Gender-transformative health promotion addresses the reciprocal transactions between the socio-cultural contexts that shape gender-based values and the gender-normative behaviors and health experiences of individuals. A scoping review was conducted to (a) highlight how, when and under what circumstances gender-transformative health promotion is applied in practice, and (b) critically assess the operationalization of gender-transformative health promotion principles in practice to develop a clearer understanding of potential barriers (both conceptual and practical) that may detract from the broader employment of gender-transformative health promotion as a mainstream programming approach. Specific recommendations, based on the findings of this review, are made in an effort to further the operationalization of gender-transformative health promotion as a mainstream health promotion approach, globally.