Patton Dorothy L, Cosgrove Sweeney Yvonne T, Paul Kathleen J
Department of Obstetrics and Gynecology, Box 356460, University of Washington, Seattle, WA 98195-6460, USA.
Sex Transm Dis. 2008 Oct;35(10):889-97. doi: 10.1097/OLQ.0b013e31817dfdb8.
The development of topical microbicides represents a new and exciting field in the prevention of sexually transmitted diseases, and it is especially important that candidate products undergo rigorous preclinical safety and efficacy testing before advancing to clinical trials.
We have developed a standardized protocol for preclinical vaginal safety and efficacy assessment of topical microbicide candidates in a nonhuman primate model. Over 7 years of funding under an NIH contract, we evaluated a total of 28 test compounds for vaginal safety (via colposcopy, vaginal pH, and microflora) and 9 compounds for efficacy against cervical chlamydial infection. In this article, we describe our methods in detail and summarize our results, particularly noting the ability of our model to distinguish products with deleterious effects on the cervicovaginal environment. We also outline the specific criteria used to determine which products should move into efficacy trials and which should be recommended for reformulation to the manufacturer.
Overall, we noted acceptable safety profiles for 24 of 28 candidate products. Common findings included a transient decrease in vaginal pH, petechiae, and mild erythema. Four products were associated with significant adverse colposcopic findings including blisters, epithelial abrasions, and friability; all 4 products were successfully reformulated and showed acceptable safety profiles at lower concentrations. No products showed complete protection against cervical chlamydial infection.
The macaque preclinical safety and efficacy model is critical to maintaining the pace of topical microbicide development, which could ultimately offer a significant opportunity for intervention in the global HIV/AIDS epidemic.
局部用杀微生物剂的研发是预防性传播疾病领域一个全新且令人兴奋的方向,尤为重要的是,候选产品在进入临床试验之前需经过严格的临床前安全性和有效性测试。
我们已制定了一项标准化方案,用于在非人灵长类动物模型中对局部用杀微生物剂候选产品进行临床前阴道安全性和有效性评估。在国立卫生研究院(NIH)一项合同的7年多资助下,我们总共评估了28种测试化合物的阴道安全性(通过阴道镜检查、阴道pH值和微生物群落)以及9种化合物对宫颈衣原体感染的有效性。在本文中,我们详细描述了我们的方法并总结了结果,特别指出了我们的模型区分对宫颈阴道环境有有害影响的产品的能力。我们还概述了用于确定哪些产品应进入有效性试验以及哪些产品应建议制造商重新配方的具体标准。
总体而言,我们注意到28种候选产品中有24种具有可接受的安全性概况。常见的发现包括阴道pH值短暂下降、瘀点和轻度红斑。有4种产品与明显的阴道镜检查不良发现相关,包括水疱、上皮擦伤和脆性增加;所有4种产品均成功重新配方,且在较低浓度下显示出可接受的安全性概况。没有产品对宫颈衣原体感染显示出完全保护作用。
猕猴临床前安全性和有效性模型对于维持局部用杀微生物剂的研发速度至关重要,这最终可能为全球艾滋病毒/艾滋病流行的干预提供重大机会。