Stampidine

Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLV_IIIB (B-envelope subtype) and primary clinical isolates with IC₅₀s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC₅₀s of 8.7 nM and 11.2 nM, respectively^[1]. IC50 & Target: IC50: 1 nM (HTLV_IIIB), 2 nM (primary clinical isolates), 8.7 nM (NRTI-resistant primary clinical isolates), 11.2 nM (NRTI-resistant primary clinical isolates)^[1] In Vitro: Stampidine (7.8-1,000 μM; 24 hours) is not cytotoxic to genital tract epithelial cells^[2].
Stampidine has no effect on sperm motility in cervical mucus^[2].
In Vivo: Stampidine (50-100 mg/kg; p.o.) exhibits potent antiretroviral activity in chronically feline immunodeficiency virus (FIV)-infected cats^[3].
Stampidine (100 mg/kg; p.o.) shows the average plasma C_max, AUC, half-life (t_1/2), and mean residence time (MRT) values of 15.4 μM, 23.1 μM?h, 108.6 min and 119.4 min, respectively, in dogs^[4].
Stampidine does not cause anemia, thrombocytopenia, neutropenia, or lymphopenia suggestive of hematologic toxicity, elevations of BUN or creatinine or electrolyte disturbances suggestive of renal toxicity or metabolic abnormalities, elevations of ALT, AST, Alk in adult beagle dogs^[4].