While psychoactive drugs such as ketamine and psilocybin have been researched extensively in the past decades, scientific interest in ayahuasca has just started to grow, due to its potential therapeutic benefits. Beyond its traditional indigenous and mestizo use in the Amazon, ayahuasca is currently spreading all over the world as an alternative plant medicine in various ritualistic contexts. This rapid dissemination coincides with the observational evidence that ayahuasca facilitates transformational processes with beneficial health outcomes. However, more empirical research is needed to move beyond anecdotal evidence and further verify therapeutic efficacy and biomechanisms of ayahuasca under controlled conditions. The objective of this chapter is to outline future possibilities of ayahuasca-assisted therapies based on the biomedical literature on psychedelics and other contexts in which ayahuasca is used to support health and wellbeing. First, psychedelic medicines will be contrasted with standard psychopharmaceuticals as a novel treatment option that necessitates a paradigm shift from substitution- to transformation-based therapy. Second, various adaptogenic effects of ayahuasca will be reviewed, including effects on body, brain, and mental functioning. Third, a novel transformational psychotherapy framework will be introduced that outlines how ayahuasca could be used to support sustainable transformation. Finally, future research directions of developing pharmahuasca applications in clinical settings will be contrasted with traditional and indigenous contexts of ayahuasca use, highlighting the challenges of intercultural knowledge transfer.