The present invention relates to the use of a heterocyclic compound according to generalstructural formula (I) for the treatment of cancer. In a preferred aspect the compound according 5to formula (I) is aprepitant.BACKGROUND OF THE INVENTIONCancer is a disorder in which a population of cells has become, in varying degrees, unresponsive 10to the control mechanisms that normally govern proliferation and differentiation. Therapeuticagents used in clinical cancer therapy can be categorized into several groups, including,alkylating agents, antibiotic agents, antimetabolic agents, biologic agents, hormonal agents, andplant-derived agents.15Cancerous cells display uncontrolled growth (growth and division beyond the normal limits),invasion (intrusion on and destruction of adjacent tissues), and sometimes metastasis (spread toother locations in the body via lymph or blood). Much effort has been spent to find novel anticanceragents. Cancer therapy is also being attempted by modulating the enzymatic activity oftarget proteins in cancer cells. For example, compounds were found which inhibit enzymes used 20in purine and pyrimidine synthesis such as thymidylate synthase (TS), dihydrofolate reductase(DHFR), and glycinamide ribonucleotide formyl transferase (GARFT). By inhibiting theformation of precursor purine and pyrimidine nucleotides, the formation of DNA and RNA iscomprimised, which are necessary for the growth and survival of both normal cells and cancercells. As cancer cells are rapidly dividing they heavily rely on a sufficient supply of nucleotides 25to afford such rapid divisions. However, therapeutic target proteins, such as the aforementionedenzymes respond differently to treatment depending on the type of cancer and the the geneticpredisposition of the patient.Due to the multiple different forms of cancer there is a need for additional pharmaceutically 30active substances which can be used to treat cancer.SUMMARY OF THE INVENTION2The inventors have identified a compound which unexpectedly is useful to effectively treatcancer.

Aprepitant as anticancer drug / Michael, Khun; Peer, Bork; Costi, Maria Paola; Luciani, Rosaria. - .

Aprepitant as anticancer drug

COSTI, Maria Paola;LUCIANI, Rosaria

Abstract

The present invention relates to the use of a heterocyclic compound according to generalstructural formula (I) for the treatment of cancer. In a preferred aspect the compound according 5to formula (I) is aprepitant.BACKGROUND OF THE INVENTIONCancer is a disorder in which a population of cells has become, in varying degrees, unresponsive 10to the control mechanisms that normally govern proliferation and differentiation. Therapeuticagents used in clinical cancer therapy can be categorized into several groups, including,alkylating agents, antibiotic agents, antimetabolic agents, biologic agents, hormonal agents, andplant-derived agents.15Cancerous cells display uncontrolled growth (growth and division beyond the normal limits),invasion (intrusion on and destruction of adjacent tissues), and sometimes metastasis (spread toother locations in the body via lymph or blood). Much effort has been spent to find novel anticanceragents. Cancer therapy is also being attempted by modulating the enzymatic activity oftarget proteins in cancer cells. For example, compounds were found which inhibit enzymes used 20in purine and pyrimidine synthesis such as thymidylate synthase (TS), dihydrofolate reductase(DHFR), and glycinamide ribonucleotide formyl transferase (GARFT). By inhibiting theformation of precursor purine and pyrimidine nucleotides, the formation of DNA and RNA iscomprimised, which are necessary for the growth and survival of both normal cells and cancercells. As cancer cells are rapidly dividing they heavily rely on a sufficient supply of nucleotides 25to afford such rapid divisions. However, therapeutic target proteins, such as the aforementionedenzymes respond differently to treatment depending on the type of cancer and the the geneticpredisposition of the patient.Due to the multiple different forms of cancer there is a need for additional pharmaceutically 30active substances which can be used to treat cancer.SUMMARY OF THE INVENTION2The inventors have identified a compound which unexpectedly is useful to effectively treatcancer.
2008
EMBL-UNIMORE
61/043,299.
Nazionale
Michael, Khun; Peer, Bork; Costi, Maria Paola; Luciani, Rosaria
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11380/420214
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