GRT7019

GRT7019 is an investigational topical formulation of **tapentadol**, a centrally acting analgesic developed by **Grünenthal GmbH**. Tapentadol is characterized by a dual mechanism of action, combining **mu-opioid receptor (MOR) agonism** with **norepinephrine reuptake inhibition (NRI)**. This synergistic approach is intended to provide potent pain relief with a lower opioid load compared to traditional strong opioids. GRT7019 was specifically developed to deliver tapentadol locally through the skin, aiming to treat chronic peripheral pain conditions such as **knee osteoarthritis** while minimizing systemic exposure and associated side effects (e.g., gastrointestinal or central nervous system issues). In a Phase II clinical trial (NCT04121403), GRT7019 was evaluated against placebo, oral diclofenac, and a lidocaine patch. However, the study failed to demonstrate a statistically significant difference in pain reduction compared to placebo, leading to the cessation of its development for this indication.

Other names

topical tapentadol