USA flag logo/image

An Official Website of the United States Government

Development of Natural Product as Antimalarial Agent

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
85274
Program Year/Program:
2007 / SBIR
Agency Tracking Number:
AI072781
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
RADIX PHARMACEUTICALS, INC.
13303 Sunny Brooke Place Room 101 Potomac, MD -
View profile »
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 1
Fiscal Year: 2007
Title: Development of Natural Product as Antimalarial Agent
Agency: HHS
Contract: 1R43AI072781-01
Award Amount: $299,880.00
 

Abstract:

DESCRIPTION (provided by applicant): The long-term goal of this project is to develop a new drug (new chemical entity [NCE]) that is inexpensive, orally active, non-toxic and can provide cure for P. falciparum malaria. Radix Pharmaceuticals has isolated an d purified two natural products from the roots and rhizomes of Nardostachys chinensis Batalin. The chemical structures of both compounds were determined. These compounds showed equally potent inhibitory activity against both chloroquine sensitive malaria s train (D-6) and chloroquine resistant malaria strain (W-2). The IC50's (concentration of compound that affords 50% of inhibition) were superior to the positive controls, chloroquine and mefloquine. These compounds also demonstrated low toxicity in human ad ult liver epithelial cells and freshly isolated rat hepatocytes. Additionally, in silico modeling has confirmed that these compounds possess desirable ADME (adsorption, distribution, metabolism, and excretion) characteristics and good oral bioavailability. These compounds possess the potential to interfere hemozoin synthesis, an indispensable process for the malaria parasite. Based on these preliminary studies, the overall goal of this Phase I project is to establish pre-clinical profiles for the candidates . Under Phase I support, we will perform the scale up isolation and purification of these compounds and begin pre-clinical studies in rodent models to obtain toxicity and efficacy data. The following interactive studies will be performed to obtain rodent p re-clinical profiles efficiently and effectively: (i) The two natural products will be isolated and purified in a larger scale (1-2 kg per compound). (ii) Compounds will be tested in rodent models to obtain acute and sub-acute toxicity, fetotoxicity, anore ctic toxicity, and neurotoxicity information. (iii) Antimalarial efficacy data will be obtained in immunocompromised BXN mice infected with human malaria strains and male Swiss albino mice infected with rodent malaria strain P. berghei. On completion of th e Phase I studies, compound(s) that are orally active and possess good therapeutic index will be selected for further development in Phase II. The successful completion of rodent pre-clinical studies will enable Radix Pharmaceuticals to raise additional fu nding and attract a commercial partner to push the drug candidate to clinical stage. The efforts in Phase II would include pre-clinical studies (pharmacokinetics, toxicity, and efficacy) in Rhesus monkey, followed by GMP manufacturing and GLP evaluation. I nvestigational new drug (IND) application will then be filed with FDA.

Principal Investigator:

Shuren Zhu
3016753714
SHUREN.ZHU@GMAIL.COM

Business Contact:

Shuren Xhu
shuren.zhu@gmail.com
Small Business Information at Submission:

RADIX PHARMACEUTICALS, INC.
13303 Sunny Brooke Place Room 101 Potomac, MD 20854

EIN/Tax ID: 770619931
DUNS: N/A
Number of Employees: N/A
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No