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Purpose: This paper examined the challenges to transforming library and information services (LIS) for effective service delivery in three academic libraries in Imo state. Design/Methodology/Approach: The survey method was adopted for this study with questionnaire as the instrument for data collection. The target population comprises of library and information science professionals in three academic libraries in Imo State Nigeria. Availability and purposive sampling techniques was used to select the participant. The generated data were analysed using descriptive statistics, frequency counts and percentage was well illustrated. Findings: The findings revealed the challenges to effective transformation of academic libraries in the 21st century to include: poor funding, indifferent attitudes of library managers, absence of well-defined and uniform library policies and non-compliance with the demands of ICT. Transformation of library and information centres is all about improving product and services offered in Nigerian libraries to meet the needs and demands of knowledge society. Among other benefits, it enhances the capability of libraries to contribute positively to the reality of knowledge society in contemporary Nigerian society. Practical Implication: retraining of LIS practitioners; provision of adequate funding; provision of relevant and functional ICT facilities relevant to the Nigerian libraries and formulation of viable library policies are practical steps that can be taken to transform Nigerian Libraries by relevant bodies such as Librarians’ Registration Council (LRCN), Nigerian Library Association (NLA) and National Association of Library and Information Science Educationist (NALISE). Originality/Value: transforming academic libraries enhances the capability of libraries to contribute positively to the reality of knowledge society in contemporary Nigerian society. The paper has empirically established that there are a lot of challenges to transformation of library service for effective service delivery in the 21st century.