IMPROVED ANTI-HIV THERAPY WITH P-GLYCOPROTEIN INHIBITORS

Award Information
Agency:
Department of Health and Human Services
Branch
n/a
Amount:
$100,011.00
Award Year:
2002
Program:
SBIR
Phase:
Phase I
Contract:
1R43AI051902-01
Award Id:
60487
Agency Tracking Number:
AI051902
Solicitation Year:
n/a
Solicitation Topic Code:
n/a
Solicitation Number:
n/a
Small Business Information
APOGEE BIOTECHNOLOGY CORPORATION, 245 CANDLEWYCK LN, HERSHEY, PA, 17033
Hubzone Owned:
N
Minority Owned:
N
Woman Owned:
N
Duns:
n/a
Principal Investigator:
KEVIN FRENCH
(717) 520-9674
KFRENCH@APOGEEBIOTECH.COM
Business Contact:
CHARLES SMITH
(717) 520-9674
APOBIOSCI@AOL.COM
Research Institution:
n/a
Abstract
Current treatment protocols for AIDS involve combinations of nucleoside analogs and HIV protease inhibitors, but are not successful in curing the disease. The drug transport protein, P-glycoprotein (Pgp) effluxes a wide variety of drugs, including all FDA-approved protease inhibitors. A growing body of evidence indicates that inhibiting Pgp will enhance AIDS chemotherapy by improving the delivery of protease inhibitors to the brain, improving their oral bioavailability, and enhancing the perinatal exposure of the fetus to these drugs. The closely related transporter MRP1 is expressed by all normal tissues, so that inhibition of this protein increases drug toxicity in non-target tissues. The goal of this project is to develop new compounds that selectively inhibit Pgp to be used in combination with protease inhibitors in the therapy and prevention of AIDS. Compounds PGP- 4008 and PGP-3005 are structurally novel compounds that demonstrate excellent antagonism of Pgp in vitro, without affecting MRP1 activity. We will examine the potential utility of these compounds by determining their effects on 1) Pgp-mediated transport of protease inhibitors in vitro; and 2) the pharmacokinetics and biodistribution of protease inhibitors in vivo. These studies should allow a critical evaluation of the potential utility of these novel compounds in the improvement of AIDS chemotherapy.

* information listed above is at the time of submission.

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