The University of Texas System

University of Illinois

Case Western Reserve University

David A Boothman

Jinming Gao

Paul Joseph Hergenrother

Elizabeth I Parkinson

Joseph S Bair

Rahul Palchaudhuri

Kejin Zhou

Yiguang Wang

Xiaonan Huang

Xinpeng Ma

Xiumei Huang

Xiuquan Luo

Zachary R Moore

Erik Bey

Lifen Cao

Norased Nasongkla

John Pink

Yinjian Zhou

Ying Dong

Jimming Gao

Provided herein are block copolymers comprising a hydrophilic polymer segment and a hydrophobic polymer segment, wherein the hydrophilic polymer segment comprises a polymer selected from the group consisting of: poly(ethylene oxide) (PEO), poly(methacrylate phosphatidyl choline) (MPC), and polyvinylpyrrolidone (PVP), wherein the hydrophobic polymer segment comprises wherein R' is &#x2014;H or &#x2014;CH, wherein R is &#x2014;NRR, wherein Rand Rare alkyl groups, wherein Rand Rare the same or different, wherein Rand Rtogether have from 5 to 16 carbons, wherein Rand Rmay optionally join to form a ring, wherein n is 1 to about 10, and wherein x is about 20 to about 200 in total. Also provided are pH-sensitive micelle compositions for therapeutic and diagnostic applications.

Block copolymer and micelle compositions and methods of use thereof

The therapies described herein can be selectively lethal toward a variety of different cancer cell types and cancer conditions in a subject. The combination therapies described herein can be useful for the management, treatment, control, or adjunct treatment of diseases, where the selective legality is beneficial in chemotherapeutic therapy, particularly where the disease is accompanied by elevated levels of NQO1.

Tumor-selective combination therapy

Compositions comprising Formula (I) can be selectively lethal toward a variety of different cancer cell types. The compositions are useful for the management, treatment, control, or adjunct treatment of diseases, where the selective lethality is beneficial in chemotherapeutic therapy.

Compounds and anti-tumor NQO1 substrates

The therapies described herein can be selectively lethal toward a variety of different cancer cell types and cancer conditions in a subject. The combination therapies described herein can be useful for the management, treatment, control, or adjunct treatment of diseases, where the selective lethality is beneficial in chemotherapeutic therapy, particularly where the disease is accompanied by elevated levels of NQO1.

Disclosed herein are compounds comprising a polymer conjugated with a pH-sensitive prodrug of beta-lapachone, wherein the compound is capable of forming a micelle, and wherein the pH-sensitive prodrug comprises a pH-sensitive linker selected from the group consisting of: an aryl imine and an aliphatic imine. Also provided are micelles comprised of such polymer-prodrug conjugates. Further provided are methods for treating cancer with the micelles.

PH-sensitive compositions for delivery of beta lapachone and methods of use

Compounds of Formula (I) can be selectively lethal toward a variety of different cancer cell types. The compounds are useful for the management, treatment, control, or adjunct treatment of diseases, where the selective lethality is beneficial in chemotherapeutic therapy.

Disclosed herein are methods for determining whether an individual with cancer is suitable for a treatment with an NQO1 bioactivatable drug, predicting responsiveness of an individual with cancer to a treatment with an NQO1 bioactivatable drug, and treating an individual with cancer with an NQO1 bioactivatable drug composition.

Methods of treating cancer comprising targeting NQO1

In part, the present invention is directed to a system comprising a lapachone or a prodrug thereof and a polymer, such as a biocompatible and optionally biodegradable polymer, methods for treatment using the subject polymer compositions, and methods of making and using the same. In another part, the present invention includes inclusion complexes of a lapachone or a prodrug thereof and a cyclodextrin, preferably a &#x3b2;-cyclodextrin, such as hydroxypropyl &#x3b2;-cyclodextrin, e.g., to improve the solubility of the lapachone or prodrug thereof.

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Indianapolis, IN, United States of America

David A Boothman