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(12) United States Patent (10) Patent No.: US 8.420,592 B2 Lehoux Et Al USOO842O592B2 (12) United States Patent (10) Patent No.: US 8.420,592 B2 Lehoux et al. (45) Date of Patent: Apr. 16, 2013 (54) METHODS OF TREATMENT USING SINGLE FOREIGN PATENT DOCUMENTS DOSES OF ORITAVANCIN WO 99.10006 3, 1999 WO OOf 66144 11, 2000 (75) Inventors: Dario Lehoux, Terrebonne (CA); WO 2008/097364 8, 2008 Thomas R. Parr, Indianapolis, IN (US); Gregory Moeck, St. Laurent (CA); OTHER PUBLICATIONS Pierre Etienne, Montreal (CA) Boylan et al. Pharmacodynamics of Oritavancin (LY333328) in a Neutropenic-Mouse Thigh Model of Staphylococcus aureus Infec (73) Assignee: The Medicines Company, Parsippany, tion, Antimicrobial Agents and Chemotherapy, May 2003, p. 1700 NJ (US) 17O6.* Fetterly et al. Pharmacokinetics of Oritavancin in Plasma and Skin (*) Notice: Subject to any disclaimer, the term of this Blister Fluid following Administration of a 200-Milligram Dose for patent is extended or adjusted under 35 3 Days or a Single 800-Milligram Dose, Antimicrobial Agents and U.S.C. 154(b) by 0 days. Chemotherapy, Jan. 2005, p. 148-152.* Bhavnani, S.M. et al., Pharmacokinetics, safety, and tolerability of ascending single intravenous doses of oritavancin administered to (21) Appl. No.: 13/060,811 healthy human Subjects. Diagnostic Microbiology and Infectious Disease 50 (2004), 95-102. (22) PCT Filed: Aug. 29, 2009 Lee, S.Y. et al., Antimicrobial management of complicated skin and skin structure infections in the era of emerging resistance, Surgical (86). PCT No.: PCT/US2O09/055466 Infections, 2005, vol. 6, No. 3, pp. 283-295. Examination Report dated Oct. 15, 2012, from the New Zealand S371 (c)(1), Intellectual Property Office in corresponding New Zealand Applica (2), (4) Date: Apr. 12, 2011 tion No. 59.1525. Printout from ClinicalTrials.gov website, entitled “A Study for (87) PCT Pub. No.: WO2010/025438 Patients with Complicated Skin and Skin Structure Infections PCT Pub. Date: Mar. 4, 2010 (SIMPLIFI), ID No. NCT00514527, indicated as first received by NIH on Aug. 8, 2007. (65) Prior Publication Data Mercier, R.C. et al., Oritavancin: a new avenue for resistant Gram positive bacteria, Expert Rev. Anti. Infect. Ther. 2005, vol. 3, No. 3, US 2011 FO2O1546A1 Aug. 18, 2011 pp. 325-332. Supplementary European Search Report dated Sep. 19, 2012, from the European Patent Office in corresponding European Application Related U.S. Application Data No. 09810708.9. (60) Provisional application No. 61/093.314, filed on Aug. 30, 2008, provisional application No. 61/093,497, * cited by examiner filed on Sep. 2, 2008. Primary Examiner — Cecilia JTsang (51) Int. Cl. Assistant Examiner — Sergio Coffa AOIN37/18 (2006.01) (74) Attorney, Agent, or Firm — Roylance, Abrams, Berdo A6 IK38/04 (2006.01) & Goodman LLP (52) U.S. Cl. USPC ................ 514/1.1 : 514/2.6; 514/2.7: 514/3.1 (57) ABSTRACT (58) Field of Classification Search ........................ None Glycopeptide antibiotics, such as oritavancin, demonstrate See application file for complete search history. significant activity against a wide range of bacteria. Methods for the treatment, prophylaxis and prevention of bacterial (56) References Cited infection and disease in animals, including humans, using a single dose of oritavancin over the course of therapy, are U.S. PATENT DOCUMENTS described. 2003/0176327 A1* 9, 2003 Cassell et al. ..................... 5148 2004/O147441 A1 7/2004 Leach 4 Claims, 5 Drawing Sheets U.S. Patent Apr. 16, 2013 Sheet 1 of 5 US 8.420,592 B2 Figure 1 Daily Dose Single Dose $ infrequent Dose Oritavancin lic giml Figure 2 O.015 Oritavancin MC giml U.S. Patent Apr. 16, 2013 Sheet 2 of 5 US 8.420,592 B2 Figure 3 & NRS123 8 13709 s S O s O - -0.5 0.0 0.5 1.0 15 2.0 Log Dose of OR (mg/kg) Figure 4 -O- Utreated x OR 100mg ad rx OR 200 mg ad -- OR 400mg ad x OR 1200mg single Starting inoculum rise Limit of detection O 12 24 36 48 60 72 Time post-treatment initiation (h) U.S. Patent Apr. 16, 2013 Sheet 3 of 5 US 8.420,592 B2 Figure 5 HEQ ORI dose (mg) Daily Single Daily Single OO 200 400 200 OO 200 400 12OO () to S 2stasis SE 2 g C; Figure 6 2O - S. \ OO - 8O A.O. 2O - SO CO 20 3CO 40C 5OO 6OO 7OO 8CO OOO 20 Oritavancin Dose (mg) U.S. Patent Apr. 16, 2013 Sheet 4 of 5 US 8.420,592 B2 Figure 7 O.25 O.5. O75 1 25 15 .75 2 2.25 2.5 3 3.5 infusion. Duration (hr) All doses are included (subjects may have had more than 1 dose) Figure 8 2Ooo 1800 1600 1400 1200 1ooo 800 600 400 w 200 7 8 S.S.I.S.S. N.N. S.S.S................... 4.OO 500 6OO 700 80O 900 OOO 2CO infusion Rate (mg/hr) A doses are included (subjects may have had ?nore than 1 dose) U.S. Patent Apr. 16, 2013 Sheet 5 of 5 US 8.420,592 B2 Figure 9 OOO - OO - O 2OO 4OO 6OO 8OO OOO 12OO Time Since Start of Last infusion (hr) Oritavancin Dose (d < = 100 mg - 3 - 10t-2OO mg o C C 201 - 400 mg A A A 40 - 600 mg & & & > 600 mg US 8,420,592 B2 1. 