Cheng L, Hostetler K Y, Chaidhawangul S, Gardner M F, Ozerdem U, Bergeron-Lynn G, Mach-Hofacre B, Mueller A J, Severson G M, Freeman W R
Shiley Eye Center, University of California-San Diego, La Jolla 92093-0946, USA.
Retina. 1999;19(4):325-31. doi: 10.1097/00006982-199907000-00010.
To evaluate the clinical treatment efficacy of a long-lasting intravitreous injectable anti-cytomegalovirus (CMV) liposomal drug, 1-O-octadecyl-sn-glycerol-3-phosphonoformate (ODG-PFA).
Sixty-four pigmented rabbits were used for evaluation of the potency and duration of action of ODG-PFA after intravitreal injection using a herpes simplex virus (HSV)-1 retinitis model. For the potency evaluation, liposomal ODG-PFA was injected into rabbit vitreous at the same time that HSV-1 virus was inoculated onto the retina (simultaneous treatment). For the duration evaluation, ODG-PFA was injected days or weeks before inoculation (pretreatment). Retinitis was clinically graded by indirect ophthalmoscopy, and the retinitis scores were compared across the treatment and control groups.
Simultaneous treatment study revealed that ODG-PFA was much more potent than its parent compound, foscarnet (P = 0.0027). Pretreatment study indicated that ODG-PFA possesses a much longer antiviral effect (at least 2 weeks) than foscarnet after a single intravitreal injection.
Liposomal ODG-PFA is a potent long-lasting intravitreal injectable antiviral compound that may be an ideal alternative for treatment of CMV retinitis in patients with acquired immunodeficiency syndrome.
评估一种长效玻璃体内注射抗巨细胞病毒（CMV）脂质体药物1-O-十八烷基-sn-甘油-3-膦甲酸（ODG-PFA）的临床治疗效果。
使用单纯疱疹病毒（HSV）-1视网膜病变模型，对64只有色家兔进行玻璃体内注射ODG-PFA后的效力和作用持续时间评估。为进行效力评估，在将HSV-1病毒接种到视网膜的同时，将脂质体ODG-PFA注射到家兔玻璃体中（同步治疗）。为进行持续时间评估，在接种前数天或数周注射ODG-PFA（预处理）。通过间接检眼镜对视网膜病变进行临床分级，并比较治疗组和对照组的视网膜病变评分。
同步治疗研究表明，ODG-PFA比其母体化合物膦甲酸钠的效力更强（P = 0.0027）。预处理研究表明，单次玻璃体内注射后，ODG-PFA的抗病毒作用比膦甲酸钠长得多（至少2周）。
脂质体ODG-PFA是一种强效的长效玻璃体内注射抗病毒化合物，可能是治疗获得性免疫缺陷综合征患者CMV视网膜炎的理想替代药物。
