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§ Private Profile · South San Francisco, CA, USA
SiteOne Therapeutics is a technology company.
SiteOne Therapeutics is a clinical-stage biopharmaceutical company developing novel, highly selective small molecule inhibitors. Its technical approach leverages selective sodium ion channel modulators, creating non-opioid therapeutics. These candidates treat acute, neuropathic, visceral, and musculoskeletal pain, plus other conditions, offering a differentiated strategy for pain management.
Founded in 2010, SiteOne Therapeutics emerged from the scientific vision of co-founder John Mulcahy, Ph.D., who also served as CEO. The foundational insight was the critical need for effective, non-addictive pain solutions, prompting the company to develop targeted opioid alternatives from its inception. Dr. Mulcahy spearheaded the strategic drug discovery efforts.
SiteOne Therapeutics aims to serve patients suffering from various pain conditions with its pipeline. The company's mission is to deliver robust, non-opioid pain medicines that safely and effectively address multiple indications. Its vision is to significantly improve patient care by offering innovative solutions to a major global health challenge.
SiteOne Therapeutics has raised $117.9M across 3 funding rounds.
SiteOne Therapeutics has raised $117.9M in total across 3 funding rounds.
SiteOne Therapeutics has raised $117.9M across 3 funding rounds. Most recently, it raised $100.0M Series C in December 2024.
| Date | Round | Lead Investors | Other Investors | Status |
|---|---|---|---|---|
| Dec 1, 2024 | $100M Series C | Novo Holdings | Arix Bioscience, Atlas Venture, OrbiMed | Announced |
| Jan 8, 2017 | $15M Series B | Amgen Ventures | — | Announced |
| Sep 24, 2014 | $2.9M Grant | — | — | Announced |
SiteOne Therapeutics has raised $117.9M in total across 3 funding rounds.
SiteOne Therapeutics's investors include Novo Holdings, Arix Bioscience, Atlas Venture, OrbiMed, Amgen Ventures.
SiteOne Therapeutics was a clinical-stage biopharmaceutical company developing highly selective small molecule inhibitors of sodium channels (Nav1.7, Nav1.8, and others) as non-opioid treatments for acute and chronic pain, chronic cough, itch, and other sensory hyperexcitability disorders.[1][2][3] Targeting the peripheral nervous system, its pipeline aimed to deliver effective analgesia with fewer side effects than traditional opioids or central nervous system therapies, addressing a critical need amid the opioid crisis.[1][3] The company built therapies based on Stanford University-licensed technology using naturally occurring small molecules, serving patients with pain from conditions like chemotherapy-induced neuropathy and advancing candidates like STC-004, supported by a $15M NIDA grant.[1][2][6]
SiteOne demonstrated strong growth momentum through venture funding—$15M Series B in 2017, $100M Series C in December 2024—and culminated in its acquisition by Eli Lilly on May 27, 2025, for up to $1B, expanding Lilly's non-opioid pain pipeline.[2][3][5]
Founded in 2010, SiteOne Therapeutics emerged from breakthrough technology invented at Stanford University, focusing on highly selective NaV1.7 inhibitors derived from naturally occurring small molecules to revolutionize non-opioid pain treatment.[2][4][5] Co-founder and CEO John Mulcahy, Ph.D., led the company from its early days in Bozeman, Montana (later headquartered in South San Francisco, CA), building on over a decade of research into safer pain therapies.[2][3][5] Key early traction included SBIR grants for NaV1.7 inhibitors targeting chronic cough and neuropathic pain, plus venture rounds starting in 2015 from investors like Biobrit, Mission Bay Capital, and Next Frontier Capital, scaling to major funding from OrbiMed, Wellington Management, and others.[2][6] Pivotal moments featured potent, state-independent inhibitors with >1000-fold selectivity and a NIDA grant for STC-004, propelling clinical advancement before Lilly's acquisition.[1][6]
SiteOne rode the surging demand for non-opioid pain therapies amid the global opioid epidemic, regulatory pushes for alternatives, and advances in ion channel modulation following Vertex's non-opioid successes.[3] Timing was ideal: post-2020 biotech funding boom enabled its $100M Series C, while NIDA/HEAL Initiative grants accelerated development amid chemotherapy neuropathy and chronic pain affecting millions.[1][2][6] Market forces like Lilly's aggressive pipeline expansion in neuroscience favored SiteOne, positioning it to influence the ecosystem by validating peripheral sodium channel inhibition as a viable path, now amplified through Lilly's global reach to hasten clinical trials and commercialization.[3]
With its acquisition by Lilly, SiteOne's technology integrates into a major pharma powerhouse, likely accelerating Phase 1/2 trials for Nav1.7/1.8 inhibitors and expanding into cough/itch indications.[3] Trends like AI-driven drug design, precision neurology, and non-opioid mandates will shape its trajectory, potentially rivaling established players in a $100B+ pain market. Its influence evolves from nimble biotech innovator to cornerstone of Lilly's pain portfolio, delivering the safer therapies promised since 2010 and addressing the query's note: yes, a biotech technology company transforming pain care.[1][3]