(12) Patent Application Publication (10) Pub. No.: US 2002/0103141 A1 Mckearn Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2002/0103141 A1 Mckearn Et Al US 2002O103141A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2002/0103141 A1 McKearn et al. (43) Pub. Date: Aug. 1, 2002 (54) ANTIANGIOGENIC COMBINATION Related U.S. Application Data THERAPY FOR THE TREATMENT OF CANCER (63) Continuation-in-part of application No. 09/470,951, filed on Dec. 22, 1999. (76)76 Inventors: John P. McKearn, Wildwood, MO (60) 23,Provisional 1998. application No. 60/113,786, filed on Dec. (US); Gary B. Gordon, Highland Park, IL (US); James Cunningham, Chicago, Publication Classification IL (US); Stephen T. Gately, Palatine, IL (US); Alane T. Koki, Beaufort, MO (51) Int. Cl." .................. A61K 31/706; A61K 31/4745; (US); Jaime L. Masferrer, Ballwin, A61K 31/473; A61K 31/407; MO (US) A61K 31/415; A61K 31/277 (52) U.S. Cl. ............................ 514/43; 514/283; 514/297; Correspondence Address: 514/410; 424/450; 514/406; Pharmacia Corporation 514/521 Corporate Patent Department P.O. BOX 5110 (57) ABSTRACT Chicago, IL 60680-9889 (US) The present invention provides combinations of a DNA (21) Appl. No.: 09/843,132 topoisomerase I inhibiting agent and a Selective COX-2 inhibiting agent for preventing, treating, and/or reducing the (22) Filed: Apr. 25, 2001 risk of developing a neoplasia disorder in a mammal. US 2002/0103141 A1 Aug. 1, 2002 ANTIANGIOGENIC COMBINATION THERAPY Chemotherapy involves the disruption of cell replication or FOR THE TREATMENT OF CANCER cell metabolism. Chemotherapy is used most often in the 0001. This application is a continuation-in-part of U.S. treatment of breast, lung, and testicular cancer. patent application Ser. No. 09/479,951, filed Dec. 22, 1999, 0007. The adverse side effects of anticancer therapy is which is a continuation-in-part of U.S. patent application most feared by patients undergoing treatment for cancer. Of Serial No. 60/113,786, filed Dec. 23, 1998. these adverse effects pain, nausea and vomiting are the most common and severe side effects. Other adverse side effects FIELD OF THE INVENTION include cytopenia, infection, cachexia, mucositis in patients receiving high doses of chemotherapy with bone marrow 0002 The present invention relates to methods, combi rescue or radiation therapy, alopecia (hair loss); cutaneous nations and compositions for treating, preventing or reduc complications, Such as pruritis, urticaria, and angioedema, ing the risk of developing a neoplasia disorder in a mammal. neurological complications, pulmonary and cardiac compli cations in patients receiving radiation or chemotherapy; and BACKGROUND OF THE INVENTION reproductive and endocrine complications. Anticancer therapy induced Side effects significantly impact the quality 0.003 Cancer is now the second leading cause of death in of life of the patient and may dramatically influence patient the United States. In 1995 over 8,000,000 persons in the compliance with treatment. United States have been diagnosed with cancer and has accounted for 23.3% of all reported deaths. 0008 Additionally, the adverse side effects associated with anticancer therapy is generally the major dose-limiting 0004 Cancer is not fully understood on the molecular toxicity (DLT) in the administration of the therapy. For level. It is known that exposure of a cell to a carcinogen Such example, mucositis, is one of the major dose limiting as certain viruses, certain chemicals, or radiation, leads to DNA alteration that inactivates a “Suppressive' gene or toxicity for Several anticancer agents, including the antime activates an “oncogene.” Suppressive genes are growth tabolite cytotoxic agents 5-FU, and methotrexate, and anti regulatory genes, which upon mutation, can no longer tumor antibiotics, Such as doxorubicin. Many of these che control cell growth. Oncogenes are initially normal genes motherapy-induced Side effects if Severe, may lead to (called prooncogenes) that by mutation or altered context of hospitalization, or require treatment with analgesics for the expression become transforming genes. The products of treatment of pain. transforming genes cause inappropriate cell growth. More 0009 Adverse side effects induced by anticancer therapy than twenty different normal cellular genes can become have become of major importance in the clinical manage oncogenes by genetic alteration. Transformed cells differ ment of patients undergoing treatment for cancer or neopla from normal cells in many ways, including cell morphology, sia disease. cell-to-cell interactions, membrane content, cytoskeletal Structure, protein Secretion, gene expression and mortality BRIEF DESCRIPTION OF THE INVENTION (transformed cells can grow indefinitely). 