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United States Patent (19) 11 Patent Number: 6,096,728 Collins Et Al

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United States Patent (19) 11 Patent Number: 6,096,728 Collins Et Al US006096728A United States Patent (19) 11 Patent Number: 6,096,728 Collins et al. (45) Date of Patent: Aug. 1, 2000 54) COMPOSITION AND METHOD FOR FOREIGN PATENT DOCUMENTS TREATING INFLAMMATORY DISEASES 9173636 10/1991 Australia. 75 Inventors: David S. Collins, Lafayette; Michael P. WO 92/11359 7/1992 WIPO. Bevilacqua, Boulder, both of Colo. WO 93/07863 4/1993 WIPO. OTHER PUBLICATIONS 73 Assignee: Amgen Inc., Thousand Oaks, Calif. Thomas, Robert C.; Interleukin-1 receptor antagonist(IL-1 ra) as a probe and as a atreatment for IL-1 21 Appl. No.: 08/798,414 mediated disease; Int. J. Immunopharmac., Vol. 14. No. 3, 22 Filed: Feb. 7, 1997 pp. 475-480, 1992. Related U.S. Application Data Primary Examiner. Theodore J. Criares 60 Provisional application No. 60/011,419, Feb. 9, 1996, and Attorney, Agent, or Firm Thomas D. Zindrick; Steven M. provisional application No. 60/032,789, Dec. 6, 1996. Odre; Ron K. Levy 51 Int. Cl." .............................. A61K 31/70; CO7K 1/00 57 ABSTRACT - - - - - - 514/62; 530/351 A pharmaceutical composition comprising (a) an effective Field of Search ................................ 514/62; 530/351 amount of controlled release polymer and (b) an effective 56) References Cited amount of a proteinaceous IL-1 inhibitor. The composition exhibits a therapeutic effect on inflammation and is useful U.S. PATENT DOCUMENTS for treating IL-1 mediated inflammatory diseases, particu 4,784,991 11/1988 Nimrod et al. ........................... 514/62 larly diseases of the joint. 4,808,576 2/1989 Schultz et al. ............................ 514/54 5,858,355 1/1999 Glorioso et al. ..................... 424/93.21 20 Claims, 5 Drawing Sheets U.S. Patent Aug. 1, 2000 Sheet 1 of 5 6,096,728 8 3 O qm (u/6r) Du - WWSW U.S. Patent Aug. 1, 2000 Sheet 2 of 5 6,096,728 FG.2 1OO O L-ra in 2% HA (90/IO) O L-1rd alone 1O TIME U.S. Patent Aug. 1, 2000 Sheet 3 of 5 6,096,728 FIG. 3 O L-ro/HA(90/IO) O L-iro OO 1 O O. 1 O. Ol O 15 2O TIME (hours) U.S. Patent Aug. 1, 2000 Sheet 4 of 5 6,096,728 TOLOLE30WWWG397TILHVO LIAONÅSISI LNIO^[]TVLOL STINNV??ú] EOVWVGENOG?S O Gl O O2 GZ CN (3S uDeu) O)S OS)OOSH U.S. Patent Aug. 1, 2000 Sheet 5 of 5 6,096,728 09 OZT 08T 099 –+–+~--+~-4--+–- –+–+---+~+–+–• –+~~---+–+-----––+ –+••+---+~-~-+- -+--+-+--+-+-- Na5ÕIXVATI8?XI VEXHXICIÕYHNS"IÎLIAº? GCIaVINI"ISA?I?VEVNLDH »CIEIÕBIX3IAVN5) IZI T8I TO£ 6,096,728 1 2 COMPOSITION AND METHOD FOR tein metabolism, esp. in Sepsis); Osteoporosis; Parkinson's TREATING INFLAMMATORY DISEASES disease; pain; pre-term labor, psoriasis, reperfusion injury; Septic Shock, Side effects from radiation therapy, temporal This is a nonprovisional Application derived from U.S. mandibular joint disease, tumor metastasis, or an inflamma provisional applications Ser. Nos. 60/011,419, filed Feb. 9, tory condition resulting from Strain, Sprain, cartilage 1996; 60/032,789, filed Dec. 6, 1996; and Attorney Docket damage, trauma, Orthopedic Surgery, infection or other dis ease proceSSeS. #A-365B-P (serial # not yet available), filed Jan. 23, 1997. Inflammatory conditions of a joint are chronic joint dis FIELD OF THE INVENTION eases that afflict and disable, to varying degrees, millions of people worldwide. Rheumatoid arthritis is a disease of The present invention relates to the field of inflammation. articular joints in which the cartilage and bone are slowly More specifically, the present invention relates to a compo eroded away by a proliferative, invasive connective tissue Sition for the purpose of preventing or treating inflammatory called pannus, which is derived from the Synovial mem diseases. brane. The disease may involve peri-articular structures Such 15 as bursae, tendon Sheaths and tendons as well as extra BACKGROUND OF THE INVENTION articular tissueS Such as the Subcutis, cardiovascular System, Inflammation is the body's defense reaction to injuries lungs, Spleen, lymph nodes, Skeletal muscles, nervous Sys Such as those caused by mechanical damage, infection or tem (central and peripheral) and eyes (Silberberg (1985), antigenic Stimulation. An inflammatory reaction may be Anderson's Pathology, Kissane (ed.), II:1828). Osteoarthri expressed pathologically when inflammation is induced by tis is a common joint disease characterized by degenerative an inappropriate Stimulus Such as an autoantigen, is changes in articular cartilage and reactive proliferation of expressed in an exaggerated manner or persists well after the bone and cartilage around the joint. Osteoarthritis is a removal of the injurious agents. cell-mediated active process that may result from the inap While the etiology of inflammation is poorly understood, propriate response of chondrocytes to catabolic and anabolic considerable information has recently been gained regarding 25 Stimuli. Changes in Some matrix molecules of articular the molecular aspects of inflammation. This research has led cartilage reportedly occur in early osteoarthritis (Thonar et to identification of