Abstract: Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of “warhead” anthracycline or anthracycline derivative to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compounds comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer undesirable fibrosis and undesirable inflammation.
Type:
Grant
Filed:
March 4, 2022
Date of Patent:
March 12, 2024
Assignee:
Bach Biosciences, LLC
Inventors:
William W. Bachovchin, Hung-sen Lai, David G. Sanford, Sarah E. Poplawski, Wengen Wu
Abstract: Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of “warhead” anthracycline or anthracycline derivative to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compounds comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, undesirable fibrosis, and undesirable inflammation.
Type:
Grant
Filed:
June 5, 2020
Date of Patent:
March 8, 2022
Assignee:
BACH BIOSCIENCES, LLC
Inventors:
William W. Bachovchin, Hung-sen Lai, David G. Sanford, Sarah E. Poplawski, Wengen Wu
Abstract: Disclosed are prodrugs of cytotoxic anthracyclines (such as doxorubicin) and other therapeutic agents that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of cytotoxic and other agents to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compounds comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, fibrosis, and inflammation.
Type:
Grant
Filed:
February 13, 2019
Date of Patent:
June 15, 2021
Assignee:
BACH BIOSCIENCES, LLC
Inventors:
William W. Bachovchin, Hung-sen Lai, David G. Sanford, Sarah E. Poplawski, Wengen Wu
Abstract: Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of “warhead” anthracycline or anthracycline derivative to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compounds comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, undesirable fibrosis, and undesirable inflammation.
Type:
Grant
Filed:
October 16, 2018
Date of Patent:
July 14, 2020
Assignee:
BACH BIOSCIENCES, LLC
Inventors:
William W. Bachovchin, Hung-sen Lai, David G. Sanford, Sarah E. Poplawski, Wengen Wu
Abstract: Disclosed are prodrugs of therapeutic or imaging agents, which prodrugs are selectively cleaved by fibroblast activating protein (FAP) to release the agents. Upon cleavage by FAP of the FAP substrate, the prodrug releases the agent in its active form or in a form that is readily metabolized to its active form. Pharmaceutical compositions comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation are also disclosed.
Type:
Grant
Filed:
June 15, 2015
Date of Patent:
April 2, 2019
Assignee:
BACH BIOSCIENCES, LLC
Inventors:
William W. Bachovchin, Hung-sen Lai, David G. Sanford, Sarah E. Poplawski, Wengen Wu
Abstract: Disclosed are prodrugs of anthracyclines (such as doxorubicin) and derivatives thereof that are selectively cleaved and activated by fibroblast activating protein (FAP). The prodrugs are useful for targeted delivery of “warhead” anthracycline or anthracycline derivative to FAP-expressing tissues, including cancer (e.g., solid tumors). Also provided are pharmaceutical compositions comprising the prodrugs, as well as methods of using the prodrugs to treat a disorder characterized by FAP upregulation, e.g., cancer, undesirable fibrosis, and undesirable inflammation.
Type:
Grant
Filed:
July 20, 2017
Date of Patent:
November 6, 2018
Assignee:
BACH BIOSCIENCES, LLC
Inventors:
William W. Bachovchin, Hung-sen Lai, David G. Sanford, Sarah E. Poplawski, Wengen Wu