Antineoplastic composition and use thereof
A composition and anti-tumor technology, which can be used in anti-tumor drugs, drug combinations, active ingredients of heavy metal compounds, etc., can solve the problems of reduced topoisomerase activity, reduced tumor efficacy of platinum drugs, and reduced drug potency.
Inactive Publication Date: 2008-12-31
NANJING MEDICAL UNIV
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Problems solved by technology
On the other hand, after platinum-based drugs act on tumor cells, the cells will develop acquired drug resistance, which affects the clinical dosage and efficacy of such drugs
It is known that tumor cell resistance to platinum-based drugs is associated with overexpression of P-glycoprotein (P-gp) and mdr-1 genes, increased glutathione S-transferase activity, and decreased topoisomerase activity , and p53 expression level decreased, bc1-2 expression level increased, etc.
Existing studies have shown that tumor cells can reduce the accumulation of platinum drugs in the body by changing the permeability of the cell membrane, so as to reduce the drug effect; enhance the DNA repair ability of their own cells, and block the apoptosis pathway and other mechanisms , thus showing resistance to platinum-based drugs, reducing the efficacy of platinum-based drugs in treating tumors[5-7]
However, the mechanism of tumor cell resistance to platinum-based drugs remains to be further studied
At present, there is no drug that can effectively overcome the resistance of tumors to platinum drugs in clinical practice.
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preparation Embodiment 1
[0034] Take 100-300mg of CDDP and 300mg of RX-0201 (AKT inhibitor), add appropriate amount of commonly used excipients for injection, and make injection by conventional injection techniques.
preparation Embodiment 2
[0036] Take 100-300mg of CDDP and 10-200mg of tricilibine, add appropriate amount of commonly used auxiliary materials for injection, and make injection by conventional injection technology.
preparation Embodiment 3
[0038] Take 100-300 mg of CDDP, 100-900 mg of siRNA (siAKT) against AKT, add appropriate amount of commonly used auxiliary materials for injection, and make injection by conventional injection techniques. We also plan to use other biological and chemical AKT inhibitors to make compound injections with cisplatin in a similar way.
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The invention discloses an anti-tumor combination and the application thereof; the anti-tumor combination which includes effective dose of platinum-based chemotherapy and AKT inhibitor and / or p70S6K1 inhibitor has the function of inhibiting the drug resistance of the tumor to the platinum-based chemotherapy, improves the effects of anti-tumor drugs, and can be used for preparing drugs that can resist various tumors, such as lung cancer, ovarian cancer, prostate cancer, breast cancer, stomach cancer, nasopharyngeal cancer, esophageal cancer, malignant lymphoma, head and neck squamous cell carcinoma, thyroid cancer, osteosarcoma, etc.
Description
technical field [0001] The invention belongs to the field of pharmacy, and relates to an antitumor composition and its application. Background technique [0002] Since Rosenberg et al. [1] discovered that platinum group compounds have anticancer activity in 1965, the research and application of platinum group metal anticancer drugs have developed rapidly. Cisplatin (cisplatin, cis-dichlorodiammine platinum, Cisplatin, Cis-Diaminodichloroplatin Platinol, CDDP) is one of the most effective. CDDP has the characteristics of broad anti-cancer spectrum, strong effect, and synergistic effect with various anti-tumor drugs. It is one of the most commonly used drugs in current combination chemotherapy. Esophageal cancer, malignant lymphoma, breast cancer, head and neck squamous cell carcinoma, thyroid cancer and osteosarcoma and other solid tumors can show curative effect. [2]. According to statistics, in my country, CDDP-based or compatible chemotherapy regimens with CDDP account ...
Claims
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IPC IPC(8): A61K45/06A61K33/24A61K31/282A61K31/7064A61P35/00
Inventor 江秉华刘凌志
Owner NANJING MEDICAL UNIV
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