Diversification of therapeutic modalities has led to groundbreaking drug development, enabling effective treatment strategies for diseases that were previously challenging to address. During the era when small–molecule drugs were predominant, self–sufficiency among large pharmaceutical companies was central to innovation. However, in the era of diversified modalities, open innovation led by academia and academic startups has become indispensable. This marks a significant transformation in the drug discovery process, highlighting the essential role of open innovation activation in the emergence of revolutionary new drugs. The global distribution of pharmaceutical startups is overwhelmingly concentrated in the United States, with the United Kingdom and France following as remaining hotspots. Interestingly, the headquarters of eight out of the top 10 leading pharmaceutical companies, excluding the two based in Switzerland, coincide with these hotspots. On the other hand, turning attention to Japan, a country advocating for a science and technology–driven nation, there are limited success stories in drug discovery through open innovation, suggesting the existence of specific bottlenecks.