A growing body of literature has examined the role of physical activity (PA) in modifying the effects of estrogen withdrawal on cardiovascular health in postmenopausal women, but the impact of PA on androgens is less clear. Changes in androgen concentrations following regular PA may improve cardiovascular health. This narrative review summarizes the literature assessing the impact of PA interventions on androgens in postmenopausal women. The association between changes in androgen concentrations and cardiovascular health following PA programs is also examined. Randomized controlled trials were included if they (i) implemented a PA program of any type and duration in postmenopausal women and (ii) measured changes in androgen concentrations. Following PA interventions, no changes in androstenedione, conflicting changes in dehydroepiandrosterone/dehydroepiandrosterone-sulfate, and increases in sex hormone-binding globulin concentrations were found. Total testosterone decreased following aerobic PA but increased after resistance training. Most aerobic PA interventions led to reductions in free testosterone. A combination of caloric restriction and/or fat loss enhanced the influence of PA on most androgens. Evidence exploring the relationship between changes in androgens and cardiovascular health indicators was scarce and inconsistent. PA has shown promise in modifying the concentrations of some androgens (free and total testosterone, sex hormone-binding globulin), and remains a well-known beneficial adjuvant option for postmenopausal women to manage their cardiovascular health. Fat loss influences the effect of PA on androgens, but the synergistic role of PA and androgens on cardiovascular health merits further examination. Many research gaps remain regarding the relationship between PA, androgens, and cardiovascular disease in postmenopausal women.