OBJECTIVES:  This study summarizes the uptake rates of chemoprevention drugs among postmenopausal women at high risk of being diagnosed with breast cancer. METHODS: A systematic literature review was conducted for articles published between January 1996 and October 2016, using databases Medline (Ovid), and PubMed (NLM). Chemoprevention was defined as the use of tamoxifen or raloxifene or exemestane. The eligibility criteria considered in this study were, post-menopausal women at a high risk of breast cancer. Only articles published in English from peer reviewed journals were included in this review. Two reviewers independently screened a random sample of 25 titles and abstracts. A moderate agreement (Cohen's κ = 0.65) was obtained. The elements of PICOS were reviewed within each article. RESULTS: A total of 10 full text articles were included in this review. The overall decision to initiate chemoprevention ranged from 4.7% - 47.0% affirmative in the articles included in the review. An average of 70% women declined chemoprevention. Only one study measured the uptake of chemoprevention immediately after an intervention, while nine studies measured the uptake after a follow up of 3-14 months. The presence of a control group indicates a stronger study design and only three studies had a control group. The chemoprevention uptake rates were about 10% on an average in the target population. The most common reasons for refusal of chemoprevention were chemoprevention side effect profile and the duration of therapy. CONCLUSIONS:  Chemoprevention uptake rates were low among post-menopausal women with high risk of breast cancer. Since risk of adverse events and duration of therapy were the most cited reasons of low chemoprevention uptake, appropriate patient counselling with focus on chemoprevention risk-benefit profile may be designed and implemented.