A supramolecular prodrug nanoplatform (HA‐CD‐PPa/JQ1 NP) was prepared through the host–guest interaction between cyclodextrin‐grafted hyaluronic acid (HA‐CD) and adamantine conjugated heterodimers (AD‐SS‐JQ1 and AD‐SS‐PPa) to target tumor cells overexpressing CD44; after CD44‐mediated endocytosis, pyropheophorbide a (PPa) and JQ1 were released from the nanoplatform in response to intracellular GSH. Here, CD44 is linked to neoplasm.