Cytochalasin compositions and therapeutic methods

Details Cytochalasin compositions and therapeutic methods Cytochalasin compositions and therapeutic methods

A - Human Necessities

61

K

167/233

A61K 31/40 (2006.01) C07D 491/10 (2006.01)

Patent

CA 2031520

ABSTRACT OF THE DISCLOSURE The present invention is directed to naturally occurring and synthetic cytochalasin compositions and therapeutic treatments utilizing these compositions. More specifically, the present invention relates to certain synthetic analogues of Cytochalasin B (CB) and sustained release formulations containing a cyctochalasin, for example, cytochalasin B and other natural cytochalasins, for example, Cytochalasin D, E, H or J, among others and one or more of its synthetic analogues. This invention also relates to the surprising discovery that the administration of cytochalasins including CB produces transient immunosuppression which is controllable by dose or route of administration and is reversible spontaneously or with the use of IL-2. Thus, a therapeutic regimen of cytochalasins may be used to treat the undesirable hyperimmunity of transplant patients and patients with autoimmune disease. In addition, anti-tumor therapy utilizing CB and other cytoshalasins, and optionally antineoplastic agents other than cytochalasins may be signifantly enhanced by combining the administration of these agents with effective amounts of IL-2 or other lymphokines for reversing the immunosuppression produced during administration of cytochalasins with other antineoplastic agents. This invention also relates to sustained release formulations utilizing liposomes of microcapsules which are effective for delivering high concentrations of cytochalasins and optionally, additional antineoplastic agents to the active site of the tumor without producing undesirable immunosuppression.

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