KR-102961847-B1 - Pharmaceutical composition for preventing or treating cancer comprising antivirals, and antidepressants thereof as active ingredients

Abstract

The present invention relates to a pharmaceutical composition for the prevention or treatment of cancer containing an antiviral agent and an antidepressant as active ingredients, and capable of adding a biguanide-based compound. More specifically, it has been confirmed that when efavirenz, etravirine, rilpivirine, lopinavir, atazanavir, darunavir, and ritonavir are administered as antiviral agents, and fluoxetine, fluvoxamine, paroxetine, sertraline, duloxetine, amitriptyline, clomipramine, nortriptyline, desipramine, amoxapin, maprotiline, trimipramine, protriptyline, and melitracen are administered as antidepressants in combination, mixed, or concomitantly, or when metformin, a biguanide-based compound, is added to efavirenz and fluoxetine and administered in combination, mixed, or concomitantly, significantly higher synergistic anticancer activity is exhibited compared to when each is administered alone. Therefore, the antiviral agent according to the present invention and Antidepressants can be usefully used as active ingredients in compositions for the prevention or treatment of cancer.

Inventors

• 박수현
• 김샛별
• 김정훈
• 모영원

Assignees

• (주)메디언스

Dates

Publication Date

20260507

Application Date

20220728

Priority Date

20210729

Claims (15)

1. As a combination, mixed, or concomitant preparation for use in the prevention or treatment of cancer, As a first component, an antiviral agent; and It contains an antidepressant as an active ingredient as the second component, and The above antiviral agents are efavirenz, lopinavir, atazanavir, darunavir, or ritonavir, and The above antidepressants are fluoxetine, fluvoxamine, or sertraline, and A pharmaceutical composition for the prevention or treatment of cancer, wherein the cancer is lung cancer, stomach cancer, prostate cancer, breast cancer, brain cancer, liver cancer, or bile duct cancer.
2. In paragraph 1, It additionally contains a biguanide-based compound or a pharmaceutically acceptable salt thereof as a third active ingredient, and The above antiviral agent is efavirenz, and The above antidepressant is fluoxetine, and A pharmaceutical composition for the prevention or treatment of cancer, wherein the above-mentioned biguanide-based compound is metformin.
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13. As a combination, mixed, or combination kit for the prevention or treatment of cancer, Preparations comprising antiviral agents; and It includes preparations containing antidepressants, and The above antiviral agents are efavirenz, lopinavir, atazanavir, darunavir, or ritonavir, and The above antidepressants are fluoxetine, fluvoxamine, or sertraline, and A combination, mixed, or combination kit for the prevention or treatment of cancer, wherein the above cancer is lung cancer, stomach cancer, prostate cancer, breast cancer, brain cancer, liver cancer, or bile duct cancer.
14. In Paragraph 13, A formulation further comprising a biguanide-based compound or a pharmaceutically acceptable salt thereof, and The above antiviral agent is efavirenz, and The above antidepressant is fluoxetine, and A combination, mixed, or combination kit for the prevention or treatment of cancer, wherein the above-mentioned biguanide-based compound is metformin.
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Description

Pharmaceutical composition for preventing or treating cancer comprising antivirals and antidepressants as active ingredients The present invention relates to a pharmaceutical composition for the prevention or treatment of cancer containing an antiviral agent and an antidepressant as active ingredients, and more specifically, to a pharmaceutical composition for the prevention or treatment of cancer containing a first component containing an antiviral agent; and a second component containing an antidepressant as active ingredients of a complex, mixed, or combination formulation. The present invention also relates to a pharmaceutical composition for the prevention or treatment of cancer comprising the first component; the second component; and a biguanide compound or a pharmaceutically acceptable salt thereof as a third component. Cancer is a disease caused by the abnormal growth of uncontrolled cells that can spread to tissues or other parts of the body; cancer cells can form solid tumors where they are clustered together, or exist as dispersed cells, as in leukemia. Normal cells differentiate until they mature and then replace damaged or dead cells as needed, but cancer cells differentiate continuously, eventually displacing nearby cells and spreading to other parts, which is why they are called malignant. Malignant tumor cells metastasize to other parts of the body through the bloodstream or lymphatic system, where they proliferate and form new tumors. Despite the development of various treatment methods, cancer continues to pose a serious threat to human health worldwide. Currently, major cancer treatments include surgical removal, radiation therapy, hormone therapy, and chemotherapy; among these, chemotherapy is a method that uses one or more anticancer drugs to directly treat cancer or alleviate its symptoms. Traditional chemotherapy agents exert cytotoxicity on cancer cells by interfering with cell division and metabolism, or by inhibiting the biosynthesis of nucleic acids or proteins. However, these agents present problems, such as the development of resistance in cancer cells and toxicity to normal tissues, leading to serious side effects. In particular, substances currently used as anticancer agents often cause various side effects by affecting both cancer cells and normal cells. Therefore, there is a need for an anticancer therapeutic agent that exhibits superior selective toxicity only to cancer cells without affecting normal cells, while possessing excellent anticancer activity. Antiviral drugs are medications that treat infectious diseases caused by viruses by weakening or eliminating the action of viruses that have invaded the human body, and they have the effect of inhibiting viral replication. Based on their mechanism of action, they can be classified into viral adhesion and penetration inhibitors and viral replication inhibitors. Most antiviral drugs exert their antiviral effects by inhibiting various types of enzymes necessary for viral replication. Human Immunodeficiency Virus (HIV), particularly strains known as HIV type-1 (HIV-1) and type-2 (HIV-2), have been etiologically linked to an immunosuppressive disease known as acquired immunodeficiency syndrome (AIDS). Since HIV is a retrovirus, the HIV replication cycle requires the transcription of the viral RNA genome into DNA via reverse transcriptase. Therefore, compounds that inhibit the enzymatic activity of HIV reverse transcriptase are being developed as HIV antiviral agents. Compounds that inhibit the enzymatic activity of HIV reverse transcriptase include nucleoside reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs). NRTIs are primarily administered as precursors; upon entering host cells, they become phosphorylated and converted into nucleotides, thereby acquiring drug activity. Because NRTIs lack the 3-OH (hydroxyl group) on the nucleoside sugar molecule, they intercalate into the DNA strand during viral DNA synthesis and terminate DNA synthesis by blocking the 3'-5' phosphate ester bond with the next nucleotide in the chain. FDA-approved NRTIs include zidovudine, didanosine, zalcitabine, stavudine, lamivudine, abacavir, tenofovir disoproxil fumarate, emtricitabine, and tenofovir alafenamide fumarate. Unlike NRTIs, NNRTIs do not act as viral DNA synthesis terminators; instead, they inhibit enzyme activity by directly binding to the hydrophobic pocket near the active site of reverse transcriptase and altering the enzyme's structure. FDA-approved NNRTIs include efavirenz, etravirine, nevirapine, doravirine, rilpivirine, and delavirdine. Protease inhibitors (PIs) are compounds that inhibit the enzyme responsible for shearing the Gag and Gag-Pol precursor proteins contained in non-infectious virions, thereby transforming them into infectious mature viruses. Initially, it was expected that resistance would be unlikely to develop because this enzyme plays a crucial role in viral replicati