<p>Anemia is a global health problem with diverse etiologies and significant impacts on morbidity and mortality. Despite the widespread use of antianemic drugs, therapeutic outcomes vary considerably between male and female. Biological sex and gender roles influence anemia risk, symptom presentation, drug metabolism, tolerability, and response, yet these dimensions are often underexplored in clinical practice and research. This review was undertaken to synthesize current knowledge on sex- and gender-specific differences in anemia and antianemic therapy. The rationale lies in the growing recognition that precision medicine requires integration of sex and gender into pharmacological and clinical frameworks, moving beyond uniform treatment strategies. The review demonstrates that sex hormones, baseline physiology, and gendered behaviors collectively shape anemia risk and therapeutic trajectories. Females often present earlier with symptoms, experience higher rates of adverse drug reactions (ADR), and respond differently to iron and erythropoiesis-stimulating agent (ESA) therapy, while males show delayed symptom recognition, require higher ESA doses, and underreport side effects. Drug metabolism stages—absorption, distribution, and elimination—also diverge via sex, influencing exposure and efficacy. This review provides a comprehensive synthesis of sex- and gender-specific differences in anemia and antianemic therapy. The rationale for this work is to inform clinicians, researchers, and policymakers that integrating sex and gender into diagnostic thresholds, dosing strategies, monitoring protocols, and patient counseling is essential to optimize outcomes, reduce adverse events, and advance equity in anemia management.</p>