Among all the 63 CHMs, formulae Gui Zhi Fu Ling Wan (GZ) and Chia Wei Hsiao Yao San (CW) exhibited significant inhibitions on hOAT1-mediated [3H]-PAH uptake in vitro and PAH clearance and net secretion in vivo. The gene discussed is SLC22A6; the disease is pulmonary arterial hypertension.