,331 A 10, 1979 Biddlecom Beach, CA (US); R. Scott Jordan, 4,183,870 A 1/1980 Caton Trabuco Canyon, CA (US); Joan-En 4,303,796 A 12/1981 Nelson Chang-Lin, Tustin, CA (US) 4,382,953. A 5, 1983 Ishii 4,543,353 A 9, 1985 Faustini 4,599,353 A 7, 1986 Bito (73) Assignee: Allergan, Inc., Irvine, CA (US) 4,812.457 A 3/1989 Narumiya 4,994,274 A 2f1991 Chan (*) Notice: Subject to any disclaimer, the term of this 5,034413 A 7, 1991 Chan patent is extended or adjusted under 35 5,281.591 A 1/1994 Burke 5,352,708 A 10, 1994 Woodward U.S.C. 154(b) by 0 days. 5,474,979 A 12/1995 Ding 5,510,383 A 4/1996 Bishop This patent is Subject to a terminal dis 5,545,665 A 8, 1996 Burk claimer. 5,587,391 A 12, 1996 Burk 5,607,978 A 3, 1997 Woodward (21) Appl. -
Adverse Periocular Reactions to Five Types of Prostaglandin Analogs
Eye (2012) 26, 1465–1472 & 2012 Macmillan Publishers Limited All rights reserved 0950-222X/12 www.nature.com/eye 1 1 1 1 Adverse periocular K Inoue , M Shiokawa , R Higa , M Sugahara , CLINICAL STUDY T Soga1, M Wakakura1 and G Tomita2 reactions to five types of prostaglandin analogs Abstract Purpose We investigated the appearance explained to patients before PG frequency of eyelid pigmentation and administration. eyelash bristles after the use of five types of Eye (2012) 26, 1465–1472; doi:10.1038/eye.2012.195; prostaglandin (PG) analogs. published online 5 October 2012 Methods This study included 250 eyes from 250 patients diagnosed with primary open- Keywords: prostaglandin analogs; adverse angle glaucoma or ocular hypertension who reactions; eyelid pigmentation; eyelash bristles; were treated with either latanoprost, patient’s subjective evaluation; physician’s travoprost, tafluprost, bimatoprost, or subjective evaluation isopropyl unoprostone for 43 months in only one eye. Photographs of both eyes were obtained, and the images were assessed by Introduction three ophthalmologists who were masked to treatment type. The existence of eyelid Prostaglandin (PG) analogs are the primary pigmentation and eyelash bristles was treatment for glaucoma because of their judged, and images of the left and right eyes powerful intraocular pressure (IOP) decreasing were compared. Subjective symptoms effect, few systematic adverse reactions, and regarding the existence of eyelid convenience of once a day administration (other pigmentation and eyelash bristles were than isopropyl unoprostone (unoprostone)).1 Five types of PG analogs (latanoprost, investigated through a questionnaire. 1Inouye Eye Hospital, Tokyo, Results There was no significant difference travoprost, tafluprost, bimatoprost, and Japan between the five types of medications with unoprostone) are currently available in Japan. -
Tafluprost: the First Preservative-Free Prostaglandin to Treat Open-Angle Glaucoma and Ocular Hypertension
See discussions, stats, and author profiles for this publication at: https://www.researchgate.net/publication/232647942 Tafluprost: The First Preservative-Free Prostaglandin to Treat Open-Angle Glaucoma and Ocular Hypertension Article in Annals of Pharmacotherapy · October 2012 DOI: 10.1345/aph.1R229 · Source: PubMed CITATIONS READS 13 154 2 authors, including: Michael Neville Wingate University School of Pharmacy 11 PUBLICATIONS 87 CITATIONS SEE PROFILE All content following this page was uploaded by Michael Neville on 21 November 2014. The user has requested enhancement of the downloaded file. ARTICLES New Drug Approvals Tafluprost: The First Preservative-Free Prostaglandin to Treat Open-Angle Glaucoma and Ocular Hypertension Cory Swymer and Michael W Neville afluprost 0.0015% ophthalmic solu- tion (Zioptan) was approved by the T OBJECTIVE: To review the pharmacology, pharmacokinetics, clinical trial data, Food and Drug Administration on Febru- efficacy data, and adverse effect incidence of tafluprost. ary 10, 2012, for the treatment of elevated DATA SOURCES: A literature search was completed using PubMed, Web of intraocular pressure (IOP) in patients with Science, and Google Scholar. Tafluprost was the primary search term. Articles open-angle glaucoma, in addition to ocular published between January 2008 and April 2012 were included in this review. hypertension.1 Although it has been used Additional limits placed on the searches were “human” and “English.” Citations in in other countries since 2008, tafluprost is which tafluprost appeared in the title were 36, 29, and more than 300 in PubMed, Web of Science, and Google Scholar, respectively. the first preservative-free prostaglandin STUDY SELECTION AND DATA EXTRACTION: Three clinical trials were included in analogue commercially available in the this review. -
Additive Effect of Unoprostone and Latanoprost in Patients with Elevated Intraocular Pressure
