Yamamoto A, Sudo H, Endo A
Atherosclerosis. 1980 Mar;35(3):259-66. doi: 10.1016/0021-9150(80)90124-0.
ML-236B, a competitive inhibitor of 3-hydroxy-3-methylglutaryl CoA reductase, was administered to 11 patients with primary hypercholesterolemia. After 4--8 weeks of drug treatment at doses of 50--150 mg/day, serum cholesterol levels were reduced by 11--37% (27% on average) in cases of heterozygous familial hypercholesterolemia and combined hyperlipidemia. A marked reduction in tuberous xanthomas was noticed in a homozygous case of familial hypercholesterolemia, but here the drug was less effective in reducing the serum cholesterol level and a higher dose was required for treatment. Softening of Achilles tendon xantomas was observed in a case of combined hyperlipidemia.
ML-236B是3-羟基-3-甲基戊二酰辅酶A还原酶的竞争性抑制剂，对11例原发性高胆固醇血症患者进行了给药治疗。在以50-150毫克/天的剂量进行4-8周的药物治疗后，杂合子家族性高胆固醇血症和混合性高脂血症患者的血清胆固醇水平降低了11%-37%（平均27%）。在一例纯合子家族性高胆固醇血症患者中，结节性黄瘤明显减少，但在此病例中，该药物降低血清胆固醇水平的效果较差，需要更高剂量进行治疗。在一例混合性高脂血症患者中，观察到跟腱黄瘤软化。
