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The low- and middle-income countries (LMICs) are characterised by the highest burden of diseases and resource constraints. Thus, reforms imperative for responsive healthcare systems must be supported by context-appropriate evidence. However, lacunae persist with respect to the gap in terms of knowledge related to the level, barriers and inequities associated with effective healthcare coverage. The study was, thus, conducted to identify, describe, appraise and synthesise various bottlenecks impeding the trajectory towards effective coverage in LMICs. The study employed Preferred Reporting Items for Systematic Reviews and Meta-analysis (PRISMA) guidelines. A search of published articles was conducted on six electronic databases along with a manual and bibliographic search of grey literature. A gamut of peer-reviewed articles and technical reports evaluating the measure of—and barriers to—effective coverage in LMICs was included using an exhaustive set of inclusion criteria. A quality assessment of included studies was conducted using a standardised checklist adopted from the Joanna Briggs Institute. Further, selected studies were transcribed using data extraction and assessment templates adapted from the Cochrane Review Group, and a content analysis was performed within the Tanahashi framework of effective coverage. The search strategy retrieved 736 articles from the database, out of which 65 met the eligibility criterion. The majority of studies were characterised by cross-sectional and quantitative design, maternal and child health (MCH) interventions and availability/accessibility barriers. Analogously, most of the studies were conducted in the Sub-Saharan African region and were representative at the multi-country/national level. Conversely, the evidence on socio-economic determinants associated with effective health coverage was exiguous. The literature underscores supply-side constraints such as health workforce shortage, suboptimal structural quality and inefficient fund allocation as the most pronounced bottlenecks. Demand-side barriers, such as negative attitudes towards providers, lack of knowledge and community engagement, were also unravelled to exert an adverse impact on coverage. The study divulged that most of the literature on effective health coverage is underpinned by skewed representation. An evidence gap was found with respect to the studies from South-East Asian, Latin American and Caribbean LMICs and disaggregated administrative levels. Methodological deficiencies were also found in measurement metrics with respect to the assessment of a comprehensive package of services, equity, quality and robustness checks.