College of Medicine and Health, University of Exeter, Exeter, Devon EX2 5DW, UK.
GlaxoSmithKline, Collegeville, PA 19426, USA.
Hum Mol Genet. 2023 Jan 13;32(3):496-505. doi: 10.1093/hmg/ddac215.
Prolyl hydroxylase (PHD) inhibitors are in clinical development for anaemia in chronic kidney disease. Epidemiological studies have reported conflicting results regarding safety of long-term therapeutic haemoglobin (Hgb) rises through PHD inhibition on risk of cardiovascular disease. Genetic variation in genes encoding PHDs can be used as partial proxies to investigate the potential effects of long-term Hgb rises. We used Mendelian randomization to investigate the effect of long-term Hgb level rises through genetically proxied PHD inhibition on coronary artery disease (CAD: 60 801 cases; 123 504 controls), myocardial infarction (MI: 42 561 cases; 123 504 controls) or stroke (40 585 cases; 406 111 controls). To further characterize long-term effects of Hgb level rises, we performed a phenome-wide association study (PheWAS) in up to 451 099 UK Biobank individuals. Genetically proxied therapeutic PHD inhibition, equivalent to a 1.00 g/dl increase in Hgb levels, was not associated (at P < 0.05) with increased odds of CAD; odd ratio (OR) [95% confidence intervals (CI)] = 1.06 (0.84, 1.35), MI [OR (95% CI) = 1.02 (0.79, 1.33)] or stroke [OR (95% CI) = 0.91 (0.66, 1.24)]. PheWAS revealed associations with blood related phenotypes consistent with EGLN's role, relevant kidney- and liver-related biomarkers like estimated glomerular filtration rate and microalbuminuria, and non-alcoholic fatty liver disease (Bonferroni-adjusted P < 5.42E-05) but these were not clinically meaningful. These findings suggest that long-term alterations in Hgb through PHD inhibition are unlikely to substantially increase cardiovascular disease risk; using large disease genome-wide association study data, we could exclude ORs of 1.35 for cardiovascular risk with a 1.00 g/dl increase in Hgb.
脯氨酰羟化酶(PHD)抑制剂正在开发用于治疗慢性肾脏病的贫血。流行病学研究报告称,通过 PHD 抑制长期治疗性血红蛋白(Hgb)升高对心血管疾病风险的安全性结果存在矛盾。编码 PHD 的基因的遗传变异可用作部分替代物来研究长期 Hgb 升高的潜在影响。我们使用孟德尔随机化来研究通过遗传上替代 PHD 抑制长期 Hgb 水平升高对冠状动脉疾病(CAD:60801 例;123504 例对照)、心肌梗死(MI:42561 例;123504 例对照)或中风(40585 例;406111 例对照)的影响。为了进一步描述 Hgb 水平升高的长期影响,我们在多达 451099 名英国生物库个体中进行了表型全基因组关联研究(PheWAS)。相当于 Hgb 水平升高 1.00g/dl 的治疗性 PHD 抑制的遗传替代物与 CAD 发生几率的增加(P<0.05)无关;比值比(OR)[95%置信区间(CI)] =1.06(0.84,1.35)、MI [OR(95%CI)=1.02(0.79,1.33)]或中风[OR(95%CI)=0.91(0.66,1.24)]。PheWAS 揭示了与血液相关表型的关联,这些表型与 EGLN 的作用一致,与肾脏和肝脏相关的生物标志物如估计肾小球滤过率和微量白蛋白尿有关,与非酒精性脂肪性肝病有关(Bonferroni 校正的 P<5.42E-05),但这些没有临床意义。这些发现表明,通过 PHD 抑制长期改变 Hgb 不太可能显著增加心血管疾病风险;使用大型疾病全基因组关联研究数据,我们可以排除 Hgb 升高 1.00g/dl 时心血管风险的 OR 为 1.35。