Background: Substance use trends are complex; they often rapidly evolve and necessitate an intersectional approach in research, service, and policy making. Current and emerging digital tools related to substance use are promising but also create a range of challenges and opportunities. Objective: This paper reports on a backcasting exercise aimed at the development of a roadmap that identifies values, challenges, facilitators, and milestones to achieve optimal use of digital tools in the substance use field by 2030. Methods: A backcasting exercise method was adopted, wherein the core elements are identifying key values, challenges, facilitators, milestones, cornerstones and a current, desired, and future scenario. A structured approach was used by means of (1) an Open Science Framework page as a web-based collaborative working space and (2) key stakeholders’ collaborative engagement during the 2022 Lisbon Addiction Conference. Results: The identified key values were digital rights, evidence-based tools, user-friendliness, accessibility and availability, and person-centeredness. The key challenges identified were ethical funding, regulations, commercialization, best practice models, digital literacy, and access or reach. The key facilitators identified were scientific research, interoperable infrastructure and a culture of innovation, expertise, ethical funding, user-friendly designs, and digital rights and regulations. A range of milestones were identified. The overarching identified cornerstones consisted of creating ethical frameworks, increasing access to digital tools, and continuous trend analysis. Conclusions: The use of digital tools in the field of substance use is linked to a range of risks and opportunities that need to be managed. The current trajectories of the use of such tools are heavily influenced by large multinational for-profit companies with relatively little involvement of key stakeholders such as people who use drugs, service providers, and researchers. The current funding models are problematic and lack the necessary flexibility associated with best practice business approaches such as lean and agile principles to design and execute customer discovery methods. Accessibility and availability, digital rights, user-friendly design, and person-focused approaches should be at the forefront in the further development of digital tools. Global legislative and technical infrastructures by means of a global action plan and strategy are necessary and should include ethical frameworks, accessibility of digital tools for substance use, and continuous trend analysis as cornerstones.