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Long Circulating Liposomal Camptothecins CAP and EAP

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
55610
Program Year/Program:
2001 / STTR
Agency Tracking Number:
2R42CA075761-02
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
TIGEN PHARMACEUTICALS
UNIVERSITY OF KENTUCKY ASTECC BLDG, RM 346 LEXINGTON, KY 40506
View profile »
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 1
Fiscal Year: 2001
Title: Long Circulating Liposomal Camptothecins CAP and EAP
Agency: HHS
Contract: PHS2001-2
Award Amount: $0.00
 

Abstract:

DESCRIPTION (provided by applicant): Based on the extensive data generated during the phase I portion of our studies, there is sufficient and compelling information to support the further development of the highly lipophilic and blood-stable topoisomerase inhibitor, DB-67. In part, the pre-clinical and clinical evaluation of DB-67 is currently being supported by the NCI through the RAID program; the RAID program studies focus on the non-targeted, liposomal delivery of DB-67, in which DB-67 is formulated in the bilayer of the liposome vesicle. This phase II STTR proposal focuses on the liposomal delivery of core-loaded DB-67 prodrug esters. Liposomal core-loading is a feature of FDA-approved liposomal products such as Doxil and DaunoXome and tumor-targeting has been documented for these formulations. The phase II studies proposed below focus on a novel approach allowing for the liposomal delivery of core-loaded DB-67 prodrug esters, which will permit tumor targeting and, accordingly, effect lower systemic toxicity to the DB-67 agent. The chemistry of the liposomal carriers will be adjusted in order to optimize the following: drug retention in the particle in circulation; particle targeting to the tumor by passive mechanisms; the controlled, slow and continuous release of the active, S-phase specific agent at the tumor site resulting in optimal anticancer activity with minimal systemic toxicity. Thus, the specific aims are as follows: 1) scale-up synthesis of chemically-activated pro-drug (CAP) and enzymatically-activated pro-drug (EAP) esters of DB-67 which actively load info the aqueous core of liposomes and 2) liposomal core-loading of CAP and EAP DB-67 esters and optimization of drug retention; and 3) in vitro and in vivo evaluation of liposomal core-loading of CAP and EAP DB-67 esters. Ultimately, we will seek formulation(s) that display optimized drug retention and in vivo and in vitro performance. PROPOSED COMMERCIAL APPLICATION: Not Available

Principal Investigator:

Thomas G. Burke
8592572300
TGBURKE@UKY.EDU

Business Contact:

Thomas g burke
6062572300
TGBURKE@POP.UKY.EDU
Small Business Information at Submission:

TIGEN PHARMACEUTICALS
UNIVERSITY OF KENTUCKY ASTECC BLDG, RM 346 LEXINGTON, KY 40506

EIN/Tax ID: 611324772
DUNS: N/A
Number of Employees: N/A
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
Research Institution Information:
NEW YORK UNIVERSITY OF MEDICINE
NEW YORK UNIVERSITY OF MEDICINE
NEW YORK, NY 12101
RI Type: Nonprofit college or university