2 METHODS OF TREATMENT USING SINGLE chlorophenyl)benzyl)A82846B and LY333328, demon DOSES OF ORTAVANCIN strates clinically significant therapeutic activity against bacterial infections when administered to a subject in one BACKGROUND OF THE INVENTION dose over a course of therapy. The present invention is directed to methods of treatment, prophylaxis and/or preven Oritavancin diphosphate (oritavancin) is a semi-synthetic tion of bacterial infections in a subject, such as a human, using lipoglycopeptide derivative of a naturally occurring glyco one dose of oritavancin (or its pharmaceutically acceptable peptide. Its structure confers potent antibacterial activity salts, hydrates, or solvates thereof, or a mixture thereof). against gram-positive bacteria, including Vancomycin-resis In a first embodiment, the present invention is directed to tant enterococci (VRE), methicillin- and Vancomycin-resis- 10 methods of treating bacterial infections in a subject by admin tant staphylococci, and penicillin-resistant streptococci. The istering one dose of oritavancin, or a pharmaceutically rapidity of its bactericidal activity against exponentially acceptable salt thereof, preferably formulated as a pharma growing S. aureus (23-log reduction within 15 minutes to 2 ceutical composition, over a course of therapy to a subject. hours against MSSA, MRSA, and VRSA) is one of the fea In a first aspect of this embodiment, the present invention is tures that distinguishes it from the prototypic glycopeptide is directed to a method of treating a bacterial infection in a Vancomycin (McKay et al., J Antimicrob Chemother. 63(6): Subject, comprising administering one dose of a therapeuti 1191-9 (2009), Epub 2009 Apr. 15). cally effective amount of a pharmaceutical composition com Oritavancin inhibits the synthesis of peptidoglycan, the prising oritavancin, or a pharmaceutically acceptable salt major structural component of the bacterial cell wall by a thereof, and a pharmaceutically acceptable carrier or diluent, mechanism that is shared with glycopeptides, such as Vanco over a course of therapy to a subject having a bacterial infec mycin (Allen et al., Antimicrob Agents Chemother 41(1):66 tion, thereby treating a bacterial infection in a subject. In a 71 (1997); Cegelski et al., J Mol Biol 357: 1253-1262 (2006); preferred aspect, the pharmaceutical composition comprises Arhin et al., Poster C1-1471: Mechanisms of action of orita at least about 400 mg oritavancin, or a pharmaceutically vancin in Staphylococcus aureus poster. 47th Intersci Conf acceptable salt thereof. In a further preferred aspect, the phar Antimicro Agents Chemo, Sep. 17-20, 2007: Chicago, Ill.). maceutical composition comprises between about 400 mg to Oritavancin, like Vancomycin, binds to the Acyl-D-Alanyl- 25 about 1800 mg oritavancin, or a pharmaceutically acceptable D-Alanine terminus of the peptidoglycan precursor, lipid salt thereof. In specific aspects, the pharmaceutical composi bound N-acetyl-glucosamine-N-acetyl-muramic acid-pen tion comprises about 800 mg,900 mg, 1000 mg, 1100 mg, or tapeptide (Reynolds, EurJ Clin Microbiol Infect Dis 8(11): 1200 mg oritavancin, or a pharmaceutically acceptable salt 943-950 (1989); Nicas and Allen, Resistance and mechanism thereof. of action. In: Nagarajan R, editor. Glycopeptide antibiotics. 30 In a variation of this first aspect, a single subsequent dose of New York: Marcel Dekker 195-215 (1994); Allen et al., Anti oritavancin may be administered to the subject. Thus, the microb Agents Chemother 40(10): 2356–2362 (1996); Allen method of the first aspect may further comprise administering and Nicas, FEMS Microbiology Reviews 26:51 1-532 (2003); a second dose of a therapeutically effective amount of a Kim et al., Biochemistry 45:5235-5250 (2006)). However, pharmaceutical composition comprising oritavancin, or a oritavancin inhibits cell wall biosynthesis even when the sub- is pharmaceutically acceptable salt thereof, and a pharmaceuti Strate is the altered peptidoglycan precursor that is present in cally acceptable carrier or diluent, within the course of VRE and Vancomycin-resistant S. aureus (VRSA). Thus, the therapy. Preferably, the second dose comprises an amount of spectrum of oritavancin antibacterial activity extends beyond oritavancin less than or equal to that of the first dose. Also that of Vancomycin to include glycopeptide-resistant entero preferably, the second dose is administered about 4 days or cocci and staphylococci (Ward et al., Expert Opin Investig more after the first dose. Drugs 15:417-429 (2006); Scheinfeld, J Drugs Dermatol 40 In a second aspect of this embodiment, the present inven 6:97-103 (2007)). Oritavancin may inhibit resistant bacteria tion is directed to
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