Abacavir monosulfate is an orally active, competitive nucleoside reverse transcriptase inhibitor that effectively inhibits HIV replication. Additionally, it exhibits anticancer properties in prostate cancer cell lines, and has the ability to penetrate the blood-brain-barrier and suppress telomerase activity [1] [2] [3].

Abacavir (15 and 150 μM, 0-120 h) monosulfate inhibits cell growth, affects cell cycle progression, induces senescence and modulates LINE-1 mRNA expression in prostate cancer cell lines [1]. Abacavir (15 and 150 μM, 18 h) monosulfate significantly reduces cell migration and inhibits cell invasion [1]. Abacavir monsulfate induces fat apoptosis [4]. Cell Proliferation Assay [1] Cell Line: PC3, LNCaP and WI-38 Concentration: 15 and 150 μM Incubation Time: 0, 24, 48, 72 and 96 h Result: Showed a dose-dependent growth inhibition on PC3 and LNCaP. Cell Cycle Analysis [1] Cell Line: PC3 and LNCaP Concentration: 150 μM Incubation Time: 0, 18, 24, 48, 72, 96 and 120 h Result: Caused a very high accumulation of cells in S phase in PC3 and LNCaP cells, and G2/M phase increment was observed in PC3 cells. Cell Migration Assay [1] Cell Line: PC3 and LNCaP Concentration: 15 and 150 μM Incubation Time: 18 h Result: Significantly reduced cell migration. Cell Invasion Assay [1] Cell Line: PC3 and LNCaP Concentration: 15 and 150 μM Incubation Time: 18 h Result: Significantly inhibited cell invision.

Abacavir (0-7.5 μg/mL, 100 μL, intrascrotal administration; 100 and 200 mg/kg, p.o.; 4 h) monosulfate dose-dependently promoted thrombus formation [2]. Abacavir (50 mg/kg/d; i.p.; 14 days) monosulfate with 0.1 mg/kg/d Decitabine enhances survival of high-risk medulloblastoma-bearing mice [3]. Animal Model: Male mice (9-weeks old, 22-30 g) - wild-type (WT) C57BL/6 or homozygous knockout (P2rx7 KO, B6.129P2-P2rx7 tm1Gab /J) [2] Dosage: 2.5, 5 and 7.5 μg/mL, 100 μL or 100 and 200 mg/kg Administration: Intrascrotal or oral administration for 4 h Result: Dose-dependently promoted thrombus formation. Animal Model: NSG TM mice, patient-derived xenograft (PDX) cells of non-WNT/non-SHH, Group 3 and of SHH/ TP53-mutated medulloblastoma [3] Dosage: 50 mg/kg/d with 0.1 mg/kg/d Decitabine Administration: Intraperitoneal injection, daily for 14 days Result: Inhibited tumor growth and enhanced mouse survival.