certain cytokines which are believed to al. (1993), Rheumatic disease clinics of North America, figure prominently in the mediation of inflammation. Cytok Moskowitz (ed.), 19:635–657 and Shinmei et al. (1992), ines are extracellular proteins that modify the behavior of Arthritis Rheum., 35:1304–1308). cells, particularly those cells that are in the immediate area It is believed that rheumatoid arthritis results from the of cytokine Synthesis and release. One of the most potent presentation of a relevant antigen to an immunogenetically inflammatory cytokines yet discovered and a cytokine which Susceptible host. The antigens that could potentially initiate is thought to be a key mediator in many diseases and medical an immune response that results in rheumatoid arthritis conditions is interleukin-1 (IL-1). IL-1, which is manufac might be endogenous or exogenous. Possible endogenous tured (though not exclusively) by cells of the macrophage/ 35 antigens include collagen, mucopolysaccharides and rheu monocyte lineage, may be produced in two forms: IL-1 matoid factors. Exogenous antigens include mycoplasms, alpha (IL-1C) and IL-1 beta (IL-1f8). mycobacteria, Spirochetes and viruses. By-products of the A disease or medical condition is considered to be an immune reaction inflame the Synovium (i.e., prostaglandins “interleukin-1 mediated disease' if the Spontaneous or and oxygen radicals) and trigger destructive joint changes experimental disease or medical condition is associated with 40 (i.e., collagenase). elevated levels of IL-1 in bodily fluids or tissue or if cells or There is a wide spectrum of disease Severity, but many tissues taken from the body produce elevated levels of IL-1 patients run a course of intermittent relapses and remissions in culture. In many cases, Such interleukin-1 mediated with an overall pattern of Slowly progressive joint destruc diseases are also recognized by the following additional two tion and deformity. The clinical manifestations may include conditions: (1) pathological findings associated with the 45 Symmetrical polyarthritis of peripheral joints with pain, disease or medical condition can be mimicked experimen tenderneSS, SWelling and loSS of function of affected joints; tally in animals by the administration of IL-1; and (2) the morning Stiffness, and loSS of cartilage, erosion of bone pathology induced in experimental animal models of the matter and Subluxation of joints after persistent inflamma disease or medical condition can be inhibited or abolished tion. Extra-articular manifestations include rheumatoid by treatment with agents which inhibit the action of IL-1. In 50 nodules, rheumatoid vasculitis, pleuropulmonary most interleukin-1 mediated diseases at least two of the three inflammations, Scleritis, Sicca Syndrome, Felty's Syndrome conditions are met, and in many interleukin-1 mediated (splenomegaly and neutropenia), osteoporosis and weight diseases all three conditions are met. A non-exclusive list of loss (Katz (1985), Am. J. Med, 79:24 and Krane and Simon acute and chronic interleukin-1 (IL-1)-mediated inflamma (1986), Advances in Rheumatology, Synderman (ed.), 70(2) tory diseases includes but is not limited to the following: 55 :263-284). The clinical manifestations result in a high acute pancreatitis, ALS, Alzheimer's disease, cachexia/ degree of morbidity resulting in disturbed daily life of the anorexia; asthma, atherosclerosis, chronic fatigue patient. Syndrome, fever, diabetes (e.g., insulin diabetes); glomeru The involvement of interleukin-1 in arthritis has been lonephritis, graft versus host rejection; hemohorragic shock; implicated by two distinct lines of evidence. First, increased hyperalgesia, inflammatory bowel disease; inflammatory 60 levels of interleukin-1, and of the mRNA encoding it, have conditions of a joint, including osteoarthritis, psoriatic been found in the synovial tissue and fluid of arthritic joints. arthritis and rheumatoid arthritis; ischemic injury, including See, for example, Buchan et al., “Third Annual General cerebral ischemia (e.g., brain injury as a result of trauma, Meeting of the British Society for Rheumatology,” London, epilepsy, hemorrhage or Stroke, each of which may lead to England, Nov. 19-21, 1988, J. Rheumatol., 25(2); Fontana neurodegeneration); lung diseases (e.g., ARDS); multiple 65 et al. (1982), Rheumatology Int., 2:49-53; and Duff et al. myeloma; multiple Sclerosis, myelogenous (e.g., AML and (1988), Monokines and Other Non-Lymphocytic Cytokines, CML) and other leukemias, myopathies (e.g., muscle pro M. Powanda et al. (eds), pp. 387–392 (Alan R. Liss, Inc.). 6,096,728 3 4 Second, the administration of interleukin-1 to healthy although Symptoms Such as pain and Stiffness become a joint tissue has been shown on numerous occasions to result Serious problem in the treatment of joint diseases, hyalu in the erosion of cartilage and bone. In one experiment, ronic acid does not directly improve Such Symptoms. intra-articular injections of IL-1 into rabbits were shown to Additionally, hyaluronic acid has been used for drug cause cartilage destruction in vivo (Pettipher et al. (1986), delivery.
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