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TECHNOLOGY BRIEF
Phosphor-6-ethylthioinosine for cancer treatment
Invention Summary
The inventors have disclosed a highly specific and effective inhibitor for cancers that
overexpress adenosine kinase (ADK).
Technology Overview
The Kaposi’s sarcoma herpesvirus (KSHV) causes Kaposi’s sarcoma (KS), primary effusion
lymphoma (PEL) and multicentric Castleman’s disease (MCD). KS is widely prevalent in
Sub-Saharan Africa, and is a common AIDS complication. Although highly active
antiretroviral treatment (HAART) has played a key role in enhancing the survival rates of
AIDS patients, almost 50% of KS patients relapse. The age-adjusted survival for KS is only
12%, hence there is an urgent need for the development of a more reliable cure.
Similarly, PEL is a rare but highly aggressive malignancy, with most patients surviving for
only 6 month post-diagnosis. There is no therapeutic cure for this disease, and all
patients receive only palliative care.
Inventors: Utthara Nayar
and Ethel Cesarman
Patents:
Filed
Licensing Contact:
Dan-Oscar Antson
(646) 962-7042
[email protected]
Cornell Reference:
D-6918
The inventors performed a high-throughput screen for inhibitors of PEL, and discovered
a potent inhibitor called 6-ethylthioinosine (6-ETI), which is a pro-drug. The drug is
converted into phosphor-6-ETI by adenosine kinase (ADK), an enzyme commonly
overexpressed in several cancers. Further studies have shown that phosphor-6-ETI can be used to treat cancer, thereby
bypassing the enzymatic conversion step. This opens up the possibility of using this drug to treat cancers that do not
overexpress ADK. This inhibitor holds great promise for the treatment of KS and PEL, along with other cancers such as
colorectal cancer and astrocytic tumors.
Potential Applications


This inhibitor can provide the first and only known cure for serious diseases such as PEL
Cancers overexpressing ADK may be highly susceptible to treatment with this drug
Advantages

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ADK expression levels can serve as a clinical biomarker for response to treatment
Large quantities of the compound can be easily synthesized by standard chemistry
Publication
Exquisite Sensitivity of Plasma Cell Malignancies to a Novel Nucleoside Analog Is Mediated By Overexpressed Adenosine
Kinase. Nayar U. et. al., Blood 2015 126:1812.
413 East 69th Street, Room 612, New York, NY 10021 •P: 646-962-7045 •F: 646-962-0427 •E: [email protected] •www.ctl.cornell.edu