Spatz S, Rudnicka A, McDonald C J
Br J Dermatol. 1978 Apr;98(4):429-35. doi: 10.1111/j.1365-2133.1978.tb06537.x.
Mycophenolic acid (MPA) is a fermentation product of a penicillium mould which has shown antitumour acitivity in certain animal models. It blocks nucleic acid synthesis by interfering with the interconversions of inosine monophosphate (IMP), xanthine monophosphate (XMP) and guanine monophosphate (GMP) thereby inhibiting growth and/or replication of tumour cells. In vivo activity depends on the presence of a beta-glucuronidase which is abundant in the cell wall of epithelial tissues. Encouraged by results obtained in earlier clinical trials, we have studied 28 patients with psoriasis, 21 in double-blind fashion. A comparison of disease severity in patients before and after receiving MPA versus patients receiving placebo clearly showed the superiority of drug over placebo. The mean severity score of patients receiving MPA as an initial course of therapy improved by 56% versus 9% in patients receiving placebo. Patients receiving MPA after an initial course of placebo therapy showed improvement in their mean severity score averaging 86%. Those patients receiving placebo after an initial course of MPA showed worsening of their mean severity score averaging 70%. Overall, about 75% of MPA treated patients have shown good to excellent responses, and toxicity appears low. Evidence suggests that MPA may be very useful in treating severe psoriasis.
霉酚酸(MPA)是一种青霉菌的发酵产物,在某些动物模型中显示出抗肿瘤活性。它通过干扰肌苷单磷酸(IMP)、黄嘌呤单磷酸(XMP)和鸟嘌呤单磷酸(GMP)的相互转化来阻断核酸合成,从而抑制肿瘤细胞的生长和/或复制。体内活性取决于β-葡萄糖醛酸酶的存在,该酶在上皮组织的细胞壁中含量丰富。受早期临床试验结果的鼓舞,我们研究了28例银屑病患者,其中21例采用双盲方式。比较接受MPA治疗前后的患者与接受安慰剂治疗的患者的疾病严重程度,清楚地显示了药物优于安慰剂。作为初始治疗疗程接受MPA的患者的平均严重程度评分改善了56%,而接受安慰剂的患者为9%。在初始疗程接受安慰剂治疗后接受MPA的患者,其平均严重程度评分平均改善了86%。那些在初始疗程接受MPA后接受安慰剂的患者,其平均严重程度评分平均恶化了70%。总体而言,约75%接受MPA治疗的患者显示出良好至优异的反应,且毒性似乎较低。有证据表明,MPA可能对治疗重度银屑病非常有用。