75 CLINICAL SCIENCE Br J Ophthalmol: first published as 10.1136/bjo.86.1.75 on 1 January 2002. Downloaded from Additive effect of unoprostone and latanoprost in patients with elevated intraocular pressure Tin Aung, Paul T K Chew, Francis T S Oen, Yiong-Huak Chan, Lennard H Thean, Leonard Yip, Boon-Ang Lim, Steve K L Seah ............................................................................................................................. Br J Ophthalmol 2002;86:75–79 Aims: To assess the additive effect of unoprostone and latanoprost in patients with primary open angle glaucoma (POAG) or ocular hypertension (OHT) Methods: 32 patients with POAG or OHT were randomised to receive either latanoprost once daily or unoprostone twice daily for 4 weeks. After 4 weeks, all patients received both latanoprost and unoprostone for another 4 weeks. The IOP was measured at 9 am and 5 pm on the baseline, day 28, and day 56 visits, and at 9 am on day 14 and day 42 visits. The medications were given to the patients in an open label fashion. The observer was masked to the treatment given. The mean of the measure- ments was calculated. Safety parameters were also recorded. The additive effect of the medications was assessed by the reduction in intraocular pressure (IOP) when both medications were used, compared with when one medication was used. Results: 28 patients completed both treatment periods and had IOP data available for evaluation. See end of article for After 1 month of treatment, latanoprost significantly reduced IOP (mean by 6.1 (SEM 0.8) mm Hg authors’ affiliations (p<0.001) and unoprostone by 4.9 (1.0) mm Hg (p<0.001) from the baseline of 24.4 (0.6) mm Hg ...................... -
Effect of Non-Steroidal Anti-Inflammatory Ophthalmic Solution on Intraocular Pressure Reduction by Latanoprost K Kashiwagi, S Tsukahara
297 CLINICAL SCIENCE Br J Ophthalmol: first published as 10.1136/bjo.87.3.297 on 1 March 2003. Downloaded from Effect of non-steroidal anti-inflammatory ophthalmic solution on intraocular pressure reduction by latanoprost K Kashiwagi, S Tsukahara ............................................................................................................................. Br J Ophthalmol 2003;87:297–301 Aim: To investigate the effects of a non-steroidal anti-inflammatory drug (NSAID) ophthalmic solution on latanoprost induced intraocular pressure (IOP) reduction using normal volunteers. Methods: This study was conducted as a prospective and observer masked clinical trial. 13 normal volunteers were enrolled. After measurement of basal IOP and ophthalmic examination, latanoprost ophthalmic solution was initially administered to both eyes once daily. Four weeks later, an NSAID ophthalmic solution, sodium 2-amino-3-(4-bromobenzoyl) phenylacetate sesquihydrate (refer to bromfenac sodium hydrate), was co-administered to one randomly selected eye (NSAID group) twice daily for 2 weeks. The other eye was employed as a control (non-NSAID group). After withdrawal of the NSAID ophthalmic solution, latanoprost ophthalmic solution was continuously administered for another 2 weeks and was then withdrawn. After a 4 week washout, only bromfenac sodium hydrate See end of article for authors’ affiliations ophthalmic solution was administered to the eyes of the NSAID group for 2 weeks. During the study ....................... period, ophthalmic examination, including IOP measurement was performed in an observer masked fashion. Correspondence to: Results: Kenji Kashiwagi, MD, Before initiation of bromfenac sodium hydrate, baseline IOPs of the non-NSAID group and the Department of NSAID group were 15.73 (SD 1.97) mm Hg and 15.86 (2.06) mm Hg, respectively (p=0.88). -
Update on the Mechanism of Action of Topical Prostaglandins for Intraocular Pressure Reduction Carol B
SURVEY OF OPHTHALMOLOGY VOLUME 53 SUPPLEMENT 1 NOVEMBER 2008 Update on the Mechanism of Action of Topical Prostaglandins for Intraocular Pressure Reduction Carol B. Toris, PhD,1 B’Ann T. Gabelt, MS,2 and Paul L. Kaufman, MD2 1Department of Ophthalmology and Visual Sciences, University of Nebraska Medical Center, Omaha, Nebraska, USA; and 2Department of Ophthalmology and Visual Sciences, University of Wisconsin, Madison, Wisconsin, USA Abstract. A decade has passed since the first topical prostaglandin analog was prescribed to reduce intraocular pressure (IOP) for the treatment of glaucoma. Now four prostaglandin analogs are available for clinical use around the world and more are in development. The three most efficacious of these drugs are latanoprost, travoprost, and bimatoprost, and their effects on IOP and aqueous humor dynamics are similar. A consistent finding is a substantial increase in uveoscleral outflow and a less consistent finding is an increase in trabecular outflow facility. Aqueous flow appears to be slightly stimulated as well. Prostaglandin receptors and their associated mRNAs have been located in the trabecular meshwork, ciliary muscle, and sclera, providing evidence that endogenous prostaglandins have a functional role in aqueous humor drainage. Earlier evidence found that topical PG analogs release endogenous prostaglandins. One well-studied mechanism for the enhancement of outflow by prostaglandins is the regulation of matrix metalloproteinases and remodeling of extracellular matrix. Other proposed mechanisms include widening of the connective tissue-filled spaces and changes in the shape of cells. All of these mechanisms alter the permeability of tissues of the outflow pathways leading to changes in outflow resistance and/or outflow rates.