Objective: To investigate whether tamoxifen inhibits hepatic VLDL secretion.
Design: Eight healthy, normolipidemic women (BMI 23.7±1.2 kg/m2, age 64.4±2.2 years) were studied at baseline and after 2 weeks of tamoxifen (20 mg/d) treatment. We quantified apolipoprotein B (apoB), the structural protein of VLDL particles, by stable isotope 2H3-leucine turnover technique using steady state methodology. The enrichment of labelled leucine into VLDL-apoB was measured using gas chromatography mass spectroscopy. VLDL-apoB fractional catabolic rate (FCR) was determined using a multicompartment model. VLDL-apoB secretion was estimated as the product of FCR and VLDL-apoB concentration. Circulating levels of IGF-I, FFA, and TG were measured at baseline and following tamoxifen treatment.
Results: At baseline, mean VLDL-apoB concentration was 94±19.8 mg/L. VLDL-apoB FCR and secretion were 3.7±0.6 pools/d and 4.6±1.1 mg/kg/d, respectively. Tamoxifen significantly (p<0.05) lowered VLDL-apoB concentration and secretion by 27.6±7.8% and 30.7±9.8%, respectively. Tamoxifen also significantly lowered circulating IGF-I concentration (14.8±5.3%; p<0.05). There were no significant changes in plasma TG and FFA levels following tamoxifen treatment.
Summary: Tamoxifen significantly lowered VLDL-apoB concentration as a consequence of a lower production rate. Tamoxifen significantly reduced IGF-I, a hepatic marker of GH action.
Conclusion: The suppression of GH-IGF-I axis by tamoxifen is associated with lower rates of VLDL-apoB secretion. Diminished hepatic VLDL secretion may contribute to the development of fatty liver during tamoxifen therapy.
Supported by the Princess Alexandra Hospital Research Support Scheme and the NHMRC Australia.