Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1996-10-23
1998-08-18
Goldberg, Jerome D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
514 28, A61K 3170
Patent
active
057958718
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a pharmaceutical composition effective as an anticancer agent for non-small cell lung cancer comprising a 14- or 15-membered-ring macrolide compound as an effective ingredient.
BACKGROUND ART
In many countries including Japan, Europe and America, the number of patients with lung cancer is fairly large and further increasing year after year with deterioration of atmospheric environment on the earth, contrary to the number of patients with gastric cancer which is reducing year after year. Lung cancers can be histologically classified into non-small cell lung cancers (e.g. squamous cell carcinoma, adeno carcinoma, large cell carcinoma, etc.) and small cell lung cancer. Non-small cell lung cancer has very largely different biological properties and responses to chemotherapeutics from those of small cell lung cancer. Thus, chemo-therapeutic formulas are different between these two types of lung cancer.
It is reported that non-small cell lung cancers are the tumors of which chemotherapy is the most difficult, and any useful therapies for advanced inoperable cancers have not been established (Journal of Clinical Oncology, vol. 10, pp. 829-838 (1992)). The combination therapy of cisplatin and interferon is reported (European Journal of Cancer, vol. 30A, No. 1, pp. 11-15 (1994)). However, this remedy can not be widely acceptable because of insufficient therapeutic effect and harmful side effects.
Japanese Patent Kokai 5-163293 refers to some specified antibiotics of 16-membered-ring macrolides as a drug delivery carrier capable of transporting anthoracycline-type anticancer drugs into the lungs for the treatment of lung cancers. However, the macrolide antibiotics specified herein are disclosed to be only a drug carrier, and there is no reference to the therapeutic use of macrolides against non-small cell lung cancers.
WO 93/18652 refers to the effectiveness of the specified 16-membered-ring macrolides such as bafilomycin, etc. in treating non-small cell lung cancers, but they have not yet been clinically practicable.
Pharmacology, vol. 41, pp. 177-183 (1990) describes that a long-term use of erythromycin increases productions of interleukins 1, 2 and 4, all of which contribute to host immune responses, but there is no reference to the effect of this drug on non-small cell lung cancers.
Tetragenesis, Carcinogenesis, and Mutagenesis, vol. 10, pp. 477-501 (1990) describes that some of antimicrobial drugs can be used as an anticancer agent, but does not refer to their application to non-small cell lung cancers.
In addition, interleukins are known to have an antitumor effect, but have not been reported to be effective against non-small cell lung cancers.
Any 14 - or 15-membered-ring macrolides have not been reported to be effective against non-small cell lung cancers.
As stated above, at present, there is no disclosure about practical chemotherapeutic drugs of non-small cell lung cancer, and any chemotherapeutic drugs clinically available are not practicable for the treatment of non-small cell lung cancer. Accordingly, apart from the conventional concept of anticancer chemotherapy, there is a strong need for the development of therapeutic drugs practicably effective for the treatment of non-small cell lung cancers.
DISCLOSURE OF THE INVENTION
As a result of extensive research of antitumor activity of various compounds in order to solve the above problem, unexpectedly, the present inventors have found that certain 14- or 15-membered-ring macrolide compounds have the ability to inhibit the growth and metastasis of non-small cell lung cancers, a useful effect on the malignant tumor which distantly metastasized to other organs and an excellent treatment effect in patients with advanced inoperable non-small cell lung cancers, and improve the quality of life of the patients. Based on these findings, the present invention has been accomplished.
The present invention is a pharmaceutical composition for the treatment of non-small cell lung cancers comprising as an effective
REFERENCES:
patent: 4331803 (1982-05-01), Watanabe et al.
patent: 4349545 (1982-09-01), d'Ambrieres et al.
patent: 4517359 (1985-05-01), Kobrehel et al.
The Merck Index, 7th Ed., 1989,Merck & Co, Inc, Rahway, N.J. pp. 146, 365, 577, 578 and 1316.
Chem. Abst., vol. 96 (1982) Columbus, OH, USA #1869.
Kita Eiji
Mikasa Keiichi
Narita Nobuhiro
Sawaki Masayoshi
Goldberg Jerome D.
Nobuhiro Narita
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