A. ARV Activity of Stampidine in Acutely HIV-Infected Hu-PBL-SCID Mice+

Stampidine Dose Level
(mg/kg/d)

HIV-NASBA+

Histopathology (Toxic lesions)

Spleen P-value (Chi-square value) Peritoneal Lavage P-value (Chi-square value)
50 4/10 0.007 (7.2) 7/10 0.06 (3.5) ND
100 7/20 0.0002 (14.2) 12/20 0.002 (9.7) 0/10
200 10/30 <0.0001 (19.2) 17/28 0.0008 (11.2) 0/19
400 1/19 <0.0001(36.9) 2/18 <0.0001 (41.3) 0/19
Vehicle 35/42* ----- 40/43* ----- ND
 

B. ARV Activity of Stampidine in Chronically FIV-Infected Cats++

Stampidine Dose Level (mg/kg xbid)

Log10 FIV-load in PBMC

Log Reduction of FIV-load

Average Log Reduction Mean±SE (P-value)

Pre Post
50 (#1) 1 0 1 1.33±0.33 (P=0.008)
50 (#2) 2 0 1
50 (#3) 1 0 1
100 (#1) 2 1 1 1.25±0.25 (P=0.002)
100 (#2) 3 2 2
100 (#3) 2 0 1
100 (#4) 2 1 1
Placebo (#1) 1 2 -1 -2.0±0.6
Placebo (#2) 2 5 -2
Placebo (#3) 2 4 -3
+The anti-HIV activity of Stampidine against BR/92/019, a genotypically and phenotypically NRTI-resistant HIV-1 isolate was evaluated in Hu-PBL-SCID mice. Stampidine was administered via gavage or by addition to the food starting on the day of virus inoculation. Throughout the experimental period, mice were monitored daily for morbidity and mortality. Two weeks after virus inoculation, Hu-PBL-SCID mice were electively killed, and their peritoneal lavage cells as well as spleen cells were examined for evidence of HIV-1 infection by NASBA. At the time of necropsy, 18 selected tissues were submitted for standard hispathological examinations.
* Log10 HIV-load (Mean±SE): 4.4±1.0
++The anti-retroviral activity of Stampidine was examined in chronically FIV-infected shorthair domestic cats, as described in Materials and Methods. The FIV load of PBMCs from Stampidine- treated vs. placebo-treated cats was determined in standard PBMC co-culture experiments, as previously reported (30).
Table 2: Anti-Retroviral Activity of Stampidine in HIV-Infected Hu-PBL-SCID Mice and FIV Infected Shorthair Domestic Cats.