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Novel Small Molecule Inhibitors of Tyrosyl-DNA Phosphodiesterase 1 (TDP1) for Treatment of Solid Tumors

Summary: The NCI seeks proposals from parties interested in licensing and/or co-development for commercializing the use of TDP1 inhibitors as part of a potent and selective anti-cancer combination therapy. Description of Technology: Topoisomerase 1 (TOP1) is an essential enzyme that plays a critical role in DNA transcription and replication. TOP1...

Published: 4/23/2026 | Updated: 8/2/2023 | Inventor(s): Xue Zhao, George Lountos, Evgeny Kiselev, David Waugh, Yves Pommier, Terrence Burke

Keywords(s): Burke, CANCER, solid tumor, Tdp1, TOP1, Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1, Zhao

Category(s): Application > Therapeutics, Collaboration Sought > Collaboration, Collaboration Sought > Licensing, TherapeuticArea > Oncology

Small Molecule Inhibitors of Drug Resistant Forms of HIV-1 Integrase

Abstract: Integrase strand transfer inhibitors (“INSTIs”) are currently in use as a component of prophylactic antiretroviral therapy for preventing HIV-1 infection from progressing to AIDS. Three INSTIs are approved by the FDA for inclusion in antiretroviral regiments: raltegravir (RAL), elvitegravir (EVG) and dolutegravir (DTG). Clinicians have already...

Published: 4/22/2025 | Updated: 8/2/2023 | Inventor(s): Xue Zhao, Terrence Burke, Yves Pommier, Stephen Hughes, Mathieu Metifiot, Stephen Smith, Barry Johnson, Christophe Marchand

Keywords(s): dolutegravir, drug resistant HIV, elvitegravir, HIV therapy, Integrase, raltegravir, strand transfer

Category(s): Collaboration Sought > Collaboration, Application > Therapeutics, TherapeuticArea > Infectious Disease, Collaboration Sought > Licensing