Synthesis of (1)-beta-elemene, (-)-beta-elemenal, (-)-beta-elemenol, (-)-beta-elemene fluoride and their analogues, intermediates, and composition and uses thereof

A method for reducing the normal dosage of a chemotherapeutic agent given to a patient in need thereof for the treatment of a cancer without substantially reducing the effectiveness of said agent, said agent selected from the group consisting essentially of cisplatin, paclitaxel, docetaxel and fluorouracil (5-FU), said method comprising the steps of administering a therapeutically effective reduced dosage of said agent, and concurrently or sequentially administering an effective amount of (−)-beta-elemene.

A method for reducing the side effect(s) in a patient requiring a treatment for a tumor, said method comprising administering to said patient a reduced effective amount of a known active substance having antitumor effect selected from the group consisting essentially of cisplatin, paclitaxel, docetaxel and fluorouracil (5-FU), and an effective amount of (−)-beta-elemene, wherein said tumor is sensitive to said substance and wherein the administration of the (−)-beta-elemene reduces the side effects(s) experienced by said patient.

A method for reducing the toxicity associated with a known active substance having antitumor effect selected from the group consisting essentially of cisplatin, paclitaxel, docetaxel and fluorouracil (5-FU), the method comprising concurrently or sequentially administering to a patient in need of such antitumor effect an effective amount of (−)-beta-elemene and a substantially reduced amount of said substance when compared with the effective amount of said substance administered without (−)-beta-elemene.

In a method for minimizing either the individual or cumulative dose of a neoplastic agent used in the treatment of a patient suffering from a cancer that exhibits a dose dependent response to said agent, said agent selected from the group consisting essentially of cisplatin, paclitaxel, docetaxel and fluorouracil (5-FU), the improvement comprising the administration of said agent and the concurrent administration of (−)-beta-elemene in an amount sufficient to permit the individual or cumulative dose of said agent to be minimized without substantially reducing the efficacy of said agent, whereby unacceptably severe side effects are also minimized.

A method for enhancing the efficacy of a chemotherapeutic agent given to a patient in need thereof for the treatment of a cancer, said agent selected from the group consisting essentially of cisplatin, paclitaxel, docetaxel and fluorouracil (5-FU), said method comprising administering said agent to said patient and concurrently or sequentially administering to said patient an effective amount of (−)-beta-elemene.

A pharmaceutical composition having antitumor activity with reduced side effect(s) comprising a therapeutically effective reduced amount of a known active substance having antitumor effect selected from the group consisting essentially of cisplatin, paclitaxel, docetaxel and fluorouracil (5-FU), and an effective amount of (-−)-beta-elemene, together with a pharmaceutically acceptable carrier.

A method of imaging a tumor, comprising administering to a patient having a tumor a diagnostically effective amount of a detectable agent that is (−)-beta-elemene fluoride labeled with radioactive fluorine.

A method for performing a diagnostic procedure to detect or image a tumor or for performing a therapeutic procedure on a tumor, the method comprising administering to a patient an effective amount of fluorine-labeled (−)-beta-elemene fluoride, and performing the diagnostic or therapeutic procedure.

An imaging agent for imaging of a tumor site which comprises radioactive fluorine-labeled (−)-beta-elemene fluoride.