National Genetics Education and Development Centre, Morris House, C/o Birmingham Women's Hospital, Edgbaston, Birmingham, United Kingdom.
Br J Clin Pharmacol. 2011 Jul;72(1):6-17. doi: 10.1111/j.1365-2125.2011.03929.x.
The translational path from pharmacological insight to effective therapy can be a long one. We aim to describe the management of Marfan syndrome as a case-example of how pharmacological and genomic insights can contribute to improved therapy. We undertook a literature search for studies of Marfan syndrome, to identify milestones in description, understanding and therapy of the syndrome. From the studies retrieved we then weaved an evidence-based description of progress. Marfan syndrome shows considerable heterogeneity in clinical presentation. It relies on defined clinical criteria with confirmation based on FBN1 mutation testing. Surgical advances have prolonged life in Marfan syndrome. First-line prophylaxis of complications with β-adrenoceptor blockers became established on the basis that reduction of aortic pressure and heart rate would help. Over-activity of proteinases, first suggested in 1980, has since been confirmed by evidence of over-expression of matrix metalloproteinases (MMP), notably MMP-2 and MMP-9. The search for MMP inhibitors led to the evaluation of doxycycline, and both animal studies and small trials, provided early evidence that this widely used antimicrobial agent was useful. Identification of the importance of TGF-β led to evaluation of angiotensin II type I receptor (AT(1) R) blockers with highly promising results. Combination prophylactic therapy would appear rational. Pharmacological and genomic research has provided good evidence that therapy with losartan and doxycycline would prevent the aortic complications of Marfan syndrome. If on-going well designed trials confirm their efficacy, the outlook for Marfan syndrome patients would be improved considerably.
从药理学见解到有效治疗的转化过程可能是漫长的。我们旨在以马凡综合征的管理为例,描述药理学和基因组学见解如何有助于改善治疗。我们对马凡综合征的研究进行了文献检索,以确定该综合征的描述、理解和治疗的里程碑。从检索到的研究中,我们编织了一个基于证据的进展描述。马凡综合征在临床表现上存在很大的异质性。它依赖于明确的临床标准,并通过 FBN1 突变测试进行确认。外科手术的进步延长了马凡综合征患者的寿命。β-肾上腺素能受体阻滞剂作为预防并发症的一线药物,其理论依据是降低主动脉压力和心率有助于预防并发症,该理论已得到确立。1980 年首次提出的蛋白酶过度活跃的观点,后来通过证实基质金属蛋白酶(MMP),特别是 MMP-2 和 MMP-9 的过度表达得到了证实。寻找 MMP 抑制剂导致了强力霉素的评估,动物研究和小型试验都提供了早期证据,证明这种广泛使用的抗菌剂是有用的。TGF-β 重要性的确定导致了对血管紧张素 II 型 1 型受体(AT(1)R)阻滞剂的评估,结果非常有前景。联合预防性治疗似乎是合理的。药理学和基因组学研究提供了充分的证据,表明使用氯沙坦和强力霉素治疗可以预防马凡综合征的主动脉并发症。如果正在进行的精心设计的试验证实它们的疗效,马凡综合征患者的前景将得到极大改善。