0010. In brief, the present invention provides a method 0005. A neoplasm, or tumor, is an abnormal, unregulated, for treating, preventing or reducing the risk of developing a and disorganized proliferation of cell growth, and is gener neoplasia disorder in a mammal in need thereof, comprising ally referred to as cancer. A neoplasm is malignant, or administering to the mammal in a combination therapy an cancerous, if it has properties of destructive growth, inva amount of a DNA topoisomerase I inhibiting agent and an Siveness and metastasis. Invasiveness refers to the local amount of a Selective cyclooxygenase-2 inhibiting agent Spread of a neoplasm by infiltration or destruction of Sur wherein the amount of the DNA topoisomerase I inhibiting rounding tissue, typically breaking through the basal lami agent and the Selective cyclooxygenase-2 inhibiting agent nas that define the boundaries of the tissues, thereby often together make a neoplasia disorder effective amount. entering the body's circulatory System. Metastasis typically 0011. The present invention further provides a pharma refers to the dissemination of tumor cells by lymphotics or ceutical composition comprising a DNA topoisomerase I blood vessels. Metastasis also refers to the migration of inhibiting agent and a cyclooxygenase-2 inhibiting agent tumor cells by direct extension through Serous cavities, or Subarachnoid or other spaces. Through the process of wherein the DNA topoisomerase I inhibiting agent and the metastasis, tumor cell migration to other areas of the body Selective cyclooxygenase-2 inhibiting agent together make a establishes neoplasms in areas away from the Site of initial neoplasia disorder effective amount. appearance. 0012. In another embodiment, the present invention pro 0006 Cancer today is primarily treated with one or more vides a use of a composition in preparation of a medicament types of anticancer therapy, including Surgery, radiation and useful in treating, preventing or lowering the risk of devel chemotherapy. Surgery involves the bulk removal of dis oping a neoplasia disorder in a mammal in need thereof, the eased tissue. While Surgery is Sometimes effective in remov composition comprising an amount of a DNA topoisomerase ing tumors located at certain Sites, for example, in the breast, I inhibiting agent and an amount of a cyclooxygenase-2 colon, or skin, it cannot be used in the treatment of tumors inhibiting agent wherein the amount of the DNA topoi located in other areas, Such as the backbone, nor in the Somerase I inhibiting agent and the Selective cyclooxyge treatment of disseminated neoplastic conditions Such as nase-2 inhibiting agent together make a neoplasia disorder leukemia. Radiation therapy involves the exposure of living effective amount. tissue to ionizing radiation causing death or damage to the 0013 The present invention further provides a kit com exposed cells. Side effects from radiation therapy may be prising a DNA topoisomerase I inhibiting agent and a acute and temporary, while others may be irreversible. Selective cyclooxygenase-2 inhibiting agent wherein the US 2002/0103141 A1 Aug. 1, 2002 DNA topoisomerase I inhibiting agent and the Selective 0020. The term “acyl', alone or in combination, means a cyclooxygenase-2 inhibiting agent together make a neopla radical provided by the residue after removal of hydroxyl sia disorder effective amount. from an organic acid. Examples of Such acyl radicals include alkanoyl and aroyl radicals. Examples of Such alkanoyl 0.014) Another embodiment of the present invention pro radicals include formyl, acetyl, propionyl, butyryl, isobu vides a method for the prevention or treatment of DNA topoisomerase I inhibiting agent-related diarrhea in a Subject tyryl, Valeryl, isoValeryl, pivaloyl, hexanoyl, trifluoroacetyl, in need of Such prevention or treatment wherein the method and the like. comprises administering to the Subject a diarrhea preventing 0021. The term “carbonyl” or “oxo”, alone or in combi or treating-effective amount of a source of a COX-2 inhib nation, i.e., used with other terms, Such as “alkoxycarbonyl', iting agent, thereby preventing or treating the DNA topoi means a -C(=O)- group wherein the remaining two Somerase I inhibiting agent-related diarrhea. bonds (valences) can be independently substituted. The term carbonyl is also intended to encompass a hydrated carbonyl DETAILED DESCRIPTION OF THE group -C(OH)-. INVENTION 0022. The term “hydrido”, alone or in combination, means a single hydrogen atom (H). This hydrido radical may 0015) Definitions be attached, for example, to an oxygen atom to form a 0016. In the written descriptions of molecules and hydroxyl radical or two hydrido radicals may be attached to groups, molecular descriptors can be combined to produce a carbon atom to form a methylene (-CH-) radical. words or phrases that describe Structural groups or are combined to describe
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