Receptor Agonists and Antagonists
7 compounds in this family, each with its recorded mechanism, routes of administration, safety notes and references to published literature.
- HiltonolHiltonol (poly-ICLC) is a synthetic double‑stranded RNA that functions as a Toll‑like receptor 3 (TLR3) agonist. It is being investigated as an immunostimulatory adjuvant for vaccines and as a monotherapy or component of combination regimens in cancer, including glioblastoma, prostate cancer and other solid tumours. The compound is currently classified as investigational and is administered by injection (intramuscular, intratumoral, subcutaneous or intranasal).
- IbodutantIbodutant is an investigational peptide that selectively blocks the neurokinin‑2 (NK2) receptor, a G‑protein‑coupled receptor for tachykinins in the gastrointestinal tract. It has been studied primarily for diarrhea‑predominant irritable bowel syndrome (IBS‑D), where early clinical data suggested symptom relief, especially in female patients. The compound remains in development and has not received regulatory approval for any indication.
- Neladenoson bialanateNeladenoson bialanate is an investigational oral pro‑drug that delivers a partial agonist of the adenosine A1 receptor. It has been developed to treat chronic heart failure, both with reduced (HFrEF) and preserved (HFpEF) ejection fraction, by exploiting the cardioprotective actions of adenosine while aiming to avoid the bradycardia and AV‑block seen with full agonists.
- NepadutantNepadutant (MEN‑11420) is an investigational, selective antagonist of the tachykinin NK2 (neurokinin‑A) receptor. It is being explored for functional gastrointestinal disorders such as irritable bowel syndrome, for asthma‑related bronchoconstriction, and for infant colic, but it has not received regulatory approval for any indication.
- PMX-205PMX‑205 is a cyclic hexapeptide that blocks the complement C5a receptor 1 (C5aR1), a G‑protein‑coupled receptor involved in inflammatory signaling. In pre‑clinical studies it has been used to explore treatment of radiation‑induced cognitive decline, neurodegenerative disease, inflammatory bowel disease, and glioblastoma. The compound is currently a research tool and has not received regulatory approval for any therapeutic indication.
- RuxotemitideRuxotemitide (also known as LTX‑315) is an investigational peptide that acts as an agonist of Toll‑like receptor 2 (TLR2). It is being explored as an immune‑modulating agent, particularly in pre‑clinical cancer immunotherapy where it is incorporated into nanoparticle‑laden bacterial bio‑hybrids to trigger anti‑tumour immune responses.
- TAK-448TAK‑448 (also known as RVX‑TAK‑448) is an investigational synthetic peptide that mimics the C‑terminal segment of kisspeptin‑54 and acts as an agonist of the kisspeptin receptor (Kiss1R/GPR54). It has been studied primarily for its ability to suppress testosterone production, with early‑phase clinical trials in healthy men and men with prostate cancer, and pre‑clinical work in rodents. The compound is administered subcutaneously as a bolus, infusion, or depot formulation.