Pioneering TRPM3 Inhibitors
for Non‑Opioid Pain Relief
From academic insight to industry momentum
In 2009, Prof. Voets approached CD3 to co‑develop first‑in‑class TRPM3 inhibitors as non‑opioid analgesics. CD3 contributed end‑to‑end small‑molecule discovery capabilities which resulted in a high throughput screening in 2011 followed by intensive hit-to-lead development to turn this breakthrough biology insight into tractable drug leads.
Early pharmacology confirmed target engagement on TRPM3. As translational evidence accumulated, including promising efficacy in an ex vivo human DRG model, a mouse post‑operative pain, and a mouse neuropathic pain model, the value proposition crystallized and attracted pharma interest.
“There is still a high unmet medical need in pain management. Chronic pain is the most common cause of long-term disability, affecting up to one third of adults at some point of their lifetime. Identifying TRPM3 as a heat‑pain sensor was only the beginning. CD3 gave us access to top drug discovery expertise and was pivotal in bringing industry to the table.”
Prof. Thomas VoetsKU Leuven, Laboratory of Ion Channel Research
Advancing with pharma partners
In 2018, convinced by the compelling science and the significant unmet need in chronic pain, Grünenthal, a global leader in pain therapeutics, entered a collaboration to advance the first-in-class non-opioid TRPM3 inhibitor program. Together, the teams evaluated approximately 1,000 additional compounds, further optimizing the series and ultimately nominating the first clinical candidate.
In the course of this collaboration, the program was significantly de-risked through extensive medicinal chemistry, DMPK characterization, early safety assessment, and translational efficacy studies across multiple preclinical pain models. These efforts established a strong foundation for future development.
Following the conclusion of the collaboration in 2020, the program continued to attract strong industry interest. In 2022, Biohaven entered an exclusive license and research collaboration to advance TRPM3 antagonists toward clinical development. Today BHV‑2100, a selective, peripherally restricted TRPM3 antagonist, has completed Phase 1 with a favorable safety, tolerability, and PK profile and has entered Phase 2 development.
From the first biological insight at KU Leuven to a Phase 2 clinical program, this success story illustrates CD3’s core strength: bridging academic innovation with industrial‑grade drug discovery to deliver therapeutic candidates that matter.